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RU2016137677A - Арильные, гетероарильные и гетероциклические соединения для лечения опосредованных комплементом расстройств - Google Patents

Арильные, гетероарильные и гетероциклические соединения для лечения опосредованных комплементом расстройств Download PDF

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Publication number
RU2016137677A
RU2016137677A RU2016137677A RU2016137677A RU2016137677A RU 2016137677 A RU2016137677 A RU 2016137677A RU 2016137677 A RU2016137677 A RU 2016137677A RU 2016137677 A RU2016137677 A RU 2016137677A RU 2016137677 A RU2016137677 A RU 2016137677A
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Russia
Prior art keywords
alkyl
compound
cycloalkyl
independently selected
halogen
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RU2016137677A
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RU2016137677A3 (ru
RU2707749C2 (ru
Inventor
Венкат Рао ГАДХАЧАДА
Цюпин Ван
Годвин Пэйс
Акихиро Хашимото
Давей Чэнь
Сянчжу Ван
Атул Агарвал
Милинд ДЕШАПНДЕ
Авинаш С. Фадке
Джейсое Аллан ВАЙЛС
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Ачиллион Фармасьютикалс, Инк.
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Publication of RU2016137677A publication Critical patent/RU2016137677A/ru
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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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Claims (191)

1. Соединение Формулы I
Figure 00000001
или его фармацевтически приемлемые соли, где:
Q1 представляет собой N(R1) или C(R1R1');
Q2 представляет собой C(R2R2'), C(R2R2')-C(R2R2'), S, О, N(R2) или C(R2R22')O;
Q3 представляет собой N(R3), S или C(R3R3');
X1 и X2 независимо представляют собой N, СН или X1 и X2 вместе представляют собой С=С;
Z представляет собой F, Cl, NH2, СН3, CH2D, CHD2 или CD3;
или
Figure 00000002
выбирается из
Figure 00000003
Figure 00000004
и
Figure 00000005
q равно 0, 1, 2 или 3;
r равно 1, 2 или 3;
R1, R1', R2, R2', R3 и R3' независимо выбраны из водорода, галогена, гидроксила, нитро, циано, амино, C1-С6алкила, С2-С6алкенила, С2-С6алкинила, C1-С6алкокси, С2-С6алкинила, С2-С6алканоила, C1-C6тиоалкила, гидроксиC1-C6алкила, аминоC1-C6алкила, -C0-C4aлкилNR9R10, -C(O)OR9, -OC(O)R9, -NR9C(O)R10, -C(O)NR9R10, -OC(O)NR9R10, -NR9C(O)OR10, С1-С2галогеналкила и C1-C2галогеналкокси,
R9 и R10 независимо выбраны из водорода, C1-C6алкила, (С3-С7циклоалкил)С0-С4алкила, -С0-С4алкил(С3-С7циклоалкила) и -O-С0-С4алкил(С3-С7циклоалкила);
или R1 и R2 связаны с образованием 3-6-членного карбоциклического или арильного кольца;
или R2 и R3 связаны с образованием 3-6-членного карбоциклического кольца;
или R1 и R1', или R2 и R2', или R3 и R3' связаны с образованием 3-6-членного карбоциклического спиро кольца;
или R1 и R1', R2 и R2', или R3 и R3' связаны с образованием 3-6-членного гетероциклического спиро кольца;
каждое из колец является незамещенным или замещенным 1 или более заместителями, независимо выбранными из галогена, гидроксила, циано, -СООН, C1-С4алкила, С2-С4алкенила, С2-С4алкинила, -С1-С4алкокси, С2-С4алканоила, C1-C4гидроксиалкила, (моно- и ди-С1-С4алкиламино)С0-С4алкила, -С0-С4алкил(С3-С7циклоалкила), -O-С0-С4алкил(С3-С7циклоалкила), С1-С2галоалкила и С1-С2галоалкокси;
или R1 и R1' или R2 и R2' связаны с образованием карбонильной группы;
или R1 и R2 или R2 и R3 могут быть взяты вместе с образованием двойной связи углерод-углерод;
R и R' независимо выбраны из Н, алкила, циклоалкила, циклоалкилалкила, гетероцикла, гетероциклоалкила, арила, арилалкила, гетероарила и гетероарилалкила;
А представляет собой группу, выбранную из:
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
и
Figure 00000011
R4 выбран из -СНО, -CONH2, С2-С6алканоила, водорода, -SO2NH2, -C(CH2)2F, -CH(CF3)NH2, C1-C6алкила, -С0-С4алкил(С3-С7циклоалкила), -С(О)С0-С2алкил(С3-С7циклоалкила),
Figure 00000012
и
Figure 00000013
каждый из R4, отличный от водорода, -СНО и -CONH2, является незамещенным или замещенным одним или более из амино, имино, галогена, гидроксила, циано, цианимино, C1-С2алкила, C1-С2алкокси, -С0-С2алкил(моно- и ди-С1-С4алкиламино), C1-С2галогеналкила и С1-С2галогеналкокси;
