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HRP20140061T1 - Antagonisti histaminskog receptora h3 - Google Patents

Antagonisti histaminskog receptora h3 Download PDF

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Publication number
HRP20140061T1
HRP20140061T1 HRP20140061TT HRP20140061T HRP20140061T1 HR P20140061 T1 HRP20140061 T1 HR P20140061T1 HR P20140061T T HRP20140061T T HR P20140061TT HR P20140061 T HRP20140061 T HR P20140061T HR P20140061 T1 HRP20140061 T1 HR P20140061T1
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pyrrolidin
ylmethylphenyl
fluoro
alkyl
cis
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HRP20140061TT
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Travis T. Wager
Ramalakshmi Yegna Chandrasekaran
Todd William Butler
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Pfizer Products Inc.
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Publication of HRP20140061T1 publication Critical patent/HRP20140061T1/hr

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Claims (15)

1. Spoj formule I [image] , ili njegov stereoizomer, geometrijski izomer ili tautomerni oblik, ili farmaceutski prihvatljiva sol spoja formule I ili njegovog stereoizomera, geometrijskog izomera ili tautomernog oblika, naznačen time što: svakog od R1 i R2 se neovisno bira iz skupine koju čine vodik; C1-C8 alkil, izborno supstituiran s 1 do 4 halogena; C1-C4 alkilna skupina, izborno supstituirana sa supstituentom kojeg se bira iz skupine koju čine OH, jedan do četiri C1-C4 alkila, C3-C7 cikloalkil, C1-C4 dialkilamino, C6-C14 aril, izborno supstituiran s halogenom i izborno supstituiran s C6-C10 ariloksi, izborno supstituiranim s jednim do dva halogena, i 5-10-eročlani heteroaril, izborno supstituiran s C6-C10 arilnom skupinom i izborno supstituiran s jednom do tri C1-C4 alkilne skupine; C3-C7 cikloalkil; C6-C4 aril; -(C0-C3)alkil-O-(C1-C3)alkil, izborno supstituiran s (C1-C3)alkilom; -(C1-C3)alkil-C(=O)O-(C1-C3)alkil; 3-8-eročlani heterocikloalkil, izborno supstituiran s jednom ili više C1-C4 alkilkarbonilnih skupina; C6-C10 arilsulfonil, izborno supstituiran s jednim ili više C1-C2 alkila; 5-10-eročlani heteroaril; i C6-C14 aril-C0-C4 alkilen-O-C0-C4 alkil, gdje je svaki C0-C4 alkil i svaki C0-C4 alkilen izborno supstituiran s jednim do četiri C1-C4 alkila; ili izborno R1 i R2, zajedno s dušikom na kojeg su vezani, tvore 4-, 5-, 6- ili 7-eročlani zasićeni ili nezasićeni alifatski prsten, gdje je jedan od ugljika u navedenom alifatskom prstenu izborno zamijenjen s O, S, NR3 ili CO, te gdje je navedeni prsten izborno kondenziran s C6-C10 arilenom i izborno je supstituiran na ugljiku u prstenu sa supstituentom kojeg se bira iz skupine koju čine -OH, 5-10-eročlani heteroaril, izborno supstituiran s jednim ili više halogena i izborno supstituiran s jednim ili više C1-C2 alkila, C1-C4 alkoksi, izborno supstituiran s jednim ili više C1-C2 alkoksi i izborno supstituiran s jednim ili više C1-C4 dialkilaminokarbonila, i jedan ili dva C1-C4 alkila, izborno i neovisno supstituirana s jednim ili više C1-C2 alkoksi; gdje je R3 vodik; C1-C8 alkil, izborno supstituiran s 1 do 4 halogena; 5-10-eročlani heteroaril, izborno supstituiran sa supstituentom kojeg se bira iz skupine koju