AR046967A1 - Compuesto de pirazol[1,5-a]pirimidina, composicion farmaceutica que lo comprende y su uso para preparar dicha composicion - Google Patents
Compuesto de pirazol[1,5-a]pirimidina, composicion farmaceutica que lo comprende y su uso para preparar dicha composicionInfo
- Publication number
- AR046967A1 AR046967A1 ARP040104790A ARP040104790A AR046967A1 AR 046967 A1 AR046967 A1 AR 046967A1 AR P040104790 A ARP040104790 A AR P040104790A AR P040104790 A ARP040104790 A AR P040104790A AR 046967 A1 AR046967 A1 AR 046967A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- heteroaryl
- arylalkyl
- heterocycloalkyl
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Abstract
Un compuesto de pirazolo[1,5-A]pirimidina caracterizado porque tiene la estructura de formula (1), o una sal, éster, solvato, estereoisomero o profármaco farmacéuticamente aceptable de la misma, en la que: ôlínea punteadaö representa el segundo enlace de un doble enlace opcional; R1 es hidrogeno, alquilo, alquilo sustituido, heteroarilo, heteroarilo sustituido, -NH2, o halogeno; R2 es alquilo, alquilo sustituido, -C(O)NR7R8, arilo, arilo sustituido, ariloxialquilo, ariloxialquilo sustituido, heteroarilalcoxialquilo, heteroarilalcoxialquilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilo, o heteroarilo sustituido, en el que dicho heteroarilo o heteroarilo sustituido se une al anillo de pirimidina vía un enlace carbono-carbono; R3 es nada, hidrogeno, o alquilo; Y es =(CR4)- o -(C=O)-; R4 es hidrogeno, alquilo, alquilo sustituido, tioalquilo, alquilsulfinilo, o alquilsulfonilo; Ar es fenilo, fenilo sustituido con 1 o 2 R5, piridilo o piridinilo sustituido con 1 o 2 R5; R5 en cada ocurrencia es hidroxi, alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, ciano, halogeno, alquilsulfonilo, o alquilsulfinilo; Het es heteroarilo opcionalmente sustituido con 1 o 2 R6; R6 en cada ocurrencia es hidroxi, alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, ciano, o halogeno; y R7 y R8 son independientemente hidrogeno, alquilo, alquilo sustituido, arilo, arilo sustituido, heterociclo, heterociclo sustituido, arilalquilo, arilalquilo sustituido, heterocicloalquilo, o heterocicloalquilo sustituido; o R7 y R8 tomados juntos con el nitrogeno al cual están unidos forman un anillo heterocíclico o un anillo heterocíclico sustituido. Composicion farmacéutica que comprende el compuesto anterior en combinacion con un vehículo o diluyente farmacéuticamente aceptable. Uso del compuesto de pirazolo[1,5-A]pirimidina para preparar dicha composicion farmacéutica de utilidad para tratar un trastorno que manifiesta hipersecrecion de CRF en un mamífero, mediante la administracion al animal de una cantidad eficaz de dicha composicion farmacéutica. Dicho trastorno puede ser: ictus, depresion, trastorno relacionado con la ansiedad, trastorno obsesivo-compulsivo, síndrome del intestino irritable, o anorexia nerviosa.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53203103P | 2003-12-22 | 2003-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR046967A1 true AR046967A1 (es) | 2006-01-04 |
Family
ID=34738733
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040104790A AR046967A1 (es) | 2003-12-22 | 2004-12-20 | Compuesto de pirazol[1,5-a]pirimidina, composicion farmaceutica que lo comprende y su uso para preparar dicha composicion |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7737154B2 (es) |
| EP (1) | EP1697374B1 (es) |
| JP (1) | JP4926720B2 (es) |
| KR (1) | KR20070009537A (es) |
