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 (enExample) | 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 (enExample) |
| EP (1) | EP1910367A2 (enExample) |
| JP (3) | JP5463034B2 (enExample) |
| KR (1) | KR20080087070A (enExample) |
| CN (1) | CN101238127A (enExample) |
| AU (1) | AU2006251989B2 (enExample) |
| BR (1) | BRPI0609802A2 (enExample) |
| CA (1) | CA2608890C (enExample) |
| CR (1) | CR9614A (enExample) |
| EA (1) | EA013525B1 (enExample) |
| IL (1) | IL187495A0 (enExample) |
| NO (1) | NO20076554L (enExample) |
| WO (1) | WO2006128184A2 (enExample) |
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 |
| US20090221703A1 (en) | 2006-07-09 | 2009-09-03 | Chongxi Yu | High penetration composition and uses thereof |
| US20090238763A1 (en) | 2006-07-09 | 2009-09-24 | Chongxi Yu | High penetration compositions and uses thereof |
| CA2670044A1 (en) * | 2006-11-20 | 2008-05-29 | Alantos Pharmaceuticals Holding, Inc. | Heterobicyclic matrix metalloprotease inhibitors |
| US20080176870A1 (en) * | 2006-11-20 | 2008-07-24 | Bert Nolte | Heterobicyclic metalloprotease inhibitors |
| US20080221093A1 (en) * | 2007-03-07 | 2008-09-11 | Christian Gege | Metalloprotease inhibitors containing a heterocyclic moiety |
| KR20220107078A (ko) | 2007-06-04 | 2022-08-01 | 테크필즈 인크 | 매우 높은 피부 및 막 침투율을 가지는 비스테로이드성 소염제(ｎｓａｉａ) 약물전구체 및 이들의 새로운 의약적 용도 |
| WO2009075790A1 (en) * | 2007-12-07 | 2009-06-18 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors for intra-articular application |
| CA2723302C (en) | 2008-05-05 | 2013-08-20 | Sanofi-Aventis | Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals |
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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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| BR112013014242B1 (pt) | 2010-12-08 | 2022-02-22 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Composição farmacêutica e composto ou seu sal farmaceuticamente aceitável |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| KR101935868B1 (ko) | 2011-12-30 | 2019-04-03 | 에스케이이노베이션 주식회사 | 폴리프로필렌 카보네이트 발포체 조성물 제조방법 및 이로부터 제조된 성형품 |
| CN107929743B (zh) | 2012-01-18 | 2023-09-01 | 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 |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
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| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | 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 |
| JP2016512239A (ja) | 2013-03-15 | 2016-04-25 | 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化合物 |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| 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 |
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| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| EP3529230B1 (en) | 2016-10-19 | 2020-09-30 | Eastman Chemical Company | Synthesis of bicyclo(2.2.2)octanes |
| EP3694831A1 (en) | 2017-10-11 | 2020-08-19 | Eastman Chemical Company | Synthesis of bicyclo[2.2.2]octane derivatives |
| TWI835770B (zh) * | 2018-01-19 | 2024-03-21 | 美商胞質動力學公司 | 心肌節抑制劑 |
| 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 |
| CN110950868B (zh) * | 2018-09-27 | 2022-05-13 | 苏州锐明新药研发有限公司 | 吡唑并嘧啶化合物及制备方法与制备抗癌症药物的应用 |
| 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 WO PCT/US2006/020970 patent/WO2006128184A2/en not_active Ceased
- 2006-05-22 AU AU2006251989A patent/AU2006251989B2/en not_active Ceased
- 2006-05-22 JP JP2008512617A patent/JP5463034B2/ja not_active Expired - Fee Related
- 2006-05-22 CA CA2608890A patent/CA2608890C/en not_active Expired - Fee Related
- 2006-05-22 US US11/440,087 patent/US20060293345A1/en not_active Abandoned
- 2006-05-22 EA EA200702568A patent/EA013525B1/ru not_active IP Right Cessation
- 2006-05-22 BR BRPI0609802A patent/BRPI0609802A2/pt not_active IP Right Cessation
- 2006-05-22 KR KR1020077029688A patent/KR20080087070A/ko not_active Abandoned
- 2006-05-22 EP EP20060760560 patent/EP1910367A2/en not_active Withdrawn
- 2006-05-22 CN CNA2006800262633A patent/CN101238127A/zh active Pending
-
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 CR CR9614A patent/CR9614A/es not_active Application Discontinuation
- 2007-12-19 NO NO20076554A patent/NO20076554L/no 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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