AR071619A1 - Compuestos de pirazina fusionados utiles para el tratamiento de enfermedades degenerativas e inflamatorias y composiciones farmaceuticas que los contienen. - Google Patents
Compuestos de pirazina fusionados utiles para el tratamiento de enfermedades degenerativas e inflamatorias y composiciones farmaceuticas que los contienen.Info
- Publication number
- AR071619A1 AR071619A1 ARP090101598A ARP090101598A AR071619A1 AR 071619 A1 AR071619 A1 AR 071619A1 AR P090101598 A ARP090101598 A AR P090101598A AR P090101598 A ARP090101598 A AR P090101598A AR 071619 A1 AR071619 A1 AR 071619A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- cycloalkyl
- independently
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000003412 degenerative effect Effects 0.000 title 1
- 208000027866 inflammatory disease Diseases 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos se pueden preparar como composiciones farmacéuticas, y se pueden utilizar para la prevencion y el tratamiento de una variedad de afecciones, que incluye a modo de ejemplo no limitativo, dolor, inflamacion, y otros. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en donde cada uno de W, W', Y, e Y' es independientemente CR2a o N; con la condicion de que no más de dos de W, W', Y, e Y' puedan ser N al mismo tiempo; X es N o CH; L se selecciona de un enlace simple, -CO-, -SO-, -SO2-, -N(R2c)CO-, y -N(R2c)SO2-; el anillo P se encuentra sustituido o no sustituido, grupo de formulas (2), R1es H, o alquilo C1-6, sustituido o no sustituido; cada uno de R2a se selecciona independientemente de H, alquilo C1-6 sustituido o no sustituido, haloalquilo C1-6 no sustituido, cicloalquilo C3-8 sustituido o no sustituido, alcoxi C1-6 sustituido o no sustituido, ciano, y halo; cada uno de R2c se selecciona independientemente de H y alquilo C1-6; R2d es H, cicloalquilo C3-8, o alquilo C1-6 opcionalmente sustituido con halo, o cicloalquilo C3-8; cada uno m1, m2 y m3 es independientemente 1 o 2; r3 se selecciona de arilo sustituido o no sustituido, y heteroarilo sustituido o no sustituido; y o su sal farmacéuticamente aceptable o un solvato del compuesto o la sal farmacéuticamente aceptable. Reivindicacion 2: Un compuesto de acuerdo con la formula (3) en donde cada uno de W, W', Y, e Y' s independientemente CR2a o N; con la condicion de que no más de dos de W, W', Y, e Y' puedan ser N en el mismo momento; X es N o CH; L se selecciona de un enlace simple, -CO-, -SO-, -SO2-, -N(R2c)CO-, y -N(R2c)SO2-; el anillo P se encuentra sustituido o no sustituido, grupo de formulas (2); R1 es H, o alquilo C1-6 sustituido o no sustituido; cada uno de R2a se selecciona independientemente de H, alquilo C1-6 sustituido o no sustituido, haloalquilo C1-6 no sustituido, cicloalquilo C3-8 sustituido o no sustituido, alcoxi C1-6 sustituido o no sustituido, ciano, y halo; cada uno de R2c se selecciona independientemente de H y alquilo C1-6; R2d es H, cicloalquilo C3-8, o alquilo C1-6 opcionalmente sustituido con halo, o cicloalquilo C3-8; cada uno de m1, m2 y m3 es independientemente 1 o 2; R3 se selecciona de arilo sustituido o no sustituido, y heteroarilo sustituido o no sustituido; y o su sal farmacéuticamente aceptable o un solvato del compuesto o la sal farmacéuticamente aceptable.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12683308P | 2008-05-07 | 2008-05-07 | |
| US14582709P | 2009-01-20 | 2009-01-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR071619A1 true AR071619A1 (es) | 2010-06-30 |
Family
ID=40935606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090101598A AR071619A1 (es) | 2008-05-07 | 2009-05-04 | Compuestos de pirazina fusionados utiles para el tratamiento de enfermedades degenerativas e inflamatorias y composiciones farmaceuticas que los contienen. |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8012983B2 (es) |
| EP (1) | EP2307426A1 (es) |
| JP (1) | JP2011519897A (es) |
| KR (1) | KR20110028445A (es) |
| CN (1) | CN102036997A (es) |
| AR (1) | AR071619A1 (es) |
| AU (1) | AU2009245731A1 (es) |
| BR (1) | BRPI0912412A2 (es) |
| CA (1) | CA2723745A1 (es) |
| CL (1) | CL2009001064A1 (es) |
| CO (1) | CO6321159A2 (es) |
| CR (1) | CR11823A (es) |
| EA (1) | EA201071275A1 (es) |
| IL (1) | IL209104A0 (es) |
