BRPI0518424A2 - derivados de 2,4 (4,6) pirimidina - Google Patents
derivados de 2,4 (4,6) pirimidinaInfo
- Publication number
- BRPI0518424A2 BRPI0518424A2 BRPI0518424-0A BRPI0518424A BRPI0518424A2 BR PI0518424 A2 BRPI0518424 A2 BR PI0518424A2 BR PI0518424 A BRPI0518424 A BR PI0518424A BR PI0518424 A2 BRPI0518424 A2 BR PI0518424A2
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- het
- piperazinyl
- hydrogen
- pyrrolidinyl
- 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
-
- 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
-
- 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
- C07D487/22—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
Abstract
DERIVADOS DE 2,4 (4,6) PIRIMIDINA. A presente invenção refere-se a compostos da fórmula. As formas de N-óxido, os sais de adição farmaceuticamente aceitáveis e as formas estereoquimicamente isoméricas dos mesmos, em que: Z¹ e Z² representa NH; Y representa -C~ 3-9~ alquila-, -C~ 3-9~ alquenila-, -C~ 1-5~ alquil-NR^ 6^-C~ 1-5~ alquila-, -C~ 1-5~ alquil-NR^ 7^-CO-C~ 1-5~ alquila-, -C~ 1-6~ alquil-CO-NH-, -C~ 1-6~ alquil- NH-CO-, -C~ 1-2~ alquil-CO-Het^ 10^-CO-, -C~ 1-3~ alquil-NH-CO-Hetü-, -Het^ 4^-C.~ 1-3~ alquil-CO-NH-C~ 1-3~ alquila-, -C~ 1-2~ alquil-NH-CO-L¹-NH-, -NH-CO-L²-NH-, -C~ 1-2~ alquil-CO-NH-Lü-CO-, -C~ 1-2~ alquil-NH-CO-L¹-NH-CO-C~ 1-3~ alquila-, -C~ 1-2~ alquil- CO-NH-Lü-CO-NH-C~ 1-3~ alquila-, -C~ 1-2~ alquil-NR¹¹-CH~ 2~-CO-NH-C~ 1-3~ alquila-, Het^ 5^-CO-C~ 1-2~ alquila, -C~ 1-5~ aIquiI-CO-NH-C~ 1-3~ alquil-CO-NH-, -C~ 1-5~ alquil- NR¹ü-CO-C~ 1-3~ alquil-NH-, -C13 alquil-NH-CO-Het^ 27^-CO- ou -C~ 1-3~ alquil-CO- Het^ 28^-CO-NH-; X¹ representa uma ligação direta, O, -O-C~ 1-2~ alquila-, -CO-C~ 1-2~ alquila-, -NR^ 16^-C~ 1-2~ alquila-, -CO-NR^ 17^-, Het^ 23^-C~ 1-2~ alquila- ou C~ 1-2~ alquila; X² representa uma ligação direta, O, -O-C~ 1-2~ alquila-, -CO-C~ 1-2~ alquila-, -NR^ 18^-C~ 1-2~ alquila-, -CO-NR^ 19^-, Het^ 24^-C~ 1-2~ alquila- ou C~ 1-2~ alquila; R¹ e R^ 5^ representam, cada um independentemente, hidrogênio, halo, C~ 1-6~ alquilóxi- ou C~ 1-6~ alquilóxi- substituído por Het¹ ou C~ 1-4~ alquilóxi-; R² e R^ 4^ representam, cada um independentemente, hidrogênio ou halo; Rü representa hidrogênio ou ciano; R^ 6^, R^ 7^, R^ 13^, R^ 17^ e R^ 19^ representam hidrogênio; R¹¹ representa hidrogênio ou C~ 1-4~ alquila; R^ 16^e R^ 18^ representa hidrogênio, C~ 1-4~ alquila ou Het^ 17^-C~ 1-4~ alquila-; L¹, L¹ e Lü representam, cada um independentemente, C~ 1-8~ alquila opcionalmente substituida por um ou, onde possível, dois ou mais substituintes selecionados de fenita, metil-sulfeto, ciano, C~ 1-4~ polihaloalquil- fenila-, C~ 1-4~ alquilóxi, piridinila, mono- ou di(C~ 1-4~ alquil)-amino- ou C~ 3-6~ ciclo alquila; Het¹, Het², Het^ 17^ representam, cada um independentemente, morfolinila, oxazolila, isoxazolila ou piperazinila; Hetü, Het^ 4^, Het^ 5^ representam, cada um independentemente, mor- folinila, piperazinila, piperidinila ou pirrolidinila; Het^ 10^ representa piperazinila, piperidinila, pirrolidinila ou azetidinila; Het²² representa morfolinila, oxazolila, isoxazolila ou piperazinila em que o referido Het²² é opcionalmente substituido por C~ 1-4~ alquila; Het²ü e Het^ 24^ representam, cada um independentemente, um heterociclo selecionado de pirrolidinila, piperazinila ou piperidinila em que os referidos Het²ü ou Het^ 24^ são opcionalmente substituidos por Het²²-carbonila; Het^ 27^ e Het^ 28^ representam, cada um independentemente, um heterociclo selecionado de morfolinila, piperazinila, piperidinila ou pirrolidinila.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63429104P | 2004-12-08 | 2004-12-08 | |
