AR063318A1 - Pirazoliltienopiridinas terapeuticas - Google Patents
Pirazoliltienopiridinas terapeuticasInfo
- Publication number
- AR063318A1 AR063318A1 ARP070104581A ARP070104581A AR063318A1 AR 063318 A1 AR063318 A1 AR 063318A1 AR P070104581 A ARP070104581 A AR P070104581A AR P070104581 A ARP070104581 A AR P070104581A AR 063318 A1 AR063318 A1 AR 063318A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- independently selected
- group
- thieno
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
Abstract
Son utiles como agentes terapéuticos en el tratamiento de trastornos mediados por TGF, incluyendo el cáncer y trastornos fibroticos. También se proporcionan composiciones farmacéuticas que comprenden uno o más compuestos de formula (1). Reivindicacion 1:Un compuesto caracterizado porque es de formula 1 o su sal farmacéuticamente aceptable, en la que: R1 es un tieno[3,2-c]piridinilo, un tieno[3,2-b]piridinilo, un tieno[2,3-c]piridinilo o un tieno[2,3-b]piridinilo, cada uno de los cuales puede estar opcionalmente sustituido con uno a tres sustituyentes, seleccionados cada uno independientemente del grupo que consiste en: alquilo C1-3, alquil C1-3-S-alquilo C1-3, -S-alquilo C1-3, alquil C1-3-O-alquilo C1-3, -O-alquilo C1-3, - C(O)O-alquilo C1-3, -C(O)O-H, -C(O)NR30R31, halogeno, -CN, -OH, en la que R30 y R31 se seleccionan cada uno independientemente del grupo que consiste en: H, y alquil C1-3-OH, alquilo C1-3, halogeno, y -O-alquilo C1-3; R2 y R3 se seleccionan independientemente del grupo que consiste en: hidrogeno, alquilo C1-3, alquil C1-3-S-alquilo C1-3, -S-alquilo C1-3, alquil C1-3-O-alquilo C1-3, -O-alquilo C1-3, -C(O)O-alquilo C1-3. -C(O)O-H, -C(O)NR30R31, halogeno, -CN, -OH, y un cicloalquilo C3-6, en la que R30 y R31 se seleccionan cada uno independientemente del grupo que consiste en: H, y alquilo C1-3, o R2 y R3 pueden tomarse conjuntamente para formar un heteroarilo de 5 o 6 miembros, un fenilo, un cicloalquilo C4-6, o un heterocicloalquilo de 4-6 miembros, en la que dicho cicloalquilo C4-6 o heterocicloalquilo de 4-6 miembros puede estar opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente de halogeno, -OH, oxo, y alquilo C1-3;. en la que dicho heteroarilo de 5 o 6 miembros o fenilo puede estar opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente de halogeno, -CN, -OH, -O-alquilo C1-3 y alquilo C1-3; y R4, R5, R6, y R7 se seleccionan del grupo que consiste en: H, OH, cicloalquilo C3, alquilo C1-3, alquil C1-3-S-alquilo C1-3, -S-alquilo C1-3, alquil C1-3-O-alquilo C1-3, -O-alquilo C1-3, -C(O)O-alquilo C1-3, -C(O)O-H, -C(O)NR30R31, halogeno, -CN, -OH, en la que R30 y R31 se seleccionan cada uno independientemente del grupo que consiste en: H, y alquilo C1-3-alquilo C1-3, -O-alquilo C1-3, y halogeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85198206P | 2006-10-16 | 2006-10-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR063318A1 true AR063318A1 (es) | 2009-01-21 |
Family
ID=38962671
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104581A AR063318A1 (es) | 2006-10-16 | 2007-10-16 | Pirazoliltienopiridinas terapeuticas |
Country Status (16)
| Country | Link |
|---|---|
| US (5) | US7964612B2 (es) |
| EP (2) | EP2074128B1 (es) |
| JP (1) | JP5443988B2 (es) |
| KR (1) | KR20090066297A (es) |
| CN (1) | CN101528752A (es) |
| AR (1) | AR063318A1 (es) |
| AU (1) | AU2007311560B2 (es) |
| CA (1) | CA2666603C (es) |
| CL (1) | CL2007002916A1 (es) |
| ES (2) | ES2435430T3 (es) |
| IL (1) | IL197750A0 (es) |
| MX (1) | MX2009003157A (es) |
| NO (1) | NO20091247L (es) |
| TW (1) | TW200825094A (es) |
| UY (1) | UY30641A1 (es) |
| WO (1) | WO2008047198A1 (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20090066297A (ko) * | 2006-10-16 | 2009-06-23 | 화이자 프로덕츠 인크. | 치료용 피라졸릴 티에노피리딘 |
