CO5190696A1 - ANTAGONISTS OF IL-8 RECEIVERS - Google Patents
ANTAGONISTS OF IL-8 RECEIVERSInfo
- Publication number
- CO5190696A1 CO5190696A1 CO00043846A CO00043846A CO5190696A1 CO 5190696 A1 CO5190696 A1 CO 5190696A1 CO 00043846 A CO00043846 A CO 00043846A CO 00043846 A CO00043846 A CO 00043846A CO 5190696 A1 CO5190696 A1 CO 5190696A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- heteroaryl
- optionally substituted
- aryl
- heterocycle
- Prior art date
Links
- 108090001007 Interleukin-8 Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 17
- 125000000623 heterocyclic group Chemical group 0.000 abstract 16
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 14
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 10
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical group 0.000 abstract 9
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 8
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 4
- 125000004447 heteroarylalkenyl group Chemical group 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000004104 aryloxy group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 108010012236 Chemokines Proteins 0.000 abstract 2
- 102000019034 Chemokines Human genes 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 2
- 241000700605 Viruses Species 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 150000001540 azides Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000007565 gingivitis Diseases 0.000 abstract 1
- 230000003394 haemopoietic effect Effects 0.000 abstract 1
- 208000006454 hepatitis Diseases 0.000 abstract 1
- 231100000283 hepatitis Toxicity 0.000 abstract 1
- -1 heteroaryl-C1-4alkyl Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 201000004792 malaria Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000000241 respiratory effect Effects 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
- 241001529453 unidentified herpesvirus Species 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un método de tratamiento de un estado de enfermedadmediado por quimiocinas en un mamífero que se encuentra en necesidad de aquél, en el que la quimiocina se fija a unreceptor a o ß de IL-8, seleccionado del grupo constituido por malaria, restenosis, angiogénesis, ateroesclerosis, osteoporosis, gingivitis, liberación de células primordiales hematopoyéticas no deseada y enfermedades causadas por virus respiratorios, herpesvirus y virus de hepatitis, método que comprende administrar a dicho mamífero una cantidad eficaz de un compuesto de acuerdo con la fórmula:<EMI FILE="00043846_1" ID="1" IMF=JPEG >en la cualR es -NH-C(X2) -NH- (CR13R14)v-Z;<EMI FILE="00043846_2" ID="2" IMF=JPEG >Z es W, HET, , un alquilo C1-10 opcionalmente sustituido, un alquenilo C2-10 opcionalmente sustituido, o un alquinilo C2-10 opcionalmente sustituido;X es C(X1)2, C(O), C(S), S(O)2, PO(OR4), o C=N-R19;X1 es independientemente hidrógeno, halógeno, alquilo C1-10, NR4R5, alquil C1-10-NR4R5, C(O)NR4R5, alquilo C1-10 opcionalmente sustituido, alcoxi C1-10, alcoxi C1-10 sustituido con halógeno, hidroxi, arilo, aril-alquilo C1-4, ariloxi, aril-alquiloxi C1-4, heteroarilo, heteroarilalquilo, heterociclo, heterociclo-alquilo C1-4, o heteroaril-alquiloxi C1-4;X2 es =O, o =S;R1 se selecciona de manera independiente de hidrógeno; halógeno; nitro; ciano; alquilo C1-10 sustituido con halógeno; alquilo C1-10; alquenilo C2-10; alcoxi C1-10; alcoxi C1-10 