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1. 发明申请

WO1995000146A1 AMINO BI- AND TRI-CARBOCYCLIC ALKANE BIS-ARYL SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译：氨基双 - 和三 - 碳环烷烃双 - 亚芳基磺酰基合成酶抑制剂
公开(公告)号：WO1995000146A1
公开(公告)日：1995-01-05
申请号：PCT/US1994007030
申请日：1994-06-23
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , MORRIS, Robert, L. , NEUENSCHWANDER, Kent, W. , LEARN, Keith, S. , SCOTESE, Anthony, C.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： A61K31/42
CPC分类号： C07D263/57
摘要： This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further 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：本发明涉及一类具有双芳基取代的新型氨基双 - 和三 - 碳环烷烃化合物，其表现出角鲨烯合酶抑制性质。双 - 和三 - 碳环烷烃环包含一个氨基，并且该环进一步连接或桥连至两个单环和/或双环。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。

2. 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。

3. 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.

4. 发明申请

WO2011034832A1 SUBSTITUTED PHENOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF 审中-公开
标题翻译：取代的羟基甲基二氢氧杂环糊精，其制备和使用
公开(公告)号：WO2011034832A1
公开(公告)日：2011-03-24
申请号：PCT/US2010/048697
申请日：2010-09-14
申请人： SANOFI-AVENTIS , KOSLEY, Raymond Walter, Jr. , SHER, Rosy , NEUENSCHWANDER, Kent W. , GURUNIAN, Vieroslava
发明人： KOSLEY, Raymond Walter, Jr. , SHER, Rosy , NEUENSCHWANDER, Kent W. , GURUNIAN, Vieroslava
IPC分类号： C07D498/04 , A61K31/519 , A61K31/522 , A61P25/00
CPC分类号： C07D498/04
摘要： The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
摘要翻译：本发明涉及本文定义的一系列式（I）的取代的苯氧基甲基二氢恶唑啉嘧啶酮。本发明还涉及制备这些化合物的方法，包括新型中间体。本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。因此，本发明的化合物可用作药剂，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，认知缺陷障碍，惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐。

5. 发明申请

WO2009007015A1 MALONAMIDE DERIVATIVES WITH ANTITHROMBOTIC ACTIVITY 审中-公开
标题翻译：具有抗血栓活性的马来酰胺衍生物
公开(公告)号：WO2009007015A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/005187
申请日：2008-06-26
申请人： SANOFI-AVENTIS , STEINHAGEN, Henning , SZILLAT, Hauke , FOLLMANN, Markus , KIRSCH, Reinhard , WEHNER, Volkmar , MATTER, Hans , LORENZ, Martin , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
发明人： STEINHAGEN, Henning , SZILLAT, Hauke , FOLLMANN, Markus , KIRSCH, Reinhard , WEHNER, Volkmar , MATTER, Hans , LORENZ, Martin , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
IPC分类号： C07D213/30 , C07D213/80 , C07C15/00 , C07D211/42 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12 , A61K31/44 , A61P7/00
CPC分类号： C07D213/80 , C07C257/18 , C07C311/08 , C07C311/46 , C07C317/22 , C07C317/32 , C07C2601/14 , C07D211/42 , C07D213/30 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds of the formula (I). The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIla and can in general be applied in conditions in which an undesired activity of factor VIla is present or for the cure or prevention of which an inhibition of factor VIla is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式（I）化合物。式（I）的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶的抑制剂，特别是因子VIla，并且通常可用于其中存在不需要的因子VIla的活性或用于治疗或预防因子VIla的抑制的病症。本发明还涉及式（I）化合物的制备方法，其用途，特别是药物中的活性成分，以及包含它们的药物制剂。