čine halogen, C1-C4 alkil, C1-C2 alkoksi, C6-C10 aril, C1-C4 alkilaminokarbonil i cijano; C1-C4 alkilna skupina, izborno supstituirana sa supstituentom kojeg se bira iz skupine koju čine C1-C2 alkoksikarbonil, 5-10-eročlani heteroaril, izborno supstituiran s jednim ili više C1-C2 alkila, jedan do četiri C1-C4 alkila, C3-C7 cikloalkil i C6-C14 aril; C6-C10 aril, izborno supstituiran s jednim ili dva C1-C2 alkila; C1-C4 alkilkarbonil; ili C6-C14 aril-C0-C4 alkilen-O-C0-C4 alkil, gdje je svaki C0-C4 alkil i svaki C0-C4 alkilen izborno supstituiran s jednim do četiri C1-C4 alkila; R4 se neovisno bira iz skupine koju čine vodik, C1-C4 alkil, C1-C4 alkoksil, halogen, nitril, -SO2C1-C4, -SO2NHC1-C4 i -C(=O)NHC1-C4; n je 0, 1, 2, 3 ili 4; R5 je OH, -O (C1-C3)alkil, halogen ili vodik; R6 je vodik, C1-C4 alkil, izborno supstituiran s 1 do 4 halogena, ili C3-C7 cikloalkil-C0-C4 alkil; R7 je vodik, C1-C8 alkil, izborno supstituiran s 1 do 4 halogena, ili C3-C7 cikloalkil-C0-C4 alkil, gdje je svaki C0-C4 izborno supstituiran s jednim do četiri C1-C4 alkila i; R8 je vodik, C1-C8 alkil, izborno supstituiran s 1 do 4 halogena, ili C3-C7 cikloalkil-C0-C4 alkil; ili izborno R7 i R8, zajedno s dušikom na kojeg su vezani, tvore 4-, 5-, 6- ili 7-eročlani heterociklički prsten, gdje je navedeni heterociklički prsten izborno supstituiran s jednim ili dva C1-C4 alkila; i gdje je jedan od ugljika u navedenom heterocikličkom prstenu koji je odmaknut za najmanje dva atoma navedenog dušika u navedenom heterocikličkom prstenu izborno zamijenjen s O, S, NR9 ili C=O, gdje je R9 vodik, C1-C8 alkil, izborno supstituiran s 1 do 4 halogena, ili C3-C7 cikloalkil-C0-C4 alkil, te gdje je svaki C0-C4 alkil izborno supstituiran s jednim do četiri C1-C4 alkila.
2. Spoj formule I, u skladu s patentnim zahtjevom 1, naznačen time što R7 i R8, zajedno s dušikom na kojeg su vezani, tvore 4-, 5-, 6- ili 7-eročlani heterociklički prsten, gdje je navedeni heterociklički prsten izborno supstituiran s jednim ili dva C1-C4 alkila; i gdje je jedan od ugljika u navedenom heterocikličkom prstenu koji je odmaknut za najmanje dva atoma navedenog dušika u navedenom heterocikličkom prstenu izborno zamijenjen s O, S, NR9 ili C=O, gdje je R9 vodik, C1-C8 alkil, izborno supstituiran s 1 do 4 halogena, ili C3-C7 cikloalkil-C0-C4 alkil, te gdje je svaki C0-C4 alkil izborno supstituiran s jednim do četiri C1-C4 alkila.
3. Spoj formule I, u skladu s patentnim zahtjevom 2, naznačen time što R7 i R8, zajedno s dušikom na kojeg su vezani, tvore 5- ili 6-eročlani zasićeni heterocikl.
4. Spoj formule I, u skladu s patentnim zahtjevom 3, naznačen time što je navedeni zasićeni heterocikl pirolidinilna skupina.
5. Spoj formule I, u skladu s patentnim zahtjevom 2, naznačen time što je R1 vodik; R4 i R5 su neovisno vodik ili F; R6 je vodik ili C1-C6 alkil.
6. Spoj formule 1, u skladu s patentnim zahtjevom 1, naznačen time što je R5 H ili F.
7. Spoj formule 1, u skladu s patentnim zahtjevom 2, naznačen time što je R5 H ili F.
8. cis-Ciklobutilni izomer ili trans-ciklobutilni izomer formule I, naznačen time što je u skladu s patentnim zahtjevom 1.
9. cis-Ciklobutilni izomer ili trans-ciklobutilni izomer formule I, naznačen time što je u skladu s patentnim zahtjevom 2.
