JP2002506878A5 - - Google Patents
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- JP2002506878A5 JP2002506878A5 JP2000536738A JP2000536738A JP2002506878A5 JP 2002506878 A5 JP2002506878 A5 JP 2002506878A5 JP 2000536738 A JP2000536738 A JP 2000536738A JP 2000536738 A JP2000536738 A JP 2000536738A JP 2002506878 A5 JP2002506878 A5 JP 2002506878A5
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- Prior art keywords
- alkyl
- aryl
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- hydrogen atom
- carbon atom
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 description 100
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 56
- 229910052799 carbon Inorganic materials 0.000 description 54
- 150000001875 compounds Chemical class 0.000 description 36
- 229910052757 nitrogen Inorganic materials 0.000 description 21
- 125000004122 cyclic group Chemical group 0.000 description 20
- 125000004433 nitrogen atom Chemical group N* 0.000 description 20
- 125000004429 atom Chemical group 0.000 description 19
- 125000003118 aryl group Chemical group 0.000 description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 12
- 125000002877 alkyl aryl group Chemical group 0.000 description 9
- 125000005213 alkyl heteroaryl group Chemical group 0.000 description 8
- 125000003275 alpha amino acid group Chemical group 0.000 description 8
- 125000000753 cycloalkyl group Chemical group 0.000 description 8
- 201000010099 disease Diseases 0.000 description 8
- 125000003341 7 membered heterocyclic group Chemical group 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 6
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000000304 alkynyl group Chemical group 0.000 description 4
- OKTJSMMVPCPJKN-BJUDXGSMSA-N carbon-11 Chemical compound [11C] OKTJSMMVPCPJKN-BJUDXGSMSA-N 0.000 description 4
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 125000000623 heterocyclic group Chemical group 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 230000001404 mediated effect Effects 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 208000034578 Multiple myelomas Diseases 0.000 description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 2
- 208000020084 Bone disease Diseases 0.000 description 2
- 0 CC1N(C)N(*)CCC1 Chemical compound CC1N(C)N(*)CCC1 0.000 description 2
- 206010009900 Colitis ulcerative Diseases 0.000 description 2
- 208000011231 Crohn disease Diseases 0.000 description 2
- 206010012438 Dermatitis atopic Diseases 0.000 description 2
- 206010058314 Dysplasia Diseases 0.000 description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 2
- 206010033645 Pancreatitis Diseases 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- 206010040070 Septic Shock Diseases 0.000 description 2
- 206010052779 Transplant rejections Diseases 0.000 description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 description 2
- 208000006673 asthma Diseases 0.000 description 2
- 201000008937 atopic dermatitis Diseases 0.000 description 2
- 206010014599 encephalitis Diseases 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 230000002757 inflammatory effect Effects 0.000 description 2
- 208000032839 leukemia Diseases 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 201000008482 osteoarthritis Diseases 0.000 description 2
- 206010034674 peritonitis Diseases 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 230000036303 septic shock Effects 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 230000009529 traumatic brain injury Effects 0.000 description 2
- 208000030507 AIDS Diseases 0.000 description 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 1
- 201000004384 Alopecia Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010055128 Autoimmune neutropenia Diseases 0.000 description 1
- 208000004429 Bacillary Dysentery Diseases 0.000 description 1
- 208000023328 Basedow disease Diseases 0.000 description 1
- 201000006474 Brain Ischemia Diseases 0.000 description 1
