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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 composicion

Info

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
Application number
ARP040104790A
Other languages
English (en)
Original Assignee
Sb Pharmco Inc
Neurocrine Biosciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sb Pharmco Inc, Neurocrine Biosciences Inc filed Critical Sb Pharmco Inc
Publication of AR046967A1 publication Critical patent/AR046967A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

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.
ARP040104790A 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 AR046967A1 (es)

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 (17)

* Cited by examiner, † Cited by third party
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
JP2008517060A (ja) * 2004-10-19 2008-05-22 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の製法
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
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
AU2007297421B2 (en) 2006-09-20 2012-03-08 Eli Lilly And Company Thiazole pyrazolopyrimidines as CRF1 receptor antagonists
CA2662000C (en) 2006-09-20 2013-01-08 Eli Lilly And Company Thiophene pyrazolopyrimidine compounds
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
CN102753527B (zh) * 2010-02-02 2014-12-24 诺华股份有限公司 用作crf受体拮抗剂的环己基酰胺衍生物
WO2014060381A1 (de) 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
BR112015009751A2 (pt) 2012-10-31 2017-07-11 Bayer Cropscience Ag novos compostos heterocíclicos como pesticidas
US9856262B2 (en) * 2014-04-10 2018-01-02 Hubei Bio-Pharmaceutical Industrial Technological Institute Inc. Analogues of 4H-pyrazolo[1,5-a] benzimidazole compound as PARP inhibitors
CN110996943A (zh) 2017-08-14 2020-04-10 云杉生物科学公司 促肾上腺皮质激素释放因子受体拮抗剂
KR20230092870A (ko) * 2020-07-27 2023-06-26 에스팜 바이오테크 피티와이 엘티디 화합물
KR20240023691A (ko) 2020-08-12 2024-02-22 스프루스 바이오사이언시스 인코포레이티드 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물
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 (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2168237T3 (es) * 1996-02-07 2007-04-01 Neurocrine Biosciences, Inc. Pirazolopirimidinas como antagonistas de receptores de crf.
PT915880E (pt) 1996-07-24 2007-12-31 Bristol Myers Squibb Pharma Co Azol triazinas e pirimidinas
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
CN1227554A (zh) 1996-08-28 1999-09-01 辉瑞大药厂 取代的6,5-杂二环衍生物
CA2291709A1 (en) * 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
ATE301657T1 (de) * 1998-01-28 2005-08-15 Bristol Myers Squibb Pharma Co Azolo-pyrimidine
WO2000059908A2 (en) 1999-04-06 2000-10-12 Du Pont Pharmaceuticals Company Pyrazolopyrimidines as crf antagonists
CA2379633C (en) 1999-09-30 2006-06-20 Neurogen Corporation 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
MXPA03009938A (es) 2001-04-30 2005-09-07 Glaxo Group Ltd Pirimidinas fusionadas como antagonistas del factor liberador de corticotropina.
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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
US20070293511A1 (en) 2003-12-22 2007-12-20 Sb Pharmco Puerto Rico Inc. And Neurocrine Biosciences, Inc., A Corporation Crf Receptor Antagonists and Methods
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
JP2008517060A (ja) 2004-10-19 2008-05-22 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の製法
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

Also Published As

Publication number Publication date
MA29984B1 (fr) 2008-12-01
CN1938309B (zh) 2011-11-09
RU2006126675A (ru) 2008-01-27
IS8526A (is) 2006-07-11
JP4926720B2 (ja) 2012-05-09
JP2007515472A (ja) 2007-06-14
RU2394035C2 (ru) 2010-07-10
BRPI0417943A (pt) 2007-04-17
EP1697374B1 (en) 2012-08-29
AU2004309168B2 (en) 2009-04-23
WO2005063755A1 (en) 2005-07-14
EP1697374A1 (en) 2006-09-06
US7737154B2 (en) 2010-06-15
US20070287705A1 (en) 2007-12-13
CA2550948A1 (en) 2005-07-14
TW200530242A (en) 2005-09-16
AU2004309168A1 (en) 2005-07-14
ZA200604574B (en) 2007-11-28
CN1938309A (zh) 2007-03-28
IL176350A0 (en) 2006-10-05
NZ547990A (en) 2010-04-30
KR20070009537A (ko) 2007-01-18
MY143499A (en) 2011-05-31
NO20063230L (no) 2006-09-12

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