JP2010529991A5 - - Google Patents
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- Publication number
- JP2010529991A5 JP2010529991A5 JP2010512311A JP2010512311A JP2010529991A5 JP 2010529991 A5 JP2010529991 A5 JP 2010529991A5 JP 2010512311 A JP2010512311 A JP 2010512311A JP 2010512311 A JP2010512311 A JP 2010512311A JP 2010529991 A5 JP2010529991 A5 JP 2010529991A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- substituted
- ylmethyl
- alkyl
- nhco
- 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
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- -1 substituted Chemical class 0.000 claims 158
- 125000000217 alkyl group Chemical group 0.000 claims 45
- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 229910052760 oxygen Inorganic materials 0.000 claims 29
- 229910052731 fluorine Inorganic materials 0.000 claims 26
- 125000005842 heteroatom Chemical group 0.000 claims 26
- 229910052799 carbon Inorganic materials 0.000 claims 24
- 229910052717 sulfur Inorganic materials 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
- 125000004432 carbon atom Chemical group C* 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000001721 carbon Chemical group 0.000 claims 12
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 10
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 230000009424 thromboembolic effect Effects 0.000 claims 7
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000004523 tetrazol-1-yl group Chemical group N1(N=NN=C1)* 0.000 claims 6
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 6
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000006288 3,5-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(C([H])=C1F)C([H])([H])* 0.000 claims 3
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims 3
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 2
- 125000003287 1H-imidazol-4-ylmethyl group Chemical group [H]N1C([H])=NC(C([H])([H])[*])=C1[H] 0.000 claims 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 2
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000010102 embolization Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 210000002837 heart atrium Anatomy 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
- 0 CC(C*(C)N(C1)C(C(C)(*)I*)=O)c2c1cccc2 Chemical compound CC(C*(C)N(C1)C(C(C)(*)I*)=O)c2c1cccc2 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94379107P | 2007-06-13 | 2007-06-13 | |
| US60/943,791 | 2007-06-13 | ||
| US4951608P | 2008-05-01 | 2008-05-01 | |
| US61/049,516 | 2008-05-01 | ||
| PCT/US2008/066506 WO2008157162A1 (en) | 2007-06-13 | 2008-06-11 | Dipeptide analogs as coagulation factor inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529991A JP2010529991A (ja) | 2010-09-02 |
| JP2010529991A5 true JP2010529991A5 (enExample) | 2010-11-04 |
| JP5318094B2 JP5318094B2 (ja) | 2013-10-16 |
Family
ID=39714076
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010512311A Expired - Fee Related JP5318094B2 (ja) | 2007-06-13 | 2008-06-11 | 凝固因子阻害剤としてのジペプチド類似体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8367709B2 (enExample) |
| EP (1) | EP2152664B1 (enExample) |
| JP (1) | JP5318094B2 (enExample) |
| KR (1) | KR20100037600A (enExample) |
| CN (1) | CN101784516B (enExample) |
| AR (1) | AR067329A1 (enExample) |
| AU (1) | AU2008266228A1 (enExample) |
| CL (1) | CL2008001724A1 (enExample) |
| MX (1) | MX2009012847A (enExample) |
| PE (1) | PE20091002A1 (enExample) |
| TW (1) | TW200848024A (enExample) |
| WO (1) | WO2008157162A1 (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1567487A4 (en) | 2002-11-15 | 2005-11-16 | Bristol Myers Squibb Co | OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION |
| ATE543811T1 (de) * | 2008-03-13 | 2012-02-15 | Bristol Myers Squibb Co | Pyridazinderivate als faktor-xia-inhibitoren |
| MX2010012242A (es) * | 2008-05-19 | 2010-12-06 | Actelion Pharmaceuticals Ltd | Tetrahidroisoquinolinas como agentes antimalariales. |
| BRPI1015145A2 (pt) * | 2009-04-22 | 2018-01-30 | Actelion Pharmaceuticals Ltd | derivados de tiazol e seu uso como receptores antagonistas de p2y12 |
| ES2822130T3 (es) | 2010-02-11 | 2021-04-29 | Bristol Myers Squibb Co | Macrociclos como inhibidores del factor XIa |