sustituido con halógeno; azida; (CR8R8)qS(O)tR4; hidroxi; hidroxi-alquilo C1-4; arilo; aril-alquilo C1-4; ariloxi; aril-alquiloxi C1-4; heteroarilo; heteroarilalquilo; heterociclo, heterociclo-alquilo C1-4; heteroaril-alquiloxi C1-4; aril-alquenilo C2-10; heteroaril-alquenilo C2-10, heterociclo-alquenilo C2-10; (CR8R8)qNR4R5; alquenil C2-10-C(O)NR4R5; (CR8R8)qC(O)NR4R5; (CR8R8)qC(O)NR4R10; S(O)3R8; (CR8-R8)qC(O)R11; alquenil C2-10-C(O)R11; alquenil C2-10-C(O)OR11; C(O)R11; (CR8R8)qC(O)OR12; (CR8R8)qOC(O)R11; (CR8R8)qC(NR4)-NR4-R5; (CR8R8)qNR4C(NR5)R11; (CR8R8)qNR4C(O)R11; (CR8R8)qNHS-(O)2R17; (CR8N8)qS(O)2NR4R5; o dos restos R1 juntos pueden formar O-(CH2)SO o un anillo saturado o insaturado de 5 a 6 miembros; y en los cuales los restos que contienen arilo, heteroarilo, y heterociclo pueden estar todos ellos opcionalmente sustituidos; n es un número entero que tiene un valor de 1 a 3;- 2 -m es un número entero que tiene un valor de 1 a 3;q es 0, o un número entero que tiene un valor de 1 a 10;s es un número entero que tiene un valor de 1 a 3;t es 0, o un número entero que tiene un valor de 1 ó 2;v es 0, o un número entero que tiene un valor de 1 a 4;p es un número entero que tiene un valor de 1 a 3;HET es un heteroarilo opcionalmente sustituido;R4 y R5 son de manera independiente hidrógeno, alquilo C1-4 opcionalmente sustituido, arilo opcionalmente sustituido, aril-alquilo C1-4 opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroaril-alquilo C1-4 opcionalmente sustituido, heterociclo, o heterociclo-alquilo C1-4, o R4 y R5, junto con el nitrógeno al que están unidos forman un anillo de 5 a 7 miernbros que puede contener opcionalmente un heteroátomo adicional seleccionado de O/N/S;Y se selecciona de manera independiente de hidrógeno; halógeno, nitro; ciano; alquilo C1-10 sustituido con halógeno; alquilo C1-10; alquenilo C2-10; alcoxi C1-10; alcoxi C1-10 sustituido con halógeno; azida; (CR8R8)qS(O)tR4; hidroxi; hidroxi-alquilo C1-4; arilo; aril-alquilo C1-4, ariloxi; aril-alquiloxi C1-4; heteroarilo; heteroarilalquilo; heteroaril-alquiloxi C1-4; heterociclo, heterociclo-alquilo C1-4; aril-alquenilo C2-10; heteroaril-alquenilo C2-10; heterociclo-alquenilo C2-10; (CR8R8)qNR4R5; alquenil C2-10-C(O)NR4R5;(CR8R8)qC(O)NR4R5; (CR8R8)qC(O)NR4R10; S(O)3R8;(CR8R8)qC(O)R11; alquenil C2-10-C(O)R11; alquenil C2-10-C(O)OR11; (CR8R8)qC(O)OR12; (CR8R8)qOC(O)R11; (CR8R8)qNR4C(O)-R11; (CR8R8)qC(NR4)NR4R5;(CR8R8)qNR4C(NR5)R11; (CR8R8)qNHS(O)2Ra;(CR8R8)qS(O)2NR4R5; o dos restos y juntos pueden formar O-(CH2)sO o un anillo saturado o insaturado de 5 a 6 miembros; y en los cuales los restos que contienen arilo, heteroarilo, y heterociclo pueden estar todos ellos opcionalmente sustituidos;R6 y R7 son de manera independiente hidrógeno o un grupo alquilo C1-4, O R6 y R7 junto con el nitrógeno al cual están unidos forman un anillo de 5 a 7 miembros, anillo que puede contener opcionalmente un heteroátomo adicional, heteroátomo que se selecciona de oxígeno, nitrógeno o azufre;R8 es independientemente hidrógeno o alquilo C1-4;R10 es alquil C1-10-C(O)2R8;R11 es hidrógeno, alquilo C1-4, arilo opcionalmente sustituido, aril-alquilo C1-4 opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroaril-alquilo C1-4 opcionalmente sustituido, heterociclo opcionalmente sustituido, o heterociclo-alquilo C1-4 opcionalmente sustituido;R12 es hidrógeno, alquilo C1-10, arilo opcionalmente