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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

US5880122A 3-Carboxamide derivatives of 5H-pyrrolo�2,1-c!�1,4!-benzodiazepines 失效
标题翻译： 3,5-吡咯并[2,1-c] [1,4] - 苯并二氮杂卓的3-甲酰胺衍生物
公开(公告)号：US5880122A
公开(公告)日：1999-03-09
申请号：US955511
申请日：1997-10-22
申请人： Eugene J. Trybulski , Albert J. Molinari , Jehan F. Bagli , Mark A. Ashwell , Thomas J. Caggiano
发明人： Eugene J. Trybulski , Albert J. Molinari , Jehan F. Bagli , Mark A. Ashwell , Thomas J. Caggiano
IPC分类号： C07D487/04 , A61K31/55 , C07D487/12
CPC分类号： C07D487/04
摘要： This invention relates to tricyclic non-peptide vasopressin antagonists which are useful in treating conditions where decreased vasopressin levels are desired, such as in congestive heart failure, in disease conditions with excess renal water reabsorption and in conditions with increased vascular resistance and coronary vasoconstriction, the compounds having the general structure: ##STR1##
摘要翻译：本发明涉及三环非肽加压素拮抗剂，其可用于治疗需要血管升压素水平降低的病症，例如充血性心力衰竭，具有过量肾脏水吸收的疾病状况和血管阻力增加和冠状动脉血管收缩增加的病症。具有一般结构的化合物：

3. 发明授权

US07138393B2 Biologically active vasopressin agonist metabolites 失效
公开(公告)号：US07138393B2
公开(公告)日：2006-11-21
申请号：US10320761
申请日：2002-12-16
申请人： Albert J. Molinari , Eugene J. Trybulski
发明人： Albert J. Molinari , Eugene J. Trybulski
IPC分类号： A61P13/00 , A61K31/55 , C07D487/12
CPC分类号： C07D487/04 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical formulations containing such compounds which are useful as anti-aquaretic agents in the treatment of nocturnal urinary enuresis, nocturnal urinary urgency, and/or similar conditions.

4. 发明授权

US4454319A Pyrimido[6,1-a]isoguinoline-4-one derivatives 失效
标题翻译：嘧啶并[6,1-a]异喹啉-4-酮衍生物
公开(公告)号：US4454319A
公开(公告)日：1984-06-12
申请号：US383422
申请日：1982-06-01
申请人： Bruce E. Maryanoff , Albert J. Molinari
发明人： Bruce E. Maryanoff , Albert J. Molinari
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： Pyrimido[6,1-a]isoquinoline-4-one derivatives of the formula: ##STR1## wherein R is C.sub.1 -C.sub.6 lower alkyl or 2-haloethyl (halo=Cl, Br or I) having antihypertensive activity.
摘要翻译：具有下式的嘧啶并[6,1-a]异喹啉-4-酮衍生物：其中R是具有抗高血压活性的C 1 -C 6低级烷基或2-卤代乙基（卤代= Cl，Br或I）。

5. 发明授权

US5438064A Derivatives of 4-anilinoquinoline-3-carboxamide as analgesic agents 失效
标题翻译： 4-苯胺基喹啉-3-甲酰胺的衍生物作为止痛剂
公开(公告)号：US5438064A
公开(公告)日：1995-08-01
申请号：US812791
申请日：1991-12-23
申请人： Dominick Mobilio , Albert J. Molinari
发明人： Dominick Mobilio , Albert J. Molinari
IPC分类号： C07D401/12 , C07D401/14 , C07D215/46 , A61K31/47
CPC分类号： C07D401/12 , C07D401/14
摘要： Derivatives of 4-anilinoquinoline having the formula: ##STR1## where X is O or H.sub.2 and Z is 1-substituted-4-piperidinylamino or diloweralkylaminoloweralkyl inhibit binding of tritiated bradykinin to guinea pig ileum and inhibit bradykinin-induced writhing in mice. Bradykinin is a nonapeptide formed in plasma as a result of inflammation or injury and produces pain when it binds with pain receptors. A drug which inhibits the binding of bradykinin therefore has analgetic properties.
摘要翻译：具有下式的4-苯胺基喹啉的衍生物：其中X是O或H 2，Z是1-取代-4-哌啶基氨基或二低级烷基氨基低级烷基抑制氚化缓激肽与豚鼠回肠的结合，并抑制小鼠中缓激肽诱导的扭体。缓激肽是由于炎症或损伤而在血浆中形成的非肽，当它与疼痛受体结合时会产生疼痛。因此抑制缓激肽结合的药物具有止痛特性。

6. 发明授权

US5212182A Substituted quinolinyl- and naphthalenylbenzamides or benzylamines and related compounds useful as analgesics 失效
标题翻译：取代的喹啉基 - 和萘基苯甲酰胺或苄胺和相关化合物可用作镇痛药
公开(公告)号：US5212182A
公开(公告)日：1993-05-18
申请号：US592160
申请日：1990-10-03
申请人： John H. Musser , Albert J. Molinari , Dominick Mobilio
发明人： John H. Musser , Albert J. Molinari , Dominick Mobilio
IPC分类号： C07D211/58 , C07D401/12
CPC分类号： C07D401/12 , C07D211/58
摘要： This invention relates to novel quinolinyl- and naphthalenylbenzamides or benylamines and related disclosed compounds of the formula ##STR1## wherein X is nitrogen, NO or CR.sup.1 ; Y is C(R.sup.1)(R.sup.2)O, OC(R.sup.1)(R.sup.2), C(R.sup.1)(R.sup.2)N(R.sup.3), N(R.sup.3)C(R.sup.1)(R.sup.2) or C(R.sup.1).dbd.C(R.sup.2); wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl containing 1 to 10 carbon atoms; Z is oxygen or (R.sup.1)(R.sup.2); R.sup.4 is R.sup.1, benzyl, benzyl ring substituted with R.sup.5, benzyl alpha monosubstituted with R.sup.1, benzyl ring substituted with R.sup.5 and alpha monosubstituted with R.sup.1, phenyl, phenylalkyl containing 2 to 10 carbon atoms in the alkyl group or phenylalkyl ring substituted with R.sup.5 and containing 2 to 10 carbon atoms in the alkyl group; wherein R.sup.5 is R.sup.1, lower alkoxy containing 1 to 10 carbon atoms, halogen, trihalomethyl, NO.sub.2, N(R.sup.1)(R.sup.2) or C(O)N(R.sup.1)(R.sup.2); R.sup.6 is R.sup.1 or R.sup.6 is C(O)(R.sup.7) with the proviso that Z is not oxygen; and wherein R.sup.7 is R.sup.1, phenyl, perfluoroalkyl containing 1 to 10 carbon atoms, phenylalkyl containing 1 to 10 carbon atoms in the alkyl group; or a pharmaceutically acceptable acid addition salt thereof, and their use in the treatment of pain mediated by the biological peptide, bradykinin. In particular, the preferred compounds are where X is nitrogen, and Y is CH.sub.2 O of the above structure.
摘要翻译：本发明涉及新颖的喹啉基和萘基苯甲酰胺或联苯胺及其相关公开的式（I）的化合物，其中X是氮，NO或CR 1; Y是C（R1）（R2）O，OC（R1）（R2），C（R1）（R2）N（R3），N（R3）C（R1）（R2）或C（R1） R2）; 其中R1，R2和R3独立地是氢或含有1-10个碳原子的低级烷基; Z是氧或（R1）（R2）; R4是R1，苄基，被R5取代的苄基环，被R1单取代的苄基，被R5取代的苄基环和被R1单取代的α，苯基，在烷基中含有2-10个碳原子的苯基烷基或被R5取代的苯基烷基，烷基中的2至10个碳原子; 其中R 5为R 1，含有1至10个碳原子的低级烷氧基，卤素，三卤代甲基，NO 2，N（R 1）（R 2）或C（O）N（R 1）（R 2） R6是R1或R6是C（O）（R7），条件是Z不是氧; 并且其中R 7为R 1，苯基，含有1至10个碳原子的全氟烷基，烷基中含有1至10个碳原子的苯基烷基; 或其药学上可接受的酸加成盐，以及它们在治疗由生物肽缓激肽介导的疼痛的用途。特别优选的化合物是其中X是氮，Y是上述结构的CH 2 O.

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