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1. 发明申请

WO1997048687A1 PROCESS FOR THE PREPARATION OF CHIRAL KETO-HETEROCYCLES OF BASIC AMINO ACIDS 审中-公开
标题翻译：制备基础氨基酸的手性杂环化合物的方法
公开(公告)号：WO1997048687A1
公开(公告)日：1997-12-24
申请号：PCT/US1997009496
申请日：1997-05-30
申请人： WARNER-LAMBERT COMPANY , BERRYMAN, Kent, Alan , DOHERTY, Annette, Marian , EDMUNDS, Jeremy, John , PLUMMER, Janet, Samartino
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D277/28
CPC分类号： C07D417/06 , C07D213/50 , C07D235/14 , C07D277/28 , C07D277/64 , C07D417/12
摘要： A process for the preparation of novel keto heterocycle derivatives of basic natural and unnatural amino acids which affords products of high enantiomeric excess where a metalated heterocycle is reacted with N,O-dialkyl amide of an amino acid containing arylsulphonamide protected side chain amine in high chemical and optical yield as well as the novel compounds obtained by the process.
摘要翻译：制备碱性天然和非天然氨基酸的新型酮基杂环衍生物的方法，其提供高对映异构体过量的产物，其中金属化杂环与高度化学的含有芳基磺酰胺保护的侧链胺的氨基酸的N，O-二烷基酰胺反应和光学收率以及通过该方法获得的新型化合物。

2. 发明申请

WO1997008169A1 FURANONE ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译： FURANONE内皮素拮抗剂
公开(公告)号：WO1997008169A1
公开(公告)日：1997-03-06
申请号：PCT/US1996012431
申请日：1996-07-29
申请人： WARNER-LAMBERT COMPANY , CHENG, Xue-Min , DOHERTY, Annette, Marian , PATT, William, Chester , REPINE, Joseph, Thomas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D407/04
CPC分类号： C07D407/04 , C07D307/58
摘要： Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prostatic hyperplasia (BPH), and diabetes.
摘要翻译：描述了内皮素（I）的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗塞，心肌缺血，脑血管痉挛，脑缺血，脑梗塞，肝硬化，脓毒性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血性休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

3. 发明申请

WO1997048706A1 PYRROLO[1,2-A]PYRAZINE-1,4-DIONE SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：吡咯并[1,2-A]吡嗪-1,4-二酮丝氨酸蛋白酶抑制剂
公开(公告)号：WO1997048706A1
公开(公告)日：1997-12-24
申请号：PCT/US1997009832
申请日：1997-06-10
申请人： WARNER-LAMBERT COMPANY , BERRYMAN, Kent, Alan , DOHERTY, Annette, Marian , EDMUNDS, Jeremy, John , SIDDIQUI, M., Arshad
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to pyrrolo[1,2-a]pyrazine-1,4-diones of general formula (I), wherein B is carbonyl or methylene, R , R , R , and R are hydrogen, alkyl, or substituted alkyl, A is a basic group, and Q is hydrogen or a keto heterocycle group. The compounds are inhibitors of serine proteases, typically thrombin, Factor Xa, and Factor VIIa, and are useful for treating and preventing thrombotic disorders.
摘要翻译：本发明涉及通式（I）的吡咯并[1,2-a]吡嗪-1,4-二酮，其中B为羰基或亚甲基，R 2，R 4，R 5和R C 6是氢，烷基或取代的烷基，A是碱性基团，Q是氢或酮基杂环基。这些化合物是丝氨酸蛋白酶，通常是凝血酶，因子Xa和因子VIIa的抑制剂，并且可用于治疗和预防血栓形成障碍。