10. Spoj formule I, u skladu s patentnim zahtjevom 1, naznačen time što se spoj bira iz skupine koju čine: dimetilamid cis-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; cis-[3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; etil(metil)amid cis-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; metilamid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; metilamid cis-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; cis-{3-[3-klor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]ciklobutil}pirolidin-1-ilmetanon; dimetilamid cis-3-(2,3-diklor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etilamid cis-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; izobutilamid cis-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; cis-(3-azabiciklo[3.2.2]non-3-il)-[3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]metanon; dimetilamid trans-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; trans-[3-(3-fluor4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; etil(metil)amid trans-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; metilamid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; metilamid trans-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; trans-{3-[3-klor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]ciklobutil}pirolidin-1-ilmetanon; dimetilamid trans-3-(2,3-diklor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etilamid trans-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; izobutilamid trans-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; trans-(3-azabiciklo[3.2.2]non-3-il)-[3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]metanon; cis-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; dimetilamid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; cis-[3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutil]piperidin-1-ilmetanon; izobutil(metil)amid cis-3-(-3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; ciklopropilmetilamid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; cis-[3-(3,5-difluor-pirolidin-1-ilmetilfenil)-3-fluorciklobutil]pirolidin-1-ilmetanon; metilamid cis-3-(2,6-difluor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; izobutilamid cis-3-(5-klor-2-fluor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; etilamid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; metil(tetrahidropiran-4-ilmetil)amid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; metilamid cis-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; cis-{3-[3-klor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]-3-fluorciklobutil}pirolidin-1-ilmetanon; ciklopropilmetil(metil)amid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; dimetilamid cis-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etilamid cis-3-fluor-3-[3-fluor-4-((S)-2-metilpirolidin-1-ilmetil)fenil]ciklobutankarboksilne kiseline; cis-[3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutil](2,3-dihidro-5H-benzo[f][1,4]oksazepin-4-il)-metanon; etilamid cis-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etil(metil)amid cis-3-fluor-3-(3-fluor-4-pirolidin-1--ilmetilfenil)ciklobutankarboksilne kiseline; metil(3-metilpiridin-2-ilmetil)amid cis-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; etilamid cis-3-fluor-3-[3-fluor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]ciklobutankarboksilne kiseline; izobutilamid cis-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; cis-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; cis-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; dimetilamid cis-3-(2,3-diklor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; trans-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; dimetilamid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; trans-[3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutil]piperidin-1-ilmetanon; izobutil(metil)amid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; ciklopropilmetilamid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; trans-[3-(3,5-difluor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutil]pirolidin-1-ilmetanon; metilamid trans-3-(2,6-difluor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; izobutilamid trans-3-(5-klor-2-fluor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; etilamid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; metil(tetrahidropiran-4-ilmetil)amid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; metilamid trans-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; trans-{3-[3-klor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]-3-fluorciklobutil}pirolidin-1-ilmetanon; ciklopropilmetil(metil)amid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; dimetilamid trans-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etilamid trans-3-fluor-3-[3-fluor-4-((S)-2-metilpirolidin-1-ilmetil)fenil]ciklobutankarboksilne kiseline; trans-[3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutil](2,3-dihidro-5H-benzo[f][1,4]oksazepin-4-il)-metanon; etilamid trans-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; etil(metil)amid trans-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; metil(3-metilpiridin-2-ilmetil)amid trans-3-(3-klor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline; etilamid trans-3-fluor-3-[3-fluor-4-((R)-2-metilpirolidin-1-ilmetil)fenil]ciklobutankarboksilne kiseline; izobutilamid trans-3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutankarboksilne kiseline; trans-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidine-1-ilmetanon; trans-[3-fluor-3-(3-fluor-4-pirolidin-1-ilmetilfenil)ciklobutil]pirolidin-1-ilmetanon; i dimetilamid trans-3-(2,3-diklor-4-pirolidin-1-ilmetilfenil)-3-fluorciklobutankarboksilne kiseline.
11. Spoj formule (I), u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u liječenju poremećaja ili stanja kod sisavca kojeg se može liječiti antagoniziranjem histaminskih receptora H3.
12. Spoj formule (I), u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u liječenju poremećaja ili stanja kod sisavca, koje se bira iz skupine koju čine depresija, poremećaji raspoloženja, shizofrenija, anksiozni poremećaji, kognitivni poremećaji, Alzheimerova bolest, poremećaj nedostatka pažnje, poremećaj nedostatka pažnje uz hiperaktivnost, psihotični poremećaji, poremećaji spavanja, pretilost, vrtoglavica, epilepsija, kinetoza, dišne bolesti, alergija, reakcije dišnih puteva uzrokovane alergijom, alergijski rinitis, nosna kongestija, alergijska kongestija, kongestija, hipotenzija, kardiovaskularna bolest, bolesti GI sustava, hiper- i hipomotilitet i izlučivanje kiseline u gastrointestinalom sustavu.
