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1. 发明申请

WO1993000357A1 THERAPEUTIC POLYPEPTIDES BASED ON VON WILLEBRAND FACTOR 审中-公开
标题翻译：基于VON WILLEBRAND因子的治疗性多糖
公开(公告)号：WO1993000357A1
公开(公告)日：1993-01-07
申请号：PCT/US1992005472
申请日：1992-06-29
申请人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC. , THE SCRIPPS RESEARCH INSTITUTE , CHANG, Michael, N. , MCGARRY, Daniel, G. , REGAN, John, R. , RUGGERI, Zaverio, M. , WARE, Jerry, L.
发明人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC. , THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07K03/08
CPC分类号： C07K14/755 , A61K38/00
摘要： A polypeptide patterned on a fragment of wild type mature von Willebrand factor (vWF) subunit having one or more binding sites of predetermined affinity for one or more of the ligands selected from the group consisting of collagen, glycosaminoglycans, proteoglycans, platelet glycoprotein Ib alpha , platelet glycoprotein IIb/IIIa, or coagulation factor VIII, said polypeptide having a modified amino acid sequence relative to that of said fragment and an increased binding affinity, relative to said predetermined affinity, for one or more of said ligands, including also such a polypeptide prepared by mutagenesis of a DNA sequence and patterned on wild type mature vWF subunit, and also a polypeptide in purified form patterned upon a parent polypeptide which comprises the wild type amino acid sequence of mature von Willebrand factor subunit, or a fragment thereof, and including also purified DNA sequences encoding such polypeptides, expression plasmids and viral expression vectors containing the DNA sequences, and therapeutic compositions comprising such polypeptides effective in the treatment of thrombosis, and methods for the use thereof, and also preparation of such polypeptides by mutagenesis of an encoding DNA sequence or covalent modification of wild type vWF.
摘要翻译：在野生型成熟血管性血友病因子（vWF）亚基的片段上图案化的多肽，其具有一种或多种预定亲和力的结合位点，所述结合位点选自胶原，糖胺聚糖，蛋白聚糖，血小板糖蛋白Ibα，血小板糖蛋白IIb / IIIa或凝血因子VIII，所述多肽相对于所述片段具有修饰的氨基酸序列，相对于所述预定亲和力，对于一种或多种所述配体，包括此类多肽通过DNA序列的诱变制备并在野生型成熟vWF亚基上图案化的多肽，以及在包含成熟血管性血友病因子亚基的野生型氨基酸序列或其片段的母体多肽图案化的纯化形式的多肽，并且包括还纯化编码这种多肽的DNA序列，表达质粒和含有的病毒表达载体 DNA序列和包含有效治疗血栓形成的这些多肽的治疗组合物，及其使用方法，以及通过编码DNA序列的突变或野生型vWF的共价修饰来制备这些多肽。

2. 发明申请

WO2009015067A3 GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 审中-公开
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：WO2009015067A3
公开(公告)日：2009-09-11
申请号：PCT/US2008070596
申请日：2008-07-21
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , KUZMICH DANIEL , REGAN JOHN R
发明人： KUZMICH DANIEL , REGAN JOHN R
IPC分类号： C07D209/10 , C07D209/42 , C07D211/04 , C07D215/06 , C07D215/227 , C07D215/233 , C07D217/04 , C07D217/24 , C07D231/12 , C07D235/06 , C07D295/13 , C07D307/79 , C07D471/04
CPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D209/42 , C07D215/06 , C07D215/18 , C07D215/48
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：其中R1，R2，R3，R4，R5，R6和R7如本文所定义的式（I）化合物或其互变异构体，前药，溶剂化物或盐; 含有这些化合物的药物组合物以及调节糖皮质激素受体功能的方法以及使用这些化合物治疗患者的糖皮质激素受体功能介导的疾病状态或病症或以炎症，变应原或增殖过程为特征的方法。

3. 发明申请

WO1992014692A1 ENANTIOSELECTIVE PREPARATION OF ACETYLENIC OR OLEFINIC SUBSTITUTED CYCLOALKENYL DIHYDROXYBUTYRATES AND 4-HYDROXY-TETRAHYDROPYRAN-2-ONES 审中-公开
标题翻译：乙酰基或烯丙基取代环己基二羟基丁酸酯和4-羟基四氢吡喃-2-酮的选择性制备
公开(公告)号：WO1992014692A1
公开(公告)日：1992-09-03
申请号：PCT/US1992001105
申请日：1992-02-11
申请人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC. , ULLRICH, John, W. , REGAN, John, R.
发明人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC.
IPC分类号： C07C43/184
CPC分类号： C07C49/753 , C07C45/58 , C07C49/657 , C07C49/697 , C07C49/747 , C07C69/732 , C07C69/738 , C07C205/45 , C07F7/081 , C07F7/1804
摘要： Disclosed are intermediates and a process of making an anticholesterolemic compound of formula (I), the corresponding ring-opened hydroxy acid derived therefrom or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了中间体和制备式（I）的抗胆固醇血型化合物，由其衍生的相应的开环羟基酸或其药学上可接受的盐的方法。

4. 发明申请

WO1992013542A1 APPLICATION OF BIOLOGICALLY ACTIVE POLYMERS TO OBTAIN A MEDICAMENT FOR THE TREATMENT OF RETROVIRUS INFECTIONS 审中-公开
标题翻译：生物活性聚合物应用于获得治疗逆转录病毒感染的药物
公开(公告)号：WO1992013542A1
公开(公告)日：1992-08-20
申请号：PCT/FR1992000079
申请日：1992-01-29
申请人： RHONE-POULENC RORER S.A. , BEN-SASSON, Schmuel , LEMAITRE, Marc , REGAN, John, R. , ZERIAL, Aurélio
发明人： RHONE-POULENC RORER S.A.
IPC分类号： A61K31/765
CPC分类号： A61K31/74 , A61K31/765 , A61K31/775
摘要： Application of biologically active aromatic polymers having an alkylaryl structure comprising from 5 to 50 repetitive aromatic units capable of forming a linear skeleton having a helical secondary structure in order to obtain a medicament used for the preventive and/or curative treatment of retrovirus infections.

5. 发明申请

WO1994027601A1 ALIPHATIC AMINO BIS-ARYL SQUALENE SYNTHASE INHIBITORS 审中-公开
公开(公告)号：WO1994027601A1
公开(公告)日：1994-12-08
申请号：PCT/US1994005283
申请日：1994-05-11
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , GRONEBERG, Robert, D. , REGAN, John, R. , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： A61K31/42
CPC分类号： C07D263/57 , C07C217/22 , C07C233/75 , C07C235/56 , C07D413/12
摘要： This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is furhter linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
摘要翻译：本发明涉及一类新的含有至少四个碳原子的脂族氨基双芳基化合物和在其上取代或并入其中的氨基，并且与两个单环和/或双环环交链或桥接。本发明化合物降低体内血清胆固醇水平，而不显着降低甲羟戊酸代谢物合成。本发明还涉及使用本发明化合物降低血清胆固醇水平的药物组合物和治疗方法。

6. 发明申请

WO1992020350A1 AROMATIC OLIGOMERIC COMPOUNDS USEFUL AS MIMICS OF BIOACTIVE MACROMOLECULES 审中-公开
标题翻译：芳香族低分子化合物作为生物活性分子的聚合物有用
公开(公告)号：WO1992020350A1
公开(公告)日：1992-11-26
申请号：PCT/US1992004274
申请日：1992-05-20
申请人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC. , REGAN, John, R. , MCGARRY, Daniel, G. , CHANG, Michael, N. , BARTON, Jeffrey, N. , NEWMAN, Jack , BEN-SASSON, Schmuel
发明人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC.
IPC分类号： A61K31/775
CPC分类号： C08G8/04 , A61K31/765
摘要： This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, or abnormal smooth muscle cell proliferation, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and their use in the treatment of such disorders.
摘要翻译：本发明涉及可用于治疗心血管，骨代谢，降血脂症，神经元，胃肠和弹性蛋白酶介导的结缔组织降解障碍和可由有效结合DNA的试剂或异常平滑肌细胞增殖的病症的芳族低聚物，制备这种低聚化合物的方法，包括这种低聚化合物的药物组合物，及其在治疗这些疾病中的用途。

7. 发明申请

WO1991007183A1 POLYMERS WITH ALKYL- OR HETEROALKYL-ARYL BACKBONE AND PHARMACEUTICAL COMPOSITIONS INCORPORATING SAME 审中-公开
标题翻译：聚合物与烷基或异丁基亚胺基反应物和药物组合物
公开(公告)号：WO1991007183A1
公开(公告)日：1991-05-30
申请号：PCT/US1990006847
申请日：1990-11-21
申请人： RORER INTERNATIONAL (OVERSEAS) INC. , CHANG, Michael, N. , REGAN, John, R.
发明人： RORER INTERNATIONAL (OVERSEAS) INC.
IPC分类号： A61K31/765
CPC分类号： A61K31/765 , C08G8/08 , C08G8/18 , C08G8/20
摘要： A biologically active polymeric compound comprising an alkylaryl or heteroalkylaryl backbone and from about 5 to about 50 repeating aromatic ring-containing units and which, according to the computer program marketed as SYBYL version 5.2 running on a DEC VAX 11/750 computer, is capable of forming a linear backbone having a helical secondary structure, and wherein the maximum diameter of the helical structure, as measured by the alkylaryl or heteroalkylaryl backbone, is less than 3 times greater than the maximum diameter of the aryl group of the alkylaryl or heteroalkylaryl backbone.
摘要翻译：包含烷基芳基或杂烷基芳基主链和约5至约50个含重复芳环的单元的生物活性聚合物，并且根据在DEC VAX 11/750计算机上运行的以SYBYL版本5.2销售的计算机程序，能够形成具有螺旋二级结构的线性主链，并且其中由烷基芳基或杂烷基芳基主链测量的螺旋结构的最大直径小于烷基芳基或杂烷基芳基主链的芳基的最大直径的3倍。

8. 发明申请

WO2009015067A2 GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 审中-公开
标题翻译：葡萄糖酸化物质，其制备方法，药物组合物及其用途
公开(公告)号：WO2009015067A2
公开(公告)日：2009-01-29
申请号：PCT/US2008/070596
申请日：2008-07-21
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , KUZMICH, Daniel , REGAN, John R.
发明人： KUZMICH, Daniel , REGAN, John R.
CPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D209/42 , C07D215/06 , C07D215/18 , C07D215/48
摘要： Compounds of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义的式（I）化合物或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

9. 发明申请

WO1991004736A1 SUBSTITUTED CYCLOHEXENE DERIVATIVES AS HMG-CoA REDUCTASE INHIBITORS 审中-公开
标题翻译：作为HMG-CoA还原酶抑制剂的替代环己酮衍生物
公开(公告)号：WO1991004736A1
公开(公告)日：1991-04-18
申请号：PCT/US1990005058
申请日：1990-09-07
申请人： RORER INTERNATIONAL (OVERSEAS) INC. , REGAN, John, R. , BRUNO, Joseph, G. , NEUENSCHWANDER, Kent, W.
发明人： RORER INTERNATIONAL (OVERSEAS) INC.
IPC分类号： A61K31/365
CPC分类号： C07D405/08 , C07C59/54 , C07C59/56 , C07C59/64 , C07D309/30 , C07D405/12 , C07D407/06 , C07D409/08 , Y10S514/824
摘要： Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by formula (I), and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.
摘要翻译：公开了用作由式（I）表示的抗高胆固醇血症药物的新型3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂及其衍生的相应的开环羟基酸及其药学上可接受的盐。还公开了含有所述化合物的药物组合物和抑制胆固醇生物合成的方法。

10. 发明申请

WO1989005639A1 NOVEL HMG-CoA REDUCTASE INHIBITORS 审中-公开
标题翻译：新型HMG-CoA还原抑制剂
公开(公告)号：WO1989005639A1
公开(公告)日：1989-06-29
申请号：PCT/US1988004572
申请日：1988-12-21
申请人： RORER INTERNATIONAL (OVERSEAS) INC. , NEUENSCHWANDER, Kent, W. , REGAN, John, R. , KOSMIDER, Benedict, J. , SCOTESE, Anthony, C.
发明人： RORER INTERNATIONAL (OVERSEAS) INC.
IPC分类号： A61K31/365
CPC分类号： C07C59/56 , C07C59/54 , C07C59/64 , C07D309/30
摘要： Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by formula (I) and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

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