BRPI0518424B8 - derivados de 2,4 (4,6) pirimidina, composição farmacêutica que os compreende, intermediários e uso dos mesmos - Google Patents
derivados de 2,4 (4,6) pirimidina, composição farmacêutica que os compreende, intermediários e uso dos mesmosInfo
- Publication number
- BRPI0518424B8 BRPI0518424B8 BRPI0518424A BRPI0518424A BRPI0518424B8 BR PI0518424 B8 BRPI0518424 B8 BR PI0518424B8 BR PI0518424 A BRPI0518424 A BR PI0518424A BR PI0518424 A BRPI0518424 A BR PI0518424A BR PI0518424 B8 BRPI0518424 B8 BR PI0518424B8
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- independently represent
- piperazinyl
- alkyloxy
- 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
- C07D487/22—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
-
- 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
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (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
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 -c3-9 alquila-, -c3-9 alquenila-, -c1-5 alquil-nr6-c1-5 alquila-, -c1-5 alquil-nr7-co-c1-5 alquila-, -c1-6 alquil-co-nh-, -c1-6 alquil- nh-co-, -c1-2 alquil-co-het10-co-, -c1-3 alquil-nh-co-het3-, -het4-c1-3~ alquil-co-nh-c1-3 alquila-, -c1-2 alquil-nh-co-l¹-nh-, -nh-co-l²-nh-, -c1-2 alquil-co-nh-l³-co-, -c1-2 alquil-nh-co-l¹-nh-co-c1-3 alquila-, -c1-2 alquil- co-nh-l³-co-nh-c1-3 alquila-, -c1-2 alquil-nr¹¹-ch2-co-nh-c1-3 alquila-, het5-co-c1-2 alquila, -c1-5 aiquii-co-nh-c 1-3 alquil-co-nh-, -c 1-5 alquil- nr¹³-co-c1-3 alquil-nh-, -c13 alquil-nh-co-het27-co- ou -c1-3 alquil-co- het 28-co-nh-; x¹ representa uma ligação direta, o, -o-c1-2 alquila-, -co-c1-2 alquila-, -nr16-c1-2 alquila-, -co-nr17-, het23-c 1-2 alquila- ou c1-2 alquila; x² representa uma ligação direta, o, -o-c1-2 alquila-, -co-c1-2 alquila-, -nr18-c1-2 alquila-, -co-nr 19-, het24-c1-2 alquila- ou c1-2 alquila; r¹ e r5 representam, cada um independentemente, hidrogênio, halo, c1-6 alquilóxi- ou c1-6 alquilóxi- substituído por het¹ ou c1-4 alquilóxi-; r² e r4 representam, cada um independentemente, hidrogênio ou halo; r³ representa hidrogênio ou ciano; r6, r7, r13, r17 e r19 representam hidrogênio; r¹¹ representa hidrogênio ou c1-4 alquila; r16 e r18 representa hidrogênio, c1-4 alquila ou het17-c1-4 alquila-; l¹, l2 e l³ representam, cada um independentemente, c1-8 alquila opcionalmente substituída por um ou, onde possível, dois ou mais substituintes selecionados de fenita, metil-sulfeto, ciano, c1-4 polihaloalquil-fenila-, c1-4 alquilóxi, piridinila, mono- ou di(c1-4 alquil)-amino- ou c3-6 ciclo alquila; het¹, het², het17 representam, cada um independentemente, morfolinila, oxazolila, isoxazolila ou piperazinila; het³, het4, het5 representam, cada um independentemente, mor- folinila, piperazinila, piperidinila ou pirrolidinila; het10 representa piperazinila, piperidinila, pirrolidinila ou azetidinila; het²² representa morfolinila, oxazolila, isoxazolila ou piperazinila em que o referido het²² é opcionalmente substituido por c1-4 alquila; het²³ e het24 representam, cada um independentemente, um heterociclo selecionado de pirrolidinila, piperazinila ou piperidinila em que os referidos het²³ ou het24 são opcionalmente substituidos por het²²-carbonila; het 27 e het28 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 | |
| EP04106384.3 | 2004-12-08 | ||
| EP04106384 | 2004-12-08 | ||
| US60/634,291 | 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 BRPI0518424A2 (pt) | 2008-11-25 |
| BRPI0518424B1 BRPI0518424B1 (pt) | 2020-10-13 |
| BRPI0518424B8 true 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 (22)
| 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) |
| 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 (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA83881C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
| ES2442857T3 (es) * | 2004-08-10 | 2014-02-13 | Janssen Pharmaceutica Nv | Derivados de 1,2,4-triazin-6-ona inhibidores de VIH |
| 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 |
| NZ568325A (en) | 2005-11-16 | 2011-05-27 | S Bio Pte Ltd | Macrocyclic oxygen linked pyrimidine derivatives |
| CA2654583C (en) | 2006-07-13 | 2015-11-24 | 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 |
| ES2562218T3 (es) | 2007-07-27 | 2016-03-03 | Janssen Pharmaceutica, N.V. | Pirrolopirimidinas útiles para el tratamiento de enfermedades proliferativas |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| CN105367503A (zh) | 2007-10-19 | 2016-03-02 | 阿维拉制药公司 | 杂芳基化合物和其用途 |
| EP2283024B1 (en) | 2008-03-10 | 2013-05-15 | Janssen Pharmaceutica, N.V. | 4-aryl-2-anilino-pyrimidines as plk kinase inhibitors |
| WO2009132202A2 (en) * | 2008-04-24 | 2009-10-29 | 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 |
| US8815872B2 (en) * | 2008-09-08 | 2014-08-26 | Merck Patent Gmbh | Macrocyclics pyrimidines as aurora 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 |
| MX382354B (es) | 2010-11-01 | 2025-03-13 | Celgene Car Llc | Compuestos heterocíclicos y usos de los mismos. |
| US9133224B2 (en) * | 2010-11-29 | 2015-09-15 | OSI Pharmaceuticals, LLC | Macrocyclic kinase inhibitors |
| DK2688883T3 (en) | 2011-03-24 | 2016-09-05 | Noviga Res Ab | pyrimidine |
| PL2825042T3 (pl) | 2012-03-15 | 2019-02-28 | Celgene Car Llc | Sole inhibitora kinazy receptora czynnika wzrostu naskórka |
| KR102081042B1 (ko) | 2012-03-15 | 2020-02-26 | 셀젠 카르 엘엘씨 | 상피 성장 인자 수용체 키나제 억제제의 고체 형태 |
| CN105164136B (zh) * | 2013-05-06 | 2017-12-22 | 默克专利股份公司 | 作为激酶抑制剂的大环化合物 |
| 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 |
| EP3253764B1 (en) * | 2015-02-05 | 2021-06-09 | Merck Patent GmbH | Macrocyclic compounds as irak1/4 inhibitors and uses thereof |
| EP3601253B1 (en) | 2017-03-28 | 2021-09-15 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| WO2020249692A1 (en) * | 2019-06-12 | 2020-12-17 | Nouryon Chemicals International B.V. | Method for isolating carboxylic acid from an aqueous side stream |
| WO2020249689A1 (en) | 2019-06-12 | 2020-12-17 | Nouryon Chemicals International B.V. | Process for the production of peroxyesters |
| ES2963382T3 (es) | 2019-06-12 | 2024-03-26 | Nouryon Chemicals Int Bv | Proceso para la producción de peróxidos de diacilo |
| US11976035B2 (en) | 2019-06-12 | 2024-05-07 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| EP3983369B1 (en) | 2019-06-12 | 2023-08-02 | Nouryon Chemicals International B.V. | Process for the production of diacyl peroxides |
| KR20220153582A (ko) * | 2020-02-14 | 2022-11-18 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | 마크로시클릭 ulk1/2 억제제 |
| 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 |
| CA3250447A1 (en) * | 2021-12-15 | 2025-07-09 | Whan In Pharmaceutical Co., Ltd. | MACROCYCLIC PYRIMIDINE DERIVATIVE, ITS PREPARATION PROCESS, AND PHARMACEUTICAL COMPOSITION INTENDED FOR THE PREVENTION OR TREATMENT OF A NEURODEGENERATIVE DISEASE AND CONTAINING THIS DERIVATIVE AS AN ACTIVE INGREDIENT |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2274634T3 (es) * | 1998-08-29 | 2007-05-16 | Astrazeneca Ab | Compuestos de pirimidina. |
| 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 |
| UA83881C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
| ATE446750T1 (de) | 2003-12-18 | 2009-11-15 | Janssen Pharmaceutica Nv | 3-cyano-chinolin-derivate mit antiproliferativer wirkung |
-
2005
- 2005-12-06 MY MYPI20055703A patent/MY169441A/en unknown
- 2005-12-07 TW TW094143059A patent/TWI374140B/zh not_active IP Right Cessation
- 2005-12-07 AR ARP050105123A patent/AR051788A1/es unknown
- 2005-12-08 CN CN2005800420717A patent/CN101072779B/zh not_active Expired - Lifetime
- 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 not_active Expired - Lifetime
- 2005-12-08 JP JP2007544917A patent/JP5022909B2/ja not_active Expired - Lifetime
- 2005-12-08 US US11/720,681 patent/US8148388B2/en active Active
- 2005-12-08 EA EA200701245A patent/EA013368B1/ru not_active IP Right Cessation
- 2005-12-08 WO PCT/EP2005/056606 patent/WO2006061415A1/en not_active Ceased
- 2005-12-08 CA CA2588761A patent/CA2588761C/en not_active Expired - Lifetime
- 2005-12-08 AU AU2005313348A patent/AU2005313348B2/en not_active Expired
- 2005-12-08 UA UAA200705051A patent/UA90693C2/ru unknown
- 2005-12-08 EP EP05819148.7A patent/EP1824856B1/en not_active Expired - Lifetime
- 2005-12-08 NZ NZ554820A patent/NZ554820A/en not_active IP Right Cessation
- 2005-12-08 KR KR1020077011771A patent/KR101428506B1/ko not_active Expired - Lifetime
- 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
-
2011
- 2011-10-20 US US13/277,651 patent/US8394955B2/en not_active Expired - Lifetime
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