13. Spoj u skladu s patentnim zahtjevom 12, naznačen time što se poremećaj ili stanje bira iz skupine koju čine anksiozni poremećaji, poremećaj nedostatka pažnje uz hiperaktivnost, poremećaj nedostatka pažnje, dišne bolesti, pretilost, kognitivni poremećaji i psihotični poremećaji.
14. Spoj u skladu s patentnim zahtjevom 12, naznačen time što poremećaj ili stanje je dišna bolest, koju se bira iz skupine koju čine sindrom dišnog distresa kod odraslih, akutni sindrom dišnog distresa, bronhitis, kronični bronhitis, kronična opstruktivna plućna bolest, cistična fibroza, astma, emfizem, rinitis i kronični sinusitis.
15. Postupak dobivanja spoja formule I u patentnom zahtjevu 1, naznačen time što se postupak sastoji u koraku reakcije spoja formule 4 [image] s organometalnim reagensom dobivenim iz spoja formule 2 [image] , uz izravno dobivanje amida kako bi se dobilo spoj formule I.
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Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
DK2124933T3 (da) 2007-01-22 2012-11-19 Pfizer Prod Inc Tosylatsalt af en terapeutisk forbindelse og farmaceutiske sammensætninger deraf
WO2008108445A1 (ja) 2007-03-07 2008-09-12 Takeda Pharmaceutical Company Limited ベンゾオキサゼピン誘導体およびその用途
DK2195293T3 (da) 2007-08-22 2014-02-03 Astrazeneca Ab Cyclopropylamidderivater
AU2008332880C1 (en) * 2007-12-07 2012-07-19 Pfizer Inc. Tosylate salt of trans-N-isobutyl-3-fluoro-3- [3-fluoro-4- (pyrrolidin-1-yl-methyl) -phenyl] cyclobut anecarboxamide
US8691804B2 (en) 2008-05-08 2014-04-08 Evotec Ag Azetidines and cyclobutanes as histamine H3 receptor antagonists
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
ES2541857T3 (es) 2010-02-18 2015-07-27 Astrazeneca Ab Procesos para preparar ciclopropilamidas e intermedios asociados con estas
JP5767393B2 (ja) 2011-03-31 2015-08-19 ファイザー・インク 新規二環式ピリジノン
WO2012172449A1 (en) 2011-06-13 2012-12-20 Pfizer Inc. Lactams as beta secretase inhibitors
ES2605565T3 (es) 2011-08-31 2017-03-15 Pfizer Inc Compuestos de hexahidropirano [3,4-D][1,3]tiazin-2-amina
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
ES2585262T3 (es) 2012-05-04 2016-10-04 Pfizer Inc Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2
MD20140130A2 (ro) 2012-06-29 2015-04-30 Pfizer Inc. 4-(amino-substituite)-7H-pirolo[2,3-d]pirimidine noi ca inhibitori de LRRK2
US9260455B2 (en) 2012-09-20 2016-02-16 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
JP2016502978A (ja) 2012-12-11 2016-02-01 ファイザー・インク ＢＡＣＥ１の阻害剤としてのヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
WO2014097038A1 (en) 2012-12-19 2014-06-26 Pfizer Inc. CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS
EP2956458B1 (en) 2013-02-13 2017-08-09 Pfizer Inc Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
MX2015010714A (es) 2013-02-19 2016-06-14 Pfizer Compuestos de azabencimidazol.