| US60/634,291 | 2004-12-08 | ||
| EP04106384 | 2004-12-08 | ||
| EP04106384.3 | 2004-12-08 | ||
| PCT/EP2005/056606 WO2006061415A1 (en) | 2004-12-08 | 2005-12-08 | 2,4 (4,6) pyrimidine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0518424A2 true BRPI0518424A2 (pt) | 2008-11-25 |
| BRPI0518424B1 BRPI0518424B1 (pt) | 2020-10-13 |
| BRPI0518424B8 BRPI0518424B8 (pt) | 2021-05-25 |
Family
ID=34930016
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0518424A BRPI0518424B8 (pt) | 2004-12-08 | 2005-12-08 | derivados de 2,4 (4,6) pirimidina, composição farmacêutica que os compreende, intermediários e uso dos mesmos |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8148388B2 (pt) |
| EP (1) | EP1824856B1 (pt) |
| JP (1) | JP5022909B2 (pt) |
| KR (1) | KR101428506B1 (pt) |
| CN (1) | CN101072779B (pt) |
| AR (1) | AR051788A1 (pt) |
| AU (1) | AU2005313348B2 (pt) |
| BR (1) | BRPI0518424B8 (pt) |
| CA (1) | CA2588761C (pt) |
| CR (1) | CR9234A (pt) |
| DK (1) | DK1824856T3 (pt) |
| EA (1) | EA013368B1 (pt) |
| ES (1) | ES2442458T3 (pt) |
| HK (1) | HK1112455A1 (pt) |
| IL (1) | IL183706A0 (pt) |
| MX (1) | MX2007006821A (pt) |
| MY (1) | MY169441A (pt) |
| NO (1) | NO340130B1 (pt) |
| NZ (1) | NZ554820A (pt) |
| TW (1) | TWI374140B (pt) |
| UA (1) | UA90693C2 (pt) |
| WO (1) | WO2006061415A1 (pt) |
| ZA (1) | ZA200705040B (pt) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA06007017A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidina como agentes antiproliferativos. |
| 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 |
| US8143255B2 (en) | 2005-11-16 | 2012-03-27 | S*Bio Pte Ltd. | Heteroalkyl linked pyrimidine derivatives |
| WO2008006884A2 (en) * | 2006-07-13 | 2008-01-17 | Janssen Pharmaceutica N.V. | Mtki quinazoline derivatives |
| WO2008060248A1 (en) * | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| DK2185562T3 (en) | 2007-07-27 | 2016-02-22 | Janssen Pharmaceutica Nv | PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| TWI475996B (zh) | 2007-10-19 | 2015-03-11 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| US8318929B2 (en) | 2008-03-10 | 2012-11-27 | Janssen Pharmaceutica Nv | 4-aryl-2-anilino-pyrimidines |
| JP2011518836A (ja) * | 2008-04-24 | 2011-06-30 | インサイト・コーポレイション | 大環状化合物およびそれらのキナーゼ阻害剤としての使用 |
| 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 |
| CA2735420C (en) | 2008-09-08 | 2016-06-28 | Merck Patent Gmbh | Macrocyclic pyrimidines as protein kinase inhibitors |
| US8765727B2 (en) | 2009-01-23 | 2014-07-01 | 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 |
| US8927547B2 (en) | 2010-05-21 | 2015-01-06 | Noviga Research Ab | Pyrimidine derivatives |
| NZ710636A (en) | 2010-11-01 | 2017-02-24 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| PL2646448T3 (pl) * | 2010-11-29 | 2017-12-29 | OSI Pharmaceuticals, LLC | Makrocykliczne inhibitory kinazy |
| WO2012127032A1 (en) | 2011-03-24 | 2012-09-27 | Chemilia Ab | Novel pyrimidine derivatives |
