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1. 发明授权

US5506262A Cholesterol lowering compounds 失效
标题翻译：胆固醇降低化合物
公开(公告)号：US5506262A
公开(公告)日：1996-04-09
申请号：US146100
申请日：1993-11-10
申请人： Robert M. Burk , William H. Parsons , John J. Acton, III , Gregory D. Berger , Tesfaye Biftu , Robert L. Bugianesi , Yuan-Ching P. Chiang , Claude Dufresne , Narindar N. Girotra , Robert W. Marquis, Jr. , Chan-Hwa Kuo , Sandra P. Plevyak , Mitree M. Ponpipom , Lori L. Whiting , James D. Bergstrom , Conrad Santini
发明人： Robert M. Burk , William H. Parsons , John J. Acton, III , Gregory D. Berger , Tesfaye Biftu , Robert L. Bugianesi , Yuan-Ching P. Chiang , Claude Dufresne , Narindar N. Girotra , Robert W. Marquis, Jr. , Chan-Hwa Kuo , Sandra P. Plevyak , Mitree M. Ponpipom , Lori L. Whiting , James D. Bergstrom , Conrad Santini
IPC分类号： C07D493/08 , C07H19/01 , A61K31/335 , A61K31/365 , C07D319/04 , C07D405/06
CPC分类号： C07D493/08 , C07H19/01
摘要： Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.
摘要翻译： PCT No.PCT / US92 / 03941 Sec。 371日期：1993年11月10日 102（e）日期1993年11月10日PCT提交1992年5月8日PCT公布。 WO92 / 20336 PCT公开号日期：1992年11月26日。在此公开的是可用作降胆固醇剂的结构式（I）化合物。这些化合物还可用作角鲨烯合成酶抑制剂，真菌生长抑制剂，法呢基蛋白转移酶抑制剂和致癌基因蛋白Ras的法呢基化。这些化合物也可用于治疗癌症。

2. 发明授权

US5369125A Cholesterol-lowering agents 失效
标题翻译：降胆固醇剂
公开(公告)号：US5369125A
公开(公告)日：1994-11-29
申请号：US033913
申请日：1993-03-19
申请人： Gregory D. Berger , James D. Bergstrom , Tesfaye Biftu , Robert L. Bugianesi , Robert M. Burk , Narindar N. Girotra , C. H. Kuo , William H. Parsons , Mitree M. Ponpipom , Lori L. Whiting
发明人： Gregory D. Berger , James D. Bergstrom , Tesfaye Biftu , Robert L. Bugianesi , Robert M. Burk , Narindar N. Girotra , C. H. Kuo , William H. Parsons , Mitree M. Ponpipom , Lori L. Whiting
IPC分类号： C07D493/08 , A61K31/335 , C07D319/04
CPC分类号： C07D493/08
摘要： This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
摘要翻译：本发明涉及结构式（I）的化合物：作为角鲨烯合酶抑制剂，因此可用作胆固醇降低剂和抗真菌剂。这些化合物也是法呢基蛋白转移酶的抑制剂和致癌基因蛋白Ras的法呢基化，因此可用于治疗癌症。

3. 发明授权

US4996203A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US4996203A
公开(公告)日：1991-02-26
申请号：US362915
申请日：1989-06-08
申请人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
发明人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
IPC分类号： A61K31/34 , A61K31/341 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/54 , A61P1/04 , A61P9/00 , A61P9/02 , A61P11/08 , A61P13/02 , A61P15/00 , A61P29/00 , A61P37/08 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/18 , C07D307/20 , C07D307/42 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/10 , C07D417/04 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/18 , C07D307/20 , C07D307/42 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/04 , C07D417/12
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.
摘要翻译：本发明涉及式（I）的具体取代的四氢呋喃其中R 4是烷硫基，烷基亚磺酰基或烷基磺酰基基团，并且3,4或5位的至少一个取代基含有杂环，杂芳基或取代的苯硫基部分。

