JO3088B1 - مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف - Google Patents
مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهدافInfo
- Publication number
- JO3088B1 JO3088B1 JOP/2005/0188A JOP20050188A JO3088B1 JO 3088 B1 JO3088 B1 JO 3088B1 JO P20050188 A JOP20050188 A JO P20050188A JO 3088 B1 JO3088 B1 JO 3088B1
- Authority
- JO
- Jordan
- Prior art keywords
- alkyl
- alkyloxy
- hydrogen
- 5alkyl
- 2alkyl
- Prior art date
Links
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- -1 C3-6 cycloalkyl R 25 Chemical compound 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Chemical group 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
- 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
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
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- 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)
Abstract
يتعلق الاختراع الحالي بمركبات ( compounds) من الصيغه باشكال N- اوكسيد( N-oxide forms) باملاح الاضافة( addition salts) المقبولة دوائيا وبالاشكال الايزومرية الكيميائية الفراغية ( stereochemically isomeric forms) منها حيث: Z يمثل NH Y يمثل C3-9 الكيل( C3-9alkyl) ، c1-5 الكيل C1-5NR13 الكيل، ( C1-5alkyl – NR13-C1-5alkyl) C1-5 الكيل C1-5-CO-NR14 الكيل- ( C1-5alkyl –NR14-CO-C1-5alkyl) C1-2 الكيل C1-3 NH-CO-CH2-NR21 الكيل – (C1-2ALKYL-NR21-CH2-CO-NH-C1-3alkyl) او C1-2 الكيل NH-CR16R17-CO-NR23 ) (C1-2alkyl-NR23-CO-CR16R17-NH X1 يمثل O او C1-2 O الكيل( O-C1-2alkyl-) X2 يمثل رابطة مباشرة ( direct bond) C1-2 الكيل ( C1-2alkyl)، c1-2 co الكيل ( -CO-C1-2alkyl) او C1-2NR12 الكيل ( NR12C1-2alkyl) R1 يمثل هيدروجين ( hydrogen ) او هالو ( halo) R2 يمثل هالو ( halo) استيلين ( acetylene) او Het1 R3 يمثل هيدروجين ( hydrogen) او سيانو ( cyano) R4 يمثل C1-4-Ar4 الكيل اوكسي ( Ar4-C1-4alkoxy) C1-4 الكيل اوكسي (C1-4alkoxy) او C1-4 الكيل اوكسي (C1-4alkoxy) مستبدل مع بديل واحد او اذا امكن مع اثنين او اكثر من بدائل مختراة من Het2 ، NR7R8 هيدروكسي ( hydroxy) و C1-4 الكيل اوكسي C1-4 الكيل اوكسي ( C1-4alkyloxy – C1-4alkyoxy) R7 يمثل هيدروجين ( hydrogen) او c1-4 الكيل( C1-4 alkyl) R8 يمثل c1-4 الكيل( c1-4alkyl) مستبدل مع NR25R26 او C1-4 الكيل سلفونيل ( C1-4 alkylsulfonyl ) R12 يمثل هيدرويجين ( hydrogen) او C1-4 الكيل –( C1-4 alkyl) R13 يمثل AR6 سلفونيل ( AR6-sulfonyl) او C1-6 الكيل اوكسي كربونيل ( C1-6 alkyloxycarbonyl) مستبدل اختياريا مع فنيل ( phenyl) R16 و R17 يمثلان هيدروجين ( hydrogen) C1-4 الكيل( C1-4 alkyl) او يؤخذ R16 و R17 معا مع ذرة الكربون ( carbon atom) المرتبطة معها لتشكيل C3-6 الكيل دائري( C3-6 cycloakyl) R23 يمثل c1-4 الكيل ( C1-4alkyl) و R23 يمثل هيدروجين ( hydrogen) عنما يؤخذ r16 و r17 معا مع ذرة الكربون ( carbon atom) المرتبطة معهما لتشكيل c3-6 الكيل دائري ( C3-6cycloalkyl) R27,R26,R25 و R28 كل منهم على حدة يمثل هيدروجين ( hydrogen) او C1-4 الكيل كربونيل( C1-4alkylcarbonyl) Het1 يمثل 2- بورا-1، 3 ثنائي اوكسولانيل( 2-boro 1.3-dioxolanyl) Het2 يمثل بيبريدينيل ( piperidiny
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106383 | 2004-12-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3088B1 true JO3088B1 (ar) | 2017-03-15 |
Family
ID=34930015
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2005/0188A JO3088B1 (ar) | 2004-12-08 | 2005-11-28 | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20100152174A1 (ar) |
| EP (1) | EP1828201B1 (ar) |
| JP (1) | JP5140431B2 (ar) |
| KR (1) | KR101320431B1 (ar) |
| CN (2) | CN102532163B (ar) |
| AR (1) | AR051985A1 (ar) |
| AU (1) | AU2005313350B2 (ar) |
| BR (1) | BRPI0518394B8 (ar) |
| CA (1) | CA2588764C (ar) |
| DK (1) | DK1828201T3 (ar) |
| EA (1) | EA013995B1 (ar) |
| ES (1) | ES2559305T3 (ar) |
| HU (1) | HUE027253T2 (ar) |
| JO (1) | JO3088B1 (ar) |
| MX (1) | MX2007006820A (ar) |
| MY (1) | MY148503A (ar) |
| NZ (1) | NZ555496A (ar) |
| PA (1) | PA8654501A1 (ar) |