| CA2866857C (en) | 2012-03-15 | 2021-03-09 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| ES2880109T3 (es) | 2012-03-15 | 2021-11-23 | Celgene Car Llc | Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico |
| ES2637721T3 (es) * | 2013-05-06 | 2017-10-16 | Merck Patent Gmbh | Macrociclos como inhibidores de quinasa |
| MA39822A (fr) | 2014-04-03 | 2018-02-06 | Janssen Pharmaceutica Nv | Dérivés de pyrimidine bicycle |
| MA39823A (fr) | 2014-04-03 | 2018-01-09 | Janssen Pharmaceutica Nv | Dérivés de pyridine macrocyclique |
| JP6835727B2 (ja) * | 2015-02-05 | 2021-02-24 | 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 | Ｉｒａｋ１／４阻害剤としての大環状化合物及びその使用 |
| US11242356B2 (en) | 2017-03-28 | 2022-02-08 | Bayer Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
| PL3601253T3 (pl) | 2017-03-28 | 2022-01-17 | Bayer Aktiengesellschaft | Nowe hamujące ptefb związki makrocykliczne |
| BR112021024870A2 (pt) * | 2019-06-12 | 2022-01-18 | Nouryon Chemicals Int Bv | Método para isolar ácido carboxílico de uma corrente lateral aquosa de um processo de produção de peróxido orgânico |
| US11976034B2 (en) | 2019-06-12 | 2024-05-07 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| JP7336541B2 (ja) | 2019-06-12 | 2023-08-31 | ヌーリオン ケミカルズ インターナショナル ベスローテン フェノーツハップ | 過酸化ジアシルを生成するためのプロセス |
| EP4103183A4 (en) * | 2020-02-14 | 2024-02-28 | Salk Inst For Biological Studi | MACROCYCLIC ULK1/2 INHIBITORS |
| 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 |
| 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 |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| 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 |
| ES2445208T3 (es) * | 2002-07-29 | 2014-02-28 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias |
| DE10239042A1 (de) * | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| PA8603801A1 (es) | 2003-05-27 | 2004-12-16 | Janssen Pharmaceutica Nv | Derivados de la quinazolina |
| MXPA06007017A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidina como agentes antiproliferativos. |
| WO2005058318A1 (en) | 2003-12-18 | 2005-06-30 | Janssen Pharmaceutica N.V. | 3-cyano-quinoline derivatives with antiproliferative activity |
-
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 ES ES05819148.7T patent/ES2442458T3/es active Active
- 2005-12-08 EA EA200701245A patent/EA013368B1/ru not_active IP Right Cessation
- 2005-12-08 KR KR1020077011771A patent/KR101428506B1/ko active IP Right Grant
- 2005-12-08 CN CN2005800420717A patent/CN101072779B/zh active Active
- 2005-12-08 EP EP05819148.7A patent/EP1824856B1/en active Active
- 2005-12-08 DK DK05819148.7T patent/DK1824856T3/da 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 MX MX2007006821A patent/MX2007006821A/es active IP Right Grant
- 2005-12-08 BR BRPI0518424A patent/BRPI0518424B8/pt active IP Right Grant
- 2005-12-08 JP JP2007544917A patent/JP5022909B2/ja active Active
- 2005-12-08 CA CA2588761A patent/CA2588761C/en active Active
- 2005-12-08 AU AU2005313348A patent/AU2005313348B2/en active Active
- 2005-12-08 NZ NZ554820A patent/NZ554820A/en unknown
- 2005-12-08 US US11/720,681 patent/US8148388B2/en active 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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