- ZKJMEUDMEWCSLN-UHFFFAOYSA-N CC(C1)C11CN(C)C(C)C1 Chemical compound CC(C1)C11CN(C)C(C)C1 ZKJMEUDMEWCSLN-UHFFFAOYSA-N 0.000 description 1
- KIIVOWBOBNLXLC-UHFFFAOYSA-N CC(CC1)N(C)N1I Chemical compound CC(CC1)N(C)N1I KIIVOWBOBNLXLC-UHFFFAOYSA-N 0.000 description 1
- MXNLMAXYAXLGOZ-UHFFFAOYSA-N CC1N(C)C2C(CC(CC3)N(C)N3I)CC1C2 Chemical compound CC1N(C)C2C(CC(CC3)N(C)N3I)CC1C2 MXNLMAXYAXLGOZ-UHFFFAOYSA-N 0.000 description 1
- VYGNGGAWKOTHPL-UHFFFAOYSA-N CC1N(C)CC(CC2N(C)CCSC2)C2=C1C=CCC2 Chemical compound CC1N(C)CC(CC2N(C)CCSC2)C2=C1C=CCC2 VYGNGGAWKOTHPL-UHFFFAOYSA-N 0.000 description 1
- PLYTVAFAKDFFKM-UHFFFAOYSA-N CC1N(C)CCOC1 Chemical compound CC1N(C)CCOC1 PLYTVAFAKDFFKM-UHFFFAOYSA-N 0.000 description 1
- YTDZUPBPWJAQDV-UHFFFAOYSA-N CC1N(C)N=CC1 Chemical compound CC1N(C)N=CC1 YTDZUPBPWJAQDV-UHFFFAOYSA-N 0.000 description 1
- XBLIBPCVUHVKRQ-UHFFFAOYSA-N CC1NN(C)C(C)CC1 Chemical compound CC1NN(C)C(C)CC1 XBLIBPCVUHVKRQ-UHFFFAOYSA-N 0.000 description 1
- ZKRXWYLRHMCOMH-UHFFFAOYSA-N CC1SC(CC2(C3)N(C)CC3C2)=NN1C Chemical compound CC1SC(CC2(C3)N(C)CC3C2)=NN1C ZKRXWYLRHMCOMH-UHFFFAOYSA-N 0.000 description 1
- GVHGKIMUVGJKJV-UHFFFAOYSA-N CC1SC=NN1C Chemical compound CC1SC=NN1C GVHGKIMUVGJKJV-UHFFFAOYSA-N 0.000 description 1
- GXQTWFFYZDGBLN-UHFFFAOYSA-N CCCC(C)N(C)N Chemical compound CCCC(C)N(C)N GXQTWFFYZDGBLN-UHFFFAOYSA-N 0.000 description 1
- 206010008120 Cerebral ischaemia Diseases 0.000 description 1
- 206010008909 Chronic Hepatitis Diseases 0.000 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 208000001490 Dengue Diseases 0.000 description 1
- 206010012310 Dengue fever Diseases 0.000 description 1
- 206010014596 Encephalitis Japanese B Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010017915 Gastroenteritis shigella Diseases 0.000 description 1
- 206010018364 Glomerulonephritis Diseases 0.000 description 1
- 208000009329 Graft vs Host Disease Diseases 0.000 description 1
- 208000015023 Graves' disease Diseases 0.000 description 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 description 1
- 208000005176 Hepatitis C Diseases 0.000 description 1
- 206010019773 Hepatitis G Diseases 0.000 description 1
- 206010019755 Hepatitis chronic active Diseases 0.000 description 1
- 101000960954 Homo sapiens Interleukin-18 Proteins 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 102100037850 Interferon gamma Human genes 0.000 description 1
- 108010074328 Interferon-gamma Proteins 0.000 description 1
- 102000000589 Interleukin-1 Human genes 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 102100039898 Interleukin-18 Human genes 0.000 description 1
- 201000005807 Japanese encephalitis Diseases 0.000 description 1
- 241000710842 Japanese encephalitis virus Species 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 1
- 206010039710 Scleroderma Diseases 0.000 description 1
- 206010040047 Sepsis Diseases 0.000 description 1
- 206010043781 Thyroiditis chronic Diseases 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 description 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 231100000360 alopecia Toxicity 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 201000005000 autoimmune gastritis Diseases 0.000 description 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 208000025729 dengue disease Diseases 0.000 description 1
- 230000001066 destructive effect Effects 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 210000004392 genitalia Anatomy 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 208000002672 hepatitis B Diseases 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 208000021039 metastatic melanoma Diseases 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 206010028417 myasthenia gravis Diseases 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 230000001338 necrotic effect Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 201000005113 shigellosis Diseases 0.000 description 1