| SI (1) | SI1828201T1 (ar) |
| TW (2) | TWI511970B (ar) |
| UA (1) | UA91522C2 (ar) |
| WO (1) | WO2006061417A2 (ar) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (ar) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | مشتقات الكوينازولين |
| MXPA06007017A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidina como agentes antiproliferativos. |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| JP2009542778A (ja) * | 2006-07-13 | 2009-12-03 | 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 | Ｍｔｋｉキナゾリン誘導体 |
| CA2664148A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Vegfr3 inhibitors |
| JP2010507628A (ja) * | 2006-10-27 | 2010-03-11 | 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 | 骨ガンの処置又は予防のためのｍｔｋｉ１の使用 |
| CA2687909C (en) * | 2007-06-21 | 2015-09-15 | Janssen Pharmaceutica Nv | Indolin-2-ones and aza-indolin-2-ones |
| AU2008281849B2 (en) * | 2007-07-27 | 2013-11-28 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| MY169791A (en) | 2008-10-22 | 2019-05-15 | Array Biopharma Inc | Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| RU2733405C2 (ru) * | 2014-02-07 | 2020-10-01 | Экзитера Фармасьютикалз Инк. | Терапевтические соединения и композиции |
| 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 |
| CN113354649B (zh) | 2014-11-16 | 2024-12-10 | 阵列生物制药公司 | 一种新的晶型 |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| 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 |
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| 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 |
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| MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| US8778919B2 (en) * | 2005-06-30 | 2014-07-15 | Janssen Pharmaceutica Nv | Cyclic anilino—pyridinotriazines |
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| JP2009542778A (ja) * | 2006-07-13 | 2009-12-03 | 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 | Ｍｔｋｉキナゾリン誘導体 |
| CA2687909C (en) * | 2007-06-21 | 2015-09-15 | Janssen Pharmaceutica Nv | Indolin-2-ones and aza-indolin-2-ones |
| AU2008281849B2 (en) * | 2007-07-27 | 2013-11-28 | Janssen Pharmaceutica Nv | Pyrrolopyrimidines |
| US8318929B2 (en) * | 2008-03-10 | 2012-11-27 | Janssen Pharmaceutica Nv | 4-aryl-2-anilino-pyrimidines |
-
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 TW TW102141302A patent/TWI511970B/zh not_active IP Right Cessation
- 2005-12-07 TW TW094143060A patent/TWI432440B/zh not_active IP Right Cessation
- 2005-12-07 AR ARP050105124A patent/AR051985A1/es not_active Application Discontinuation
- 2005-12-08 NZ NZ555496A patent/NZ555496A/en not_active IP Right Cessation
- 2005-12-08 MX MX2007006820A patent/MX2007006820A/es active IP Right Grant
- 2005-12-08 JP JP2007544918A patent/JP5140431B2/ja not_active Expired - Lifetime
- 2005-12-08 KR KR1020077013133A patent/KR101320431B1/ko not_active Expired - Lifetime
- 2005-12-08 ES ES05826362.5T patent/ES2559305T3/es not_active Expired - Lifetime
- 2005-12-08 SI SI200532035T patent/SI1828201T1/sl unknown
- 2005-12-08 UA UAA200705396A patent/UA91522C2/ru unknown
- 2005-12-08 DK DK05826362.5T patent/DK1828201T3/en active
- 2005-12-08 CA CA2588764A patent/CA2588764C/en not_active Expired - Lifetime
- 2005-12-08 AU AU2005313350A patent/AU2005313350B2/en not_active Expired
- 2005-12-08 BR BRPI0518394A patent/BRPI0518394B8/pt active IP Right Grant
- 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 EP EP05826362.5A patent/EP1828201B1/en not_active Expired - Lifetime
- 2005-12-08 CN CN2005800420435A patent/CN101072781B/zh not_active Expired - Lifetime
- 2005-12-08 WO PCT/EP2005/056609 patent/WO2006061417A2/en not_active Ceased
- 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
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