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31. 发明申请

WO9962538A8 ALPHA-KETO OXADIAZOLES AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译： ALPHA-KETO OXADIAZOLES作为丝氨酸蛋白酶抑制剂
公开(公告)号：WO9962538A8
公开(公告)日：2000-02-24
申请号：PCT/US9912354
申请日：1999-06-03
申请人： CORTECH INC
发明人： GYORKOS ALBERT , SPRUCE LYLE
IPC分类号： A61K38/00 , A61K38/55 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/28 , A61P27/02 , A61P27/16 , A61P31/04 , A61P35/00 , A61P37/06 , A61P43/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , C12N9/99 , A61K38/05 , A61K38/06 , C07K5/097
CPC分类号： C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06052 , C07K5/0806 , C07K5/12
摘要： The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids containing valine and proline residues and nonpeptoids containing pyrimidinone residues useful as inhibitors of serine proteases, for example human neutrophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.
摘要翻译：本发明涉及含有缬氨酸和脯氨酸残基的某些取代的恶二唑，噻二唑和三唑拟肽，以及含有可用作丝氨酸蛋白酶抑制剂（例如人嗜中性粒细胞弹性蛋白酶（HNE））的嘧啶酮残基的非头孢菌素。本发明化合物可用于治疗或改善成人呼吸窘迫综合征，败血性休克和多器官功能衰竭的症状。由HNE介导的过程也涉及诸如关节炎，牙周病，肾小球性肾炎和囊性纤维化的病症。

32. 发明申请

WO99031121A3 BRANCHED BUILDING UNITS FOR SYNTHESIZING CYCLIC PEPTIDES 审中-公开
标题翻译：用于合成循环肽的分支建筑单元
公开(公告)号：WO99031121A3
公开(公告)日：1999-08-19
申请号：PCT/EP1998/008187
申请日：1998-12-14
IPC分类号： C07C229/36 , C07C237/10 , C07C271/20 , C07C271/22 , C07K5/02 , C07K5/06 , C07K5/065
CPC分类号： C07K5/06052 , C07C229/36 , C07C237/10 , C07C271/20 , C07C271/22 , C07K5/02 , C07K5/06078 , Y02P20/55
摘要： The present invention relates to building units suitable for the synthesis of backbone cyclized peptides. The building units of this invention have structures of the formula (I): X-AAm-U-AAp-Y wherein AAm and AAp are residues of natural or synthetic amino acids and U is C ON[(CH2)n+1W] or PSI (C H2N)[CO(CH2)qW], in which C is a carbon atom and is the alpha carbon of AAm if m > 0. W is NH-X or COY, and X is H, Boc, Z, Fmoc, or Alloc while Y is the hydroxyl group of a carboxylic acid moiety or a carboxylic acid protecting group. The letter m refers to an integer from 0 to 10; n is a number from 0 to 6; p is a number from 1 to 10; and q is a number from 1 to 6. The present invention is also directed to methods of synthesizing building units of formula (I) via different routes.
摘要翻译：本发明涉及适用于合成骨架环化肽的构建单元。本发明的构建单元具有式（I）的结构：X-AAm-U-AAp-Y，其中AAm和AAp是天然或合成氨基酸的残基，U是C [ON（O）n + 1W]或PSI（C H2N）[CO（CH 2）qW]，其中Cα是碳原子，如果m> 0，则是AAm的α碳.W是NH-X或COY，以及 X是H，Boc，Z，Fmoc或Alloc，而Y是羧酸部分或羧酸保护基的羟基。字母m表示从0到10的整数; n是从0到6的数字; p是从1到10的数字; 并且q是1至6的数字。本发明还涉及通过不同途径合成式（I）的建筑单元的方法。

33. 发明申请

WO99037668A1 THROMBIN INHIBITORS 审中-公开
标题翻译：凝血酶抑制剂
公开(公告)号：WO99037668A1
公开(公告)日：1999-07-29
申请号：PCT/EP1999/000434
申请日：1999-01-23
IPC分类号： A61K38/00 , A61P1/18 , A61P7/02 , A61P11/06 , A61P17/04 , A61P19/02 , A61P27/16 , A61P29/00 , C07K5/06 , C07K5/065 , A61K38/05
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/06078
摘要： The invention relates to compounds of the formula A-B-D-E-F, in which A, B, D, E and F have the meanings given in the description, and to their production. These new compounds are suitable for producing medicines.
摘要翻译：是式A-B-D-E-F，其中A，B，D，E和F具有说明书中给出的含义的化合物，和描述它们的制备。这些新化合物是适用于制备药物。

34. 发明申请

WO99037667A1 EFFLUX PUMP INHIBITORS 审中-公开
标题翻译： EFFLUX泵抑制剂
公开(公告)号：WO99037667A1
公开(公告)日：1999-07-29
申请号：PCT/US1999/001422
申请日：1999-01-22
IPC分类号： A61K38/00 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/06
CPC分类号： C07K5/06095 , A61K38/00 , C07K5/06078 , C07K5/06086 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.
摘要翻译：描述了具有外排泵抑制剂活性的化合物。还描述了使用这种外排泵抑制剂化合物和包括这些化合物的药物组合物的方法。

