JP2008540687A5 - - Google Patents
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- JP2008540687A5 JP2008540687A5 JP2008512617A JP2008512617A JP2008540687A5 JP 2008540687 A5 JP2008540687 A5 JP 2008540687A5 JP 2008512617 A JP2008512617 A JP 2008512617A JP 2008512617 A JP2008512617 A JP 2008512617A JP 2008540687 A5 JP2008540687 A5 JP 2008540687A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- aryl
- heteroaryl
- cycloalkyl
- 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.)
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 403
- 125000000217 alkyl group Chemical group 0.000 claims 244
- 125000003118 aryl group Chemical group 0.000 claims 195
- 125000000753 cycloalkyl group Chemical group 0.000 claims 193
- 125000001072 heteroaryl group Chemical group 0.000 claims 193
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 163
- 125000005343 heterocyclic alkyl group Chemical group 0.000 claims 161
- 125000003710 aryl alkyl group Chemical group 0.000 claims 124
- 229910052739 hydrogen Inorganic materials 0.000 claims 116
- 239000001257 hydrogen Substances 0.000 claims 116
- 150000002431 hydrogen Chemical class 0.000 claims 106
- 125000001188 haloalkyl group Chemical group 0.000 claims 92
- 150000001875 compounds Chemical class 0.000 claims 88
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 88
- 125000000304 alkynyl group Chemical group 0.000 claims 85
- 229910052717 sulfur Inorganic materials 0.000 claims 72
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 70
- 229910052799 carbon Inorganic materials 0.000 claims 56
- 125000005843 halogen group Chemical group 0.000 claims 55
- 125000003342 alkenyl group Chemical group 0.000 claims 49
- 125000000623 heterocyclic group Chemical group 0.000 claims 49
- 229910052760 oxygen Inorganic materials 0.000 claims 42
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 36
- 150000001602 bicycloalkyls Chemical group 0.000 claims 32
- 125000005842 heteroatom Chemical group 0.000 claims 30
- 150000001721 carbon Chemical group 0.000 claims 26
- 125000004103 aminoalkyl group Chemical group 0.000 claims 24
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 125000003545 alkoxy group Chemical group 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 18
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 230000001404 mediated effect Effects 0.000 claims 10
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 8
- 150000001204 N-oxides Chemical class 0.000 claims 7
- YUCFVHQCAFKDQG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH] YUCFVHQCAFKDQG-UHFFFAOYSA-N 0.000 claims 7
- 238000009472 formulation Methods 0.000 claims 7
- 239000000651 prodrug Substances 0.000 claims 7
- 229940002612 prodrug Drugs 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 102000005741 Metalloproteases Human genes 0.000 claims 4
- 108010006035 Metalloproteases Proteins 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 102100027995 Collagenase 3 Human genes 0.000 claims 2
- 108050005238 Collagenase 3 Proteins 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- VKUYLANQOAKALN-UHFFFAOYSA-N 2-[benzyl-(4-methoxyphenyl)sulfonylamino]-n-hydroxy-4-methylpentanamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)N(C(CC(C)C)C(=O)NO)CC1=CC=CC=C1 VKUYLANQOAKALN-UHFFFAOYSA-N 0.000 claims 1
- 102100027400 A disintegrin and metalloproteinase with thrombospondin motifs 4 Human genes 0.000 claims 1
- 108091005664 ADAMTS4 Proteins 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 102100027998 Macrophage metalloelastase Human genes 0.000 claims 1
- 101710187853 Macrophage metalloelastase Proteins 0.000 claims 1
- 102100030411 Neutrophil collagenase Human genes 0.000 claims 1
- 101710118230 Neutrophil collagenase Proteins 0.000 claims 1
- 102100030416 Stromelysin-1 Human genes 0.000 claims 1
- 101710108790 Stromelysin-1 Proteins 0.000 claims 1
- 239000003435 antirheumatic agent Substances 0.000 claims 1
- 230000008512 biological response Effects 0.000 claims 1
- 229940111134 coxibs Drugs 0.000 claims 1
- 239000003260 cyclooxygenase 1 inhibitor Substances 0.000 claims 1
- 230000016396 cytokine production Effects 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003384 small molecules Chemical class 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 claims 1