| CN (1) | CN1938309B (es) |
| AR (1) | AR046967A1 (es) |
| AU (1) | AU2004309168B2 (es) |
| BR (1) | BRPI0417943A (es) |
| CA (1) | CA2550948A1 (es) |
| IL (1) | IL176350A0 (es) |
| IS (1) | IS8526A (es) |
| MA (1) | MA29984B1 (es) |
| MY (1) | MY143499A (es) |
| NO (1) | NO20063230L (es) |
| NZ (1) | NZ547990A (es) |
| RU (1) | RU2394035C2 (es) |
| TW (1) | TW200530242A (es) |
| WO (1) | WO2005063755A1 (es) |
| ZA (1) | ZA200604574B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0308208D0 (en) | 2003-04-09 | 2003-05-14 | Glaxo Group Ltd | Chemical compounds |
| US8815599B2 (en) | 2004-06-01 | 2014-08-26 | Pronai Therapeutics, Inc. | Methods and compositions for the inhibition of gene expression |
| GB0519957D0 (en) * | 2005-09-30 | 2005-11-09 | Sb Pharmco Inc | Chemical compound |
| ATE430746T1 (de) * | 2004-10-19 | 2009-05-15 | Smithkline Beecham Cork Ltd | Crf-rezeptor-antagonisten und zugehörige verfahren |
| US8088779B2 (en) * | 2005-09-30 | 2012-01-03 | Smithkline Beecham (Cork) Limited | Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists |
| WO2008036579A1 (en) * | 2006-09-20 | 2008-03-27 | Eli Lilly And Company | Thiazole pyrazolopyrimidines as crf1 receptor antagonists |
| KR101088196B1 (ko) | 2006-09-20 | 2011-11-30 | 일라이 릴리 앤드 캄파니 | 티오펜 피라졸로피리미딘 화합물 |
| KR100854679B1 (ko) * | 2007-02-03 | 2008-08-27 | 김기형 | 심플 서비스 로케이션 프로토콜 네트워크 시스템 및 이를구성하는 에이전트. |
| EP2282998B1 (en) * | 2008-04-21 | 2014-09-10 | Albemarle Corporation | Processes for producing n-alkylpyrazole |
| ES2527849T3 (es) * | 2010-02-02 | 2015-01-30 | Novartis Ag | Derivados de ciclohexilamida como antagonistas del receptor de CRF |
| WO2014060381A1 (de) | 2012-10-18 | 2014-04-24 | Bayer Cropscience Ag | Heterocyclische verbindungen als schädlingsbekämpfungsmittel |
| WO2014067962A1 (de) | 2012-10-31 | 2014-05-08 | Bayer Cropscience Ag | Neue heterocylische verbindungen als schädlingsbekämpfungsmittel |
| DK3130592T3 (da) * | 2014-04-10 | 2019-11-04 | Hubei Bio Pharmaceutical Industrial Tech Institute Inc | ANALOGER AF 4H-PYRAZOLO[1,5-á]BENZIMIDAZOL-FORBINDELSER SOM PARPINHIBITORER |
| CN116829558A (zh) * | 2020-07-27 | 2023-09-29 | 艾斯法姆生物技术股份有限公司 | 化合物 |
| CN116322544A (zh) | 2020-08-12 | 2023-06-23 | 云杉生物科学公司 | 用于治疗***的方法和组合物 |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP9900575A3 (en) * | 1996-02-07 | 2001-11-28 | Neurocrine Biosciences Inc San | Pyrazolopyrimidines as crf receptor antagonists |
| ATE375344T1 (de) | 1996-07-24 | 2007-10-15 | Bristol Myers Squibb Pharma Co | Azolotriazine und pyrimidine |
| US6060478A (en) | 1996-07-24 | 2000-05-09 | Dupont Pharmaceuticals | Azolo triazines and pyrimidines |
| US6313124B1 (en) * | 1997-07-23 | 2001-11-06 | Dupont Pharmaceuticals Company | Tetrazine bicyclic compounds |
| EP0923582B1 (en) | 1996-08-28 | 2006-09-20 | Pfizer Inc. | Substituted 6,5-hetero-bicyclic derivatives |
| WO2000059908A2 (en) | 1999-04-06 | 2000-10-12 | Du Pont Pharmaceuticals Company | Pyrazolopyrimidines as crf antagonists |
| IL148904A0 (en) | 1999-09-30 | 2002-09-12 | Neurogen Corp | Amino substituted pyrazolo {1,5,-a}-1,5- pyrimidines and pyrazolo{1,5,-a}-1,3,5-triazines |
| CO5271670A1 (es) | 1999-10-29 | 2003-04-30 | Pfizer Prod Inc | Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas |
| HUP0304054A2 (hu) | 2001-04-30 | 2004-04-28 | Glaxo Group Limited | A kortikotropin-realising faktor (CRF) antagonistáiként alkalmazható kondenzált pirimidinek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