- 208000002320 spinal muscular atrophy Diseases 0.000 description 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 description 1
- 206010043554 thrombocytopenia Diseases 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7877098P | 1998-03-19 | 1998-03-19 | |
| US60/078,770 | 1998-03-19 | ||
| PCT/US1999/005919 WO1999047545A2 (en) | 1998-03-19 | 1999-03-19 | Inhibitors of caspases |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006075461A Division JP2006206600A (ja) | 1998-03-19 | 2006-03-17 | カスパーゼのインヒビター |
| JP2010151471A Division JP2010241822A (ja) | 1998-03-19 | 2010-07-01 | カスパーゼのインヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002506878A JP2002506878A (ja) | 2002-03-05 |
| JP2002506878A5 true JP2002506878A5 (enExample) | 2006-06-01 |
| JP4594520B2 JP4594520B2 (ja) | 2010-12-08 |
Family
ID=22146109
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000536738A Expired - Lifetime JP4594520B2 (ja) | 1998-03-19 | 1999-03-19 | カスパーゼのインヒビター |
| JP2006075461A Withdrawn JP2006206600A (ja) | 1998-03-19 | 2006-03-17 | カスパーゼのインヒビター |
| JP2010151471A Withdrawn JP2010241822A (ja) | 1998-03-19 | 2010-07-01 | カスパーゼのインヒビター |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006075461A Withdrawn JP2006206600A (ja) | 1998-03-19 | 2006-03-17 | カスパーゼのインヒビター |
| JP2010151471A Withdrawn JP2010241822A (ja) | 1998-03-19 | 2010-07-01 | カスパーゼのインヒビター |
Country Status (33)
Families Citing this family (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7244677B2 (en) | 1998-02-04 | 2007-07-17 | Semitool. Inc. | Method for filling recessed micro-structures with metallization in the production of a microelectronic device |
| PL204619B1 (pl) * | 1998-03-19 | 2010-01-29 | Vertex Pharma | Pochodna peptydowa, kompozycja farmaceutyczna zawierająca taką pochodną i zastosowanie pochodnej peptydowej |
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| US7326542B2 (en) | 1998-12-02 | 2008-02-05 | Princeton University | Compositions and methods for regulating bacterial pathogenesis |
| US6720415B2 (en) | 1998-12-02 | 2004-04-13 | Princeton University | Compositions and methods for regulating bacterial pathogenesis |
| WO2001027085A1 (en) * | 1999-10-13 | 2001-04-19 | Merck Frosst Canada & Co. | Nicotinyl aspartyl ketones as inhibitors of caspase-3 |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| US6525024B1 (en) | 2000-04-17 | 2003-02-25 | Idun Pharmaceuticals, Inc. | Inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6559176B1 (en) | 2000-05-10 | 2003-05-06 | Princeton University | Compounds and methods for regulating bacterial growth and pathogenesis |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| JP2004509120A (ja) * | 2000-09-13 | 2004-03-25 | 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 | カスパーゼ阻害剤およびそれらの用途 |
| US20030039661A1 (en) * | 2001-03-02 | 2003-02-27 | Teresa Aja | Methods, compositions and kits for preserving antigenicity |
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| FR2839309B1 (fr) | 2002-05-03 | 2004-07-23 | Aventis Pharma Sa | Nouveaux derives de l'acide hexahydro-pyridazine-3- carboxylique, chimiotheques les contenant, leur utilisation comme medicaments, compositions pharmaceutiques les contenant et leurs procedes de preparation |
| US7001899B2 (en) | 2002-06-10 | 2006-02-21 | The Procter & Gamble Company | Interleukin converting enzyme inhibitors |
| AU2003263393A1 (en) * | 2002-09-04 | 2004-03-29 | Glenmark Pharmaceuticals Limited | New heterocyclic amide compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them |
| MXPA05002514A (es) | 2002-09-06 | 2005-05-27 | Amgen Inc | Anticuerpo monoclonal anti-il-1r1 humano terapeutico. |
| KR20050065624A (ko) | 2002-10-23 | 2005-06-29 | 그렌마크 파머수티칼스 엘티디. | 염증성 및 알레르기 질환의 치료에 유용한 신규한트리사이클릭 화합물, 이의 제조 방법 및 이를 함유하는약제 조성물 |
| FR2846969A1 (fr) * | 2002-11-08 | 2004-05-14 | Salles Jean Pierre | Nouveaux vecteurs moleculaires amphiphiles fluorocarbones a usage biomedical et medical |
| AU2003295041A1 (en) * | 2002-11-20 | 2004-06-18 | L'oreal | Composition for hair care or eyelashes containing a pyrazol-carboxamide, its use for stimulating hair and eyelash growth and/or for preventing loss thereof |
| FR2847160A1 (fr) * | 2002-11-20 | 2004-05-21 | Oreal | Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute |
| SI1620429T1 (sl) | 2003-04-11 | 2009-08-31 | Glenmark Pharmaceuticals Sa | Nove heterociklične spojine, uporabne za zdravljenje vnetnih in alergijskih motenj: postopek za njihovo pripravo in farmacevtski sestavki, ki jih vsebujejo |
| AU2003902704A0 (en) * | 2003-05-29 | 2003-06-19 | Crc For Waste Management And Pollution Control Limited Of Unsw | Process for producing a nanoscale zero-valent metal |
| JP2007513092A (ja) * | 2003-12-01 | 2007-05-24 | 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 | Ice阻害剤を使用する感染性疾患の処置 |
| ES2320643T3 (es) * | 2003-12-12 | 2009-05-27 | Dr. Straetmans Chemische Produkte Gmbh | Composiciones con acido anisico y gliceridos. |
| CA2820541A1 (en) * | 2004-02-27 | 2005-09-15 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| RU2382780C2 (ru) * | 2004-02-27 | 2010-02-27 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы каспаз и их применение |
| AU2011226946B2 (en) * | 2004-02-27 | 2012-05-03 | Vertex Pharmaceuticals Incoporated | Caspase Inhibitors and Uses Thereof |
| AU2005223767B2 (en) | 2004-03-12 | 2011-12-01 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
| ES2393324T3 (es) * | 2004-05-14 | 2012-12-20 | Emisphere Technologies, Inc. | Compuestos y composiciones para administrar principios activos |
| AU2012200214B2 (en) * | 2004-05-14 | 2013-10-24 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| PL217743B1 (pl) * | 2004-05-15 | 2014-08-29 | Vertex Pharma | Zastosowanie inhibitorów ICE/kaspazy-1 do leczenia napadów i konwulsji w epilepsji oraz zawierające je kompozycja farmaceutyczna i zestaw |
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| UA88795C2 (ru) | 2004-12-17 | 2009-11-25 | Гленмарк Фармасьютікалс С.А. | Гетероциклические соединения, которые применяются для лечения воспалителных и аллергических нарушений |
| PL1831227T3 (pl) | 2004-12-17 | 2013-10-31 | Glenmark Pharmaceuticals Sa | Nowe związki heterocykliczne użyteczne w leczeniu stanów zapalnych i dolegliwości alergicznych |
| JP4673068B2 (ja) * | 2005-01-19 | 2011-04-20 | 独立行政法人科学技術振興機構 | Th1型アレルギー疾患治療用組成物 |
| DE102005017116A1 (de) | 2005-04-13 | 2006-10-26 | Novartis Ag | Hemmstoffe für Inhibitoren von Apoptose Proteinen (IAP) |
| KR20080038369A (ko) | 2005-07-28 | 2008-05-06 | 버텍스 파마슈티칼스 인코포레이티드 | 카스파제 억제제 프로드럭 |
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| JP2009542689A (ja) * | 2006-07-07 | 2009-12-03 | ザ ボード オブ トラスティーズ オブ ザ リーランド スタンフォード ジュニア ユニバーシティ | 選択的カスパーゼ阻害剤 |
| MX2009005252A (es) * | 2006-11-17 | 2009-05-28 | Abbott Lab | Aminopirrolidinas como antagonistas del receptor de quimiocina. |
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| US9365612B2 (en) | 2010-01-29 | 2016-06-14 | United States Of America As Represented By The Secretary, Department Of Health And Human Services | Caspase inhibitors |
| GB201011411D0 (en) | 2010-07-06 | 2010-08-18 | St Georges Hosp Medical School | Therapeutic compounds and their use |
| JP6006908B2 (ja) | 2010-11-05 | 2016-10-12 | ブランダイス ユニバーシティBrandeis University | Ice阻害化合物およびその使用 |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| IN2014CN02806A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| IN2014CN02805A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| LT2766346T (lt) | 2011-10-14 | 2017-06-12 | Bristol-Myers Squibb Company | Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai |
| KR20150046259A (ko) | 2012-08-23 | 2015-04-29 | 앨리오스 바이오파마 인크. | 파라믹소바이러스 바이러스성 감염의 치료용 화합물 |
| HRP20180465T1 (hr) | 2012-10-12 | 2018-05-04 | Bristol-Myers Squibb Company | Kristalni oblici inhibitora faktora xia |
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