UA91522C2 - Macrocyclic quinazole derivatives and their use as mtki - Google Patents
Macrocyclic quinazole derivatives and their use as mtkiInfo
- Publication number
- UA91522C2 UA91522C2 UAA200705396A UAA200705396A UA91522C2 UA 91522 C2 UA91522 C2 UA 91522C2 UA A200705396 A UAA200705396 A UA A200705396A UA A200705396 A UAA200705396 A UA A200705396A UA 91522 C2 UA91522 C2 UA 91522C2
- Authority
- UA
- Ukraine
- Prior art keywords
- calkyl
- rrepresents
- hydrogen
- rand
- calkyloxy
- Prior art date
Links
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 abstract 1
- -1 2-bora-1,3-dioxolanyl Chemical group 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
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
- C07D498/04—Ortho-condensed 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
- C07D498/06—Peri-condensed 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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- 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
- C07D487/04—Ortho-condensed 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
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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106383 | 2004-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA91522C2 true UA91522C2 (en) | 2010-08-10 |
Family
ID=34930015
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA200705396A UA91522C2 (en) | 2004-12-08 | 2005-12-08 | Macrocyclic quinazole derivatives and their use as mtki |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20100152174A1 (ru) |
| EP (1) | EP1828201B1 (ru) |
| JP (1) | JP5140431B2 (ru) |
| KR (1) | KR101320431B1 (ru) |
| CN (2) | CN101072781B (ru) |
| AR (1) | AR051985A1 (ru) |
| AU (1) | AU2005313350B2 (ru) |
| BR (1) | BRPI0518394B8 (ru) |
| CA (1) | CA2588764C (ru) |
| DK (1) | DK1828201T3 (ru) |
| EA (1) | EA013995B1 (ru) |
| ES (1) | ES2559305T3 (ru) |
| HU (1) | HUE027253T2 (ru) |
| JO (1) | JO3088B1 (ru) |
| MX (1) | MX2007006820A (ru) |
| MY (1) | MY148503A (ru) |
| NZ (1) | NZ555496A (ru) |
| PA (1) | PA8654501A1 (ru) |
| SI (1) | SI1828201T1 (ru) |
| TW (2) | TWI511970B (ru) |
| UA (1) | UA91522C2 (ru) |
| WO (1) | WO2006061417A2 (ru) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| WO2005058913A1 (en) | 2003-12-18 | 2005-06-30 | Janssen Pharmaceutica N.V. | Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| ES2569428T3 (es) * | 2006-07-13 | 2016-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina como MTKI |
| CA2664165A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of mtki 1 for treating or preventing bone cancer |
| EA200970419A1 (ru) * | 2006-10-27 | 2009-10-30 | Янссен Фармацевтика Нв | Микроциклические хиназолиновые производные в качестве ингибиторов vegfr3 |
| ES2435454T3 (es) * | 2007-06-21 | 2013-12-19 | Janssen Pharmaceutica, N.V. | Indolin-2-onas y aza-indolin-2-onas |
| EP2185562B1 (en) * | 2007-07-27 | 2015-12-02 | Janssen Pharmaceutica, N.V. | Pyrrolopyrimidines useful for the treatment of proliferative diseases |
| US8450322B2 (en) | 2008-09-22 | 2013-05-28 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors |
| KR102037619B1 (ko) | 2008-10-22 | 2019-10-28 | 어레이 바이오파마 인크. | ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５ａ］ 피리미딘 화합물 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ES2628418T3 (es) * | 2010-05-20 | 2017-08-02 | Array Biopharma, Inc. | Compuestos macrocíclicos como inhibidores de la TRK cinasa |
| EP3102200B1 (en) * | 2014-02-07 | 2023-04-05 | Exithera Pharmaceuticals Inc. | Therapeutic compounds and compositions |
| 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 |
| CA2967951C (en) | 2014-11-16 | 2023-11-07 | Array Biopharma, Inc. | Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| CN108697708A (zh) | 2015-10-26 | 2018-10-23 | 洛克索肿瘤学股份有限公司 | Trk抑制剂抗性癌症中的点突变以及与此相关的方法 |
| SI3439662T1 (sl) | 2016-04-04 | 2024-11-29 | Loxo Oncology, Inc. | Tekoče formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin -1-il)-pirazološ1,5-aćpirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| DK3458456T3 (da) | 2016-05-18 | 2020-12-14 | Array Biopharma Inc | Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2423536A1 (de) * | 1974-05-15 | 1975-11-27 | Bayer Ag | 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide |
| US4110333A (en) * | 1976-05-17 | 1978-08-29 | Janssen Pharmaceutica N.V. | 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds |
| US4442278A (en) * | 1981-12-03 | 1984-04-10 | Hughes Aircraft Company | Ethynyl-substituted s-triazine derivatives, polymers thereof and process for making the same |
| US5721237A (en) * | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| PT657458E (pt) * | 1993-12-07 | 2002-02-28 | Lilly Co Eli | Inibidores de proteina cinase c |
| US5654307A (en) * | 1994-01-25 | 1997-08-05 | Warner-Lambert Company | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| IL112249A (en) * | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| WO1996013529A1 (en) * | 1994-10-31 | 1996-05-09 | Dsm N.V. | Catalyst composition and process for the polymerization of an olefin |
| GB9508538D0 (en) * | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| EA199800372A1 (ru) * | 1995-11-14 | 1998-10-29 | Дзе Дюпон Мерк Фармасьютикал Компани | Новые макроциклические соединения-ингибиторы |
| DE19608588A1 (de) * | 1996-03-06 | 1997-09-11 | Thomae Gmbh Dr K | Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| NZ332119A (en) * | 1996-04-12 | 2001-08-31 | Warner Lambert Co | Quinazoline compounds which are irreversible inhibitors of tyrosine kinases |
| GB9718972D0 (en) * | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| US6002008A (en) * | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6288082B1 (en) * | 1998-09-29 | 2001-09-11 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| DE50012136D1 (en) * | 1999-08-27 | 2006-04-13 | Boehringer Ingelheim Pharma | Substituierte indolinone als tyrosinkinase inhibitoren |
| ATE396978T1 (de) * | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| US6864255B2 (en) * | 2001-04-11 | 2005-03-08 | Amgen Inc. | Substituted triazinyl amide derivatives and methods of use |
| BR0210391A (pt) * | 2001-06-12 | 2004-06-15 | Elan Pharm Inc | Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto |
| JP4326328B2 (ja) * | 2001-07-16 | 2009-09-02 | アストラゼネカ アクチボラグ | キノリン誘導体及びそれらのチロシンキナーゼ阻害薬としての使用 |
| US6924285B2 (en) * | 2002-03-30 | 2005-08-02 | Boehringer Ingelheim Pharma Gmbh & Co. | Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them |
| EP1528925B1 (en) * | 2002-07-09 | 2009-04-22 | Astrazeneca AB | Quinazoline derivatives for use in the treatment of cancer |
| DE10239042A1 (de) * | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| US20050021480A1 (en) * | 2003-05-16 | 2005-01-27 | Hyperspace Communications, Inc. | Method and apparatus for creating and validating an encrypted digital receipt for third-party electronic commerce transactions |
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| CN1893944B (zh) * | 2003-12-18 | 2011-07-06 | 詹森药业有限公司 | 具有抗增殖活性的3-氰基喹啉衍生物 |
| WO2005058913A1 (en) * | 2003-12-18 | 2005-06-30 | Janssen Pharmaceutica N.V. | Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents |
| MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| ATE439349T1 (de) * | 2005-06-30 | 2009-08-15 | Janssen Pharmaceutica Nv | Cyclische anilinopyridinotriazine als gsk-3- inhibitoren |
| WO2007058628A1 (en) * | 2005-11-16 | 2007-05-24 | S*Bio Pte Ltd | Heteroalkyl linked pyrimidine derivatives |
| ES2569428T3 (es) * | 2006-07-13 | 2016-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina como MTKI |
| ES2435454T3 (es) * | 2007-06-21 | 2013-12-19 | Janssen Pharmaceutica, N.V. | Indolin-2-onas y aza-indolin-2-onas |
| EP2185562B1 (en) * | 2007-07-27 | 2015-12-02 | Janssen Pharmaceutica, N.V. | Pyrrolopyrimidines useful for the treatment of proliferative diseases |
| JP5480824B2 (ja) * | 2008-03-10 | 2014-04-23 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｐｌｋキナーゼ阻害剤としての４−アリール−２−アニリノ−ピリミジン |
-
2005
- 2005-11-28 JO JOP/2005/0188A patent/JO3088B1/ar active
- 2005-12-05 PA PA20058654501A patent/PA8654501A1/es unknown
- 2005-12-06 MY MYPI20055704A patent/MY148503A/en unknown
- 2005-12-07 AR ARP050105124A patent/AR051985A1/es not_active Application Discontinuation
- 2005-12-07 TW TW102141302A patent/TWI511970B/zh active
- 2005-12-07 TW TW094143060A patent/TWI432440B/zh active
- 2005-12-08 MX MX2007006820A patent/MX2007006820A/es active IP Right Grant
- 2005-12-08 BR BRPI0518394A patent/BRPI0518394B8/pt active IP Right Grant
- 2005-12-08 CA CA2588764A patent/CA2588764C/en not_active Expired - Lifetime
- 2005-12-08 SI SI200532035T patent/SI1828201T1/sl unknown
- 2005-12-08 EA EA200701233A patent/EA013995B1/ru not_active IP Right Cessation
- 2005-12-08 US US11/720,693 patent/US20100152174A1/en not_active Abandoned
- 2005-12-08 ES ES05826362.5T patent/ES2559305T3/es not_active Expired - Lifetime
- 2005-12-08 CN CN2005800420435A patent/CN101072781B/zh not_active Expired - Lifetime
- 2005-12-08 DK DK05826362.5T patent/DK1828201T3/en active
- 2005-12-08 KR KR1020077013133A patent/KR101320431B1/ko not_active Expired - Lifetime
- 2005-12-08 UA UAA200705396A patent/UA91522C2/ru unknown
- 2005-12-08 EP EP05826362.5A patent/EP1828201B1/en not_active Expired - Lifetime
- 2005-12-08 CN CN201110392750.4A patent/CN102532163B/zh not_active Expired - Lifetime
- 2005-12-08 HU HUE05826362A patent/HUE027253T2/en unknown
- 2005-12-08 WO PCT/EP2005/056609 patent/WO2006061417A2/en not_active Ceased
- 2005-12-08 AU AU2005313350A patent/AU2005313350B2/en not_active Expired
- 2005-12-08 NZ NZ555496A patent/NZ555496A/en not_active IP Right Cessation
- 2005-12-08 JP JP2007544918A patent/JP5140431B2/ja not_active Expired - Lifetime
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