EA200701245A1 - Производные 2,4(4,6)-пиримидинов - Google Patents
Производные 2,4(4,6)-пиримидиновInfo
- Publication number
- EA200701245A1 EA200701245A1 EA200701245A EA200701245A EA200701245A1 EA 200701245 A1 EA200701245 A1 EA 200701245A1 EA 200701245 A EA200701245 A EA 200701245A EA 200701245 A EA200701245 A EA 200701245A EA 200701245 A1 EA200701245 A1 EA 200701245A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- het
- calkyl
- 6alkyl
- hydrogen
- independently
- 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
- C07D487/12—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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
-
- 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
- C07D487/22—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 four or more hetero rings
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
Abstract
Настоящее изобретение касается соединений формулы (I), их N-оксидных форм, фармацевтически приемлемых аддитивных солей и стереохимически изомерных форм, где Zи Zпредставляют собой NH; Y представляет собой -Салкил-, -Салкенил-, -Cалкил-NR-Салкил- , -Cалкил-NR-CO-Cалкил- , -Салкил-СО-NH-, -Салкил-NH-СО-, -Салкил-СО-Het-СО-, -Салкил-NH-СО-Het-, -Het-Cалкил-CO-NH-Cалкил-, -Cалкил-NH-CO-L-NH-, -NH-CO-L-NH-, -Салкил-СО-NH-L-СО-, -Салкил-NH-СО-L-NH-СО-Cалкил-, -Cалкил-CO-NH-L-CO-NH-Cалкил-, -Салкил-NR-СН-СО-NH-Салкил-, Het-CO-Cалкил-, -Салкил-СО-NH-Салкил-СО-NH-, -Салкил-NR-СО-Салкил-NH-, -Салкил-NH-CO-Het-CO- или -Cалкил-CO-Het-CO-NH-; Xпредставляет собой прямую связь, О, -О-Салкил-, -СО-Салкил-, -NR-Cалкил-, -CO-NR-, Het-Салкил- или Салкил; Xпредставляет собой прямую связь, О, -О-Салкил-, -СО-Салкил-, -NR-Cалкил-, -CO-NR-, Het-Cалкил- или Салкил; Rи R, каждый независимо, представляют собой водород, галоген, Cалкилокси- или Cалкилоксизамещенный Hetили Салкилокси-; Rи R, каждый независимо, представляют собой водород или галоген; Rпредставляет собой водород или циано; R, R, R, Rи Rпредставляют собой водород; Rпредставляет собой водород или Салкил; Rи Rпредставляют собой водород, Салкил или Het-Салкил-; L, Lи L, каждый независимо, представляют собой Салкил, необязательно замещенный одним или, где возможно, двумя или более заместителями, выбранными из фенила, метилсульфида, циано, полигалогенСалкилфенила-, Салкилокси, пиридинила, моно- или ди(Салкил)амино- или Сциклоалкила; Het, Het, Het, каждый независимо, представляют собой морфолинил, оксазолил, изоксазолил или пиперазинил; Het, Het, Het, каждый независимо, представляют собой морфолинил, пиперазинил, пиперидинил или пирролидинил; Hetпредставляет собой пиперазинил, пиперидинил, пирролидинил или азетидинил; Hetпредставляет собой морфолинил, оксазолил, изоксазолил или пиперазинил, где указанный Hetнеобязательно замещен Салкилом; Hetи Het, каждый независимо, представляют собой гетероцикл,
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63429104P | 2004-12-08 | 2004-12-08 | |
| EP04106384 | 2004-12-08 | ||
| PCT/EP2005/056606 WO2006061415A1 (en) | 2004-12-08 | 2005-12-08 | 2,4 (4,6) pyrimidine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200701245A1 true EA200701245A1 (ru) | 2007-12-28 |
| EA013368B1 EA013368B1 (ru) | 2010-04-30 |
Family
ID=34930016
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200701245A EA013368B1 (ru) | 2004-12-08 | 2005-12-08 | Производные 2,4(4,6)-пиримидинов |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8148388B2 (ru) |
| EP (1) | EP1824856B1 (ru) |
| JP (1) | JP5022909B2 (ru) |
| KR (1) | KR101428506B1 (ru) |
| CN (1) | CN101072779B (ru) |
| AR (1) | AR051788A1 (ru) |
| AU (1) | AU2005313348B2 (ru) |
| BR (1) | BRPI0518424B8 (ru) |
| CA (1) | CA2588761C (ru) |
| CR (1) | CR9234A (ru) |
| DK (1) | DK1824856T3 (ru) |
| EA (1) | EA013368B1 (ru) |
| ES (1) | ES2442458T3 (ru) |
| HK (1) | HK1112455A1 (ru) |
| IL (1) | IL183706A0 (ru) |
| MX (1) | MX2007006821A (ru) |
| MY (1) | MY169441A (ru) |
| NO (1) | NO340130B1 (ru) |
| NZ (1) | NZ554820A (ru) |
| TW (1) | TWI374140B (ru) |
| UA (1) | UA90693C2 (ru) |
| WO (1) | WO2006061415A1 (ru) |
| ZA (1) | ZA200705040B (ru) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2549869C (en) * | 2003-12-18 | 2015-05-05 | Janssen Pharmaceutica N.V. | Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents |
| US7923554B2 (en) * | 2004-08-10 | 2011-04-12 | Janssen Pharmaceutica N.V. | HIV inhibiting 1,2,4-triazin-6-one derivatives |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| WO2007058628A1 (en) * | 2005-11-16 | 2007-05-24 | S*Bio Pte Ltd | Heteroalkyl linked pyrimidine derivatives |
| BRPI0714211B8 (pt) | 2006-07-13 | 2021-05-25 | Janssen Pharmaceutica Nv | derivados de mtki quinazolina, sua utilização e composição farmacêutica que os compreende |
| WO2008060248A1 (en) * | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| CA2693715C (en) | 2007-07-27 | 2015-10-27 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
| US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| CA2716079C (en) * | 2008-03-10 | 2018-01-16 | Janssen Pharmaceutica Nv | 4-aryl-2-anilino-pyrimidines as plk kinase inhibitors |
| EP2274288A2 (en) * | 2008-04-24 | 2011-01-19 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EP2334301B1 (en) * | 2008-09-08 | 2018-02-14 | Merck Serono SA | Macrocyclics pyrimidines as aurora kinase inhibitors |
| WO2010085597A1 (en) * | 2009-01-23 | 2010-07-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| JP2012197231A (ja) * | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| EP2571867B1 (en) | 2010-05-21 | 2015-11-04 | Noviga Research AB | Novel pyrimidine derivatives |
| NZ609957A (en) | 2010-11-01 | 2015-08-28 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| PL2646448T3 (pl) * | 2010-11-29 | 2017-12-29 | OSI Pharmaceuticals, LLC | Makrocykliczne inhibitory kinazy |
| EP2688883B1 (en) | 2011-03-24 | 2016-05-18 | Noviga Research AB | Pyrimidine derivatives |
| US9108927B2 (en) | 2012-03-15 | 2015-08-18 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| CN108658873B (zh) | 2012-03-15 | 2021-09-14 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| JP6401247B2 (ja) * | 2013-05-06 | 2018-10-10 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ阻害剤としての大員環化合物 |
| MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
| MA39822A (fr) * | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
| AU2016215185B2 (en) * | 2015-02-05 | 2020-06-25 | Merck Patent Gmbh | Macrocyclic compounds as IRAK 1/4 inhibitors and uses thereof |
| US11242356B2 (en) | 2017-03-28 | 2022-02-08 | Bayer Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| ES2963382T3 (es) | 2019-06-12 | 2024-03-26 | Nouryon Chemicals Int Bv | Proceso para la producción de peróxidos de diacilo |
| ES2963357T3 (es) | 2019-06-12 | 2024-03-26 | Nouryon Chemicals Int Bv | Proceso para la producción de peróxidos de diacilo |
| EP3983340B1 (en) * | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Method for isolating carboxylic acid from an aqueous side stream |
| CN115515588A (zh) * | 2020-02-14 | 2022-12-23 | 萨克生物研究学院 | 大环ulk1/2抑制剂 |
| CN113549113A (zh) * | 2020-06-17 | 2021-10-26 | 广州百霆医药科技有限公司 | 一种含膦大环化合物及其制备方法与应用 |
| 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 |
| WO2023113510A1 (ko) * | 2021-12-15 | 2023-06-22 | 환인제약 주식회사 | 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002523497A (ja) * | 1998-08-29 | 2002-07-30 | アストラゼネカ・アクチエボラーグ | ピリミジン化合物 |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) * | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| CN1678321A (zh) * | 2002-07-29 | 2005-10-05 | 里格尔药品股份有限公司 | 用2,4－嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法 |
| DE10239042A1 (de) | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| JO2785B1 (en) | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| DE602004023876D1 (de) | 2003-12-18 | 2009-12-10 | Janssen Pharmaceutica Nv | 3-cyano-chinolin-derivate mit antiproliferativer wirkung |
| CA2549869C (en) | 2003-12-18 | 2015-05-05 | Janssen Pharmaceutica N.V. | Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents |
-
2005
- 2005-12-06 MY MYPI20055703A patent/MY169441A/en unknown
- 2005-12-07 AR ARP050105123A patent/AR051788A1/es unknown
- 2005-12-07 TW TW094143059A patent/TWI374140B/zh active
- 2005-12-08 UA UAA200705051A patent/UA90693C2/ru unknown
- 2005-12-08 WO PCT/EP2005/056606 patent/WO2006061415A1/en active Application Filing
- 2005-12-08 EA EA200701245A patent/EA013368B1/ru not_active IP Right Cessation
- 2005-12-08 CN CN2005800420717A patent/CN101072779B/zh active Active
- 2005-12-08 CA CA2588761A patent/CA2588761C/en active Active
- 2005-12-08 JP JP2007544917A patent/JP5022909B2/ja active Active
- 2005-12-08 US US11/720,681 patent/US8148388B2/en active Active
- 2005-12-08 KR KR1020077011771A patent/KR101428506B1/ko active IP Right Grant
- 2005-12-08 AU AU2005313348A patent/AU2005313348B2/en active Active
- 2005-12-08 NZ NZ554820A patent/NZ554820A/en unknown
- 2005-12-08 EP EP05819148.7A patent/EP1824856B1/en active Active
- 2005-12-08 BR BRPI0518424A patent/BRPI0518424B8/pt active IP Right Grant
- 2005-12-08 MX MX2007006821A patent/MX2007006821A/es active IP Right Grant
- 2005-12-08 ES ES05819148.7T patent/ES2442458T3/es active Active
- 2005-12-08 DK DK05819148.7T patent/DK1824856T3/da active
-
2007
- 2007-06-06 IL IL183706A patent/IL183706A0/en active IP Right Grant
- 2007-06-07 ZA ZA200705040A patent/ZA200705040B/xx unknown
- 2007-07-06 CR CR9234A patent/CR9234A/es not_active Application Discontinuation
- 2007-07-09 NO NO20073492A patent/NO340130B1/no unknown
-
2008
- 2008-02-04 HK HK08101310.3A patent/HK1112455A1/xx unknown
-
2011
- 2011-10-20 US US13/277,651 patent/US8394955B2/en active Active
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