sustituido o arilalquilo opcionalmente sustituido;R13 y R14 son de manera independiente hidrógeno, alquilo C1-4 opcionalmente sustituido, o uno de R13 y R14 puede ser arilo opcionalmente sustituido;R15 y R16 son independientemente hidrógeno, o un alquilo C1-4 opcionalmente sustituido;R17 es alquilo C1-4, arilo, arilalquilo, heteroarilo, hetero-aril-alquilo C1-4, heterociclo, o heterociclo-alquilo C1-4, en los cuales los restos arilo, heteroarilo y heterociclo pueden estar todos ellos opcionalmente sustituidos;R18 es hidrógeno, alquilo C1-10 opcionalmente sustituido, alcoxi C1-10, alcoxi C1-10 sustituido con halógeno, hidroxi, aril-alquilo C1-4, aril-alquenilo C2-4, heteroarilo, heteroaril-alquilo C1-4, heteroaril-alquenilo C2-4, heterociclo, o heterociclo-alquilo C1-4, en los cuales los restos que contienen arilo, heteroarilo y heterociclo pueden estar todos ellos opcionalmente sustituidos;R19 es ciano, nitro, S(O)2NR4R5, S(O)2R17, alquilo, aril-alquilo C1-4, aril-alquenilo C2-4, heteroarilo, heteroaril-alquilo C1-4, heteroaril-alquenilo C2-4, heterociclo, o heterociclo-alquilo C1-4, en los cuales los restos que contienen alquilo, arilo, heteroarilo y heterociclo pueden estar todos ellos opcionalmente sustituidos;Ra es NR6R7, alquilo, aril-alquilo C1-4, aril-alquenilo C2-4, heteroarilo, heteroaril-alquilo C1-4, heteroaril-alquenilo C2-4, heterociclo, o heterociclo-alquilo C1-4, en los cuales los restos que contienen arilo, heteroarilo y heterociclo pueden estar todos ellos opcionalmente sustituidos;W es<EMI FILE="00043846_3" ID="3" IMF=JPEG >el anillo que contiene E se selecciona opcionalmente de<EMI FILE="00043846_4" ID="4" IMF=JPEG >;designando el asterisco * el punto de unión del anillo;o una de sus sales farmacéuticamenteaceptables.A method of treating a state of chemokine-mediated disease in a mammal that is in need thereof, in which the chemokine is fixed to an α-β receptor of IL-8, selected from the group consisting of malaria, restenosis, angiogenesis, atherosclerosis , osteoporosis, gingivitis, release of unwanted hematopoietic primordial cells and diseases caused by respiratory viruses, herpesviruses and hepatitis viruses, a method comprising administering to said mammal an effective amount of a compound according to the formula: <EMI FILE = "00043846_1 "ID =" 1 "MFI = JPEG> in which R is -NH-C (X2) -NH- (CR13R14) vZ; <EMI FILE =" 00043846_2 "ID =" 2 "MFI = JPEG> Z is W, HET ,, an optionally substituted C1-10 alkyl, an optionally substituted C2-10 alkenyl, or an optionally substituted C2-10 alkynyl; X is C (X1) 2, C (O), C (S), S (O) 2 , PO (OR4), or C = N-R19; X1 is independently hydrogen, halogen, C1-10 alkyl, NR4R5, C1-10 alkyl-NR4R5, C (O) NR4R5, a optionally substituted C1-10 alkyl, C1-10 alkoxy, halogen substituted C1-10 alkoxy, hydroxy, aryl, arylC 1-4 alkyl, aryloxy, arylC 1-4 alkyloxy, heteroaryl, heteroarylalkyl, heterocycle, heterocycle-C1 alkyl -4, or heteroarylC 1-4 alkyloxy; X2 is = O, or = S; R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-10 alkyl substituted with halogen; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; C1-10 alkoxy substituted with halogen; azide; (CR8R8) qS (O) tR4; hydroxy; hydroxyC 1-4 alkyl; aryl; arylC 1-4 alkyl; aryloxy; C 1-4 aryl-alkyloxy; heteroaryl; heteroarylalkyl; heterocycle, heterocycle-C1-4 alkyl; heteroaryl-C1-4 alkyloxy; C2-10 aryl-alkenyl; C2-10 heteroaryl-alkenyl, C2-10 