ES2742078T3 (es) 2013-10-04 2020-02-13 Pfizer Piridonas bicíclicas novedosas como moduladores de gamma-secretasa
WO2015092592A1 (en) 2013-12-17 2015-06-25 Pfizer Inc. Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
CR20160454A (es) 2014-04-01 2016-12-06 Pfizer CROMENO Y 1,1 a,2,7b—TETRAHIDROCICLOPROPA[C]CROMENO PIRIDOPIRAZINADIONAS NOVEDOSAS
PE20170327A1 (es) 2014-04-10 2017-04-21 Pfizer 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS
US10131669B2 (en) 2014-07-24 2018-11-20 Pfizer Inc. Pyrazolopyrimidine compounds
EA031201B1 (ru) 2014-08-06 2018-11-30 Пфайзер Инк. Соединения имидазопиридазина
EA033423B1 (ru) 2015-02-03 2019-10-31 Pfizer Циклопропанбензофуранилпиридопиразиндионы
CN107787322B (zh) 2015-06-17 2023-07-07 辉瑞大药厂 三环化合物以及它们作为磷酸二酯酶抑制剂的用途
MX2018003215A (es) 2015-09-14 2018-06-08 Pfizer Derivados de imidazo[4,5-c]quinolina e imidazo[4,5-c][1,5]naftirid ina novedosos como inhibidores de lrrk2.
JP2018531923A (ja) 2015-09-24 2018-11-01 ファイザー・インク Ｎ−［２−（２−アミノ−６，６−二置換−４，４ａ，５，６−テトラヒドロピラノ［３，４−ｄ］［１，３］チアジン−８ａ（８Ｈ）−イル）−１，３−チアゾール−４−イル］アミド
EP3353182A1 (en) 2015-09-24 2018-08-01 Pfizer Inc Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
JP2018534251A (ja) 2015-09-24 2018-11-22 ファイザー・インク Ｂａｃｅ阻害剤として有用なｎ−［２−（３−アミノ−２，５−ジメチル−１，１−ジオキシド−５，６−ジヒドロ−２ｈ−１，２，４−チアジアジン−５−イル）−１，３−チアゾール−４−イル］アミド
US10323042B2 (en) 2016-02-23 2019-06-18 Pfizer Inc. 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds
ES2878160T3 (es) 2016-07-01 2021-11-18 Pfizer Derivados de 5,7-dihidro-pirrolo-piridina para el tratamiento de enfermedades neurológicas y neurodegenerativas
CN111201226B (zh) 2017-03-10 2022-07-22 辉瑞大药厂 环状被取代的咪唑并[4,5-c]喹啉衍生物
JP7219223B2 (ja) 2017-03-10 2023-02-07 ファイザー・インク ＬＲＲＫ２阻害剤としての新規のイミダゾ［４，５－ｃ］キノリン誘導体
CN110997693A (zh) 2017-06-07 2020-04-10 阿德克斯公司 τ聚集抑制剂
PT3642202T (pt) 2017-06-22 2023-02-02 Pfizer Derivados de dihidro-pirrolo-piridina
EP3668886A2 (en) 2017-08-18 2020-06-24 Adrx, Inc. Tau aggregation peptide inhibitors
FI3768669T3 (fi) 2018-03-23 2023-04-26 Pfizer Piperatsiiniatsaspirojohdannaisia

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6559140B2 (en) * 2000-03-09 2003-05-06 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
WO2002076925A2 (en) 2001-03-23 2002-10-03 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
US7671047B2 (en) * 2002-06-19 2010-03-02 Sanofi-Aventis Deutschland Gmbh Cationically substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
JP2004131497A (ja) * 2002-09-18 2004-04-30 Satoshi Shuto シスシクロプロパン誘導体
BRPI0413048A (pt) * 2003-07-29 2006-10-17 Novo Nordisk As composto, composição farmacêutica, uso de um composto, e, método para o tratamento de distúrbios ou doenças relacionados com o receptor h3 da histamina
WO2005028438A1 (ja) * 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. 新規ピペリジン誘導体
JP2007519707A (ja) 2004-02-02 2007-07-19 ファイザー・プロダクツ・インク ヒスタミン−３受容体モジュレーター
DE602005018758D1 (de) * 2004-04-01 2010-02-25 Lilly Co Eli Am histamin-h3-rezeptor wirksame mittel, herstellung und therapeutische anwendungen
US7456164B2 (en) * 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
EP1595881A1 (en) * 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
ES2354569T3 (es) 2005-06-22 2011-03-16 Pfizer Products Inc. Antagonistas del receptor de histamina-3.
US8158673B2 (en) * 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
DK2124933T3 (da) * 2007-01-22 2012-11-19 Pfizer Prod Inc Tosylatsalt af en terapeutisk forbindelse og farmaceutiske sammensætninger deraf

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