| GB2494851A (en) * | 2011-07-07 | 2013-03-27 | Kalvista Pharmaceuticals Ltd | Plasma kallikrein inhibitors |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| IN2014CN02805A (enExample) * | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| TWI633091B (zh) | 2011-10-14 | 2018-08-21 | Bristol-Myers Squibb Company | 作為因子ｘｉａ抑制劑之經取代四氫異喹啉化合物 |
| US9108951B2 (en) | 2011-10-14 | 2015-08-18 | Bristol-Myers Squibb Company | Substituted 5,6,7,8-tetrahydro-1,6-naphthyridines as factor XIa inhibitors |
| JP2015083542A (ja) * | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| HK1209747A1 (en) * | 2012-07-19 | 2016-04-08 | 大日本住友制药株式会社 | 1-(cycloalkyl-carbonyl)proline derivative |
| PL2880026T3 (pl) | 2012-08-03 | 2017-08-31 | Bristol-Myers Squibb Company | Dihydropirydon P1 jako inhibitory czynnika XIA |
| SG11201500270RA (en) | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| SI2906551T1 (en) | 2012-10-12 | 2018-05-31 | Bristol-Myers Squibb Company | Crystalline forms of a factor xia inhibitor |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
| US20160257668A1 (en) | 2013-10-07 | 2016-09-08 | Merck Sharp & Dohme Corp. | Factor XIa Inhibitors |
| BR112016015717B1 (pt) | 2014-01-31 | 2023-04-04 | Bristol-Myers Squibb Company | Compostos macrociclos com grupos p2' heterocíclicos como inibidores do fator xia, composição farmacêutica compreendendo os referidos compostos e uso dos mesmos |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| KR20170005871A (ko) | 2014-05-28 | 2017-01-16 | 머크 샤프 앤드 돔 코포레이션 | 인자 XIa 억제제 |
| WO2016018702A1 (en) * | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| JP6526796B2 (ja) | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｆｘｉａ阻害剤であるジアミドマクロ環 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| CN105294669B (zh) * | 2014-10-24 | 2019-01-22 | 山东凯森制药有限公司 | 一种第十因子抑制剂及其制备方法和应用 |
| MX2017009445A (es) * | 2015-01-20 | 2017-11-08 | Merck Sharp & Dohme | Inhibidores del factor xia. |
| MA42032A (fr) | 2015-02-02 | 2018-03-14 | Forma Therapeutics Inc | Acides 3-aryl-4-amido-bicyclo [4,5,0]hydroxamiques en tant qu'inhibiteurs de hdac |
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| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| JP6629958B2 (ja) | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤 |
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| US10344039B2 (en) | 2015-10-29 | 2019-07-09 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use |
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| US10555935B2 (en) | 2016-06-17 | 2020-02-11 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as HDAC inhibitors |
| IT201600074606A1 (it) * | 2016-07-18 | 2018-01-18 | Italfarmaco Spa | New benzo-N-hydroxy amide compounds having antitumor activity |
| TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
| EP3509590A4 (en) * | 2016-09-07 | 2020-12-02 | Pliant Therapeutics, Inc. | N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE |
| EP3589627A4 (en) | 2017-02-28 | 2020-08-05 | Morphic Therapeutic, Inc. | (ALPHA-V) (BETA-6) INHIBITORS INTEGRIN |
| EP3760202A1 (en) | 2017-02-28 | 2021-01-06 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| TWI780281B (zh) * | 2017-12-14 | 2022-10-11 | 丹麥商Ｎｍｄ藥品公司 | 用於治療神經肌肉病症的化合物 |
| CN109928910B (zh) * | 2017-12-19 | 2022-07-22 | 上海医药工业研究院 | 抗偏头痛药物阿莫曲坦的制备方法 |
| PL3844162T3 (pl) | 2018-08-29 | 2025-06-09 | Morphic Therapeutic, Inc. | Inhibitory integryny alfa v beta 6 |
| EP3617206A1 (en) | 2018-08-29 | 2020-03-04 | Morphic Therapeutic, Inc. | Integrin inhibitors |
| TW202028179A (zh) * | 2018-10-08 | 2020-08-01 | 美商普萊恩醫療公司 | 胺基酸化合物及使用方法 |
| EP3873916B8 (en) * | 2018-10-29 | 2025-03-26 | Shanghai Synergy Pharmaceutical Sciences, Ltd. | Novel dipeptide compounds and uses thereof |
| CN111138366B (zh) * | 2018-11-06 | 2023-03-28 | 天津药物研究院有限公司 | 吡唑氨基甲酰类衍生物、及其制备方法和用途 |
| KR20210108416A (ko) * | 2018-12-19 | 2021-09-02 | 레오 파마 에이/에스 | Il-17의 소분자 조절제로서의 아미노산 아닐라이드 |
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| CA3147564A1 (en) * | 2019-08-21 | 2021-02-25 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| CN115066417B (zh) * | 2019-12-31 | 2025-05-02 | 上海京新生物医药有限公司 | 凝血因子XIa抑制剂 |