heterocyclo-alkenyl; (CR8R8) qNR4R5; C2-10-C alkenyl (O) NR4R5; (CR8R8) qC (O) NR4R5; (CR8R8) qC (O) NR4R10; S (O) 3R8; (CR8-R8) qC (O) R11; C2-10-C (O) R11 alkenyl; C2-10-C (O) alkenyl OR11; C (O) R11; (CR8R8) qC (O) OR12; (CR8R8) qOC (O) R11; (CR8R8) qC (NR4) -NR4-R5; (CR8R8) qNR4C (NR5) R11; (CR8R8) qNR4C (O) R11; (CR8R8) qNHS- (O) 2R17; (CR8N8) qS (O) 2NR4R5; or two R1 moieties together can form O- (CH2) SO or a saturated or unsaturated ring of 5 to 6 members; and in which the moieties containing aryl, heteroaryl, and heterocycle may all be optionally substituted; n is an integer that has a value of 1 to 3; - 2 -m is an integer that has a value of 1 to 3; q is 0, or an integer that has a value of 1 to 10; s is an integer that has a value of 1 to 3; t is 0, or an integer that has a value of 1 or 2; v is 0, or an integer that has a value of 1 to 4; p is a number integer having a value of 1 to 3; HET is an optionally substituted heteroaryl; R4 and R5 are independently hydrogen, optionally substituted C1-4 alkyl, optionally substituted aryl, optionally substituted aryl-C1-4 alkyl, optionally substituted heteroaryl, optionally substituted heteroaryl-C1-4alkyl, heterocycle, or heterocycle-C1-4alkyl, or R4 and R5, together with the nitrogen to which they are attached form a ring of 5 to 7 members which may optionally contain an additional heteroatom selected from O / N / S; Y is independently selected from hydrogen; halogen, nitro; cyano; C1-10 alkyl substituted with halogen; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; C1-10 alkoxy substituted with halogen; azide; (CR8R8) qS (O) tR4; hydroxy; hydroxyC 1-4 alkyl; aryl; arylC 1-4 alkyl, aryloxy; C 1-4 aryl-alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl-C1-4 alkyloxy; heterocycle, heterocycle-C1-4 alkyl; C2-10 aryl-alkenyl; C2-10 heteroaryl-alkenyl; C2-10 heterocyclo-alkenyl; (CR8R8) qNR4R5; C2-10-C (O) NR4R5 alkenyl; (CR8R8) qC (O) NR4R5; (CR8R8) qC (O) NR4R10; S (O) 3R8; (CR8R8) qC (O) R11; C2-10-C (O) R11 alkenyl; C2-10-C (O) alkenyl OR11; (CR8R8) qC (O) OR12; (CR8R8) qOC (O) R11; (CR8R8) qNR4C (O) -R11; (CR8R8) qC (NR4) NR4R5; (CR8R8) qNR4C (NR5) R11; (CR8R8) qNHS (O) 2Ra; (CR8R8) qS (O) 2NR4R5; or two moieties and together they can form O- (CH2) sO or a saturated or unsaturated ring of 5 to 6 members; and in which the moieties containing aryl, heteroaryl, and heterocycle may all be optionally substituted; R6 and R7 are independently hydrogen or a C1-4 alkyl group, O R6 and R7 together with the nitrogen to which they are attached form a 5 to 7-membered ring, a ring that may optionally contain an additional heteroatom, a heteroatom selected from oxygen, nitrogen or sulfur; R8 is independently hydrogen or C1-4 alkyl; R10 is C1-10-C (O) 2R8 alkyl R11 is hydrogen, C1-4 alkyl, optionally substituted aryl, optionally substituted aryl-C1-4 alkyl, optionally substituted heteroaryl, optionally substituted heteroaryl-C1-4 alkyl, optionally substituted heterocycle, or optionally substituted heterocycle-C1-4 alkyl; R12 is hydrogen, C1-10 alkyl, optionally substituted aryl or optionally substituted arylalkyl; R13 and R14 are independently hydrogen, optionally substituted C1-4 alkyl, or one of R13 and R14 p it may be optionally substituted aryl; R15 and R16 are independently hydrogen, or an optionally substituted C1-4 alkyl; R17 is C1-4 alkyl, aryl, arylalkyl, heteroaryl, hetero-aryl-C1-4 