- 0 C*N(*)C(C1=O)=C(*)C1=O Chemical compound C*N(*)C(C1=O)=C(*)C1=O 0.000 description 8
- HZXKDXQJOUWZBL-WHERFPGRSA-N CCC(C1C2=CCC2[C@H](C)C1)I Chemical compound CCC(C1C2=CCC2[C@H](C)C1)I HZXKDXQJOUWZBL-WHERFPGRSA-N 0.000 description 1
- NQVGOJWKNOFTHT-UHFFFAOYSA-N OC(C1(C2C34)C5C23C2C4(CNC(c3cc(C(NCc(cc4)cc(OC(F)F)c4F)=O)nc4ccn[n]34)=O)C5C12)=O Chemical compound OC(C1(C2C34)C5C23C2C4(CNC(c3cc(C(NCc(cc4)cc(OC(F)F)c4F)=O)nc4ccn[n]34)=O)C5C12)=O NQVGOJWKNOFTHT-UHFFFAOYSA-N 0.000 description 1
- NHFDHHSIROMKHM-UHFFFAOYSA-N OC(c1ccc(CNc2n[nH]c3c2ncnc3C(NCc(cc2)cc(Cl)c2F)=O)cc1)=O Chemical compound OC(c1ccc(CNc2n[nH]c3c2ncnc3C(NCc(cc2)cc(Cl)c2F)=O)cc1)=O NHFDHHSIROMKHM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68347005P | 2005-05-20 | 2005-05-20 | |
| US60/683,470 | 2005-05-20 | ||
| US70646505P | 2005-08-08 | 2005-08-08 | |
| US60/706,465 | 2005-08-08 | ||
| US73499105P | 2005-11-09 | 2005-11-09 | |
| US60/734,991 | 2005-11-09 | ||
| PCT/US2006/020970 WO2006128184A2 (en) | 2005-05-20 | 2006-05-22 | Pyrimidine or triazine fused bicyclic metalloprotease inhibitors |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013089076A Division JP5391351B2 (ja) | 2005-05-20 | 2013-04-22 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
| JP2013254709A Division JP2014088396A (ja) | 2005-05-20 | 2013-12-10 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008540687A JP2008540687A (ja) | 2008-11-20 |
| JP2008540687A5 true JP2008540687A5 (https=) | 2009-07-30 |
| JP5463034B2 JP5463034B2 (ja) | 2014-04-09 |
Family
ID=37239216
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008512617A Expired - Fee Related JP5463034B2 (ja) | 2005-05-20 | 2006-05-22 | ピリミジン若しくはトリアジン縮合二環式メタロプロテアーゼ阻害薬 |
| JP2013089076A Expired - Fee Related JP5391351B2 (ja) | 2005-05-20 | 2013-04-22 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
| JP2013254709A Withdrawn JP2014088396A (ja) | 2005-05-20 | 2013-12-10 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013089076A Expired - Fee Related JP5391351B2 (ja) | 2005-05-20 | 2013-04-22 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
| JP2013254709A Withdrawn JP2014088396A (ja) | 2005-05-20 | 2013-12-10 | ヘテロ二環式メタロプロテアーゼ阻害薬 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US20060293345A1 (https=) |
| EP (1) | EP1910367A2 (https=) |
| JP (3) | JP5463034B2 (https=) |
| KR (1) | KR20080087070A (https=) |
| CN (1) | CN101238127A (https=) |
| AU (1) | AU2006251989B2 (https=) |
| BR (1) | BRPI0609802A2 (https=) |
| CA (1) | CA2608890C (https=) |
| CR (1) | CR9614A (https=) |
| EA (1) | EA013525B1 (https=) |
| IL (1) | IL187495A0 (https=) |
| NO (1) | NO20076554L (https=) |
| WO (1) | WO2006128184A2 (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070155737A1 (en) * | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| US20090238763A1 (en) | 2006-07-09 | 2009-09-24 | Chongxi Yu | High penetration compositions and uses thereof |
| US20090221703A1 (en) | 2006-07-09 | 2009-09-03 | Chongxi Yu | High penetration composition and uses thereof |
| AU2007321923A1 (en) * | 2006-11-20 | 2008-05-29 | Alantos Pharmaceuticals Holding, Inc. | Heterobicyclic matrix metalloprotease inhibitors |
| WO2008063671A2 (en) * | 2006-11-20 | 2008-05-29 | Alantos Pharmaceuticals Holding, Inc. | Heterobicyclic metalloprotease inhibitors |
| AU2008223348A1 (en) * | 2007-03-07 | 2008-09-12 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors containing a heterocyclic moiety |
| WO2008149181A1 (en) | 2007-06-04 | 2008-12-11 | Techfields Inc | Pro-drugs of nsaias with very high skin and membranes penetration rates and their new medicinal uses |
| WO2009075790A1 (en) * | 2007-12-07 | 2009-06-18 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors for intra-articular application |
| RU2529484C2 (ru) | 2008-05-05 | 2014-09-27 | Санофи-Авентис | Ациламино-замещенные производные конденсированных циклопентанкарбоновых кислот и их применение в качестве фармацевтических средств |
| WO2010065936A1 (en) | 2008-12-04 | 2010-06-10 | Chongxi Yu | High penetration compositions and their applications |
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| CN101709034B (zh) * | 2009-12-14 | 2017-05-31 | 大连九信精细化工有限公司 | 双环[2.2.2]辛烷‑1，4‑二羧酸单甲酯的合成方法 |