4. 发明授权

US5114961A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US5114961A
公开(公告)日：1992-05-19
申请号：US624449
申请日：1990-12-10
申请人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
发明人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
IPC分类号： C07D307/12 , C07D405/12 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D307/12 , C07D405/12 , C07D417/12
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3, 4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.
摘要翻译：本发明涉及具体取代的式（I）的四氢呋喃，其中R 4是烷硫基，烷基亚磺酰基或烷基磺酰基基团，并且在3,4或5位上的至少一个取代基含有杂环，杂芳基或取代的苯硫基部分。

5. 发明授权

US5010100A Certain 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译：某些2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US5010100A
公开(公告)日：1991-04-23
申请号：US362919
申请日：1989-06-08
申请人： Tesfaye Biftu , John C. Chabala , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo
发明人： Tesfaye Biftu , John C. Chabala , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo
IPC分类号： C07C45/00 , C07C45/72 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/18 , C07D307/20 , C07D307/24 , C07D307/34 , C07D307/42 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/14 , C07D417/04
CPC分类号： C07D307/18 , C07C45/00 , C07C45/72 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/20 , C07D307/24 , C07D307/34 , C07D307/42 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/14 , C07D417/04
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group and R.sup.6 is an alkoxy or a substituted alkoxy or alkyl group.
摘要翻译：本发明涉及式（I）的具体取代的四氢呋喃其中R 4是烷硫基，烷基亚磺酰基或烷基磺酰基，Y是烷基或取代的烷基，R 6是烷氧基或取代的烷氧基或烷基。

6. 发明授权

US5001123A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
公开(公告)号：US5001123A
公开(公告)日：1991-03-19
申请号：US362907
申请日：1989-06-08
申请人： Tesfaye Biftu , Nirindar N. Girotra , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
发明人： Tesfaye Biftu , Nirindar N. Girotra , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
IPC分类号： A61K31/44 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/54 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D405/04 , C07D405/14 , C07D417/14 , C07D521/00 , C07F9/6558
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D405/04 , C07D405/14 , C07F9/65586
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein Ar is a pyridyl, a dimethoxy-pyridyl or dimethoxy-pyrazyl group, R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio group.

7. 发明授权

US4761404A Phospholipid analogs useful as PAF synthesis inhibitors 失效
标题翻译：磷脂类似物可用作PAF合成抑制剂
公开(公告)号：US4761404A
公开(公告)日：1988-08-02
申请号：US750435
申请日：1985-07-01
申请人： Robert L. Bugianesi , Mitree M. Ponpipom , Kathleen M. Rupprecht
发明人： Robert L. Bugianesi , Mitree M. Ponpipom , Kathleen M. Rupprecht
IPC分类号： C07D521/00 , A61K31/10 , A61K31/13 , A61K31/16 , A61K31/17 , A61K31/27 , A61K31/275 , A61K31/33 , A61K31/445 , A61K31/575 , A61K31/655 , A61K31/66 , A61K31/675 , A61K31/685 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/29 , C07C49/255 , C07C67/00 , C07C313/00 , C07C317/18 , C07C317/44 , C07C325/00 , C07C381/00 , C07F9/09 , C07F9/10 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/6533 , C07J9/00
CPC分类号： C07F9/6533 , C07C45/292 , C07C49/255 , C07F9/091 , C07F9/10 , C07F9/5722 , C07F9/581
摘要： There are disclosed phospholipid analogs which are useful as PAF synthesis inhibitors. These compounds inhibit PAF (platelet-activating factor) biosynthesis and are thereby useful in the treatment of various diseases or disorders mediated by the PAF such as, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, and adult respiratory distress syndrome.
摘要翻译：公开了可用作PAF合成抑制剂的磷脂类似物。这些化合物抑制PAF（血小板活化因子）生物合成，从而可用于治疗由PAF介导的各种疾病或病症，例如疼痛，发烧，炎症，心血管疾病，哮喘，肺水肿，过敏性疾病，皮肤病，牛皮癣和成人呼吸窘迫综合征。