| MX (1) | MX2010011994A (es) |
| PE (1) | PE20091880A1 (es) |
| TW (1) | TW201002716A (es) |
| UY (1) | UY31813A (es) |
| WO (1) | WO2009135885A1 (es) |
| ZA (1) | ZA201008759B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201120043A (en) * | 2009-11-05 | 2011-06-16 | Galapagos Nv | Fused pyrazine compounds as their salts, useful for the treatment of degenerative and inflammatory diseases |
| JP6435323B2 (ja) * | 2013-06-19 | 2018-12-05 | ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． | 炎症性障害の治療のための新規化合物及びその医薬組成物 |
| EP3137454A1 (en) | 2014-04-28 | 2017-03-08 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
| JP6751203B2 (ja) | 2016-06-07 | 2020-09-02 | ジャコバイオ ファーマスーティカルズ カンパニー リミテッドＪａｃｏｂｉｏ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｃｏ．， Ｌｔｄ． | Ｓｈｐ２阻害剤として有用な新規複素環式誘導体 |
| SG11201908820VA (en) | 2017-03-23 | 2019-10-30 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| CN108379583B (zh) * | 2018-03-27 | 2021-08-17 | 北京大学 | 一种肿瘤转移药物治疗的靶标及其应用 |
| WO2020063760A1 (en) | 2018-09-26 | 2020-04-02 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
| CN113967214A (zh) * | 2021-11-30 | 2022-01-25 | 广东药科大学 | 一种咪唑并吡嗪环丙烷甲酰胺类化合物的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6413776B1 (en) | 1998-06-12 | 2002-07-02 | Galapagos Geonomics N.V. | High throughput screening of gene function using adenoviral libraries for functional genomics applications |
| US20020132823A1 (en) | 2001-01-17 | 2002-09-19 | Jiahuai Han | Assay method |
| US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| US7893058B2 (en) * | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| KR20090026288A (ko) * | 2006-05-31 | 2009-03-12 | 갈라파고스 엔.브이. | 퇴행성 및 염증성 질환의 치료에 유용한 트리아졸로피라진 화합물 |
| WO2008138842A1 (en) * | 2007-05-10 | 2008-11-20 | Galapagos N.V. | Imidazopyrazines and triazolopyrazine for the treatment of joint degenerative and inflammatory diseases |
| US8133895B2 (en) | 2007-05-10 | 2012-03-13 | Janssen Pharmaceutica N.V. | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
-
2009
- 2009-05-04 CL CL2009001064A patent/CL2009001064A1/es unknown
- 2009-05-04 AR ARP090101598A patent/AR071619A1/es unknown
- 2009-05-06 WO PCT/EP2009/055500 patent/WO2009135885A1/en not_active Ceased
- 2009-05-06 KR KR1020107027298A patent/KR20110028445A/ko not_active Withdrawn
- 2009-05-06 AU AU2009245731A patent/AU2009245731A1/en not_active Abandoned
- 2009-05-06 BR BRPI0912412A patent/BRPI0912412A2/pt not_active IP Right Cessation
- 2009-05-06 CN CN2009801163126A patent/CN102036997A/zh active Pending
- 2009-05-06 EP EP09742103A patent/EP2307426A1/en not_active Withdrawn
- 2009-05-06 US US12/436,219 patent/US8012983B2/en not_active Expired - Fee Related
- 2009-05-06 MX MX2010011994A patent/MX2010011994A/es not_active Application Discontinuation
- 2009-05-06 PE PE2009000625A patent/PE20091880A1/es not_active Application Discontinuation
- 2009-05-06 JP JP2011507918A patent/JP2011519897A/ja active Pending
- 2009-05-06 EA EA201071275A patent/EA201071275A1/ru unknown
- 2009-05-06 CA CA2723745A patent/CA2723745A1/en not_active Abandoned
- 2009-05-07 UY UY0001031813A patent/UY31813A/es unknown
- 2009-05-07 TW TW098115200A patent/TW201002716A/zh unknown
-
2010
- 2010-11-04 IL IL209104A patent/IL209104A0/en unknown
- 2010-12-03 CR CR11823A patent/CR11823A/es not_active Application Discontinuation
- 2010-12-03 CO CO10152830A patent/CO6321159A2/es not_active Application Discontinuation
- 2010-12-06 ZA ZA2010/08759A patent/ZA201008759B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2009001064A1 (es) | 2009-10-09 |
| EP2307426A1 (en) | 2011-04-13 |
| UY31813A (es) | 2010-01-05 |
| AU2009245731A1 (en) | 2009-11-12 |
| JP2011519897A (ja) | 2011-07-14 |
| TW201002716A (en) | 2010-01-16 |
| CN102036997A (zh) | 2011-04-27 |
| IL209104A0 (en) | 2011-01-31 |
| ZA201008759B (en) | 2011-08-31 |
| US8012983B2 (en) | 2011-09-06 |
| MX2010011994A (es) | 2010-11-30 |
| CR11823A (es) | 2011-03-16 |
| WO2009135885A1 (en) | 2009-11-12 |
| PE20091880A1 (es) | 2009-12-28 |
| EA201071275A1 (ru) | 2011-06-30 |
| KR20110028445A (ko) | 2011-03-18 |
| CA2723745A1 (en) | 2009-11-12 |
| US20090286798A1 (en) | 2009-11-19 |
| BRPI0912412A2 (pt) | 2016-07-26 |
| CO6321159A2 (es) | 2011-09-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |