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1. 发明授权

US06602864B1 Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds 失效
标题翻译：磺酸或磺酰氨基N-（杂芳烷基） - 杂环基酰胺化合物
公开(公告)号：US06602864B1
公开(公告)日：2003-08-05
申请号：US09090492
申请日：1998-06-03
申请人： Yong Mi Choi-Sledeski , Henry W. Pauls , Jeffrey N. Barton , William R. Ewing , Daniel M. Green , Michael R. Becker , Yong Gong
发明人： Yong Mi Choi-Sledeski , Henry W. Pauls , Jeffrey N. Barton , William R. Ewing , Daniel M. Green , Michael R. Becker , Yong Gong
IPC分类号： A61K3155
CPC分类号： C07D409/14 , A61K31/00 , A61K31/4184 , A61K31/4365 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/519 , A61K45/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
摘要翻译：本文所述的式I化合物表现出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。更具体地说，它们是因子Xa活性的抑制剂。本发明涉及式I化合物，其含有式I化合物的组合物及其用途，其用于治疗患有或经受生理条件的患者，其可通过施用活性抑制剂而改善因子Xa。

2. 发明授权

US5958918A Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-�(aminominomethyl)phenylalkyl!-azaheterocyclylamide compounds 失效
标题翻译：取代的（亚磺酸，磺酸，磺酰基氨基或亚磺酰基氨基）N - [（氨基甲基）苯基烷基] - 杂环基酰胺化合物
公开(公告)号：US5958918A
公开(公告)日：1999-09-28
申请号：US976034
申请日：1997-11-21
申请人： William R. Ewing , Michael R. Becker , Henry W. Pauls , Daniel L. Cheney , Jonathan Stephen Mason , Alfred P. Spada , Yong Mi Choi-Sledeski
发明人： William R. Ewing , Michael R. Becker , Henry W. Pauls , Daniel L. Cheney , Jonathan Stephen Mason , Alfred P. Spada , Yong Mi Choi-Sledeski
IPC分类号： C07D223/10 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/55 , A61P7/02 , A61P43/00 , C07D205/085 , C07D207/14 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D401/02 , A61K31/435
CPC分类号： C07D205/085 , C07D207/14 , C07D207/273 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14
摘要： The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
摘要翻译：式I的化合物显示出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。更特别地，它们是因子Xa的活性的抑制剂。本发明涉及式I化合物，其含有式I化合物的组合物及其用途，其用于治疗患有或经受生理条件的患者，其可通过施用活性抑制剂而改善因子Xa。

3. 发明授权

US06559313B2 Compounds having antihypertensive, cardioprotective anti-ischemic and antilipolytic properties 失效
标题翻译：具有抗高血压，心脏保护性抗缺血和抗脂解性质的化合物
公开(公告)号：US06559313B2
公开(公告)日：2003-05-06
申请号：US10104133
申请日：2002-03-22
申请人： Michael R. Myers , Martin P. Maguire , Alfred P. Spada , William R. Ewing , Henry W. Pauls , Yong Mi Choi-Sledeski
发明人： Michael R. Myers , Martin P. Maguire , Alfred P. Spada , William R. Ewing , Henry W. Pauls , Yong Mi Choi-Sledeski
IPC分类号： C07D47334
CPC分类号： C07H19/16 , C07D401/04 , C07D471/04 , C07D473/34
摘要： This invention is directed to intermediates of the formula wherein Z is 4-trifluoromethylpyridin-2-yl or 5-trifluoromethylpyridin-2-yl which are useful in the preparation of compounds useful as antihypertensive, anti-ischemic, cardioprotective, and antilipolytic agents.
摘要翻译：本发明涉及Z是4-三氟甲基吡啶-2-基或5-三氟甲基吡啶-2-基的中间体，其可用于制备可用作抗高血压，抗缺血，心脏保护和抗脂肪分解剂的化合物。