| CN113943259A (zh) * | 2020-07-17 | 2022-01-18 | 西安禾渼生物医药有限公司 | 一种氨基酸衍生物、其制备方法及应用 |
| SI4214210T1 (sl) * | 2020-09-17 | 2025-07-31 | Novartis Ag | Spojine in sestavki kot zaviralci sppl2a |
| CN112341398B (zh) * | 2020-11-11 | 2022-05-03 | 湖北文理学院 | 具有生物活性的1,2,3-三氮唑取代的查尔酮衍生物、制备方法及其应用 |
| WO2022122035A1 (zh) * | 2020-12-11 | 2022-06-16 | 上海领泰生物医药科技有限公司 | 凝血因子XIa抑制剂及其制备方法和应用 |
| MX2023008753A (es) | 2021-01-28 | 2023-08-02 | Merck Sharp & Dohme Llc | Inhibidores del factor xia. |
| CN113636982A (zh) * | 2021-04-28 | 2021-11-12 | 合肥工业大学 | 一种肉桂酸衍生物及其制备方法和用途 |
| CN116655534A (zh) * | 2023-06-07 | 2023-08-29 | 上海吉奉生物科技有限公司 | 一种Boc-3-（3-吡唑）- L -丙氨酸的合成方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1108819A (en) * | 1964-07-31 | 1968-04-03 | Rotta Research Lab | Derivatives of 2-acylaminobicarboxylic acids and method for preparing same |
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| JPS611651A (ja) * | 1984-06-12 | 1986-01-07 | Toyama Chem Co Ltd | Ｎ−アシル酸性アミノ酸ジアミド類およびその製造法並びにそれらを含有する抗潰瘍剤 |
| ATE63906T1 (de) * | 1986-03-14 | 1991-06-15 | Syntex Inc | 3,5-disubstituierte 4,5-dihydroisoxazole als transglutaminasehemmer. |
| AU680870B2 (en) * | 1993-04-28 | 1997-08-14 | Astellas Pharma Inc. | New heterocyclic compounds |
| JPH09169752A (ja) * | 1995-02-14 | 1997-06-30 | Mitsubishi Chem Corp | 含酸素複素環誘導体 |
| AR013079A1 (es) * | 1997-05-06 | 2000-12-13 | Smithkline Beecham Corp | Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios |
| JP4191825B2 (ja) * | 1998-09-10 | 2008-12-03 | あすか製薬株式会社 | ５−アミノイソキサゾール誘導体 |
| DE69924527T2 (de) * | 1999-01-02 | 2006-02-09 | Sanofi-Aventis Deutschland Gmbh | Arylalkanoylderivate, verfahren zu ihrer herstellung, ihre verwendung und diese enthaltende pharmazeutische zubereitungen |
| US6362165B1 (en) * | 1999-03-30 | 2002-03-26 | Pharmacor Inc. | Hydroxyphenyl derivatives with HIV integrase inhibitory properties |
| CA2321348A1 (en) * | 2000-09-27 | 2002-03-27 | Blaise Magloire N'zemba | Aromatic derivatives with hiv integrase inhibitory properties |
| DE10063008A1 (de) * | 2000-12-16 | 2002-06-20 | Merck Patent Gmbh | Carbonsäureamidderivate |
| JP2005504003A (ja) * | 2001-02-09 | 2005-02-10 | メルク エンド カムパニー インコーポレーテッド | トロンビン阻害剤 |
| DE10124041A1 (de) * | 2001-05-16 | 2002-11-21 | Graffinity Pharm Design Gmbh | Protease Inhibitoren |
| AU2003299901A1 (en) | 2002-10-04 | 2004-05-04 | Merck And Co., Inc. | Thrombin inhibitors |
| US20040180855A1 (en) | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
| US7217794B2 (en) * | 2003-04-02 | 2007-05-15 | Daiamed, Inc. | Compounds and methods for treatment of thrombosis |
| CA2542064A1 (en) * | 2003-10-24 | 2005-05-06 | Exelixis, Inc. | Tao kinase modulators and methods of use |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| CN101137412B (zh) | 2005-01-13 | 2012-11-07 | 布里斯托尔-迈尔斯·斯奎布公司 | 用作凝血因子XIa抑制剂的取代的二芳基化合物 |
| WO2007070818A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2007070816A2 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Thiophene derivatives as factor xia inhibitors |
| JP5225098B2 (ja) * | 2005-12-14 | 2013-07-03 | ブリストル−マイヤーズ スクイブ カンパニー | 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ |
| KR20090122931A (ko) * | 2007-03-26 | 2009-12-01 | 아스테라스 세이야쿠 가부시키가이샤 | 오르니틴 유도체 |
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2008
- 2008-06-11 MX MX2009012847A patent/MX2009012847A/es active IP Right Grant
- 2008-06-11 WO PCT/US2008/066506 patent/WO2008157162A1/en not_active Ceased
- 2008-06-11 US US12/663,861 patent/US8367709B2/en active Active
- 2008-06-11 CN CN200880103481.1A patent/CN101784516B/zh not_active Expired - Fee Related
- 2008-06-11 JP JP2010512311A patent/JP5318094B2/ja not_active Expired - Fee Related
- 2008-06-11 AR ARP080102487A patent/AR067329A1/es not_active Application Discontinuation
- 2008-06-11 PE PE2008001000A patent/PE20091002A1/es not_active Application Discontinuation
- 2008-06-11 TW TW097121816A patent/TW200848024A/zh unknown
- 2008-06-11 KR KR1020107000723A patent/KR20100037600A/ko not_active Withdrawn
- 2008-06-11 CL CL200801724A patent/CL2008001724A1/es unknown
- 2008-06-11 AU AU2008266228A patent/AU2008266228A1/en not_active Abandoned
- 2008-06-11 EP EP08770664.4A patent/EP2152664B1/en not_active Not-in-force