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1. 发明授权

US06903091B2 Biphenyl vasopressin agonists 失效
公开(公告)号：US06903091B2
公开(公告)日：2005-06-07
申请号：US10121156
申请日：2002-04-11
申请人： Amedeo A. Failli , Thomas J. Caggiano , Jay S. Shumsky , Eugene J. Trybulski , Kevin A. Memoli , John P. Dusza
发明人： Amedeo A. Failli , Thomas J. Caggiano , Jay S. Shumsky , Eugene J. Trybulski , Kevin A. Memoli , John P. Dusza
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/5517 , A61P5/02 , A61P13/00 , A61P13/02 , C07D243/10 , C07D243/38 , C07D401/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04 , A61P3/10
CPC分类号： C07D243/10 , C07D243/38 , C07D401/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04
摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

2. 发明授权

US07465722B2 Biphenyl vasopressin agonists 失效
标题翻译：联苯加压素激动剂
公开(公告)号：US07465722B2
公开(公告)日：2008-12-16
申请号：US11502982
申请日：2006-08-11
申请人： Amedeo A. Failli , John P. Dusza , Thomas J. Caggiano , Jay S. Shumsky , Kevin A. Memoli , Eugene J. Trybulski
发明人： Amedeo A. Failli , John P. Dusza , Thomas J. Caggiano , Jay S. Shumsky , Kevin A. Memoli , Eugene J. Trybulski
IPC分类号： C07D487/02 , A61K31/551
CPC分类号： C07D243/10 , C07D243/38 , C07D401/06 , C07D471/04 , C07D471/14 , C07D487/04 , C07D495/04
摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or(3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.
摘要翻译：式（I）或（II）的化合物：其中：Y是选自NR或 - （CH 2）n的部分; 其中R是氢或（C1-C6）低级烷基，n是1; （C1-C6）低级烷基，卤素，氰基，CF3，羟基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6） C 1 -C 6低级烷氧基羰基，羧基-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个氮原子的6元芳族（不饱和）杂环; 表示：（1）任选被一个或两个取代基取代的苯环，所述取代基独立地选自氢，（C 1 -C 6）低级烷基，卤素，氰基，CF 3，羟基，（C 1 -C 6）低级烷氧基或（C 1 -C 6）低级烷氧基羰基，羧基，-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，（C 1 -C 6）低级烷氧基或卤素取代的具有一个氮原子的5元芳族（不饱和）杂环; 或（3）具有一个氮原子，任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的6元芳族（不饱和）杂环; 表示任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个硫原子的5元芳族（不饱和）杂环; R1是下式的部分，R2，R3，R7，R8和R9独立地选自氢，（C1-C3）低级烷基，OCH3，卤素，CF3，-SCH3，OCF3，SCF3，或CN; 或其药学上可接受的盐或其前体药物形式。

3. 发明授权

US07329653B2 Cyclohexylphenyl vasopressin agonists 失效
标题翻译：环己基苯基加压素激动剂
公开(公告)号：US07329653B2
公开(公告)日：2008-02-12
申请号：US11403072
申请日：2006-04-11
申请人： Amedeo A. Failli , Jay S. Shumsky , Thomas J. Caggiano , John P. Dusza , Kevin A. Memoli
发明人： Amedeo A. Failli , Jay S. Shumsky , Thomas J. Caggiano , John P. Dusza , Kevin A. Memoli
IPC分类号： A61P13/00 , A61K31/55 , C07D487/00
CPC分类号： C07D471/04 , C07D243/14 , C07D471/14 , C07D487/04 , C07D495/04
摘要： The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
摘要翻译：本发明提供下列通式的化合物：其中Y是NR或 - （CH 2 CH 2）n。 R是H或烷基; “Z”表示任选取代的苯基或具有一个氮原子的6元芳环; “W”表示具有一个氮原子的任选取代的苯基或5元芳环; “X”表示具有一个硫原子的任选取代的5元芳环; 以及利用这些化合物诱导临时延迟排尿或治疗由加压素激动剂活性（包括尿崩症，夜间遗尿症，夜尿症，尿失禁或出血和凝血障碍）补救的病症的方法和药物组合物。