| EP1395591B1 (en) | 2001-06-12 | 2008-06-04 | Glaxo Group Limited | Corticotropin releasing factor antagonists |
| GB0117396D0 (en) | 2001-07-17 | 2001-09-05 | Glaxo Group Ltd | Chemical compounds |
| JP2006515334A (ja) | 2003-01-16 | 2006-05-25 | エスビー ファームコ プエルト リコ インコーポレーテッド | ＣＲＦ受容体アンタゴニストとしてのヘテロアリール置換ピロロ［２，３−ｂ］ピリジン誘導体 |
| EP1608652A1 (en) | 2003-03-31 | 2005-12-28 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
| GB0308208D0 (en) | 2003-04-09 | 2003-05-14 | Glaxo Group Ltd | Chemical compounds |
| US20070021429A1 (en) | 2003-04-09 | 2007-01-25 | Yves St-Denis | Condensed n-heterocyclic compounds and their use as crf receptor antagonists |
| JP2007515474A (ja) | 2003-12-22 | 2007-06-14 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよびそれらに関連する方法 |
| DE102004008807A1 (de) | 2004-02-20 | 2005-09-08 | Bayer Cropscience Ag | Pyrazolopyrimidine |
| GB0519957D0 (en) | 2005-09-30 | 2005-11-09 | Sb Pharmco Inc | Chemical compound |
| ATE430746T1 (de) | 2004-10-19 | 2009-05-15 | Smithkline Beecham Cork Ltd | Crf-rezeptor-antagonisten und zugehörige verfahren |
| US8088779B2 (en) | 2005-09-30 | 2012-01-03 | Smithkline Beecham (Cork) Limited | Pyrazolo [1,5-alpha] pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists |
-
2004
- 2004-12-20 MY MYPI20045253A patent/MY143499A/en unknown
- 2004-12-20 NZ NZ547990A patent/NZ547990A/en unknown
- 2004-12-20 JP JP2006546391A patent/JP4926720B2/ja not_active Expired - Fee Related
- 2004-12-20 AR ARP040104790A patent/AR046967A1/es not_active Application Discontinuation
- 2004-12-20 EP EP04820857A patent/EP1697374B1/en active Active
- 2004-12-20 BR BRPI0417943-9A patent/BRPI0417943A/pt not_active Application Discontinuation
- 2004-12-20 US US10/596,648 patent/US7737154B2/en active Active
- 2004-12-20 AU AU2004309168A patent/AU2004309168B2/en not_active Ceased
- 2004-12-20 TW TW093139578A patent/TW200530242A/zh unknown
- 2004-12-20 CN CN2004800420125A patent/CN1938309B/zh not_active Expired - Fee Related
- 2004-12-20 CA CA002550948A patent/CA2550948A1/en not_active Abandoned
- 2004-12-20 RU RU2006126675/04A patent/RU2394035C2/ru not_active IP Right Cessation
- 2004-12-20 KR KR1020067012368A patent/KR20070009537A/ko not_active Application Discontinuation
- 2004-12-20 WO PCT/IB2004/004234 patent/WO2005063755A1/en active Application Filing
-
2006
- 2006-06-05 ZA ZA200604574A patent/ZA200604574B/en unknown
- 2006-06-15 IL IL176350A patent/IL176350A0/en unknown
- 2006-06-27 MA MA29147A patent/MA29984B1/fr unknown
- 2006-07-11 NO NO20063230A patent/NO20063230L/no not_active Application Discontinuation
- 2006-07-11 IS IS8526A patent/IS8526A/is unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2394035C2 (ru) | 2010-07-10 |
| NZ547990A (en) | 2010-04-30 |
| EP1697374B1 (en) | 2012-08-29 |
| IS8526A (is) | 2006-07-11 |
| EP1697374A1 (en) | 2006-09-06 |
| NO20063230L (no) | 2006-09-12 |
| CA2550948A1 (en) | 2005-07-14 |
| JP2007515472A (ja) | 2007-06-14 |
| CN1938309A (zh) | 2007-03-28 |
| MA29984B1 (fr) | 2008-12-01 |
| US20070287705A1 (en) | 2007-12-13 |
| AU2004309168B2 (en) | 2009-04-23 |
| IL176350A0 (en) | 2006-10-05 |
| WO2005063755A1 (en) | 2005-07-14 |
| CN1938309B (zh) | 2011-11-09 |
| BRPI0417943A (pt) | 2007-04-17 |
| MY143499A (en) | 2011-05-31 |
| AU2004309168A1 (en) | 2005-07-14 |
| ZA200604574B (en) | 2007-11-28 |
| JP4926720B2 (ja) | 2012-05-09 |
| KR20070009537A (ko) | 2007-01-18 |
| US7737154B2 (en) | 2010-06-15 |
| TW200530242A (en) | 2005-09-16 |
| RU2006126675A (ru) | 2008-01-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |