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1. 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。

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

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.

4. 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。

5. 发明授权

US07223752B2 Biphenyl vasopressin agonists 失效
公开(公告)号：US07223752B2
公开(公告)日：2007-05-29
申请号：US10980939
申请日：2004-11-04
申请人： Amedeo Arturo Failli , John P. Dusza , Thomas Joseph Caggiano , Jay Scott Shumsky , Kevin A. Memoli , Eugene J. Trybulski
发明人： Amedeo Arturo Failli , John P. Dusza , Thomas Joseph Caggiano , Jay Scott Shumsky , Kevin A. Memoli , Eugene J. Trybulski
IPC分类号： C07D403/12 , C07D243/38 , 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.

6. 发明授权

US4892873A N-substituted -N-(3-(1,2,4-triazolo-(4,3-b)pyridazin-6-yl)phenyl)alkanamides, carbamates and ureas 失效
标题翻译： N-取代的-N-（3-（1,2,4-三唑并 - （4,3-b）哒嗪-6-基）苯基）烷酰胺，氨基甲酸酯和脲
公开(公告)号：US4892873A
公开(公告)日：1990-01-09
申请号：US183124
申请日：1988-04-19
申请人： Jay D. Albright , Dennis W. Powell , John P. Dusza
发明人： Jay D. Albright , Dennis W. Powell , John P. Dusza
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Novel organic compounds which are N-substituted-N-[3-(1,2,4-triazolo[4,3-b]pyridazin-6-yl)phenyl]alkanamdies, carbamates and ureas which are useful as anxiolytic or antiepileptic agents, methods of using the compounds, compositions of matter containing them as the active ingredient and processes for their production.
摘要翻译： N-取代-N- [3-（1,2,4-三唑并[4,3-b]哒嗪-6-基）苯基]烷脒的新型有机化合物，可用作抗焦虑药或抗癫痫药的氨基甲酸酯和脲试剂，使用该化合物的方法，含有它们的物质的组合物作为活性成分及其生产方法。

7. 发明授权

US4626538A [7-(3-disubstituted amino)phenyl]pyrazolo[1,5-a]pyrimidines 失效
标题翻译： [7-（3-二取代氨基）苯基]吡唑并[1,5-a]嘧啶
公开(公告)号：US4626538A
公开(公告)日：1986-12-02
申请号：US732986
申请日：1985-05-13
申请人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright
发明人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright
IPC分类号： C07D487/04 , A61K31/505 , C07D471/04
CPC分类号： C07D487/04 , Y10S514/906
摘要： Novel [7-(3-disubstituted amino)phenyl]pyrazolo[1,5-a]pyrimidines useful as anxiolytic, antiepileptic and sedative-hypnotic agents as well as skeletal muscle relaxants, methods of using these compounds, compositions of matter containing them and processes for their production.
摘要翻译：可用作抗焦虑药，抗癫痫药和镇静催眠药以及骨骼肌松弛剂的新型[7-（3-二取代氨基）苯基]吡唑并[1,5-a]嘧啶，使用这些化合物的方法，含有它们的物质组合物和生产过程。

8. 发明授权

US4521422A Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones 失效
标题翻译：芳基和杂芳基[7-（芳基和杂芳基）吡唑并[1,5-a]嘧啶-3-基]甲酮
公开(公告)号：US4521422A
公开(公告)日：1985-06-04
申请号：US612812
申请日：1984-05-24
申请人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright
发明人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04 , Y10S514/906
摘要： Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones which are new compounds active as anxiolytic, anticonvulsant, sedative-hypnotic and skeletal muscle relaxant agents in mammals and the novel process of making these compounds.
摘要翻译：芳基和杂芳基[7-（芳基和杂芳基）吡唑并[1,5-a]嘧啶-3-基]甲酮，它们是哺乳动物中作为抗焦虑药，抗惊厥药，镇静催眠药和骨骼肌松弛剂活性的新化合物，制成这些化合物。

9. 发明授权

US4236005A Imidazo[1,5-a]pyrimidines 失效
标题翻译：咪唑并[1,5-a]嘧啶
公开(公告)号：US4236005A
公开(公告)日：1980-11-25
申请号：US54104
申请日：1979-07-02
申请人： John P. Dusza , Jay D. Albright
发明人： John P. Dusza , Jay D. Albright
IPC分类号： C07D231/38 , C07D471/04 , C07D487/04 , A61K31/415
CPC分类号： C07D231/38 , C07D471/04
摘要： This disclosure describes substituted pyrazolo[1,5-a]pyrimidines and imidazo[1,5-a]pyrimidines which possess anxiolytic activity.
摘要翻译：本公开描述了具有抗焦虑活性的取代的吡唑并[1,5-a]嘧啶和咪唑并[1,5-a]嘧啶。

10. 发明授权

US06399621B1 N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-&agr;]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto 有权
标题翻译： N-甲基-N-（3- {3- [2-噻吩基羰基] - 吡唑并[1,5-a]嘧啶-7-基}苯基）乙酰胺及其组合物和方法
公开(公告)号：US06399621B1
公开(公告)日：2002-06-04
申请号：US09636381
申请日：2000-08-09
申请人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright , Bernard Beer
发明人： John P. Dusza , Andrew S. Tomcufcik , Jay D. Albright , Bernard Beer
IPC分类号： C07D40902
CPC分类号： C07D487/04
摘要： N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]-pyrimidin-7-yl}phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.
摘要翻译： N-甲基-N-（3- {3- [2-噻吩基羰基] - 吡唑并[1,5-a]嘧啶-7-基}苯基）乙酰胺，并使用其作为镇静催眠，抗焦虑，抗惊厥药和骨骼肌松弛剂。含有N-甲基-N-（3- {3- [2-噻吩基羰基] - 吡唑并[1,5-a]嘧啶-7-基}苯基）乙酰胺的组合物及其药学上可接受的盐也是披露

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