4. 发明授权

US06376472B1 Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties 失效
标题翻译：具有抗高血压，心脏保护作用，抗缺血性和抗脂解性的化合物
公开(公告)号：US06376472B1
公开(公告)日：2002-04-23
申请号：US09174191
申请日：1998-10-16
申请人： Michael R. Myers , Martin P. Maguire , Alfred P. Spada , William R. Ewing , Henry W. Pauls , Yong Mi Choi-Sledeski
发明人： Michael R. Myers , Martin P. Maguire , Alfred P. Spada , William R. Ewing , Henry W. Pauls , Yong Mi Choi-Sledeski
IPC分类号： C07D47334
CPC分类号： C07H19/16 , C07D401/04 , C07D471/04 , C07D473/34
摘要： A compound of the formula wherein K is N; Q is CH2 or O; R6 is hydrogen, alkyl, allyl, 2-methylallyl, 2-butenyl, or cycloalkyl where the nitrogen of the ring of X is substituted by Y; E is O or S; Y is hydrogen, alkyl, aralkyl, substituted aralkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, or substituted heterocyclylalkyl; and n and p are independently 0, 1, 2, or 3, provided that n+p is at least 1; T is hydrogen, alkyl, alkylcarbonyl, alkylthiocarbonyl, halo, carboxyl, A and B are independently hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR′; or a pharmaceutically acceptable salt thereof, a pharmaceutic-ally acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof.
摘要翻译：化合物K为N; Q是CH 2或O; R6是氢，烷基，烯丙基，2-甲基烯丙基，2-丁烯基或环烷基，X的环的氮被Y取代; E为O或S; Y是氢，烷基，芳烷基，取代的芳烷基，芳基，取代的芳基，杂环基，取代的杂环基，杂环基烷基或取代的杂环基烷基; n和p独立地为0,1,2或3，条件是n + p为至少1; T为氢，烷基，烷基羰基，烷硫基羰基，卤素，羧基，A和B独立地为氢，烷基，羟基烷基，烷氧基烷基或OR';或其药学上可接受的盐，其药学上可接受的前药，其N-氧化物，其水合物或其溶剂化物。

5. 发明授权

US5612353A Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds 失效
标题翻译：取代的（亚磺酸，磺酸，磺酰基氨基或亚磺酰氨基）N - [（氨基亚氨基甲基）苯基烷基] - 杂环酰胺化合物
公开(公告)号：US5612353A
公开(公告)日：1997-03-18
申请号：US481024
申请日：1995-06-07
申请人： William R. Ewing , Michael R. Becker , Henry W. Pauls , Daniel L. Cheney , Jonathan S. Mason , Alfred P. Spada
发明人： William R. Ewing , Michael R. Becker , Henry W. Pauls , Daniel L. Cheney , Jonathan S. Mason , Alfred P. Spada
IPC分类号： C07D223/10 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/55 , A61P7/02 , A61P43/00 , C07D205/085 , C07D207/14 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D401/02 , A61K31/435
CPC分类号： C07D207/273 , C07D205/085 , C07D207/14 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14
摘要： The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
摘要翻译：式I的化合物显示出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。更特别地，它们是因子Xa抑制剂。本发明涉及式I化合物，其含有式I化合物的组合物及其用途，其用于治疗患有或经受可通过施用因子Xa抑制剂而改善的病症的患者。

6. 发明授权

US5441946A Phosphonate derivatives of lipophilic amines 失效
标题翻译：亲脂胺的膦酸酯衍生物
公开(公告)号：US5441946A
公开(公告)日：1995-08-15
申请号：US227803
申请日：1994-04-14
申请人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
发明人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
IPC分类号： C07F9/38 , C07F9/40 , C07F9/653 , C07F9/6558 , A61K31/66 , C07F9/44
CPC分类号： C07F9/65583 , C07F9/3808 , C07F9/3873 , C07F9/4006 , C07F9/404 , C07F9/405 , C07F9/65324
摘要： This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. 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：本发明涉及一类表现出角鲨烯合酶抑制性质的亲脂胺的新型膦酸酯衍生物。更具体地，化合物是双芳基环烷基氨基和氮杂环烷基膦酸酯。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。