35. 发明申请

WO9901470A3 PEPTIDOMIMETIC DERIVATIVES SUICIDAL INHIBITORS OF THE HIV PROLIFERATION 审中-公开
标题翻译：抗生素衍生物艾滋病毒增长的辅助抑制剂
公开(公告)号：WO9901470A3
公开(公告)日：1999-03-25
申请号：PCT/EP9803970
申请日：1998-06-29
申请人： ZAMBON SPA , INST NAT SANTE RECH MED , UNGHERI DOMENICO , PELLACINI FRANCO , ROMAGNANO STEFANO , KRAUS JEAN LOUIS , CHERMANN JEAN CLAUDE
发明人： UNGHERI DOMENICO , PELLACINI FRANCO , ROMAGNANO STEFANO , KRAUS JEAN-LOUIS , CHERMANN JEAN-CLAUDE
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , A61K38/05
CPC分类号： C07K5/0606 , A61K38/00 , Y02P20/55
摘要： Dipeptides of formula (I) wherein X is oxygen or a group SO2 and R is hydrogen or a protecting group, are suicidal inhibitors of HIV.
摘要翻译：其中X为氧或SO 2，R为氢或保护基的式（I）的二肽为HIV的自杀抑制剂。

36. 发明申请

WO9851665A3 NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：新型MACROCYCLIC化合物作为金属蛋白酶抑制剂
公开(公告)号：WO9851665A3
公开(公告)日：1999-03-25
申请号：PCT/US9809789
申请日：1998-05-14
申请人： DU PONT PHARM CO
发明人： XUE CHU-BIO , DECICCO CARL P , CHERNEY ROBERT J , ARNER ELIZABETH , DEGRADO WILLIAM F , DUAN JINGWU , HE XIAOHUA , JACOBSON IRINA CIPORA , MAGOLDA RONALD L , NELSON DAVID
IPC分类号： A61K31/395 , A61K31/422 , A61K31/427 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K38/00 , A61P1/02 , A61P1/14 , A61P7/02 , A61P7/04 , A61P19/02 , A61P21/00 , A61P25/32 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/18 , A61P37/06 , A61P43/00 , C07D245/02 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , C07D498/08 , C07D521/00 , C07K5/06 , C07K5/065 , C07K5/078 , C12Q1/37
CPC分类号： C07D231/12 , A61K38/00 , C07D233/56 , C07D245/02 , C07D249/08 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/12 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C12Q1/37
摘要： This invention relates to macrocyclic molecules of formula (I) which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases. A novel enzymatic assay was developed to detect potential inhibitors of aggrecanase. The assay uses active aggrecanase accumulated in media from stimulated bovine nasal cartilage (BNC) or related cartilage sources and purified cartilage aggrecan monomer or a fragment thereof as a substrate.
摘要翻译：本发明涉及抑制金属蛋白酶（包括聚蛋白聚糖蛋白聚糖酶）和肿瘤坏死因子（TNF）产生的式（I）的大环分子。本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗炎性疾病的方法。开发了一种新的酶测定法来检测聚集蛋白聚糖蛋白聚糖酶的潜在抑制剂。该测定使用积聚在来自刺激的牛鼻软骨（BNC）或相关软骨来源的培养基中的活性聚集蛋白聚糖蛋白酶，并且将纯化的软骨聚集蛋白聚糖单体或其片段作为底物。

37. 发明申请

WO98053818A1 SULFONAMIDES AS CELL ADHESION INHIBITORS 审中-公开
标题翻译：磺酰胺作为细胞粘附抑制剂
公开(公告)号：WO98053818A1
公开(公告)日：1998-12-03
申请号：PCT/US1998/010952
申请日：1998-05-29
IPC分类号： A61K38/00 , A61K31/18 , A61K38/05 , A61P1/00 , A61P9/10 , A61P11/06 , A61P29/00 , A61P37/02 , A61P43/00 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/078 , A61K31/42 , A61K31/415 , A61K31/425 , A61K31/505 , C07C255/03 , C07D207/08 , C07D217/18 , C07D231/04 , C07D263/04 , C07D277/04 , C07D285/12 , C07D295/023 , C07D413/10 , C07D417/10
CPC分类号： C07K5/06191 , A61K38/05 , C07K5/06026 , C07K5/06034 , C07K5/06052 , C07K5/06078 , C07K5/06113 , C07K5/06139
摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha 4- beta 7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
摘要翻译：式（I）化合物是VLA-4和/或α4-β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化和其它炎性和自身免疫性疾病。

38. 发明申请

WO98047876A1 HETEROCYCLIC DERIVATIVES AND THEIR USE AS ANTITHROMBOTIC AGENTS 审中-公开
标题翻译：杂环衍生物及其作为抗菌药物使用
公开(公告)号：WO98047876A1
公开(公告)日：1998-10-29
申请号：PCT/EP1998/002455
申请日：1998-04-21
IPC分类号： A61K31/38 , A61K31/4355 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/5355 , A61K38/00 , A61P7/02 , C07D217/22 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/072 , C07K5/078
CPC分类号： C07D401/06 , A61K38/00 , C07D217/22 , C07D401/12 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04 , C07K5/06026 , C07K5/06078 , C07K5/06113 , C07K5/06139
摘要： The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X' being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.
摘要翻译：本发明涉及包含具有式（I）的基团Q，Q的抗血栓形成化合物，其中亚结构（i）是选自（a，b和c）的结构，其中X是O或S; X'独立地为CH或N; m为0,1,2或3; 其中基团Q通过氧原子或任选取代的氮或碳原子，或其药学上可接受的盐或其前药结合。本发明的化合物是治疗活性的，特别是抗血栓形成剂。

39. 发明申请

WO9718207A3 NOVEL MACROCYCLIC COMPOUNDS AS METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：新型MACROCYCLIC化合物作为金属蛋白酶抑制剂
公开(公告)号：WO9718207A3
公开(公告)日：1997-07-24
申请号：PCT/US9618382
申请日：1996-11-13
申请人： DU PONT MERCK PHARMA
发明人： XUE CHU-BIAO , CHERNEY ROBERT JOSEPH , DECICCO CARL PETER , DEGRADO WILLIAM FRANK , HE XIAOHUA , HODGE CARL NICOLAS , JACOBSON IRINA CIPORA , MAGOLDA RONALD LOUIS , ARNER ELIZABETH CATHERINE , DUAN JINGWU , NELSON DAVID J
IPC分类号： C12Q1/37 , A61K31/00 , A61K31/395 , A61K31/40 , A61K31/407 , A61K31/415 , A61K31/416 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K38/00 , A61K49/00 , A61P29/00 , C07D245/02 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D291/08 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D419/12 , C07D498/08 , C07D521/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/078 , A61K38/05 , C07D273/08
CPC分类号： C07D231/12 , A61K38/00 , C07D233/56 , C07D245/02 , C07D249/08 , C07D255/02 , C07D267/00 , C07D273/02 , C07D291/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D419/12 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.

40. 发明申请

WO9616982A2 ULTRASELECTIVE OPIOIDMIMETIC PEPTIDES AND PHARMACOLOGICAL AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译：超吸收性OPIOIDMIMETIC PEPTIDES及其药理和治疗用途
公开(公告)号：WO9616982A2
公开(公告)日：1996-06-06
申请号：PCT/US9515510
申请日：1995-11-30
申请人： US HEALTH , LAZARUS LAWRENCE H , SALVADORI SEV , TEMUSSI PIERO ANDREA
发明人： LAZARUS LAWRENCE H , SALVADORI SEVERO , TEMUSSI PIERO ANDREA
IPC分类号： A61K38/00 , C07K5/065 , C07K5/087 , C07K5/12 , C07K14/70 , A61K38/05 , A61K38/06
CPC分类号： C07K14/70 , A61K38/00 , C07K5/06078 , C07K5/0812 , C07K5/12
摘要： Novel opioidmimetic dipeptides, tripeptides and cyclic peptides exhibit enhanced affinity and selectivity for delta opioid receptors. The peptides are represented by the formulae L/D-Dmt-L-/D-Tic-R', L/D-R"-Dmt-L/D-Tic-R'; L/D-Dmt-L-/D-Tic-R-R'; L/D-R"-Dmt-L/D-Tic-R-R'; and cyclic (L/D-Dmt-L/D-Tic) wherein Dmt is 2',6',-dimethyl-L/D-tyrosine, Tic is L-/D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, R is a natural or unusual aliphatic amino residue, R' is a functional group at the carboxyl terminus of the peptide and R" is a functional group at the amino terminus of the pept ide. Pharmacological and therapeutic and compositions are also provided.
摘要翻译：新型阿片样物质二肽，三肽和环肽显示增强的Δ阿片受体的亲和力和选择性。肽由L / D-Dmt-L / D-Tic-R'，L / DR“-Dmt-L / D-Tic-R'，L / D-Dmt-L- Tic-R-R'; L / DR“-Dmt-L / D-Tic-R-R'; 和其中Dmt为2'，6'， - 二甲基-L / D-酪氨酸的环状（L / D-Dmt-L / D-Tic），Tic为L- / D-1,2,3,4-四氢异喹啉 - 3-羧酸，R是天然或不寻常的脂族氨基残基，R'是肽的羧基末端的官能团，R“是肽的氨基末端的官能团。药理学和治疗学和组成是也提供。

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