AR049521A1 - Derivados de pirrazol - pirimidina - Google Patents
Derivados de pirrazol - pirimidinaInfo
- Publication number
- AR049521A1 AR049521A1 ARP050102490A ARP050102490A AR049521A1 AR 049521 A1 AR049521 A1 AR 049521A1 AR P050102490 A ARP050102490 A AR P050102490A AR P050102490 A ARP050102490 A AR P050102490A AR 049521 A1 AR049521 A1 AR 049521A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- optionally substituted
- phenyl
- pyrimidine
- pyrazol
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- LPCQBTAOTIZGAE-UHFFFAOYSA-N 2h-pyrimidine-1-carboxamide Chemical compound NC(=O)N1CN=CC=C1 LPCQBTAOTIZGAE-UHFFFAOYSA-N 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 125000004367 cycloalkylaryl group Chemical group 0.000 abstract 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- 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
- A61P25/18—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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente tarta de derivados de pirrazol-pirimidina, procedimiento de preparacion, composiciones farmacéutica que los contienen y usos en enfermedades como psicosis, ezquizofrenia, Alzheimer, trastornos cognitivos. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en donde p es 0 o 1; R1 y R2 independientemente de cada uno pueden ser H; halogeno; alquilo inferior opcionalmente sustituido por alcoxilo inferior; alcoxilo inferior opcionalmente sustituido por uno o más halogenos, o CF3; R3 es alquilo inferior; hidroxi-alquilo inferior; o NRaRb; Ra y Rb son independientemente seleccionados del grupo consistente en: H; alquilo inferior opcionalmente sustituido por uno o más hidroxilo, fluoro, cicloalquilarilo, heteroarilo o NRcRd, en donde Rc y Rd se seleccionan independientemente de H o alquilo inferior; cicloalquilo; arilo; heteroarilo; o Ra y Rb pueden formar un anillo heterocíclico de 5 o 6 miembros opcionalmente sustituido junto con el átomo de N al que están unidos; R4 es H, Cl, alcoxilo inferior, cicloalquilo o alquilo inferior recto que está opcionalmente sustituido por uno o más F; R5 es H; halogeno o alquilo inferior; así como sales farmacéuticamente aceptables de los mismos: con la excepcion de los compuestos con las siguientes formulas: 7-(difluoro-metil)-5-(4-metilfenil)-N-[3-(4-morfolinil-sulfonil)fenil]-pirazol[1,5-a]pirimidina-3-carboxamida; 7-(difluoro-metil)-N-[3-(4-morfonilsulfonil)fenil]-5-fenil]-pirazol[1,5-a]pirimidina-3- carboxamida; y 7-(difluoro-metil)-5-(4-metoxifenil)-N-[3-(4-morfolinil-sulfonil)fenil]pirazol[1,5-a]pirimidina-3-carboxamida.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04102837 | 2004-06-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049521A1 true AR049521A1 (es) | 2006-08-09 |
Family
ID=34971089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102490A AR049521A1 (es) | 2004-06-21 | 2005-06-17 | Derivados de pirrazol - pirimidina |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7378417B2 (es) |
| EP (1) | EP1761541B1 (es) |
| JP (1) | JP4608542B2 (es) |
| CN (1) | CN100528876C (es) |
| AR (1) | AR049521A1 (es) |
| AT (1) | ATE383361T1 (es) |
| AU (1) | AU2005254657B2 (es) |
| BR (1) | BRPI0512330A (es) |
| CA (1) | CA2571487C (es) |
| DE (1) | DE602005004287T2 (es) |
| DK (1) | DK1761541T3 (es) |
| ES (1) | ES2299044T3 (es) |
| HR (1) | HRP20080070T3 (es) |
| IL (1) | IL179736A (es) |
| MX (1) | MXPA06014809A (es) |
| MY (1) | MY143368A (es) |
| NO (1) | NO20070249L (es) |
| NZ (1) | NZ551660A (es) |
| PL (1) | PL1761541T3 (es) |
| PT (1) | PT1761541E (es) |
| RU (1) | RU2378277C2 (es) |
| SI (1) | SI1761541T1 (es) |
| TW (1) | TWI301835B (es) |
| WO (1) | WO2005123738A1 (es) |
| ZA (1) | ZA200610102B (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0607927A2 (pt) | 2005-02-11 | 2009-10-20 | Hoffmann La Roche | derivados de pirazol-pirimidina |
| KR100973609B1 (ko) | 2005-03-23 | 2010-08-03 | 에프. 호프만-라 로슈 아게 | ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘유도체 |
| CN101273040B (zh) | 2005-09-27 | 2011-11-09 | 弗·哈夫曼-拉罗切有限公司 | 作为mglur2拮抗剂的*二唑基吡唑并嘧啶类化合物 |
| CA2626742A1 (en) * | 2005-10-21 | 2007-04-26 | Exelixis, Inc. | Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators |
| JP2010534206A (ja) * | 2007-07-20 | 2010-11-04 | メルク・シャープ・エンド・ドーム・コーポレイション | ピラゾロ［１，５−ａ］ピリミジン誘導体 |
| EP2962566A1 (en) * | 2008-10-31 | 2016-01-06 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| AR078171A1 (es) * | 2009-09-15 | 2011-10-19 | Sanofi Aventis | Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas |
| WO2012075393A2 (en) * | 2010-12-02 | 2012-06-07 | President And Fellows Of Harvard College | Activators of proteasomal degradation and uses thereof |
| RS63320B1 (sr) | 2010-12-08 | 2022-07-29 | The U S A As Represented By The Secretary Department Of Health And Human Services | Supstituisani pirazolopirimidini kao aktivatori glukocerebrozidaze |
| US10953012B2 (en) | 2011-04-26 | 2021-03-23 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of pask |
| CA2868484A1 (en) | 2012-03-28 | 2013-10-03 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Salicylic acid derivatives useful as glucocerebrosidase activators |
| KR20150070187A (ko) | 2012-10-23 | 2015-06-24 | 에프. 호프만-라 로슈 아게 | 자폐 장애의 치료를 위한 ｍｇｌｕ２／３ 길항제 |
| WO2014066743A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2014066795A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| CA2943877A1 (en) | 2014-04-23 | 2015-10-29 | F. Hoffmann-La Roche Ag | Mglu2/3 antagonists for the treatment of intellectual disabilities |
| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| EP3000814A1 (en) | 2014-09-26 | 2016-03-30 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| IL252053B2 (en) | 2014-11-06 | 2024-04-01 | Lysosomal Therapeutics Inc | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| AU2015342883B2 (en) | 2014-11-06 | 2020-07-02 | Bial - R&D Investments, S.A. | Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders |
| AU2015357169B2 (en) | 2014-12-03 | 2021-03-04 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| US10738016B2 (en) | 2015-10-13 | 2020-08-11 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | BRD4-kinase inhibitors as cancer therapeutics |
| PT3389727T (pt) | 2015-12-18 | 2020-10-30 | Janssen Pharmaceutica Nv | Ligantes pet de mglur2/3 radiomarcados |
| US11045562B2 (en) | 2015-12-18 | 2021-06-29 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| KR20180133461A (ko) * | 2016-04-06 | 2018-12-14 | 리소소말 테라퓨틱스 인크. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물 및 의학적 장애의 치료에서의 그의 용도 |
| US11124516B2 (en) | 2016-04-06 | 2021-09-21 | BIAL-BioTech Investments, Inc. | Pyrrolo[1,2-A]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| MX389579B (es) | 2016-05-05 | 2025-03-20 | Bial R&D Invest S A | IMIDAZO[1,2-b]PIRIDAZINAS SUSTITUIDAS, IMIDAZO[1,5-b]PIRIDAZINAS SUSTITUIDAS, COMPUESTOS RELACIONADOS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| US11414431B2 (en) | 2018-10-15 | 2022-08-16 | Nimbus Lakshmi, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH25866A (en) * | 1986-03-20 | 1991-12-02 | Takeda Chemical Industries Ltd | Sulfonylurea compounds and their herbicides |
| EP0729758A3 (en) * | 1995-03-02 | 1997-10-29 | Pfizer | Pyrazolopyrimidines and pyrrolopyrimidines for the treatment of neuronal and other diseases |
| GB9712718D0 (en) * | 1997-06-18 | 1997-08-20 | Heights Design Production Ltd | Binding apparatus |
| DE69804273T2 (de) * | 1997-07-18 | 2002-10-31 | F. Hoffmann-La Roche Ag, Basel | 5h-Thiazolo[3,2-a]pyrimidinderivate |
| WO2001023387A2 (en) * | 1999-09-30 | 2001-04-05 | Neurogen Corporation | CERTAIN ALKYLENE DIAMINE-SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES |
| DK1379511T3 (da) * | 2001-04-12 | 2005-11-07 | Hoffmann La Roche | Dihydro-benzo[b][1,4]diazepin-2-on-derivater som mGLuR2-antagonister II |
| DE60316542T2 (de) * | 2002-03-28 | 2008-07-03 | Eisai R&D Management Co., Ltd. | 7-azaindole als inhibitoren c-jun n-terminaler kinasen zur behandlung neurodegenerativer störungen |
| US7329662B2 (en) * | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
-
2005
- 2005-06-13 EP EP05754665A patent/EP1761541B1/en not_active Expired - Lifetime
- 2005-06-13 SI SI200530203T patent/SI1761541T1/sl unknown
- 2005-06-13 CA CA2571487A patent/CA2571487C/en not_active Expired - Fee Related
- 2005-06-13 PL PL05754665T patent/PL1761541T3/pl unknown
- 2005-06-13 DE DE602005004287T patent/DE602005004287T2/de not_active Expired - Lifetime
- 2005-06-13 HR HR20080070T patent/HRP20080070T3/xx unknown
- 2005-06-13 ES ES05754665T patent/ES2299044T3/es not_active Expired - Lifetime
- 2005-06-13 DK DK05754665T patent/DK1761541T3/da active
- 2005-06-13 CN CNB2005800187943A patent/CN100528876C/zh not_active Expired - Fee Related
- 2005-06-13 MX MXPA06014809A patent/MXPA06014809A/es active IP Right Grant
- 2005-06-13 RU RU2006143571/04A patent/RU2378277C2/ru not_active IP Right Cessation
- 2005-06-13 PT PT05754665T patent/PT1761541E/pt unknown
- 2005-06-13 NZ NZ551660A patent/NZ551660A/en unknown
- 2005-06-13 AT AT05754665T patent/ATE383361T1/de active
- 2005-06-13 WO PCT/EP2005/006302 patent/WO2005123738A1/en not_active Ceased
- 2005-06-13 AU AU2005254657A patent/AU2005254657B2/en not_active Ceased
- 2005-06-13 BR BRPI0512330-5A patent/BRPI0512330A/pt not_active IP Right Cessation
- 2005-06-13 JP JP2007517134A patent/JP4608542B2/ja not_active Expired - Fee Related
- 2005-06-17 AR ARP050102490A patent/AR049521A1/es not_active Application Discontinuation
- 2005-06-20 US US11/156,974 patent/US7378417B2/en not_active Expired - Fee Related
- 2005-06-20 TW TW094120365A patent/TWI301835B/zh not_active IP Right Cessation
- 2005-06-20 MY MYPI20052792A patent/MY143368A/en unknown
-
2006
- 2006-11-30 IL IL179736A patent/IL179736A/en not_active IP Right Cessation
- 2006-12-01 ZA ZA200610102A patent/ZA200610102B/xx unknown
-
2007
- 2007-01-15 NO NO20070249A patent/NO20070249L/no not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |