AR073551A1 - Pirimidinas macrociclicas como inhibidores de proteina cinasa - Google Patents
Pirimidinas macrociclicas como inhibidores de proteina cinasaInfo
- Publication number
- AR073551A1 AR073551A1 ARP090103426A ARP090103426A AR073551A1 AR 073551 A1 AR073551 A1 AR 073551A1 AR P090103426 A ARP090103426 A AR P090103426A AR P090103426 A ARP090103426 A AR P090103426A AR 073551 A1 AR073551 A1 AR 073551A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- aryl
- compounds
- heteroaryl
- bridge
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
- 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
- A61P25/28—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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
-
- 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
- C07D487/08—Bridged systems
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D515/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (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
Se proporcionan compuestos derivados macrocíclicos que inhiben las enzimas proteína cinasa junto con composiciones farmacéuticas que comprenden estos compuestos y métodos para sintetizar los mismos. Dichos compuestos tienen utilidad en el tratamiento de enfermedades proliferativas que resultan de una actividad de cinasa no regulada y/o alterada tales como cánceres, psoriasis, infecciones virales y bacterianas, y enfermedades inflamatorias y autoinmunitarias. Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque: X es H; halogeno; preferiblemente F; CF3 CN, NO2, N(RR'), C(O)N(RR'); C(O)OR; C(O)H; S(O)2; S(OH); S(O); o S(O)NRR'; Los anillos A y B, cada uno independientemente es arilo, un heterociclo saturado o insaturado o un unicarbociclo, bicarbociclo o tricarbociclo saturado o insaturado, que forma un puente o que no forma un puente, cualquiera de los cuales opcionalmente puede estar sustituido; ---------- representa la presencia o ausencia de un enlace doble; L1, L2, L2', L2ö, L2'ö y L3, cada uno independientemente es CH2, CH, CH(OH); C(=O), O, S, S(O), S(OH), S(O)2, NR2 o NH; R y R', cada uno independientemente es H, alquilo C1-6, heteroalquilo C1-6, arilo; heteroarilo; heterociclo; (CH2)2OH, (CH2)2-O-(CH2)2-; (CH2)2-NH2; (CH2)2NRx o (CH2)2-Ry, en donde Rx, y Ry, cada uno independientemente es CH3 o C2F5; R2 es arilo, heteroarilo o alquilo; n, p y q, cada uno independientemente, es 0 o 1; r es 0, 1, 2, 3 o 4; o una sal, profármaco, hidrato, solvato, tautomero, enantiomero o mezcla racémica farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19150508P | 2008-09-08 | 2008-09-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073551A1 true AR073551A1 (es) | 2010-11-17 |
Family
ID=41403411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103426A AR073551A1 (es) | 2008-09-08 | 2009-09-07 | Pirimidinas macrociclicas como inhibidores de proteina cinasa |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8815872B2 (es) |
| EP (1) | EP2334301B1 (es) |
| JP (1) | JP5749645B2 (es) |
| KR (1) | KR20110073500A (es) |
| CN (1) | CN102143750B (es) |
| AR (1) | AR073551A1 (es) |
| AU (1) | AU2009288021B2 (es) |
| CA (1) | CA2735420C (es) |
| EA (1) | EA201100450A1 (es) |
| ES (1) | ES2668834T3 (es) |
| HK (1) | HK1158947A1 (es) |
| IL (1) | IL211584A (es) |
| MX (1) | MX2011002470A (es) |
| WO (1) | WO2010028116A1 (es) |
| ZA (1) | ZA201101243B (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201100441A (en) | 2009-06-01 | 2011-01-01 | Osi Pharm Inc | Amino pyrimidine anticancer compounds |
| PL2646448T3 (pl) * | 2010-11-29 | 2017-12-29 | OSI Pharmaceuticals, LLC | Makrocykliczne inhibitory kinazy |
| CA2872979C (en) | 2011-05-19 | 2020-02-18 | Joaquin Pastor Fernandez | Macrocyclic compounds as protein kinase inhibitors |
| EP2817306B1 (en) | 2012-02-21 | 2015-09-16 | Merck Patent GmbH | Cyclic diaminopyrimidine derivatives as syk inhibitors |
| CA2863892C (en) * | 2012-03-06 | 2016-08-30 | Pfizer Inc. | Macrocyclic derivatives for the treatment of proliferative diseases |
| WO2014008636A1 (en) * | 2012-07-11 | 2014-01-16 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as hiv integrase inhibitors |
| PT2953952T (pt) * | 2013-02-07 | 2017-09-11 | Merck Patent Gmbh | Derivados de piridazinona macrocíclicos |
| PL3572416T3 (pl) * | 2014-01-24 | 2023-02-27 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| TWI736134B (zh) * | 2014-09-11 | 2021-08-11 | 美商特普醫葯公司 | 作為蛋白質激酶之調節劑的二芳基巨環 |
| MX2017017097A (es) | 2015-07-02 | 2018-05-23 | Tp Therapeutics Inc | Macrociclos diarílicos quirales como moduladores de proteínas quinasas. |
| EP4397665A3 (en) | 2015-07-06 | 2024-08-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
| RS66238B1 (sr) | 2015-07-21 | 2024-12-31 | Turning Point Therapeutics Inc | Hiralni diaril makrocikl i njegova primena u lečenju karcinoma |
| AU2017302019A1 (en) * | 2016-07-28 | 2019-02-07 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| RS65884B1 (sr) | 2017-07-28 | 2024-09-30 | Turning Point Therapeutics Inc | Makrociklična jedinjenja i primene istih |
| BR112020008834A2 (pt) | 2017-11-02 | 2020-12-22 | Calico Life Sciences Llc | Moduladores da via de estresse integrada |
| UY37957A (es) * | 2017-11-02 | 2019-05-31 | Abbvie Inc | Moduladores de la vía de estrés integrada |
| CN111511746B (zh) | 2017-12-19 | 2024-01-09 | 特普医药公司 | 用于治疗疾病的巨环化合物 |
| CN110950890B (zh) * | 2018-09-27 | 2022-07-01 | 北京赛林泰医药技术有限公司 | 取代的咪唑并[4,5-c]喹啉大环化合物作为多靶点激酶抑制剂 |
| TW202430498A (zh) | 2018-10-11 | 2024-08-01 | 美商嘉來克生命科學有限責任公司 | 整合應激路徑之前藥調節劑 |
| EP3878854A4 (en) * | 2018-11-09 | 2022-08-10 | Shandong Xuanzhu Pharma Co., Ltd. | MACROCYCLIC TYROSINE KINASE INHIBITOR AND USES THEREOF |
| EP3968971A1 (en) | 2019-05-17 | 2022-03-23 | Cancer Prevention Pharmaceuticals, Inc. | Methods for treating familial adenomatous polyposis |
| CN114401971A (zh) * | 2019-08-16 | 2022-04-26 | 英夫拉索姆有限公司 | 用作nlrp3抑制剂的大环磺酰脲衍生物 |
| AU2021237477A1 (en) * | 2020-03-16 | 2022-10-13 | Zomagen Biosciences Ltd | NLRP3 modulators |
| AU2021262482A1 (en) | 2020-04-28 | 2023-01-05 | Iomx Therapeutics Ag | Bicyclic kinase inhibitors and uses thereof |
| JP7495035B2 (ja) * | 2020-05-08 | 2024-06-04 | シュエンジュウ バイオファーマシューティカル カンパニー リミテッド | 大環類チロシンキナーゼ阻害剤の結晶形及びその製造方法 |
| CN113735856A (zh) * | 2020-05-29 | 2021-12-03 | 百极弘烨(南通)医药科技有限公司 | 大环jak抑制剂及其应用 |
| CA3194090A1 (en) * | 2020-09-30 | 2022-04-07 | Takahiko Ito | Macrocyclic compound |
| CN113603708B (zh) * | 2021-07-27 | 2023-08-11 | 中国药科大学 | 一种具有大环骨架结构的cdk9抑制剂的制备及其应用 |
| EP4450505A1 (en) * | 2021-12-15 | 2024-10-23 | Whan In Pharmaceutical Co., Ltd. | Macrocyclic pyrimidine derivative, method for preparing same, and pharmaceutical composition for prevention or treatment of neurodegenerative disease containing same as active ingredient |
| KR102613509B1 (ko) * | 2021-12-15 | 2023-12-13 | 환인제약 주식회사 | 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물 |
| WO2024017258A1 (zh) * | 2022-07-19 | 2024-01-25 | 百极弘烨(南通)医药科技有限公司 | Egfr小分子抑制剂、含其的药物组合物及其用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0308113B8 (pt) | 2002-03-08 | 2021-05-25 | Eisai Co Ltd | compostos macrocíclicos úteis como substâncias farmacêuticas |
| DE10239042A1 (de) * | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| US7151096B2 (en) | 2003-03-05 | 2006-12-19 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
| US7163939B2 (en) | 2003-11-05 | 2007-01-16 | Abbott Laboratories | Macrocyclic kinase inhibitors |
| US20050096324A1 (en) | 2003-11-05 | 2005-05-05 | Zhi-Fu Tao | Macrocyclic kinase inhibitors |
| CA2566531A1 (en) * | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| EP1904457B1 (en) * | 2005-06-08 | 2017-09-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070032514A1 (en) * | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
| EP1803723A1 (de) | 2006-01-03 | 2007-07-04 | Bayer Schering Pharma Aktiengesellschaft | (2,4,9-triaza-1(2,4)-pyrimidina-3(1,3)-benzenacyclononaphan-3^4-yl)-sulfoximid derivate als selektive inhibitoren der aurora kinase zur behandlung von krebs |
| WO2009132202A2 (en) | 2008-04-24 | 2009-10-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
-
2009
- 2009-09-03 MX MX2011002470A patent/MX2011002470A/es active IP Right Grant
- 2009-09-03 CN CN200980135832.1A patent/CN102143750B/zh not_active Expired - Fee Related
- 2009-09-03 AU AU2009288021A patent/AU2009288021B2/en not_active Ceased
- 2009-09-03 WO PCT/US2009/055841 patent/WO2010028116A1/en active Application Filing
- 2009-09-03 JP JP2011526185A patent/JP5749645B2/ja not_active Expired - Fee Related
- 2009-09-03 KR KR1020117008031A patent/KR20110073500A/ko not_active Application Discontinuation
- 2009-09-03 CA CA2735420A patent/CA2735420C/en not_active Expired - Fee Related
- 2009-09-03 EP EP09792214.0A patent/EP2334301B1/en not_active Not-in-force
- 2009-09-03 ES ES09792214.0T patent/ES2668834T3/es active Active
- 2009-09-03 EA EA201100450A patent/EA201100450A1/ru unknown
- 2009-09-03 US US13/062,413 patent/US8815872B2/en not_active Expired - Fee Related
- 2009-09-07 AR ARP090103426A patent/AR073551A1/es not_active Application Discontinuation
-
2011
- 2011-02-16 ZA ZA2011/01243A patent/ZA201101243B/en unknown
- 2011-03-06 IL IL211584A patent/IL211584A/en active IP Right Grant
- 2011-12-14 HK HK11113460.1A patent/HK1158947A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ES2668834T3 (es) | 2018-05-22 |
| IL211584A (en) | 2017-04-30 |
| US20110294801A1 (en) | 2011-12-01 |
| MX2011002470A (es) | 2011-04-05 |
| CN102143750B (zh) | 2014-04-02 |
| CA2735420A1 (en) | 2010-03-11 |
| AU2009288021B2 (en) | 2015-06-18 |
| US8815872B2 (en) | 2014-08-26 |
| CA2735420C (en) | 2016-06-28 |
| JP2012502043A (ja) | 2012-01-26 |
| EA201100450A1 (ru) | 2011-10-31 |
| AU2009288021A1 (en) | 2010-03-11 |
| EP2334301B1 (en) | 2018-02-14 |
| HK1158947A1 (en) | 2012-07-27 |
| EP2334301A1 (en) | 2011-06-22 |
| WO2010028116A1 (en) | 2010-03-11 |
| KR20110073500A (ko) | 2011-06-29 |
| CN102143750A (zh) | 2011-08-03 |
| JP5749645B2 (ja) | 2015-07-15 |
| ZA201101243B (en) | 2012-05-30 |
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