alkyl, heterocycle, or heterocycle-alkyl C1-4, in which the aryl, heteroaryl and heterocycle moieties may all be optionally substituted; R18 is hydrogen, optionally substituted C1-10 alkyl, C1-10 alkoxy, C1-10 alkoxy substituted with halogen, hydroxy, aryl-alkyl C1-4, C2-4 aryl-alkenyl, heteroaryl, C1-4 heteroaryl-alkyl, C2-4 heteroaryl-alkenyl, heterocycle, or C1-4 heterocycle, in which the aryl, heteroaryl and heterocycle containing moieties may be all optionally substituted; R19 is cyano, nitro, S (O) 2NR4R5, S (O) 2R17, alkyl, aryl-C1-4alkyl, aryl-C2-4alkenyl, heteroaryl, heteroaryl-C1-4alkyl, heteroaryl -C2-4alkenyl, heterocycle, or heterocycle-C1-4alkyl, in which the moieties containing alkyl, aryl, heteroaryl and heterocycle may all be optionally substituted; Ra is NR6R7, alkyl, arylC1-4alkyl, C2-4 aryl-alkenyl, heteroaryl, heteroarylC1-4alkyl, C2-4 heteroaryl-alkenyl, heterocycle, or heterocycle -C1-4 alkyl, in which the moieties containing aryl, heteroaryl and heterocycle may all be optionally substituted; W is <EMI FILE = "00043846_3" ID = "3" IMF = JPEG> the ring containing E is selected optionally of <EMI FILE = "00043846_4" ID = "4" MFI = JPEG>; designating the asterisk * the point of attachment of the ring; or one of its pharmaceutically acceptable salts.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14002499P | 1999-06-16 | 1999-06-16 |
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| Publication Number | Publication Date |
|---|---|
| CO5190696A1 true CO5190696A1 (en) | 2002-08-29 |
Family
ID=22489379
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00043846A CO5190696A1 (en) | 1999-06-16 | 2000-06-13 | ANTAGONISTS OF IL-8 RECEIVERS |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP1185265A4 (en) |
| JP (1) | JP2003501463A (en) |
| KR (1) | KR20020015347A (en) |
| CN (1) | CN1356899A (en) |
| AR (1) | AR024350A1 (en) |
| AU (1) | AU766235B2 (en) |
| BR (1) | BR0011122A (en) |
| CA (1) | CA2377386A1 (en) |
| CO (1) | CO5190696A1 (en) |
| CZ (1) | CZ20014472A3 (en) |
| HU (1) | HUP0201582A3 (en) |
| IL (1) | IL145762A0 (en) |
| MX (1) | MXPA01013005A (en) |
| NO (1) | NO20016052D0 (en) |
| NZ (1) | NZ514696A (en) |
| PL (1) | PL352213A1 (en) |
| TR (1) | TR200103638T2 (en) |
| WO (1) | WO2000076501A1 (en) |
| ZA (1) | ZA200109480B (en) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY139601A (en) | 2002-10-09 | 2009-10-30 | Schering Corp | Thiadiazoledioxides and thiadiazoleoxides as cxc-and cc-chemokine receptor ligands |
| US7094794B2 (en) | 2003-07-28 | 2006-08-22 | Sanofi-Aventis Deutschland Gmbh | Substituted thiazole-benzoisothiazole dioxide derivatives, process for their preparation and their use |
| DE10334309A1 (en) * | 2003-07-28 | 2005-03-03 | Aventis Pharma Deutschland Gmbh | Substituted thiazole-Benzoisothiazoldioxidderivate, processes for their preparation and their use |
| CA2536151A1 (en) | 2003-08-21 | 2005-03-10 | Osi Pharmaceuticals, Inc. | N-substituted pyrazolyl-amidyl-benzimidazolyl c-kit inhibitors |
| CA2535896A1 (en) | 2003-08-21 | 2005-03-10 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazolyl c-kit inhibitors |
| US7442709B2 (en) | 2003-08-21 | 2008-10-28 | Osi Pharmaceuticals, Inc. | N3-substituted imidazopyridine c-Kit inhibitors |
| US7338968B2 (en) | 2003-12-19 | 2008-03-04 | Schering Corporation | Thiadiazoles AS CXC- and CC- chemokine receptor ligands |
| US7582673B2 (en) | 2004-10-21 | 2009-09-01 | High Point Pharmaceuticals, Llc | Bissulfonamide compounds as agonists of GalR1, compositions, and methods of use |
| ATE521604T1 (en) | 2004-12-01 | 2011-09-15 | Osi Pharm Inc | N-SUBSTITUTED BENZIMIDAZOLYL-C KIT INHIBITORS AND COMBINATORY BENZIMIDAZOLE LIBRARY |
| JP2013502444A (en) | 2009-08-24 | 2013-01-24 | アスセピオン ファーマスーティカル、インコーポレイテッド | 5,6-Bicycloheteroaryl-containing urea compounds as kinase inhibitors |
| EP2377850A1 (en) * | 2010-03-30 | 2011-10-19 | Pharmeste S.r.l. | TRPV1 vanilloid receptor antagonists with a bicyclic portion |
| CN102060780B (en) | 2010-12-27 | 2014-11-05 | 雅本化学股份有限公司 | Preparation method of 2-(N-substituted).-aminobenzimidazole derivative |
| CN111116502A (en) * | 2018-10-30 | 2020-05-08 | 中国石油化工股份有限公司 | One-step method for synthesizing benzotriazole |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| ZA921120B (en) * | 1991-02-19 | 1993-01-27 | Smithkline Beecham Corp | Cytokine inhibitors |
| KR20000070368A (en) * | 1997-01-23 | 2000-11-25 | 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 | IL-8 Receptor Antagonists |
-
2000
- 2000-06-13 CO CO00043846A patent/CO5190696A1/en not_active Application Discontinuation
- 2000-06-14 AR ARP000102922A patent/AR024350A1/en not_active Application Discontinuation
- 2000-06-15 CA CA002377386A patent/CA2377386A1/en not_active Abandoned
- 2000-06-15 PL PL00352213A patent/PL352213A1/en not_active Application Discontinuation
- 2000-06-15 CZ CZ20014472A patent/CZ20014472A3/en unknown
- 2000-06-15 KR KR1020017016144A patent/KR20020015347A/en not_active Application Discontinuation
- 2000-06-15 BR BR0011122-8A patent/BR0011122A/en not_active IP Right Cessation
- 2000-06-15 CN CN00809090A patent/CN1356899A/en active Pending
- 2000-06-15 WO PCT/US2000/016506 patent/WO2000076501A1/en not_active Application Discontinuation
- 2000-06-15 TR TR2001/03638T patent/TR200103638T2/en unknown
- 2000-06-15 IL IL14576200A patent/IL145762A0/en unknown
- 2000-06-15 JP JP2001502834A patent/JP2003501463A/en not_active Withdrawn
- 2000-06-15 EP EP00941455A patent/EP1185265A4/en not_active Withdrawn
- 2000-06-15 AU AU56161/00A patent/AU766235B2/en not_active Ceased
- 2000-06-15 HU HU0201582A patent/HUP0201582A3/en unknown
- 2000-06-15 NZ NZ514696A patent/NZ514696A/en unknown
- 2000-06-15 MX MXPA01013005A patent/MXPA01013005A/en unknown
- 2000-11-16 ZA ZA200109480A patent/ZA200109480B/en unknown
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2001
- 2001-12-11 NO NO20016052A patent/NO20016052D0/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20020015347A (en) | 2002-02-27 |
| NZ514696A (en) | 2004-03-26 |
| AU5616100A (en) | 2001-01-02 |
| CZ20014472A3 (en) | 2002-06-12 |
| ZA200109480B (en) | 2002-11-18 |
| MXPA01013005A (en) | 2002-07-02 |
| JP2003501463A (en) | 2003-01-14 |
| EP1185265A4 (en) | 2004-02-04 |
| TR200103638T2 (en) | 2002-04-22 |
| NO20016052L (en) | 2001-12-11 |
| CA2377386A1 (en) | 2000-12-21 |
| HUP0201582A2 (en) | 2002-12-28 |
| BR0011122A (en) | 2002-02-26 |
| AU766235B2 (en) | 2003-10-09 |
| PL352213A1 (en) | 2003-08-11 |
| WO2000076501A1 (en) | 2000-12-21 |
| AR024350A1 (en) | 2002-10-02 |
| IL145762A0 (en) | 2002-07-25 |
| CN1356899A (en) | 2002-07-03 |
| HUP0201582A3 (en) | 2003-02-28 |
| EP1185265A1 (en) | 2002-03-13 |
| NO20016052D0 (en) | 2001-12-11 |
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