4. 发明申请

WO1997043307A1 COMPOUNDS INHIBITING THE ASSOCIATION OF THE PDGF RECEPTOR AND PHOSPHATIDYLINOSITOL 3-KINASE AND THEIR USE 审中-公开
标题翻译：化合物抑制PDGF受体和磷脂酰肌醇3激酶与其使用的关系
公开(公告)号：WO1997043307A1
公开(公告)日：1997-11-20
申请号：PCT/US1997006726
申请日：1997-04-21
申请人： WARNER-LAMBERT COMPANY , CODY, Wayne, Livingston , DOHERTY, Annette, Marian , EATON, Scott, R. , PANEK, Robert, Lee
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07K05/087
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827 , Y10S514/824 , Y10S514/825 , Y10S514/863
摘要： The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical compositions that contain a compound that inhibits the association of platelet-derived growth factor and phosphatidylinosital 3-kinase, and methods of treating cancer, restenosis, arthritis, dermatitis, atherosclerosis, vein graft intimal hyperplasia, neointimal hyperplasia of vascular smooth muscle and psoriasis using compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase.
摘要翻译：本发明提供抑制血小板衍生生长因子与磷脂酰肌醇3-激酶相关的化合物。本发明还提供了含有抑制血小板衍生生长因子和磷脂酰肌醇3-激酶的缔合的化合物的药物组合物，以及治疗癌症，再狭窄，关节炎，皮炎，动脉粥样硬化，静脉内膜内膜增生，血管新生内膜增生的方法使用抑制血小板衍生生长因子和磷脂酰肌醇3-激酶缔合的化合物的平滑肌和牛皮癣。

5. 发明申请

WO1997038983A1 IRREVERSIBLE INHIBITORS OF TYROSINE KINASES 审中-公开
标题翻译： TYROSINE KINASES的不可逆抑制剂
公开(公告)号：WO1997038983A1
公开(公告)日：1997-10-23
申请号：PCT/US1997005778
申请日：1997-04-08
申请人： WARNER-LAMBERT COMPANY , BRIDGES, Alexander, James , DENNY, William, Alexander , DOBRUSIN, Ellen, Myra , DOHERTY, Annette, Marian , FRY, David, W. , McNAMARA, Dennis, Joseph , SHOWALTER, Howard, Daniel, Hollis , SMAILL, Jeffrey, B. , ZHOU, Hairong
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D239/94
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D403/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07F9/6561
摘要： The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.
摘要翻译：本发明提供了酪氨酸激酶不可逆抑制剂的化合物。还提供了治疗癌症，再狭窄，动脉粥样硬化，子宫内膜异位症和牛皮癣的方法以及包含作为酪氨酸激酶不可逆抑制剂的化合物的药物组合物。

6. 发明申请

WO1997037985A1 NONPEPTIDE ENDOTHELIN ANTAGONISTS WITH INCREASED WATER SOLUBILITY 审中-公开
标题翻译：非特异性内皮素拮抗剂具有增加的水溶性
公开(公告)号：WO1997037985A1
公开(公告)日：1997-10-16
申请号：PCT/US1997003929
申请日：1997-03-12
申请人： WARNER-LAMBERT COMPANY , CHENG, Xue-Min , DOHERTY, Annette, Marian , PATT, William, Chester , REPINE, Joseph, Thomas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D307/60
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, male penile erectile dysfunction, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译：描述了内皮素（I）的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗动脉粥样硬化，再狭窄，雷诺氏现象，轻度或严重充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，男性阴茎勃起功能障碍，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，癌症恶性血管内皮瘤或前列腺癌，心肌梗死或缺血，急性或慢性肾功能衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素，败血症，出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生和内皮素水平升高。

7. 发明申请

WO1997000252A1 TRICYCLIC INHIBITORS OF PROTEIN FARNESYLTRANSFERASE 审中-公开
标题翻译：蛋白质蛋白酶的三聚体抑制剂
公开(公告)号：WO1997000252A1
公开(公告)日：1997-01-03
申请号：PCT/US1996008528
申请日：1996-06-04
申请人： WARNER-LAMBERT COMPANY , BOLTON, Gary, Louis , DOHERTY, Annette, Marian , KALTENBRONN, James, Stanley , QUIN, John, III , SCHOLTEN, Jeffrey, D. , SEBOLT-LEOPOLD, Judith , ZINNES, Harold
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Compounds of formula (I) wherein X is N or C-R , Y is N-R , CH2, O, S, SO, SO2, C=O or CH-OH, R is H or alkyl, R is heteroaryl, n is 1-5, and R -R are H or various substituents, are useful as inhibitors of protein farnesyltransferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.
摘要翻译：其中X是N或CR 9的式（I）化合物，Y是NR 10，CH 2，O，S，SO，SO 2，C = O或CH-OH，R是H或烷基，R 1 >为杂芳基，n为1-5，R 2 -R 10为H或各种取代基，可用作蛋白法呢基转移酶的抑制剂和用于治疗增殖性疾病，包括癌症，再狭窄和银屑病，以及作为抗病毒药物代理商。