4. 发明授权

US06511974B1 Tricyclic vasopressin agonists 失效
标题翻译：三环加压素激动剂
公开(公告)号：US06511974B1
公开(公告)日：2003-01-28
申请号：US09122020
申请日：1998-07-24
申请人： John P. Dusza , Peter S. Chan , Jay D. Albright , Jehan F. Bagli , Amedeo A. Failli , Mark A. Ashwell , Albert J. Molinari , Thomas J. Caggiano , Eugene J. Trybulski
发明人： John P. Dusza , Peter S. Chan , Jay D. Albright , Jehan F. Bagli , Amedeo A. Failli , Mark A. Ashwell , Albert J. Molinari , Thomas J. Caggiano , Eugene J. Trybulski
IPC分类号： A61K3155
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D487/04
摘要： This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
摘要翻译：本发明涉及选自通式（I）的化合物或其药学上可接受的盐，酯或前体药物形式的新化合物：其中D，E和G是N或CH，其用作加压素激动剂并且可用于治疗疾病如尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍，以及不能暂时延迟排尿及其药物组合物和方法。

5. 发明授权

US06340687B1 Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents 失效
标题翻译：用作抗动脉粥样硬化剂的取代的四氢嘧啶-2（1H） - 硫酮HDL-C电梯
公开(公告)号：US06340687B1
公开(公告)日：2002-01-22
申请号：US09145895
申请日：1998-09-02
申请人： Amedeo A. Failli , Jay S. Shumsky , Kevin A. Memoli , Donald P. Strike
发明人： Amedeo A. Failli , Jay S. Shumsky , Kevin A. Memoli , Donald P. Strike
IPC分类号： C07D23940
CPC分类号： C07D239/10
摘要： Antiatherosclerotic agents are provided having the following structure: wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供具有以下结构的抗动脉粥样硬化剂：其中：R1是氢，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的链烯基，2-7个碳原子的炔基或苯基烷基 7-10个碳原子; 和R 2，R 3，R 4，R 5和R 6各自独立地为氢，卤素，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的烯基，2-7个碳原子的炔基 7-10个碳原子的芳烷基，1-6个碳原子的烷氧基，6-12个碳原子的芳氧基，7-12个碳原子的芳烷氧基，1-6个碳原子的氟烷氧基，三氟甲基，1-3个碳原子的烷硫基，1-3个碳原子的烷基磺酰基，-SCF 3，硝基，其中烷基氨基部分具有1-6个碳原子的烷基氨基，或每个烷基具有1-6个碳原子的二烷基氨基; 或其药学上可接受的盐。

6. 发明授权

US06235900B1 Tricyclic pyridine N-oxides vasopressin agonists 失效
标题翻译：三环吡啶N-氧化物加压素激动剂
公开(公告)号：US06235900B1
公开(公告)日：2001-05-22
申请号：US09494929
申请日：2000-02-01
申请人： Amedeo A. Failli , Jay S. Shumsky , Eugene J. Trybulski
发明人： Amedeo A. Failli , Jay S. Shumsky , Eugene J. Trybulski
IPC分类号： C07D22318
CPC分类号： C07D471/04
摘要： The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.
摘要翻译：本发明提供了以下通式的化合物：以及利用这些化合物诱导临时延迟排尿或治疗可由血管加压素激动剂活性（包括尿崩症，夜间遗尿）补救或缓解的病症的方法和药物组合物，夜尿症，尿失禁，出血和凝血障碍。

7. 发明授权

US06297234B1 Arylthiophene vasopressin agonists 失效
标题翻译：芳基噻吩加压素激动剂
公开(公告)号：US06297234B1
公开(公告)日：2001-10-02
申请号：US09495505
申请日：2000-02-01
申请人： Amedeo A. Failli , David K. Williams , Thomas J. Caggiano , Jay S. Shumsky , Mark A. Ashwell
发明人： Amedeo A. Failli , David K. Williams , Thomas J. Caggiano , Jay S. Shumsky , Mark A. Ashwell
IPC分类号： C07D40910
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of the general formula: wherein Y is a moiety selected independently, from NH or —(CH2)n— wherein n is 1; m is an integer from 1 to 2; and the moiety represents: (1) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is nitrogen, and B and C are CH), (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is carbon, B is nitrogen, and C is —CH—CH—), (3) a 6-membered aromatic (unsaturated) ring (wherein A is carbon, B is CH, and C is —CH—CH—); as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.
摘要翻译：本发明提供以下通式的化合物：其中Y是独立地选自NH或 - （CH 2）n - 其中n为1的部分; m为1〜2的整数; 并且该部分表示：（1）具有一个氮的5元芳族（不饱和的）杂环（其中A是氮，B和C是CH），（2）具有一个氮的6元芳族（不饱和的）杂环（其中A为碳，B为氮，C为-CH-CH-），（3）6元芳族（不饱和的）环（其中A为碳，B为CH，C为-CH-CH- ）; 以及利用这些化合物治疗可通过加压素激动剂活性（包括尿崩症，夜间遗尿症，夜尿症，尿失禁，出血和凝血障碍）或临时排尿延迟而加以补救或减轻的病症的方法和药物组合物。

8. 发明授权

US06268360B1 1H-pyrido[2,3-b][1,5]benzodiazipine vasopressin agonists 失效
标题翻译： 1H-吡啶并[2,3-b] [1,5]苯并二氮嗪加压素激动剂
公开(公告)号：US06268360B1
公开(公告)日：2001-07-31
申请号：US09698725
申请日：2000-10-27
申请人： Amedeo A. Failli , David K. Williams , Thomas J. Caggiano , Jay S. Shumsky , Mark A. Ashwell
发明人： Amedeo A. Failli , David K. Williams , Thomas J. Caggiano , Jay S. Shumsky , Mark A. Ashwell
IPC分类号： C07D40910
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of the general formula: wherein Y is a moiety selected independently, from NH or —(CH2)n— wherein n is 1; m is an integer from 1 to 2; and the moiety represents: (1) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is nitrogen, and B and C are CH), (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is carbon, B is nitrogen, and C is —CH—CH—), (3) a 6-membered aromatic (unsaturated) ring (wherein A is carbon, B is CH, and C is —CH—CH—); as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.
摘要翻译：本发明提供以下通式的化合物：其中Y是独立地选自NH或 - （CH 2）n - 其中n为1的部分; m为1〜2的整数; 并且该部分表示：（1）具有一个氮的5元芳族（不饱和的）杂环（其中A是氮，B和C是CH），（2）具有一个氮的6元芳族（不饱和的）杂环（其中A为碳，B为氮，C为-CH-CH-），（3）6元芳族（不饱和的）环（其中A为碳，B为CH，C为-CH-CH- ）; 以及利用这些化合物治疗可通过加压素激动剂活性（包括尿崩症，夜尿，夜尿，尿失禁，出血和凝血障碍）或临时排尿延迟而补救或缓解的病症的方法和药物组合物。

9. 发明授权

US06194407B1 Tricyclic pyrido vasopressin agonists 失效
标题翻译：三环吡啶加压素激动剂
公开(公告)号：US06194407B1
公开(公告)日：2001-02-27
申请号：US09122123
申请日：1998-07-24
申请人： Amedeo A. Failli , Jay S. Shumsky , Robert J. Steffan
发明人： Amedeo A. Failli , Jay S. Shumsky , Robert J. Steffan
IPC分类号： A61K31695
CPC分类号： C07D471/04 , A61K31/55 , A61K31/695
摘要： The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.
摘要翻译：本发明提供了下列通式的化合物：其中W是任选取代的O或NH，以及利用这些化合物治疗可通过加压素激动剂活性治疗或缓解的病症的方法和药物组合物，包括尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍，或临时延迟排尿。

10. 发明授权

US6090803A Tricyclic vasopressin agonists 失效
标题翻译：三环加压素激动剂
公开(公告)号：US6090803A
公开(公告)日：2000-07-18
申请号：US122118
申请日：1998-07-24
申请人： Amedeo A. Failli , Jay S. Shumsky , Robert J. Steffan
发明人： Amedeo A. Failli , Jay S. Shumsky , Robert J. Steffan
IPC分类号： A61P7/10 , C07D471/04 , A61K31/553 , C07D498/02
CPC分类号： C07D471/04
摘要： The present invention provides compounds of the general formula: ##STR1## wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.
摘要翻译：本发明提供了下列通式的化合物：其中W是任选取代的O或NH，以及利用这些化合物治疗可通过加压素激动剂活性治疗或缓解的病症的方法和药物组合物，包括尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍，或临时延迟排尿。

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