6. 发明申请

WO1997024117A1 SUBSTITUTED (ARYL, HETEROARYL, ARYLMETHYL OR HETEROARYLMETHYL) HYDROXAMIC ACID COMPOUNDS 审中-公开
标题翻译：取代（芳基，杂芳基，芳基甲基或甲氧基）乙氧基化合物
公开(公告)号：WO1997024117A1
公开(公告)日：1997-07-10
申请号：PCT/US1997000264
申请日：1997-01-02
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , GRONEBERG, Robert, D. , NEUENSCHWANDER, Kent, W. , DJURIC, Stevan, W. , MCGEEHAN, Gerard, M. , BURNS, Christopher, J. , CONDON, Steven, M. , MORRISSETTE, Matthew, M. , SALVINO, Joseph, M. , SCOTESE, Anthony, C. , ULLRICH, John, W.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： A61K31/19
CPC分类号： C07D209/48 , C07C259/06 , C07C317/44 , C07C323/60 , C07C2601/08 , C07D215/14 , C07D317/56 , C07D317/62
摘要： This invention is directed to compounds of formula (I), wherein the variables are as described herein. Compounds within the scope of the present invention possess useful properties, more particularly pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. Compounds within the scope of the present invention may also inhibit an MMP, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting MMPs, such disease states involve tissue breakdown and those associated with a physiologically detrimental excess of TNF. The present invention is therefore also directed to the pharmaceutical use of the compounds, pharmaceutical compositions containing the compounds, intermediates leading thereto and methods for the preparation of the compounds and their intermediates.
摘要翻译：本发明涉及式（I）的化合物，其中变量如本文所述。本发明范围内的化合物具有有用的性质，更具体地说是药物性质。它们特别可用于抑制TNF治疗患有与生理有害过量的肿瘤坏死因子（TNF）相关的疾病状态的患者的生产或生理作用。本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。本发明范围内的化合物还可以抑制MMP，并且可用于治疗与通过抑制MMP调节的病理状况相关的疾病状态，这种疾病状态涉及组织分解以及与生理上有害的过量TNF相关的疾病状态。因此，本发明还涉及化合物的药物用途，含有这些化合物的药物组合物，导致其的中间体以及制备化合物及其中间体的方法。

7. 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。

8. 发明申请

WO1995031458A1 3-HYDROXYQUINUCLIDIN-3-YLPHENYLQUINOLINES AS SQUALENE SYNTHASE INHIBITORS 审中-公开
标题翻译： 3-羟基喹啉-3-基苯乙烯醇作为平均合成酶抑制剂
公开(公告)号：WO1995031458A1
公开(公告)日：1995-11-23
申请号：PCT/US1994005451
申请日：1994-05-12
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , NEUENSCHWANDER, Kent, W. , GRONEBERG, Robert, D. , MORRIS, Robert, L. , SCOTESE, Anthony, C. , MAGUIRE, Martin, P.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： This invention relates to a class of novel compounds useful in the treatment of diseases associated with undesirable cholesterol levels in the body, and particularly diseases of the cardiovascular system, such as atherosclerosis. The compounds of this invention are novel quinolinyl phenyl 3-hydroxyquinuclidines which may be linked directly or through a chain linking the quinolinyl to the phenyl and/or the phenyl to the quinuclidine. Compounds of this invention exhibit squalene synthase inhibition properties and reduce levels of serum cholesterol without significantly reducing mevalonic metabolite synthesis and thus provide a therapeutic agent having fewer side effects than agents which act by inhibiting the HMG-CoA reductase enzyme. Compounds of the present invention may also be useful in treating fungal infections. This invention further relates to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
摘要翻译：本发明涉及一类可用于治疗与身体不良胆固醇水平有关的疾病，特别是心血管系统疾病如动脉粥样硬化的新型化合物。本发明的化合物是可以直接或通过将喹啉基与苯基和/或苯基连接到奎宁环的链连接的新的喹啉基苯基3-羟基奎宁子。本发明的化合物显示出角鲨烯合成酶抑制性质并降低血清胆固醇水平，而不显着降低甲羟戊酸代谢物的合成，从而提供与通过抑制HMG-CoA还原酶起作用的药物相比具有较少副作用的治疗剂。本发明的化合物也可用于治疗真菌感染。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。

9. 发明申请

WO1994014435A1 CYCLOALKYL AMINE BIS-ARYL SQUALENE SYNTHASE INHIBITORS 审中-公开
公开(公告)号：WO1994014435A1
公开(公告)日：1994-07-07
申请号：PCT/US1993012638
申请日：1993-12-29
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , ULLRICH, John, W. , KIESOW, Terence, J. , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C. , LEARN, Keith, S. , DANKULICH, William, P.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： A61K31/42
CPC分类号： C07D263/57 , C07C217/52 , C07C2601/14 , C07D215/14 , C07D277/66 , C07D307/80
摘要： This invention relates to a class of novel polycyclic compounds containing a cycloalkyl ring having substituted thereon a primary amine and which is further linked or bridged to two mono- and/or bicyclic rings and which reduces 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多环化合物，其含有在其上被伯胺取代的环烷基环，并且其进一步连接或桥连至两个单环和/或双环，并且其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。

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