JP2011529468A5 - - Google Patents
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- Publication number
- JP2011529468A5 JP2011529468A5 JP2011520491A JP2011520491A JP2011529468A5 JP 2011529468 A5 JP2011529468 A5 JP 2011529468A5 JP 2011520491 A JP2011520491 A JP 2011520491A JP 2011520491 A JP2011520491 A JP 2011520491A JP 2011529468 A5 JP2011529468 A5 JP 2011529468A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- different
- noh
- cycloalkyl
- necessary
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000000824 cytostatic agent Substances 0.000 claims 1
- 230000001085 cytostatic effect Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 238000003419 tautomerization reaction Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08161369.7 | 2008-07-29 | ||
| EP08161369 | 2008-07-29 | ||
| PCT/EP2009/059763 WO2010012740A1 (en) | 2008-07-29 | 2009-07-28 | 5-alkynyl-pyrimidines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529468A JP2011529468A (ja) | 2011-12-08 |
| JP2011529468A5 true JP2011529468A5 (https=) | 2012-08-30 |
| JP5599791B2 JP5599791B2 (ja) | 2014-10-01 |
Family
ID=40202900
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520491A Active JP5599791B2 (ja) | 2008-07-29 | 2009-07-28 | ５−アルキニル−ピリミジン |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8916548B2 (https=) |
| EP (1) | EP2323992B1 (https=) |
| JP (1) | JP5599791B2 (https=) |
| KR (1) | KR20110041536A (https=) |
| CN (1) | CN102112450A (https=) |
| AR (1) | AR072845A1 (https=) |
| AU (1) | AU2009275957A1 (https=) |
| BR (1) | BRPI0916679A2 (https=) |
| CA (1) | CA2731909A1 (https=) |
| CL (1) | CL2011000195A1 (https=) |
| CO (1) | CO6341617A2 (https=) |
| DK (1) | DK2323992T3 (https=) |
| EA (1) | EA201100255A1 (https=) |
| EC (1) | ECSP11010786A (https=) |
| ES (1) | ES2597903T3 (https=) |
| HU (1) | HUE029837T2 (https=) |
| IL (1) | IL210343A0 (https=) |
| MA (1) | MA32505B1 (https=) |
| MX (1) | MX2011000729A (https=) |
| NZ (1) | NZ590558A (https=) |
| PE (1) | PE20110196A1 (https=) |
| PL (1) | PL2323992T3 (https=) |
| TW (1) | TW201010984A (https=) |
| UY (1) | UY32009A (https=) |
| WO (1) | WO2010012740A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010012740A1 (en) | 2008-07-29 | 2010-02-04 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| AR072538A1 (es) | 2008-07-29 | 2010-09-01 | Boehringer Ingelheim Int | Derivados de indolinonas, composiciones farmacéuticas y usos |
| AR076332A1 (es) * | 2009-04-21 | 2011-06-01 | Boehringer Ingelheim Int | Derivados heterociclicos de 5-alquinil-piridinas, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento y/o prevencion del cancer, procesos inflamatorios, autoinmunes, y/o infecciones. |
| US8618111B2 (en) * | 2010-01-26 | 2013-12-31 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US8633183B2 (en) * | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US8466162B2 (en) * | 2011-01-26 | 2013-06-18 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyridines |
| TW201245176A (en) * | 2011-01-26 | 2012-11-16 | Boehringer Ingelheim Int | New 5-alkynyl-pyridines |
| JP6016915B2 (ja) * | 2011-07-28 | 2016-10-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール |
| UA110995C2 (uk) * | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
| CA3161836A1 (en) * | 2013-12-11 | 2015-06-18 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| KR102400920B1 (ko) * | 2014-05-01 | 2022-05-20 | 셀젠 콴티셀 리서치, 인크. | 리신 특이적 데메틸라제-1의 억제제 |
| AU2015311805B2 (en) * | 2014-09-05 | 2020-04-02 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| CN104744376A (zh) * | 2015-03-14 | 2015-07-01 | 长沙深橙生物科技有限公司 | 一种2-异丙基嘧啶衍生物的制备方法 |
| CN104803921A (zh) * | 2015-03-14 | 2015-07-29 | 长沙深橙生物科技有限公司 | 一种苯取代嘧啶衍生物的制备方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3832570A1 (de) * | 1988-09-24 | 1990-03-29 | Hoechst Ag | 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte |
| EP0674627A1 (en) | 1992-12-18 | 1995-10-04 | The Wellcome Foundation Limited | Pyrimidine, pyridine, pteridinone and indazole derivatives as enzyme inhibitors |
| US5622954A (en) | 1994-05-11 | 1997-04-22 | Fmc Corporation | 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides |
| WO2001062233A2 (en) * | 2000-02-25 | 2001-08-30 | F. Hoffmann La Roche Ag | Adenosine receptor modulators |
| JP5154728B2 (ja) * | 2000-07-24 | 2013-02-27 | クレニツキー・ファーマシューティカルズ，インコーポレイテッド | 神経栄養活性を有する置換５−アルキニルピリミジン |
| CA2528938A1 (en) * | 2003-06-13 | 2005-02-24 | Zentaris Gmbh | Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof |
| ATE402705T1 (de) | 2003-12-24 | 2008-08-15 | Astrazeneca Ab | Pyrimidine mit tie2 (tek) aktivität |
| WO2005113556A1 (en) * | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| US7776869B2 (en) * | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| US20080146599A1 (en) | 2005-02-01 | 2008-06-19 | Astrazeneca Ab | Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity |
| EP1863805A1 (en) | 2005-02-01 | 2007-12-12 | AstraZeneca AB | Pyrimidine compounds having tie2 (tek) inhibitory activity |
| US20070135437A1 (en) | 2005-03-04 | 2007-06-14 | Alsgen, Inc. | Modulation of neurodegenerative diseases |
| WO2006106721A1 (ja) | 2005-03-30 | 2006-10-12 | Shionogi & Co., Ltd. | チロシンキナーゼ阻害作用を有するピリミジン誘導体 |
| JP2008534565A (ja) | 2005-03-31 | 2008-08-28 | アストラゼネカ アクチボラグ | Ｔｉｅ２阻害活性のあるアミノピリミジン誘導体 |
| US7989622B2 (en) * | 2005-10-07 | 2011-08-02 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors and methods of their use |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EP2057129A1 (en) | 2006-08-24 | 2009-05-13 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| AU2007341228B2 (en) | 2006-12-29 | 2013-04-18 | Janssen Sciences Ireland Uc | HIV inhibiting 5,6-substituted pyrimidines |
| EP2022785A1 (en) | 2007-06-20 | 2009-02-11 | Bayer Schering Pharma Aktiengesellschaft | Alkynylpyrimidines as Tie2 kinase inhibitors |
| WO2010012740A1 (en) | 2008-07-29 | 2010-02-04 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US8633183B2 (en) | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
-
2009
- 2009-07-28 WO PCT/EP2009/059763 patent/WO2010012740A1/en not_active Ceased
- 2009-07-28 EP EP09781207.7A patent/EP2323992B1/en active Active
- 2009-07-28 TW TW098125388A patent/TW201010984A/zh unknown
- 2009-07-28 ES ES09781207.7T patent/ES2597903T3/es active Active
- 2009-07-28 AU AU2009275957A patent/AU2009275957A1/en not_active Abandoned
- 2009-07-28 CA CA2731909A patent/CA2731909A1/en not_active Abandoned
- 2009-07-28 NZ NZ590558A patent/NZ590558A/xx not_active IP Right Cessation
- 2009-07-28 PE PE2011000088A patent/PE20110196A1/es not_active Application Discontinuation
- 2009-07-28 EA EA201100255A patent/EA201100255A1/ru unknown
- 2009-07-28 US US13/055,949 patent/US8916548B2/en active Active
- 2009-07-28 CN CN2009801301499A patent/CN102112450A/zh active Pending
- 2009-07-28 HU HUE09781207A patent/HUE029837T2/en unknown
- 2009-07-28 AR ARP090102873A patent/AR072845A1/es unknown
- 2009-07-28 UY UY0001032009A patent/UY32009A/es not_active Application Discontinuation
- 2009-07-28 KR KR1020117003951A patent/KR20110041536A/ko not_active Withdrawn
- 2009-07-28 MX MX2011000729A patent/MX2011000729A/es unknown
- 2009-07-28 BR BRPI0916679A patent/BRPI0916679A2/pt not_active IP Right Cessation
- 2009-07-28 PL PL09781207T patent/PL2323992T3/pl unknown
- 2009-07-28 DK DK09781207.7T patent/DK2323992T3/en active
- 2009-07-28 JP JP2011520491A patent/JP5599791B2/ja active Active
-
2010
- 2010-12-29 IL IL210343A patent/IL210343A0/en unknown
-
2011
- 2011-01-26 MA MA33560A patent/MA32505B1/fr unknown
- 2011-01-27 CO CO11009242A patent/CO6341617A2/es not_active Application Discontinuation
- 2011-01-27 EC EC2011010786A patent/ECSP11010786A/es unknown
- 2011-01-28 CL CL2011000195A patent/CL2011000195A1/es unknown
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