7. 发明授权

US4496456A Method for preparing thin regenerated cellulose membranes of high flux and selectivity for organic liquids separations 失效
标题翻译：制备高通量和有机液体分离选择性的薄再生纤维素膜的方法
公开(公告)号：US4496456A
公开(公告)日：1985-01-29
申请号：US500966
申请日：1983-06-03
申请人： Mahmoud M. Hafez , Henry W. Pauls
发明人： Mahmoud M. Hafez , Henry W. Pauls
IPC分类号： B01D67/00 , B01D71/10 , C10G73/08 , C10G73/12 , B01D13/00
CPC分类号： B01D67/0095 , B01D67/0011 , B01D71/10
摘要： A method is described for the production of regenerated cellulose membranes which method comprises the steps of:(a) dissolving a cellulose material to form a solution;(b) casting the cellulose solution into a film;(c) coagulating the cellulose solution film using an alkali alcoholic solution;(d) washing the coagulated cellulose film in an alcohol;(e) regenerating the cellulose film using acidic alcohol solution;(f) washing the regenerated cellulose membrane using an alcohol.The regenerated cellulose thus formed may be dried, if desired, preferably without a softener.The regenerated cellulose thus produced, when prepared in the form of a film or membrane, possesses higher flux and superior selectivity for organic liquid separation than regenerated cellulose membranes prepared employing aqueous solutions in steps b through e above and is most advantageously employed for the recovery of polar dewaxing solvents (e.g. ketones and mixed ketone/aromatic solvents) from dewaxed oil.
摘要翻译：描述了用于生产再生纤维素膜的方法，该方法包括以下步骤：（a）将纤维素材料溶解以形成溶液; （b）将纤维素溶液浇铸成膜; （c）使用碱醇溶液使纤维素溶液膜凝结; （d）在醇中洗涤凝固的纤维素膜; （e）使用酸性醇溶液再生纤维素膜; （f）使用酒精洗涤再生纤维素膜。如果需要，如此形成的再生纤维素可以被干燥，优选没有软化剂。因此制备的再生纤维素当以膜或膜的形式制备时，与使用上述步骤b至e中的水溶液制备的再生纤维素膜相比，具有更高的通量和对有机液体分离的优异选择性，并且最有利地用于回收来自脱蜡油的极性脱蜡溶剂（例如酮和混合酮/芳族溶剂）。

8. 发明授权

US5563128A Phosphonate derivatives of lipophilic amines 失效
公开(公告)号：US5563128A
公开(公告)日：1996-10-08
申请号：US435020
申请日：1995-05-04
申请人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
发明人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
IPC分类号： C07F9/38 , C07F9/40 , C07F9/653 , C07F9/6558 , A61K31/675 , A61K31/66
CPC分类号： C07F9/65583 , C07F9/3808 , C07F9/3873 , C07F9/4006 , C07F9/404 , C07F9/405 , C07F9/65324
摘要： This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. 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.

9. 发明授权

US5556990A Polyarylcarbamoylaza- and -carbamoylalkanedioic acids 失效
标题翻译：聚芳基氨基甲酰基氮杂 - 和 - 氨基甲酰基链烷二酸
公开(公告)号：US5556990A
公开(公告)日：1996-09-17
申请号：US357481
申请日：1994-12-16
申请人： Henry W. Pauls , Yong-Mi Choi , Robert W. Studt , Martin P. Maguire , Alfred P. Spada , Don D. Cha
发明人： Henry W. Pauls , Yong-Mi Choi , Robert W. Studt , Martin P. Maguire , Alfred P. Spada , Don D. Cha
IPC分类号： C07D277/68 , A61K31/27 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/451 , A61K31/47 , A61P9/10 , A61P43/00 , C07C233/22 , C07C235/06 , C07C235/08 , C07C235/14 , C07C235/16 , C07D211/42 , C07D211/70 , C07D241/04 , C07D263/56 , C07D263/57 , C07D265/30 , C07D277/70 , C07D277/82 , C07D401/10 , C07D405/10 , C07D413/10 , C07D413/12 , C07D207/04 , C07D211/14 , C07D223/02 , C07D403/08 , C07D417/06
CPC分类号： C07D263/57 , C07C233/22 , C07D211/42 , C07D211/70 , C07D241/04 , C07D401/10 , C07D405/10 , C07D413/10 , C07D413/12
摘要： This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. 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：本发明涉及一类表现出角鲨烯合酶抑制性质的亲脂性胺的新型二羧酰胺衍生物。更具体地，化合物是双芳基和/或杂芳基烷基或环烷基氨基二羧基酰胺。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。

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