AR041207A1 - Pirazolo piridinas - Google Patents
Pirazolo piridinasInfo
- Publication number
- AR041207A1 AR041207A1 ARP030103250A ARP030103250A AR041207A1 AR 041207 A1 AR041207 A1 AR 041207A1 AR P030103250 A ARP030103250 A AR P030103250A AR P030103250 A ARP030103250 A AR P030103250A AR 041207 A1 AR041207 A1 AR 041207A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocycloalkyl
- cycloalkyl
- alkyl
- amino
- heteroaryl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
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- 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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Abstract
Los compuestos de la fórmula (1) poseen una afinidad inesperadamente alta para Alk5 y/o Alk 4 y pueden ser útiles como antagonistas para los mismos, a fin de prevenir y/o tratar numerosas enfermedades, incluyendo trastornos fibróticos. En una forma,la presente se caracteriza por un compuesto de la fórmula (1). Reivindicación 1: Un compuesto de la siguiente fórmula (1) en donde cada uno de X1, X2, X3, y X4 es independientemente CRx o N; a condición de que solamente dos de X1, X2, X3 y X4pueden ser N simultáneamente; cada uno de Y1 e Y2 es independientemente CRy o N; a condición de que por lo menos uno de Y1 e Y2 sea N; cada R1 es independientemente alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, ciano,guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, alquilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tioureas, sulfamoilo, sulfamida, carbamoilo,cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo, arilo, ariloxi, arilsulfanilo, aroilo, heteroarilo, heteroariloxi, heteroarilsulfanilo, o heteroaroilo; cada R2 esindependientemente alquilo, alquenilo, alquinilo, acilo, halo, hidroxi, -NH2, -NH(alquilo), -NH(alquilo)2, -NH(cicloalquilo), -N(alquil)(cicloalquilo), -NH(heterociclo alquilo), -NH(heteroarilo), NH-heterocicloalquilo, -NH-alquil-heteroarilo,-NH(aralquilo), cicloalquilo, (cicloalquil)alquilo, arilo, aralquilo, aroilo, heterocicloalquilo, (heterocicloalquil)alquilo, heteroarilo, heteroaralquilo, heteroaroilo, nitro, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alcoxi,cicloalquiloxi, cicloalquil-alcoxi, ariloxi, arilalcoxi, heterocicloalquiloxi, (heterocicloalquil)alcoxi, heteroariloxi, heteroarilalcoxi, alquilsulfanilo, cicloalquilsulfanilo, (cicloalquil)alquilsulfanilo, arilsulfanilo, aralquilsulfanilo,heterocicloalquilsulfanilo, (heterocicloalquil)alquil sulfanilo, heteroarilsulfanilo, heteroaril alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, aminosulfonilo, alquilcarbonilamino, cicloalquilcarbonilamino, (cicloalquil)alquilcarbonilamino, arilcarbonilamino, aralquilcarbonilamino, (heterocicloalquil)carbonilamino, (heterocicloalquil)alquilcarbonilamino, heteroarilcarbonilamino, heteroaralquilcarbonil amino, alcoxicarbonil amino alquilamino, (heteroaril)arilcarbonilamino alquilamino, heteroaralquil carbonil amino alquilamino, (heteroaril)arilsulfonilamino alquilcarbonil amino alquilamino, arilsulfonil amino alquilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, ocarbamoilo; m es 0, 1, 2, 3, o 4; a condición de que cuando m es 2, dos grupos adyacentes R1 pueden unirse entre sí para formar una mitad cíclica de 4 a 8 miembros, opcionalmente sustituida, n es 0, 1, 2, o 3, a condición de que cuando n es 2, dosgrupos R2 adyacentes pueden unirse entre sí para formar una mitad cíclica de 4 a 8 miembros opcionalmente sustituida. Ver más adelante ejemplos de la mitad cíclica de 4 a 8 miembros opcionalmente sustituida; y cada uno de Rx y Ry esindependientemente H, alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, cicloalquilcarbonilo, (cicloalquil)alquilcarbonilo, aroilo, aralquilcarbonilo, heterocicloalquil carbonilo, (heterocicloalquil)acilo, heteroaroilo, (heteroaril)acilo, aminocarbonilo, alquilcarbonil amino, (amino)amino carbonilo, alquilsulfonilamino carbonilo, alquilsulfonilamino,cicloalquil carbonilamino, cicloalquilsulfonilamino, (cicloalquil)alquilcarbonilamino, (cicloalquil)alquil sulfonilamino, arilcarbonilamino, arilsulfonilamino, aralquilcarbonil amino, aralquilsulfonilamino, (heterocicloalquil)carbonil amino,(heterocicloalquil)sulfonilamino, (heterocicloalquil)alquilcarbonilamino, (heterocicloalquil)alquilsulfonilamino. heteroarilcarbonil amino, heteroarilsulfonilamino, heteroaralquil carbonilamino, heteroaralquil sulfonil amino, alcoxicarbonilo,alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, carbamoílo, cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, (cicloalquil)alquilo, (cicloalquil)alcoxi, (cicloalquil)alquil sulfanilo, heterocicloalquilo, heterocicloalquiloxi,heterocicloalquilsulfanilo, (heterocicloalquil)alquilo, (heterocicloalquil)alcoxi, (heterocicloalquil)alquil sulfanilo, arilo, ariloxi, arilsulfanilo, aralquilo, aralquiloxi, aralquilsulfanilo, arilalquenilo, arilalquinilo, heteroarilo,heteroariloxi, heteroarilsulfanilo, heteroaralquilo, (heteroaril)alcoxi, o (heteroaril)alquil sulfanilo; o una sal u óxido N del mismo farmacéuticamente aceptable.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US40881102P | 2002-09-06 | 2002-09-06 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR041207A1 true AR041207A1 (es) | 2005-05-11 |
Family
ID=31978684
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030103250A AR041207A1 (es) | 2002-09-06 | 2003-09-08 | Pirazolo piridinas |
Country Status (20)
Country | Link |
---|---|
US (1) | US7691865B2 (es) |
EP (1) | EP1551398A4 (es) |
JP (1) | JP2006502165A (es) |
KR (1) | KR20050057235A (es) |
CN (1) | CN1694698A (es) |
AR (1) | AR041207A1 (es) |
AU (1) | AU2003268447B2 (es) |
BR (1) | BR0314053A (es) |
CA (1) | CA2497970A1 (es) |
EA (1) | EA009441B1 (es) |
GE (1) | GEP20074125B (es) |
IS (2) | IS7726A (es) |
MX (1) | MXPA05002443A (es) |
NO (1) | NO20051503D0 (es) |
NZ (1) | NZ539069A (es) |
PL (1) | PL375699A1 (es) |
RS (1) | RS20050200A (es) |
UA (1) | UA80295C2 (es) |
WO (1) | WO2004022054A1 (es) |
ZA (1) | ZA200501856B (es) |
Families Citing this family (23)
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WO2006004194A1 (ja) * | 2004-07-02 | 2006-01-12 | Nishimoto, Tomo | TGFβ2を標的としたアルツハイマー病治療薬のスクリーニング法 |
EP1804801A2 (en) * | 2004-10-15 | 2007-07-11 | Biogen Idec MA, Inc. | Methods of treating vascular injuries |
US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
WO2007028051A2 (en) | 2005-09-02 | 2007-03-08 | Abbott Laboratories | Novel imidazo based heterocycles |
EP1873157A1 (en) * | 2006-06-21 | 2008-01-02 | Bayer Schering Pharma Aktiengesellschaft | Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
PL2083863T3 (pl) | 2006-10-03 | 2015-08-31 | Genzyme Corp | Przeciwciała przeciwko TGF-beta do stosowania w leczeniu niemowląt obarczonych ryzykiem rozwinięcia się dysplazji oskrzelowo-płucnej |
WO2009039387A1 (en) * | 2007-09-20 | 2009-03-26 | Wyeth | Pyrazolo[5, 1-c] [1,2,4] triazines, methods for preparation and use thereof |
UA108979C2 (uk) * | 2008-03-14 | 2015-07-10 | Оцука Фармасьютікал Ко., Лтд. | Застосування тетоміласту при лікуванні фіброзу або легеневої емфіземи |
CN101544634B (zh) * | 2008-03-27 | 2011-08-10 | 天津药物研究院 | 2-苯基-3-取代吡唑并[1,5-a]吡啶类衍生物及其制备方法和用途 |
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US9468612B2 (en) | 2011-10-26 | 2016-10-18 | Seattle Children's Hospital | Cysteamine in the treatment of fibrotic disease |
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JP2017501145A (ja) | 2013-12-23 | 2017-01-12 | ノージン ビーブイ | Ccr9調節因子として有用な化合物 |
CA2941206C (en) * | 2014-03-27 | 2022-09-20 | Janssen Pharmaceutica Nv | Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1h-imidazo[1,2-b]pyrazole derivatives as ros1 inhibitors |
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US20220177978A1 (en) | 2019-04-02 | 2022-06-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
CN115052663A (zh) | 2020-01-08 | 2022-09-13 | 辛瑟斯治疗股份有限公司 | Alk5抑制剂缀合物及其用途 |
CN112707902B (zh) * | 2020-03-23 | 2022-04-15 | 杭州阿诺生物医药科技有限公司 | TGF-β受体抑制剂 |
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-
2003
- 2003-05-09 UA UAA200503095A patent/UA80295C2/uk unknown
- 2003-09-05 RS YUP-2005/0200A patent/RS20050200A/sr unknown
- 2003-09-05 EP EP03749412A patent/EP1551398A4/en not_active Withdrawn
- 2003-09-05 CA CA002497970A patent/CA2497970A1/en not_active Abandoned
- 2003-09-05 MX MXPA05002443A patent/MXPA05002443A/es active IP Right Grant
- 2003-09-05 NZ NZ539069A patent/NZ539069A/en unknown
- 2003-09-05 GE GEAP20038727A patent/GEP20074125B/en unknown
- 2003-09-05 WO PCT/US2003/027722 patent/WO2004022054A1/en active Application Filing
- 2003-09-05 US US10/526,839 patent/US7691865B2/en not_active Expired - Fee Related
- 2003-09-05 PL PL03375699A patent/PL375699A1/xx not_active Application Discontinuation
- 2003-09-05 CN CNA038248670A patent/CN1694698A/zh active Pending
- 2003-09-05 JP JP2004534571A patent/JP2006502165A/ja active Pending
- 2003-09-05 EA EA200500450A patent/EA009441B1/ru not_active IP Right Cessation
- 2003-09-05 AU AU2003268447A patent/AU2003268447B2/en not_active Ceased
- 2003-09-05 BR BR0314053-9A patent/BR0314053A/pt not_active IP Right Cessation
- 2003-09-05 KR KR1020057003874A patent/KR20050057235A/ko not_active Application Discontinuation
- 2003-09-08 AR ARP030103250A patent/AR041207A1/es unknown
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2005
- 2005-03-03 ZA ZA200501856A patent/ZA200501856B/en unknown
- 2005-03-04 IS IS7726A patent/IS7726A/is unknown
- 2005-03-04 IS IS7725A patent/IS7725A/is unknown
- 2005-03-21 NO NO20051503A patent/NO20051503D0/no not_active Application Discontinuation
Also Published As
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ZA200501856B (en) | 2006-04-26 |
US20060106033A1 (en) | 2006-05-18 |
EP1551398A4 (en) | 2006-06-07 |
EA200500450A1 (ru) | 2005-08-25 |
CA2497970A1 (en) | 2004-03-18 |
US7691865B2 (en) | 2010-04-06 |
EA009441B1 (ru) | 2007-12-28 |
GEP20074125B (en) | 2007-06-11 |
AU2003268447B2 (en) | 2008-07-24 |
KR20050057235A (ko) | 2005-06-16 |
PL375699A1 (en) | 2005-12-12 |
RS20050200A (en) | 2007-08-03 |
BR0314053A (pt) | 2005-07-19 |
UA80295C2 (en) | 2007-09-10 |
NO20051503L (no) | 2005-03-21 |
MXPA05002443A (es) | 2005-09-30 |
EP1551398A1 (en) | 2005-07-13 |
JP2006502165A (ja) | 2006-01-19 |
CN1694698A (zh) | 2005-11-09 |
WO2004022054A1 (en) | 2004-03-18 |
NO20051503D0 (no) | 2005-03-21 |
NZ539069A (en) | 2007-03-30 |
IS7726A (is) | 2005-03-04 |
IS7725A (is) | 2005-03-04 |
AU2003268447A1 (en) | 2004-03-29 |
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