R5 и R6 независимо выбраны из -СНО, -C(O)NH2, -C(O)NH(CH3), С2-С6алканоила, водорода, гидроксила, галогена, циано, нитро, -СООН, -SO2NH2, винила, C1-C6алкила (в том числе, метила), С2-С6алкенила, C1-C6алкокси, -С0-С4алкил(С3-С7циклоалкила), -С(O)С0-С4алкил(С3-С7циклоалкила), -P(O)(OR9)2, -OC(O)R9, -C(O)OR9, -C(O)N(CH2CH2R9)(R10), -NR9C(O)R10, фенила и 5-6-членного гетероарила;
R6' представляет собой водород, галоген, гидроксил, С1-С4алкил, -С0-С4алкил(С3-С7циклоалкил) или C1-C4алкокси;
или R6 и R6' могут быть взяты вместе с образованием оксо, винил или иминогруппы;
R7 представляет собой водород, C1-C6алкил или -С0-С4алкил(С3-С7циклоалкил);
R8 и R8' независимо выбраны из водорода, галогена, гидроксила, C1-C6алкила, -С0-С4алкил(С3-С7циклоалкила), C1-C6алкокси и (С1-С4алкиламино)С0-С2алкила; или R8 и R8', взятые вместе, образуют оксогруппу; или R8 и R8' могут быть взяты вместе с атомом углерода, с которым они связаны, с образованием 3-членного карбоциклического кольца;
R16 отсутствует или выбран из галогена, гидроксила, нитро, циано, C1-C6алкила, С2-C6алкенила, С2-С6алканоила, C1-C6алкокси, -С0-С4алкил(моно- и ди-С1-С6алкиламино), -С0-С4алкил(С3-С7циклоалкила), С1-С2галогеналкила и С1-С2галогеналкокси;
R19 представляет собой водород, C1-C6алкил, С2-С6алкенил, С2-С6алканоил, -SO2C1-С6алкил, (моно- и ди-С1-С6алкиламино)С1-С4алкил, -С0-С4алкил(С3-С7циклоалкил), -С0-С4алкил(С3-С7гетероциклоалкил), -С0-С4алкил(арил) или С0-С4алкил(гетероарил), и где R19, отличный от водорода, является незамещенным или замещенным одним или более заместителями, независимо выбранными из галогена, гидроксила, амино, -СООН и -С(O)ОС1-С4алкила;
X11 представляет собой N или CR11.
X12 представляет собой N или CR12.
X13 представляет собой N или CR13
X14 представляет собой N или CR14, и где не более чем два из X11, X12, X13 и X14 представляют собой N;
один из R12 и R13 выбран из R31, а другой из R12 и R13 выбран из R32:
R31 выбран из водорода, галогена, гидроксила, нитро, циано, амино, -СООН, C1-С2галогеналкила, С1-С2галогеналкокси, C1-C6алкила, -С0-С4алкил(С3-С7циклоалкила), С2-С6алкенила, С2-С6алканоила, C1-C6алкокси, С2-С6алкенилокси, -C(O)OR9, C1-C6тиоалкила, -C0-C4алкилNR9R10, -C(O)NR9R10, -SO2R9, -SO2NR9R10, -OC(O)R9 и -C(NR9)NR9R10, каждый из R31, отличный от водорода, галогена, гидроксила, нитро, циано, C1-С2галогеналкила и C1-C2галогеналкокси, является незамещенным или замещенным одним или более заместителями, независимо выбранными из галогена, гидроксила, нитро, циано, амино, -СООН, -CONH2 С1-С2галогеналкила и C1-C2галогеналкокси, и каждый из R31 также необязательно замещен одним заместителем, выбранным из фенила и 4-7-членного гетероцикла, содержащего 1, 2 или 3 гетероатома, независимо выбранных из N, О и S; при этом фенил или 4-7-членный гетероцикл не замещен или замещен одним или более заместителями, независимо выбранными из галогена, гидроксила, нитро, циано, C1-С6алкила, С2-С6алкенила, С2-С6алканоила, C1-C6алкокси, (моно- и ди-С1-С6алкиламино)С0-С4алкила, C1-C6алкилэфира, -С0-С4алкил)(С3-С7циклоалкила), С1-С2галогеналкила и C1-С2галогеналкокси;
R32 выбран из арила; насыщенного или ненасыщенного гетероцикла, где гетероцикл связан через атом углерода в гетероциклическом кольце с атомом углерода кольца А в положении R12 или R13; и гетероарила, где арил, гетероцикл или гетероарильное кольцо является необязательно замещенным заместителем, выбранным из галогена, циано, гидроксила, алканоила, карбоксамида, алкила, циклоалкила, алкенила, алкинила, алкокси, арилокси, алкилтио, алкилсульфинила, алкилсульфонила, аминоалкила, арилалкила или арилалкокси;
R11, R14 и R15 независимо выбраны из водорода, галогена, гидроксила, нитро, циано, -O(PO)(OR9)2, -(PO)(OR9)2, C1-C6алкила, С2-С6алкенила, С2-С6алкинила, С2-С6алканоила, C1-C6алкокси, C1-C6тиоалкила, -С0-С4алкил(моно- и ди-С1-С6алкиламино), -С0-С4алкил(С3-С7циклоалкила), -С0-С4алкокси(С3-С7циклоалкила), C1-C2галогеналкила и C1-C2галогеналкокси;
R21 и R22 независимо выбраны из водорода, гидроксила, циано, амино, C1-C6алкила, C1-C6галогеналкила, C1-C6алкокси, (С3-С7циклоалкил)С0-С4алкила, (фенил)С0-С4алкила, -С1-С4алкилОС(O)ОС1-С6алкила, -С1-С4алкилОС(O)C1-C6-алкила, -С1-С4алкилС(O)ОС1-С6алкила, (4-7-членный гетероциклоалкил)С0-С4алкила, имеющего 1, 2 или 3 гетероатома, независимо выбранных из N, О и S, и (5- или 6-членный ненасыщенный или ароматический гетероцикл)С0-С4-алкила, имеющего 1, 2 или 3 гетероатома, независимо выбранных из N, О и S;
R23 независимо выбран из C1-C6алкила, C1-С6галогеналкила, (арил)С0-С4алкила, (С3-С7циклоалкил)С0-С4алкила, (фенил)С0-С4алкила, (4-7-членный гетероциклоалкил)С0-С4алкила, имеющего 1, 2, или 3 гетероатома, независимо выбранных из N, О и S, и (5- или 6-членный ненасыщенный или ароматический гетероцикл)С0-С4алкила, имеющего 1, 2, или 3 гетероатома, независимо выбранных из N, О, и S;
R24 и R25 вместе с атомом азота, к которому они присоединены, образуют 4-7-членную моноциклическую гетероциклоалкильную группу или 6-10-членную бициклическую гетероциклическую группу, имеющую конденсированные, спиро или мостиковые кольца;
L представляет собой связь или выбран из формул
Figure 00000014
и
Figure 00000015
R17 представляет собой водород, C1-C6алкил или -С0-С4алкил(С3-С7циклоалкил);
R18 и R18' независимо выбраны из водорода, галогена, гидроксиметила и метила; и m равно 0, 1, 2 или 3;
В представляет собой моноциклическую или бициклическую карбоциклическую; моноциклическую или бициклическую карбоцикло-окси группу; моноциклическую, бициклическую или трициклическую гетероциклическую группу, имеющую 1, 2, 3 или 4 гетероатома, независимо выбранных из N, О и S, и от 4 до 7 кольцевых атомов в кольце; С2-С6алкенила; С2-С6алкинила; -(С0-С4-алкил)(арила); -(С0-С4-алкил)(гетероарила); или -(С0-С4-алкил)(бифенила) каждый из В незамещен или замещен одним или более заместителями, независимо выбранными из R33 и R34, и 0 или 1 заместитель выбран из R35 и R36;
R33 независимо выбран из галогена, гидроксила, -СООН, циано, C1-C6алкила, С2-С6алканоила, C1-C6алкокси, -C0-C4aлкилNR9R10, -SO2R9, С1-С2галогеналкила и C1-С2галогеналкокси;
R34 независимо выбран из нитро, С2-С6алкенила, С2-С6алкинила, C1-С6тиоалкила, -JC3-С7циклоалкила, -В(ОН)2, -JC(O)NR9R23, -JOSO2OR21, -C(O)(CH2)1-4S(O)R21, -O(CH2)1-4S(O)NR21R22, -JOP(O)(OR21)(OR22), -JP(O)(OR21)(OR22), -JOP(O)(OR21)R22, JP(O)(OR21)R22, -JOP(O)R21R22, -JP(O)R21R22, -JSP(O)(OR21)(OR22), -JSP(O)(OR21)(R22), -JSP(O)(R21)(R22), -JNR9P(O)(NHR21)(NHR22), -JNR9P(O)(OR21)(NHR22), -JNR9P(O)(OR21)(OR22), -JC(S)R21, -JNR21SO2R22, -JNR9S(O)NR10R22, -JNR9SO2NR10R22, -JSO2NR9COR22, -JSO2NR9CONR21R22, -JNR21SO2R22, -JC(O)NR21SO2R22, -JC(NH2)NR22, -JC(NH2)NR9S(O)2R22, -JOC(O)NR21R22, -JNR21C(O)OR22, -JNR21OC(O)R22, -(CH2)1-4C(O)NR2R22, -JC(O)R24R25, -JNR9C(O)R21, -JC(O)R21, -JNR9C(O)NR10R22, -CCR21, -(CH2)1-4OC(O)R21 и -JC(O)OR23; каждый из R34 может быть незамещен или замещен одним или более заместителями, независимо выбранными из галогена, гидроксила, нитро, циано, амино, оксо, -В(ОН)2, -Si(CH3)3, -СООН, -CONH2, -Р(O)(ОН)2, C1-C6алкила, -С0-С4алкил(С3-С7циклоалкила), C1-C6алкокси, -С0-С2алкил(моно- и ди-С1-С4алкиламино), C1-С6алкилэфира, С1-С4алкиламино, С1-С4гидроксилалкила, С1-С2галогеналкила и C1-С2галогеналкокси;
R35 независимо выбран из нафтила, нафтилокси, инданила, (4-7-членный гетероциклоалкил)С0-С4алкила, содержащего 1 или 2 гетероатома, выбранных из N, О и S, и бициклического гетероцикла, содержащего 1, 2 или 3 гетероатома, независимо выбранных из N, О и S, и содержащего от 4 до 7 кольцевых атомов в каждом кольце; каждый из R35 незамещен или замещен одним или более заместителями, независимо выбранными из галогена, гидроксила, нитро, циано, C1-C6алкила, С2-С6алкенила, С2-С6алканоила, C1-C6алкокси, (моно- и ди-С1-С6алкиламино)С0-С4алкила, C1-С6алкилэфира, -С0-С4алкил(С3-С7циклоалкила), -SO2R9, С1-С2галогеналкила и С1-С2галогеналкокси;
R36 независимо выбран из тетразолила, (фенил)С0-С2алкила, (фенил)С1-С2алкокси, фенокси и 5- или 6-членного гетероарила, содержащего 1, 2 или 3 гетероатома, независимо выбранных из N, О, В и S, каждый из R36 незамещен или замещен одним или более заместителями, независимо выбранными из галогена, гидроксила, нитро, циано, С1-С6алкила, С2-С6алкенила, С2-С6алканоила, C1-С6алкокси, (моно- и ди-С1-С6алкиламино)С0-С4алкила, C1-C6алкилэфира, -С0-С4алкил(С3-С7циклоалкила), -SO2R9, -OSi(CH3)2C(CH3)3, -Si(CH3)2C(CH3)3, C1-C2галогеналкила и C1-C2галогеналкокси; и
J независимо выбран в каждом случае из ковалентной связи, С1-С4алкилена, -OC1-С4алкилена, С2-С4алкенилена и С2-С4алкинилена.
2. Соединение по п. 1, в котором кольцо
Figure 00000016
выбирается из:
Figure 00000017
Figure 00000018
и
Figure 00000019
3. Соединение по п. 1, в котором кольцо
Figure 00000020
выбирается из:
Figure 00000021
Figure 00000022
Figure 00000023
и
Figure 00000024
4. Соединение по п. 1, в котором кольцо
Figure 00000025
выбирается из:
Figure 00000026
Figure 00000027
и
Figure 00000028
5. Соединение по п. 1, в котором
a) R1 и R1', или R2 и R2', или R3 и R3' связаны с образованием 3-6-членного карбоциклического спиро кольца; или
b) R1 и R1', R2 и R2' или R3 и R3' связаны с образованием 3-6-членного гетероциклического спиро кольца; или
c) R1 и R2 связаны с образованием 3-6-членного карбоциклического или арильного кольца; или
d) R2 и R3 связаны с образованием 3-6-членного карбоциклического кольца.
6. Соединение по п. 1, в котором А является группой, выбранной из:
Figure 00000029
Figure 00000030
Figure 00000031
и
Figure 00000032
7. Соединение по п. 1, в котором А является группой, выбранной из:
Figure 00000033
Figure 00000034
и
Figure 00000035
8. Соединение по п. 1, в котором фрагмент R32 имеет по меньшей мере один заместитель.
9. Соединение по п. 1, в котором R32 необязательно замещен фенилом.
10. Соединение по п. 1, в котором R32 необязательно замещен гетероциклом, выбранным из группы, состоящей из морфолинила, пиперазинила и пиперидинила.
11. Соединение по п. 1, в котором R32 необязательно замещен гетероарильным кольцом, выбранным из группы, состоящей из пиридинила, имидазолила, имидазопиридинила, пиримидинила, пиразолила, триазолила, пиразинила и тетразолила.
12. Соединение по п. 11, в котором необязательный заместитель выбран из галогена, циано, гидроксила, алканоила, карбоксамида, алкила, циклоалкила, алкенила, алкинила, алкокси, арилокси, алкилтио, алкилсульфинила, алкилсульфонила, аминоалкила, арилалкила или арилалкокси.
13. Соединение по п. 11, в котором необязательный заместитель выбран из насыщенной, ненасыщенной или ароматической гетероциклической группы, имеющей от 1 до 3 отдельных или конденсированных колец с одним или более атомами N, О или S.
14. Соединение по п. 11, в котором необязательный заместитель выбран из кумаринила, хинолинила, изохинолинила, хиназолинила, пиридила, пиразинила, пиримидинила, фуранила, пирролила, тиенила, тиазолила, триазинила, оксазолила, изоксазолила, имидазолила, индолила, бензофуранила, бензотиазолила, тетрагидрофуранила, тетрагидропиранила, пиперидинила, морфолинила, пиперазинила и пирролидинила.
15. Соединение Формулы I
Figure 00000036
или его фармацевтически приемлемая соль, в котором:
Figure 00000037
является таким, как определено в п. 1;
А является таким, как определено в п. 1; и
-L-B- выбирается из:
Figure 00000038
Figure 00000039
Figure 00000040
и
Figure 00000041
R18 и R18' независимо выбраны из водорода, галогена, гидроксиметила и метила;
m равно 0 или 1;
R26, R27 и R28 независимо выбраны из водорода, галогена, гидроксила, нитро, циано, C1-C6алкила, С2-С6алкенила, С2-С6алканоила, C1-C6алкокси, C1-C6тиоалкила, (моно- и ди-C1-C6алкиламино)С0-С4алкила, (С3-С7циклоалкил)С0-С4алкила, (арил)С0-С4алкила-,(гетероарил)С0-С4алкила- и -С0-С4алкокси(С3-С7циклоалкила); каждый из которых R26, R27, R28, отличающийся от водорода, галогена, гидроксила, нитро и циано, является незамещенным или замещенным одним или более заместителями, независимо выбранными из галогена, гидроксила, амино, C1-С2алкокси, C1-C2галогеналкила, (С3-С7циклоалкил)С0-С4алкиала- и C1-C2галогеналкокси; и
R29 представляет собой водород, C1-C2алкил, С1-С2галогеналкил или -Si(CH3)2C(CH3)3.
16. Соединение по п. 1, в котором В выбирается из моноциклического карбоциклического или бициклического карбоциклического фрагмента, который незамещен или замещен одним или более заместителями, независимо выбранными из R33 и R34, и 0 или 1 заместитель выбран из R35 и R36.
17. Соединение по п. 16, в котором моноциклический карбоциклический фрагмент выбран из циклогексенила, циклогексила, циклопентенила, циклопентила, циклобутенила, циклобутила или циклопропила, необязательно замещенных галогеном, циано, гидроксилом, C1-C6алкилом, С2-С6алканоилом, C1-C6алкокси или фенилом.
18. Соединение по п. 1, в котором В выбирается из моноциклической, бициклической или трициклической гетероциклической группы, имеющей 1, 2, 3 или 4 гетероатома, независимо выбранных из N, О и S, и от 4 до 7 кольцевых атомов в кольце; где В является незамещенным или замещенным одним или более заместителями, независимо выбранными из R33 и R34, и 0 или 1 заместителем, выбранным из R35 и R36.
19. Соединение по п. 18, в котором моноциклическая, бициклическая или трициклическая гетероциклическая группа, имеющая 1, 2, 3 или 4 гетероатома, независимо выбранных из N, О и S, и от 4 до 7 кольцевых атомов в кольце, выбирается из пирролидинила, дигидрофуранила, тетрагидротиенила, тетрагидропиранила, дигидропиранила, тетрагидротиопиранила, пиперидиноа, пиперидонила, морфолино, тиоморфолино, тиоксанила или пиперазинила, необязательно замещенных галогеном, циано, гидроксилом, C1-C6алкилом, С2-С6алканоилом, C1-C6алкокси или фенилом.
20. Соединение по п. 1, в котором В выбирается из -(С0-С4алкил)(арила); -(С0-С4-алкил)(гетероарила); или -(С0-С4алкил)(бифенила), где В является незамещенным или замещенным одним или более заместителями, независимо выбранными из R33 и R34, и 0 или 1 заместителем, выбранным из R35 и R36.
21. Соединение по п. 20, в котором группа -(С0-С4алкил)(арил) представляет собой фенил или бензил, необязательно замещенный галогеном, гидроксилом, -СООН, циано, C1-C6-алкилом, С2-С6алканоилом, C1-C6алкокси, -C0-C4алкилNR9R10, -SO2R9, C1-С2галогеналкилом и C1-С2галогеналкоси, С2-С6алкенилом, С2-С6алкинилом, C1-С6тиоалкилом или -JC3-C7циклоалкилом.
22. Соединение по п. 20, в котором группа -(С0-С4алкил)(гетероарил) представляет собой имидазолил, имидазопиридинил, пиримидинил, пиразолил, триазолил, пиразинил, тетразолил, фурил, тиенил, изоксазолил, тиазолил, оксадиазолил, оксазолил, изотиазолил или пирролил, необязательно замещенный галогеном, гидроксилом, -СООН, циано, C1-C6-алкилом, С2-С6алканоилом, C1-C6алкокси, -C0-C4алкилNR9R10, -SO2R9, C1-С2галогеналкилом и C1-С2галогеналкоси, С2-С6алкенилом, С2-С6алкинилом, C1-С6тиоалкилом или -JC3-С7циклоалкилом.
23. Соединение по п. 20, в котором группа -(С0-С4алкил)(бифенил) представляет собой бифенил, необязательно замещенный галогеном, гидроксилом, -СООН, циано, C1-C6-алкилом, С2-С6алканоилом, C1-C6алкокси, -C0-C4алкилNR9R10, -SO2R9, C1-С2галогеналкилом и C1-С2галогеналкоси, С2-С6алкенилом, С2-С6алкинилом, C1-С6тиоалкилом или -JC3-С7циклоалкилом.
24. Соединение по п. 1, в котором В выбирается из:
Figure 00000042
Figure 00000043
и
Figure 00000044
25. Соединение по п. 1, в котором В выбирается из:
Figure 00000045
Figure 00000046
Figure 00000047
и
Figure 00000048
26. Соединение по п. 1, в котором В выбирается из:
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
и
Figure 00000056
27. Соединение по п. 1, в котором В выбирается из:
Figure 00000057
и
Figure 00000058
28. Соединение по п. 1, в котором В выбирается из:
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
и
Figure 00000066
29. Соединение по п. 1, в котором В выбирается из:
Figure 00000067
Figure 00000068
Figure 00000069
и
Figure 00000070
30. Соединение по п. 1, в котором R32 выбирается из:
Figure 00000071
Figure 00000072
и
Figure 00000073
31. Соединение по п. 1, в котором R32 выбирается из:
Figure 00000074
Figure 00000075
Figure 00000076
и
Figure 00000077
32. Соединение по п. 1, в котором R32 выбирается из:
Figure 00000078
и
Figure 00000079
33. Соединение по п. 1, в котором R32 выбирается из:
Figure 00000080
и
Figure 00000081
34. Соединение по п. 1, в котором соединение выбирается из:
Figure 00000082
Figure 00000083
и
Figure 00000084
35. Соединение по п. 1, в котором соединение выбирается из:
Figure 00000085
Figure 00000086
и
Figure 00000087
36. Соединение по п. 1, в котором соединение выбирается из:
Figure 00000088
Figure 00000089
и
Figure 00000090
37. Способ лечения расстройства, опосредованного путем комплемента, включающий введение субъекту, нуждающемуся в этом, эффективного количества соединения, выбранного из любого по пп. 1-36, или его фармацевтически приемлемой соли необязательно в фармацевтически приемлемом носителе.
38. Способ по п. 37, в котором расстройство является возрастной макулярной дегенерацией (AMD).
39. Способ по п. 37, в котором расстройство является дегенерацией сетчатки, офтальмологическим заболеванием, рассеянным склерозом, артритом или COPD.
40. Способ по п. 37, в котором расстройство является офтальмологическим заболеванием.
41. Способ по п. 37, в котором расстройство является пароксизмальной ночной гемоглобинурией (PNH).
42. Способ по п. 37, в котором расстройство является респираторным заболеванием.
43. Способ по п. 37, в котором расстройство является сердечно-сосудистым заболеванием.
44. Способ по п. 37, в котором расстройство является атипичным или типичным гемолитико-уремическим синдромом.
45. Способ по п. 37, в котором расстройство является ревматоидным артритом.
46. Способ по п. 37, в котором расстройство является гломерулонефритом С3.
47. Способ по любому из пп. 37-46, в котором субъект является человеком.
48. Применение соединения по любому из пп. 1-36 для производства лекарственного средства для лечения расстройства, опосредованного Фактором D комплемента.
49. Соединение по любому из пп. 1-36 для применения в лечении расстройства, опосредованного Фактором D комплемента.
50. Применение по п. 48, в котором расстройство представляет собой пароксизмальную ночную гемоглобинурию (PNH).
51. Применение по п. 48, в котором расстройство представляет собой рассеянный склероз, артрит или COPD.
52. Применение по п. 48, в котором расстройство представляет собой офтальмологическое заболевание.
53. Применение по п. 48, в котором расстройство представляет собой респираторное заболевание.
54. Применение по п. 48, в котором расстройство представляет собой сердечно-сосудистое заболевание.
55. Применение по п. 48, в котором расстройство представляет собой атипичный или типичный гемолитико-уремический синдром.
56. Применение по п. 48, в котором расстройство представляет собой ревматоидный артрит.
57. Применение по п. 48, в котором расстройство представляет собой гломерулонефрит С3.
58. Применение по любому из пп. 48 или 50-57, в котором субъект является человеком.
59. Соединение по п. 49, в котором расстройство является рассеянным склерозом, артритом, ревматоидным артритом или COPD.
60. Соединение по п. 49, в котором расстройство представляет собой респираторное заболевание.
61. Соединение по п. 49, в котором расстройство является сердечно-сосудистым заболеванием.
62. Соединение по п. 49, в котором расстройство является атипичным или типичным гемолитико-уремическим синдромом.
63. Соединение по п. 49, в котором расстройство является зрительным расстройством.
64. Соединение по п. 49, в котором расстройство является гломерулонефритом С3.
65. Фармацевтическая композиция, содержащая эффективное количество соединения, выбранного из любого по пп. 1-36, в фармацевтически приемлемом носителе.
66. Способ по п. 40, в котором соединение вводится интравитреально, субхороидально или супрахориоидально.
67. Способ по п. 37, в котором соединение вводится в комбинации с эффективным количеством дополнительного активного агента.
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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3110418T1 (sl) 2014-02-25 2020-03-31 Achillion Pharmaceuticals, Inc. Arilne, heteroarilne in heterociklične spojine za zdravljenje s komplementom posredovanih motenj
AU2016224962B2 (en) 2015-02-27 2021-10-14 The Johns Hopkins University Assay to diagnose and treat disorders of the alternative pathway of complement activation
WO2017035357A1 (en) * 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of medical disorders
AR105808A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos de amida para el tratamiento de trastornos médicos
EP3340983B1 (en) 2015-08-26 2023-10-04 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders
WO2017035351A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of medical disorders
US10385097B2 (en) 2015-08-26 2019-08-20 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of medical disorders
WO2017035361A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for the treatment of medical disorders
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
AR105809A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos médicos
AR106018A1 (es) * 2015-08-26 2017-12-06 Achillion Pharmaceuticals Inc Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos
WO2017035401A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amide compounds for treatment of immune and inflammatory disorders
ES2908479T3 (es) 2015-08-26 2022-04-29 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos inmunitarios e inflamatorios
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
AU2016358100B2 (en) 2015-11-19 2021-05-27 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2016367261A1 (en) * 2015-12-11 2018-07-26 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
BR112018012756A2 (pt) 2015-12-22 2018-12-04 Incyte Corp compostos heterocíclicos como imunomoduladores
JP2019506159A (ja) 2016-01-20 2019-03-07 ヴィトリサ セラピューティクス， インコーポレイテッド Ｄ因子を阻害するための組成物および方法
TWI747873B (zh) 2016-02-01 2021-12-01 美商百歐克斯製藥公司 苯并吡唑化合物及其類似物
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
HRP20221030T1 (hr) 2016-06-20 2022-11-11 Incyte Corporation Heterociklički spojevi kao imunomodulatori
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20190292155A1 (en) * 2016-07-15 2019-09-26 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
DE102016114392A1 (de) * 2016-08-03 2018-02-08 Eberhard Karls Universität Tübingen Medizinische Fakultät Verbindung zur Behandlung einer mit einer Desregulierung des alternativen Komplementweges assoziierten Erkrankung
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018049152A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
AR109596A1 (es) 2016-09-09 2018-12-26 Incyte Corp Compuestos pirazolopiridina y sus usos
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
MX2019007651A (es) 2016-12-22 2020-02-07 Incyte Corp Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion de ligando 1 de muerte programada (pd-l1).
CN110582493B (zh) 2016-12-22 2024-03-08 因赛特公司 作为免疫调节剂的苯并噁唑衍生物
MA47120A (fr) 2016-12-22 2021-04-28 Incyte Corp Dérivés pyridine utilisés en tant qu'immunomodulateurs
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2018136827A1 (en) 2017-01-20 2018-07-26 Vitrisa Therapeutics, Inc. Stem-loop compositions and methods for inhibiting factor d
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
ES2975416T3 (es) * 2017-02-27 2024-07-05 Regeneron Pharma Modelo humanizado de trastornos renales y hepáticos
EP3589628A4 (en) * 2017-03-01 2021-03-31 Achillion Pharmaceuticals, Inc. ARYL, HETEROARYL AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISEASES
EP3589287B1 (en) * 2017-03-01 2022-09-14 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for treatment of medical disorders
WO2018160891A1 (en) 2017-03-01 2018-09-07 Achillion Pharmaceutical, Inc. Pharmaceutical compounds for treatment of medical disorders
WO2018229543A2 (en) * 2017-06-14 2018-12-20 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
WO2019028284A1 (en) 2017-08-02 2019-02-07 Achillion Pharmaceuticals, Inc. THERAPEUTIC REGIMES FOR THE TREATMENT OF NOCTURNAL PAROXYSTIC HEMOGLOBINURIA
WO2019051199A1 (en) 2017-09-08 2019-03-14 Incyte Corporation 6-CYANO-INDAZOLE COMPOUNDS AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) MODULATORS
KR101969521B1 (ko) * 2017-10-26 2019-08-13 에스케이텔레콤 주식회사 사물인터넷용 단말과 모바일 단말의 접속을 관리하는 방법 및 이러한 방법을 수행하는 기지국
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
SG11202007917VA (en) 2018-02-20 2020-09-29 Incyte Corp N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
WO2019164847A1 (en) 2018-02-20 2019-08-29 Incyte Corporation Indazole compounds and uses thereof
DK3774791T3 (da) 2018-03-30 2023-01-23 Incyte Corp Heterocykliske forbindelser som immunmodulatorer
TW202010742A (zh) * 2018-04-06 2020-03-16 美商百歐克斯製藥公司 取代的苯并呋喃、苯并吡咯、苯并噻吩及結構相關的補體抑制劑
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
BR112020022936A2 (pt) 2018-05-11 2021-02-02 Incyte Corporation derivados de tetra-hidro-imidazo[4,5-c]piridina como imunomoduladores de pd-l1
WO2019236884A1 (en) * 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020041301A1 (en) 2018-08-20 2020-02-27 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement factor d medical disorders
MX2021002640A (es) * 2018-09-06 2021-07-16 Achillion Pharmaceuticals Inc Formas morficas de los inhibidores del factor d del complemento.
JP7443375B2 (ja) 2018-09-06 2024-03-05 アキリオン ファーマシューティカルズ， インコーポレーテッド 医学的障害の治療のための大環状化合物
ES2973117T3 (es) 2018-09-25 2024-06-18 Incyte Corp Compuestos de pirazolo[4,3-d]pirimidina como moduladores de ALK2 y/o FGFR
US11807627B2 (en) 2018-09-25 2023-11-07 Achillon Pharmaceuticals, Inc. Morphic forms of complement factor D inhibitors
WO2020092183A1 (en) 2018-11-01 2020-05-07 Merck Sharp & Dohme Corp. Novel substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
EP3886845B1 (en) * 2018-11-28 2024-09-04 Merck Sharp & Dohme LLC Novel substituted piperazine amide compounds as indoleamine 2, 3-dioxygenase (ido) inhibitors
WO2020109343A1 (en) 2018-11-29 2020-06-04 F. Hoffmann-La Roche Ag Combination therapy for treatment of macular degeneration
KR20220004024A (ko) * 2019-03-22 2022-01-11 아칠리온 파르마세우티칼스 인코포레이티드 보체 매개 장애의 치료를 위한 약제학적 조성물
TW202114680A (zh) 2019-08-06 2021-04-16 美商英塞特公司 Ｈｐｋ１抑制劑之固體形式
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
IL292524A (en) 2019-11-11 2022-06-01 Incyte Corp Salts and crystalline forms of pd-1/pd-l1 inhibitor
CN113777302A (zh) * 2020-06-09 2021-12-10 张曼 尿液补体因子d及其多肽片段在烧伤中的应用
CN111704617B (zh) * 2020-06-15 2022-08-23 嘉兴特科罗生物科技有限公司 一种小分子化合物
JP2023542949A (ja) * 2020-09-23 2023-10-12 アキリオン ファーマシューティカルズ， インコーポレーテッド 補体媒介性障害の治療のための医薬化合物
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
WO2023023227A1 (en) 2021-08-20 2023-02-23 Alexion Pharmaceuticals, Inc. Methods for treating sickle cell disease or beta thalassemia using complement alternative pathway inhibitors
JP2024533782A (ja) * 2021-09-30 2024-09-12 武漢朗来科技発展有限公司 補体因子ｄ阻害剤としての化合物、その医薬組成物及び使用
WO2023158772A1 (en) 2022-02-21 2023-08-24 Teva Pharmaceuticals International Gmbh Solid state forms of danicopan and process thereof
WO2024008121A1 (zh) * 2022-07-06 2024-01-11 南京明德新药研发有限公司 二氟取代的氮杂双环化合物及其应用
WO2024191606A1 (en) * 2023-03-13 2024-09-19 Alexion Pharmaceuticals, Inc. Formulations of danicopan and methods of use thereof

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
US6074642A (en) 1994-05-02 2000-06-13 Alexion Pharmaceuticals, Inc. Use of antibodies specific to human complement component C5 for the treatment of glomerulonephritis
AU7808198A (en) 1997-06-03 1998-12-21 Biocryst Pharmaceuticals, Inc. Novel compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
TR200003598T2 (tr) 1998-03-26 2001-06-21 Japan Tobacco Inc. Amid türevleri ve nosiseptin antagonistleri
DK1112275T3 (da) 1998-09-09 2003-11-24 Metabasis Therapeutics Inc Hidtil ukendte heteroaromatiske inhibitorer for fructose-1,6-bisphosphatase
WO2001017980A1 (fr) 1999-09-03 2001-03-15 Ajinomoto Co., Inc. Nouveaux procedes de preparation de derives d'oxazepine
US7528165B2 (en) 2001-12-13 2009-05-05 National Health Research Institutes Indole compounds
NZ537853A (en) 2002-07-16 2007-02-23 Amura Therapeutics Ltd Inhibitors of cathepsin K and related cysteine protesases of the CA clan
AU2003302084A1 (en) 2002-11-15 2004-06-15 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
US7999082B2 (en) 2004-02-10 2011-08-16 National Jewish Medical And Research Center Anti-factor B antibodies
PT1727811E (pt) 2004-03-24 2015-02-09 Shire Orphan Therapies Gmbh Novos compostos para inibição de angiogénese e a sua respectiva utilização
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
WO2006012373A2 (en) 2004-07-20 2006-02-02 Critical Therapeutics, Inc. Combination therapies of hmgb and complement inhibitors against inflammation
AU2006325754B2 (en) * 2005-12-14 2012-04-12 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIa inhibitors
JPWO2008047831A1 (ja) 2006-10-17 2010-02-25 協和発酵キリン株式会社 Ｊａｋ阻害剤
EP2119703B1 (en) * 2007-01-15 2012-12-12 Santen Pharmaceutical Co., Ltd Novel indole derivative having inhibitory activity on i b kinase
WO2009091826A2 (en) 2008-01-14 2009-07-23 The Board Of Regents Of The University Of Texas System Compositions and methods related to a human cd19-specific chimeric antigen receptor (h-car)
EP2490026A4 (en) 2009-10-16 2013-08-21 Mochida Pharm Co Ltd MARKER ASSOCIATED WITH NON ALCOHOLIC STÉATOHÉPATITE
JP5911470B2 (ja) 2010-04-16 2016-04-27 エーシー・イミューン・エス・アー アミロイドまたはアミロイド様タンパク質と関連する疾患を治療するための新規化合物
US9085555B2 (en) * 2011-01-04 2015-07-21 Novartis Ag Complement pathway modulators and uses thereof
WO2012177782A1 (en) 2011-06-20 2012-12-27 Myrexis, Inc. Compounds and therapeutic uses thereof
EP3524258A1 (en) 2011-06-22 2019-08-14 Apellis Pharmaceuticals, Inc. Methods of treating chronic disorders with complement inhibitors
NZ742005A (en) 2012-05-03 2019-04-26 Kala Pharmaceuticals Inc Pharmaceutical nanoparticles showing improved mucosal transport
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
US9579360B2 (en) 2012-06-20 2017-02-28 The Trustees Of The University Of Pennsylvania Methods of treating or preventing periodontitis and diseases associated with periodontitis
US20150191462A1 (en) * 2012-06-28 2015-07-09 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
ES2710491T3 (es) 2012-06-28 2019-04-25 Novartis Ag Moduladores de la vía del complemento y sus usos
US9464081B2 (en) 2012-06-28 2016-10-11 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6214647B2 (ja) 2012-06-28 2017-10-18 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
WO2014002053A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6155332B2 (ja) 2012-06-28 2017-06-28 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
ITMI20121156A1 (it) * 2012-06-29 2013-12-30 Consiglio Nazionale Ricerche Metodo di elaborazione di immagini di tomografia a coerenza ottica
WO2014005150A1 (en) 2012-06-29 2014-01-03 Novartis Ag Crystalline forms of l-(2-((lr,3s,5r)-3-( (2 -fluoro-3 - (trifluoromethoxy) phenyl) carbamoyl) - 2 -azabicycl o [3.1.0] hexan- 2 -yl) - 2 -oxoethyl) - 5 -methyl - 1h - pyrazolo [3, 4 -c] pyridine - 3 - carboxami de and salts thereof
WO2014002059A1 (en) 2012-06-29 2014-01-03 Novartis Ag CRYSTALLINE FORMS OF 1-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1Hpyrazolo[3,4-c]pyridine-3-carboxamide
MX2015000537A (es) * 2012-07-12 2015-05-11 Novartis Ag Moduladores de la senda del complemento y usos de los mismos.
SG11201500377UA (en) 2012-09-10 2015-02-27 Hoffmann La Roche 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
US9773428B2 (en) 2012-12-11 2017-09-26 Fluidity Software, Inc. Computerized system and method for teaching, learning, and assessing step by step solutions to stem problems
WO2014116880A1 (en) 2013-01-23 2014-07-31 Baerbel Rohrer Targeting constructs based on natural antibodies and uses thereof
JP2016169161A (ja) 2013-07-19 2016-09-23 大日本住友製薬株式会社 新規イミダゾピリジン化合物
SI3110418T1 (sl) 2014-02-25 2020-03-31 Achillion Pharmaceuticals, Inc. Arilne, heteroarilne in heterociklične spojine za zdravljenje s komplementom posredovanih motenj
WO2017035418A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for treatment of immune and inflammatory disorders
WO2017035351A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of medical disorders
AR106018A1 (es) 2015-08-26 2017-12-06 Achillion Pharmaceuticals Inc Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
WO2017035415A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of immune and inflammatory disorders
WO2017035362A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Use of complement pathway inhibitor compounds to mitigate adoptive t-cell therapy associated adverse immune responses
AR105808A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos de amida para el tratamiento de trastornos médicos
WO2017035413A2 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of immune and inflammatory disorders
WO2017035417A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of immune and inflammatory disorders
WO2017035401A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amide compounds for treatment of immune and inflammatory disorders
WO2017035361A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for the treatment of medical disorders
WO2017035352A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of medical disorders
WO2017035348A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of medical disorders
US10385097B2 (en) 2015-08-26 2019-08-20 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of medical disorders
WO2017035357A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of medical disorders
ES2908479T3 (es) 2015-08-26 2022-04-29 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos inmunitarios e inflamatorios
AR105809A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos médicos
WO2017035411A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of immune and inflammatory disorders
EP3340983B1 (en) 2015-08-26 2023-10-04 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders
AU2016367261A1 (en) 2015-12-11 2018-07-26 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
JP2019506159A (ja) 2016-01-20 2019-03-07 ヴィトリサ セラピューティクス， インコーポレイテッド Ｄ因子を阻害するための組成物および方法
WO2018160891A1 (en) 2017-03-01 2018-09-07 Achillion Pharmaceutical, Inc. Pharmaceutical compounds for treatment of medical disorders
EP3589287B1 (en) 2017-03-01 2022-09-14 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for treatment of medical disorders
EP3589628A4 (en) 2017-03-01 2021-03-31 Achillion Pharmaceuticals, Inc. ARYL, HETEROARYL AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISEASES

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