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| WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| KR101935868B1 (ko) | 2011-12-30 | 2019-04-03 | 에스케이이노베이션 주식회사 | 폴리프로필렌 카보네이트 발포체 조성물 제조방법 및 이로부터 제조된 성형품 |
| CN116898848A (zh) | 2012-01-18 | 2023-10-20 | 苏州泰飞尔医药有限公司 | 治疗肺部疾病的高穿透力前药组合物和医药组合物 |
| SI2941432T1 (en) | 2012-12-07 | 2018-07-31 | Vertex Pharmaceuticals Incorporated | 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR |
| CA3177929A1 (en) | 2012-12-21 | 2014-06-26 | Astellas Institute For Regenerative Medicine | Methods for production of platelets from pluripotent stem cells and compositions thereof |
| WO2014143242A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| EP2970289A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| DK3077397T3 (da) | 2013-12-06 | 2019-12-16 | Vertex Pharma | 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf |
| PL3152212T3 (pl) | 2014-06-05 | 2020-06-15 | Vertex Pharmaceuticals Inc. | Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych |
| LT3157566T (lt) | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
| CN104326914A (zh) * | 2014-11-18 | 2015-02-04 | 江苏恒祥化工有限责任公司 | 一种反式-4-甲酸甲酯环己烷甲酸的制备方法 |
| CN104560997B (zh) * | 2014-12-25 | 2018-05-04 | 中国科学院广州生物医药与健康研究院 | 抑制ADAMTS-5和ADAM17基因的siRNA组合物及其应用 |
| EP3237619B8 (en) | 2014-12-25 | 2021-03-10 | Guangzhou Ribobio Co., Ltd. | Compositions and methods for inhibiting expression of adamts-5 and adam17 |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| CN109843846B (zh) | 2016-10-19 | 2022-07-05 | 伊士曼化工公司 | 双环[2.2.2]辛烷的合成 |
| US11518726B2 (en) | 2017-10-11 | 2022-12-06 | Eastman Chemical Company | Synthesis of bicyclo[2.2.2]octane derivatives |
| BR112020014428A2 (pt) * | 2018-01-19 | 2020-12-01 | Cytokinetics, Inc. | composto, composição farmacêutica, e, métodos para o tratamento de uma doença cardíaca em um indivíduo, para o tratamento de uma doença ou condição que está associada com cavidade ventricular esquerda pequena e obliteração da cavidade, contração hiperdinâmica do ventrículo esquerdo, isquemia do miocárdio ou fibrose cardíaca, para o tratamento de uma doença ou condição selecionada dentre distrofias musculares e doenças de armazenamento do glicogênio e para inibição do sarcômero cardíaco |
| CN108558672B (zh) * | 2018-06-21 | 2021-04-30 | 利尔化学股份有限公司 | 2-硝基-4-三氟甲基苯甲酸及其异构体的制备方法 |
| US12054488B2 (en) * | 2018-09-27 | 2024-08-06 | Suzhou Raymon Pharmaceuticals Company, Ltd. | Pyrazolopyrimidine compound and preparation method therefor and use thereof in preparation of anti-cancer drug |
| US10836899B2 (en) | 2018-12-13 | 2020-11-17 | Eastman Chemical Company | Polyesters with specified crystallization half-times |
| CN116283995B (zh) * | 2022-09-08 | 2023-12-29 | 华中科技大学同济医学院附属同济医院 | 一种脂酰辅酶a合成酶短链家族成员3的激动剂及其应用 |
| CN116969831B (zh) * | 2023-08-01 | 2025-09-23 | 菏泽皓元医药科技有限公司 | 一种莫奈太尔的中间体及其制备方法 |
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-
2006
- 2006-05-22 CA CA2608890A patent/CA2608890C/en not_active Expired - Fee Related
- 2006-05-22 JP JP2008512617A patent/JP5463034B2/ja not_active Expired - Fee Related
- 2006-05-22 CN CNA2006800262633A patent/CN101238127A/zh active Pending
- 2006-05-22 AU AU2006251989A patent/AU2006251989B2/en not_active Ceased
- 2006-05-22 EA EA200702568A patent/EA013525B1/ru not_active IP Right Cessation
- 2006-05-22 KR KR1020077029688A patent/KR20080087070A/ko not_active Abandoned
- 2006-05-22 US US11/440,087 patent/US20060293345A1/en not_active Abandoned
- 2006-05-22 BR BRPI0609802A patent/BRPI0609802A2/pt not_active IP Right Cessation
- 2006-05-22 EP EP20060760560 patent/EP1910367A2/en not_active Withdrawn
- 2006-05-22 WO PCT/US2006/020970 patent/WO2006128184A2/en not_active Ceased
-
2007
- 2007-11-19 IL IL187495A patent/IL187495A0/en unknown
- 2007-12-07 US US12/001,041 patent/US20080161300A1/en not_active Abandoned
- 2007-12-19 NO NO20076554A patent/NO20076554L/no not_active Application Discontinuation
- 2007-12-19 CR CR9614A patent/CR9614A/es not_active Application Discontinuation
-
2013
- 2013-04-22 JP JP2013089076A patent/JP5391351B2/ja not_active Expired - Fee Related
- 2013-12-10 JP JP2013254709A patent/JP2014088396A/ja not_active Withdrawn
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