8. 发明申请

WO1996037497A1 LOW MOLECULAR WEIGHT BICYCLIC-AREA TYPE THROMBIN INHIBITORS 审中-公开
标题翻译：低分子量双体型尿素型硫胺素抑制剂
公开(公告)号：WO1996037497A1
公开(公告)日：1996-11-28
申请号：PCT/CA1996000318
申请日：1996-05-22
申请人： BIOCHEM PHARMA INC. , DIMAIO, John , GILLARD, John, W. , SIDDIQUI, M., Arshad , BACHAND, Benoit , DOHERTY, Annette, Marian , EDMONDS, Jeremy, John
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： This invention relates to heterocyclic inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof having general formula (I), wherein X, R2, R3, R4, R6, R7 and R8 are as defined herein. Also, the invention relates to the use of such compounds and compositions as anticoagulants and as agents for the treatment and prophylaxis or thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction.
摘要翻译：本发明涉及酶凝血酶的杂环抑制剂及其制备方法及其具有通式（I）的药物组合物，其中X，R 2，R 3，R 4，R 6，R 7和R 8如本文所定义。此外，本发明涉及这样的化合物和组合物作为抗凝剂和作为治疗和预防或血栓形成疾病如静脉血栓形成，肺栓塞和动脉血栓形成的药剂的用途，导致急性缺血事件，例如心肌梗死或脑梗死。

9. 发明申请

WO1998027109A1 CYCLOALKYL INHIBITORS OF PROTEIN FARNESYLTRANSFERASE 审中-公开
标题翻译：蛋白质蛋白酶的环己基抑制剂
公开(公告)号：WO1998027109A1
公开(公告)日：1998-06-25
申请号：PCT/US1997023280
申请日：1997-12-16
申请人： WARNER-LAMBERT COMPANY , DOHERTY, Annette, Marian , KALTENBRONN, James, Stanley , LEONARD, Daniele, M. , MC NAMARA, Dennis, Joseph
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07K05/078
CPC分类号： C07K5/06147 , A61K38/00
摘要： Novel inhibitors of protein farnesyltransferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer, restenosis, atherosclerosis, psoriasis, and endometriosis.
摘要翻译：描述了蛋白质法呢基转移酶的新型抑制剂，以及其制备方法及其药物组合物，其可用于控制组织增生性疾病，包括癌症，再狭窄，动脉粥样硬化，牛皮癣和子宫内膜异位症。

10. 发明申请

WO1997044350A1 INHIBITORS OF PROTEIN FARNESYL TRANSFERASE 审中-公开
标题翻译：蛋白质转化酶抑制剂
公开(公告)号：WO1997044350A1
公开(公告)日：1997-11-27
申请号：PCT/US1997006591
申请日：1997-04-29
申请人： WARNER-LAMBERT COMPANY , DOBRUSIN, Ellen, M. , DOHERTY, Annette, Marian , KALTENBRONN, James, Stanley , LEONARD, Daniele, M. , MCNAMARA, Dennis, Joseph , SEBOLT-LEOPOLD, Judith , SHULER, Kevon, R.
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/06147
摘要： Novel inhibitors of protein farnesyl transferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating cancer, restenosis, psoriasis, endometriosis, atherosclerosis, or viral infections.
摘要翻译：描述了蛋白质法呢基转移酶的新型抑制剂，以及其制备方法及其药物组合物，其可用于治疗癌症，再狭窄，牛皮癣，子宫内膜异位，动脉粥样硬化或病毒感染。

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