8. 发明授权

US4554349A Aralkyl and aralkenyl glycosides as inhibitors of antigen-specific T-cell proliferation 失效
标题翻译：芳烷基和芳烯基糖苷作为抗原特异性T细胞增殖的抑制剂
公开(公告)号：US4554349A
公开(公告)日：1985-11-19
申请号：US540594
申请日：1983-10-11
申请人： Mitree M. Ponpipom , Tsung-Ying Shen , Robert L. Bugianesi
发明人： Mitree M. Ponpipom , Tsung-Ying Shen , Robert L. Bugianesi
IPC分类号： C07H15/18 , C07H5/06
CPC分类号： C07H15/18
摘要： The invention disclosed herein relates to novel 1-deoxyglycosides, preferably 1-deoxy-D-mannopyranosides and 1-deoxy-L-rhamnopyranosides, having in the 1-position of the pyranose ring an aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy or aralkanoylamino/aralkenoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxyglycosides starting with the corresponding tetra-O-acetylglycopyranosyl bromide or amine. The 6-hydroxy group of 1-substituted-1 deoxyglycopyranosides can also be replaced by other functional groups. These aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy and aralkanoylamino/aralkenoylamino 1-deoxyglycosides are potent inhibitors of antigen-specific T-cell proliferation and are also useful as inhibitors of delayed-type hypersensitivity reactions.
摘要翻译：本文公开的本发明涉及新的1-脱氧糖苷，优选1-脱氧-D-甘露吡喃糖苷和1-脱氧-L-鼠李糖吡喃糖苷，其在吡喃糖环的1-位具有芳烷硫基/芳烯基硫基，芳烷氧基/芳烯基氧基或芳烷酰氨基/芳烯基酰氨基取代基; 以及由相应的四-O-乙酰基吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧糖苷的新方法。 1-取代-1脱氧吡喃糖苷的6-羟基也可以被其它官能团取代。这些芳烷硫基/芳烯基硫基，芳烷氧基/芳烯基氧基和芳烷酰氨基/芳烯酰氨基-1-脱氧糖苷是抗原特异性T细胞增殖的有效抑制剂，也可用作延迟型超敏反应的抑制剂。

9. 发明授权

US4228274A 1-Substituted glycopyranosides 失效
标题翻译： 1-取代的吡喃糖苷
公开(公告)号：US4228274A
公开(公告)日：1980-10-14
申请号：US922897
申请日：1978-07-10
申请人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
发明人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
IPC分类号： C07H13/04 , C07H15/04 , C07H15/14 , C07H5/06 , C07H5/08
CPC分类号： C07H13/04 , C07H15/04 , C07H15/14
摘要： The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.
摘要翻译：本文公开的本发明涉及在吡喃糖苷环的1位具有ω-氨基烷硫基，ω-氨基烷氧基或ω-氨基烷酰基氨基取代基的1-脱氧-D-甘露吡喃糖苷类的新型1-脱氧-D-吡喃甘露糖苷，以及由相应的四-O-乙酰基 - 吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧 - 糖吡喃糖苷的新方法。这些ω-氨基（烷硫基，烷氧基或烷酰氨基）-1-脱氧 - 糖吡喃糖苷，特别是1 - [（6'-氨基己基）硫代或氧基] -1-脱氧-D-甘露吡喃糖苷类，具有胰岛素样活性。

10. 发明授权

US5756507A Antagonists of gonadotropin releasing hormone 失效
公开(公告)号：US5756507A
公开(公告)日：1998-05-26
申请号：US760851
申请日：1996-12-05
申请人： Mark Goulet , Lin Chu , Wallace T. Ashton , Michael H. Fisher , Matthew J. Wyvratt , Roy G. Smith , Robert L. Bugianesi , Mitree M. Ponpipom , Yi Tien Yang , Peter Lin
发明人： Mark Goulet , Lin Chu , Wallace T. Ashton , Michael H. Fisher , Matthew J. Wyvratt , Roy G. Smith , Robert L. Bugianesi , Mitree M. Ponpipom , Yi Tien Yang , Peter Lin
IPC分类号： C07D209/14 , C07D209/16 , A61K31/405 , A61K31/495 , C07D209/10 , C07D403/06
CPC分类号： C07D209/14 , C07D209/16
摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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