| FR2949468B1 (fr) * | 2009-08-28 | 2011-09-30 | Sanofi Aventis | Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one, leur preparation et leur application en therapeutique |
| PT2382205E (pt) | 2008-12-29 | 2014-07-28 | Sanofi Sa | Derivados de 2-piridin-2-il-pirazol-3(2h)-ona, sua preparação e sua aplicação terapêutica como activadores de hif |
| ES2511917T3 (es) * | 2008-12-29 | 2014-10-23 | Sanofi | Derivados de 2-piridin-2-il-pirazol-3(2H)-ona, su preparación y su aplicación en terapéutica |
| FR2940652B1 (fr) * | 2008-12-29 | 2011-02-11 | Sanofi Aventis | Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one,leur preparation et leur application en therapeutique |
| CA2758071C (en) | 2009-04-06 | 2018-01-09 | Agios Pharmaceuticals, Inc. | Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use |
| PL2448581T3 (pl) | 2009-06-29 | 2017-06-30 | Agios Pharmaceuticals, Inc. | Kompozycje terapeutyczne i odnośne sposoby ich stosowania |
| NZ597379A (en) | 2009-06-29 | 2014-04-30 | Agios Pharmaceuticals Inc | Therapeutic compounds and compositions |
| CN102884068A (zh) * | 2010-03-15 | 2013-01-16 | 国立大学法人广岛大学 | 噻吩并吡啶衍生物及其制备方法、以及使用该衍生物的有机半导体器件 |
| JP5743418B2 (ja) * | 2010-04-09 | 2015-07-01 | Ｏａｔアグリオ株式会社 | 新規なピラゾール化合物、その製造方法及び有害生物防除剤 |
| WO2012058483A1 (en) | 2010-10-28 | 2012-05-03 | Pacira Pharmaceuticals, Inc. | A sustained release formulation of a non-steroidal anti-inflammatory drug |
| SI2651951T1 (sl) | 2010-12-16 | 2015-01-30 | F. Hoffmann-La Roche Ag | Tricikliäśne p13k inhibitorske spojine in postopki uporabe |
| CA2821975A1 (en) | 2010-12-17 | 2012-06-21 | Shunqi Yan | N-(4-(azetidine-1-carbonyl)phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase m2 pkm2 modulators |
| ES2569712T3 (es) | 2010-12-21 | 2016-05-12 | Agios Pharmaceuticals, Inc. | Activadores de PKM2 bicíclicos |
| TWI549947B (zh) | 2010-12-29 | 2016-09-21 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| CN103476767B (zh) | 2011-02-09 | 2015-06-10 | 弗·哈夫曼-拉罗切有限公司 | 作为pi3激酶抑制剂的杂环化合物 |
| HUE039269T2 (hu) | 2011-05-03 | 2018-12-28 | Agios Pharmaceuticals Inc | Piruvát-kináz aktivátorok terápiában történõ alkalmazásra |
| US9181231B2 (en) | 2011-05-03 | 2015-11-10 | Agios Pharmaceuticals, Inc | Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia |
| WO2012167261A2 (en) * | 2011-06-03 | 2012-12-06 | Yale University | Compositions and methods for treating and preventing neointimal stenosis |
| CN102660253B (zh) * | 2012-03-07 | 2014-05-21 | 泰山医学院 | 一种吡唑啉衍生物类Ni2+荧光探针及其应用 |
| EP3763367A1 (en) | 2012-12-06 | 2021-01-13 | Celgene Quanticel Research, Inc. | Pyridine-pyrazole derivatives as histone demethylase inhibitors |
| WO2014139144A1 (en) | 2013-03-15 | 2014-09-18 | Agios Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
| EP3010898A1 (en) * | 2013-06-20 | 2016-04-27 | Basf Se | Process for preparing pyridylpyrazole compounds and derivatives thereof from pyridylhydrazine |
| SI3307271T1 (sl) | 2015-06-11 | 2023-11-30 | Agios Pharmaceuticals, Inc. | Postopki za uporabo aktivatorjev piruvat kinaze |
| EP3741397A1 (en) | 2015-12-11 | 2020-11-25 | Research Institute at Nationwide Children's Hospital | Systems and methods for optimized patient specific tissue engineering vascular grafts |
| KR102434226B1 (ko) * | 2016-06-30 | 2022-08-19 | 한미약품 주식회사 | Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도 |
| AU2017336803A1 (en) * | 2016-09-30 | 2019-04-18 | Intercept Pharmaceuticals, Inc. | Crystalline forms of a bile acid derivative |
| EP3541815A4 (en) | 2016-11-18 | 2020-07-15 | Pacira Pharmaceuticals, Inc. | ZINC MELXICAM COMPLEX MICROPARTICLE MULTIVESICULAR LIPOSOME FORMULATIONS AND METHODS OF MAKING THE SAME |
| CN116249692A (zh) * | 2020-09-28 | 2023-06-09 | 四川科伦博泰生物医药股份有限公司 | 吡唑类化合物及其制备方法和用途 |
| KR20240006582A (ko) * | 2021-05-03 | 2024-01-15 | 티로나 바이오, 인코포레이티드 | Alk-5 (tgf 베타 r1) 억제제로 폐 질환을 치료하기 위한 방법 |
| WO2023212063A1 (en) * | 2022-04-29 | 2023-11-02 | Freeman John J | Method and composition for treating lung diseases |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0102672D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| UA80571C2 (en) * | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| SE0300120D0 (sv) * | 2003-01-17 | 2003-01-17 | Astrazeneca Ab | Novel compounds |
| CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| AR048669A1 (es) * | 2004-03-03 | 2006-05-17 | Syngenta Ltd | Derivados biciclicos de bisamida |
| JP2008511630A (ja) * | 2004-08-31 | 2008-04-17 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | ＴＧＦ−βインヒビターとしてのピリミジニルピラゾール |
| US7511056B2 (en) * | 2004-11-10 | 2009-03-31 | Eli Lilly And Company | TGF-β inhibitors |
| KR20090066297A (ko) | 2006-10-16 | 2009-06-23 | 화이자 프로덕츠 인크. | 치료용 피라졸릴 티에노피리딘 |
-
2007
- 2007-10-04 KR KR1020097007709A patent/KR20090066297A/ko not_active Application Discontinuation
- 2007-10-04 JP JP2009532905A patent/JP5443988B2/ja active Active
- 2007-10-04 EP EP07825309.3A patent/EP2074128B1/en active Active
- 2007-10-04 CN CNA2007800386503A patent/CN101528752A/zh active Pending
- 2007-10-04 CA CA2666603A patent/CA2666603C/en active Active
- 2007-10-04 ES ES07825309T patent/ES2435430T3/es active Active
- 2007-10-04 WO PCT/IB2007/002994 patent/WO2008047198A1/en active Application Filing
- 2007-10-04 ES ES12006019.9T patent/ES2559521T3/es active Active
- 2007-10-04 AU AU2007311560A patent/AU2007311560B2/en not_active Expired - Fee Related
- 2007-10-04 MX MX2009003157A patent/MX2009003157A/es not_active Application Discontinuation
- 2007-10-04 EP EP12006019.9A patent/EP2527345B1/en active Active
- 2007-10-10 CL CL200702916A patent/CL2007002916A1/es unknown
- 2007-10-12 TW TW096138215A patent/TW200825094A/zh unknown
- 2007-10-12 UY UY30641A patent/UY30641A1/es not_active Application Discontinuation
- 2007-10-12 US US11/871,311 patent/US7964612B2/en active Active
- 2007-10-16 AR ARP070104581A patent/AR063318A1/es active IP Right Grant
-
2009
- 2009-03-23 IL IL197750A patent/IL197750A0/en unknown
- 2009-03-25 NO NO20091247A patent/NO20091247L/no not_active Application Discontinuation
-
2011
- 2011-05-20 US US13/112,520 patent/US8455512B2/en active Active
-
2013
- 2013-04-17 US US13/864,457 patent/US9090625B2/en active Active
-
2015
- 2015-03-03 US US14/637,097 patent/US9260450B2/en active Active
-
2016
- 2016-01-14 US US14/995,556 patent/US9938289B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN101528752A (zh) | 2009-09-09 |
| JP5443988B2 (ja) | 2014-03-19 |
| ES2435430T3 (es) | 2013-12-19 |
| UY30641A1 (es) | 2008-05-31 |
| NO20091247L (no) | 2009-04-23 |
| US20150175624A1 (en) | 2015-06-25 |
| IL197750A0 (en) | 2009-12-24 |
| EP2074128B1 (en) | 2013-08-14 |
| US9938289B2 (en) | 2018-04-10 |
| AU2007311560B2 (en) | 2011-04-21 |
| KR20090066297A (ko) | 2009-06-23 |
| ES2559521T3 (es) | 2016-02-12 |
| US9090625B2 (en) | 2015-07-28 |
| TW200825094A (en) | 2008-06-16 |
| EP2527345A1 (en) | 2012-11-28 |
| CL2007002916A1 (es) | 2008-04-18 |
| MX2009003157A (es) | 2009-04-03 |
| CA2666603C (en) | 2013-08-06 |
| US20160200735A1 (en) | 2016-07-14 |
| US7964612B2 (en) | 2011-06-21 |
| AU2007311560A1 (en) | 2008-04-24 |
| US20140031385A1 (en) | 2014-01-30 |
| US8455512B2 (en) | 2013-06-04 |
| CA2666603A1 (en) | 2008-04-24 |
| JP2010506895A (ja) | 2010-03-04 |
| US20110224251A1 (en) | 2011-09-15 |
| WO2008047198A1 (en) | 2008-04-24 |
| US9260450B2 (en) | 2016-02-16 |
| EP2074128A1 (en) | 2009-07-01 |
| US20080090861A1 (en) | 2008-04-17 |
| EP2527345B1 (en) | 2015-12-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal | ||
| FG | Grant, registration |