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1. 发明申请

US20060025436A1 Processes for preparing 6-alkyl-5-arylsulfonyl-dihydrophenanthridines 失效
标题翻译：制备6-烷基-5-芳基磺酰基 - 二氢菲吩的方法
公开(公告)号：US20060025436A1
公开(公告)日：2006-02-02
申请号：US11155851
申请日：2005-06-17
申请人： Brian Ridgway , William Moore , Mark Ashwell , William Solvibile , Amy Lee , Molly Hoke , Madelene Antane , Amedeo Failli
发明人： Brian Ridgway , William Moore , Mark Ashwell , William Solvibile , Amy Lee , Molly Hoke , Madelene Antane , Amedeo Failli
IPC分类号： C07D221/12 , A61K31/473
CPC分类号： C07D221/12
摘要： Synthetic methods are provided for production of compounds of the formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and R14 are as defined in the specification.
摘要翻译：提供合成方法用于制备下式化合物：其中R 1，R 2，R 3，R 4，R 5 R 6，R 7，R 8，R 9，R 10，R 6， R 11，R 12，R 13和R 14如本说明书中所定义。。

2. 发明申请

US20060287522A1 Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists 失效
标题翻译：吡咯并苯并二氮杂吡啶甲酰胺及其衍生物作为促卵泡激素受体拮抗剂
公开(公告)号：US20060287522A1
公开(公告)日：2006-12-21
申请号：US11449376
申请日：2006-06-08
申请人： Amedeo Failli , Gavin Heffernan , Arthur Santilli , Dominick Quagliato , Richard Coghlan , Patrick Andrae , Susan Croce , Emily Shen , Eugene Trybulski
发明人： Amedeo Failli , Gavin Heffernan , Arthur Santilli , Dominick Quagliato , Richard Coghlan , Patrick Andrae , Susan Croce , Emily Shen , Eugene Trybulski
IPC分类号： C07D487/12
CPC分类号： C07D487/04
摘要： This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
摘要翻译：本发明提供了选自式（1）的吡咯并苯并二氮杂吡啶甲酰胺，其作为促卵泡激素受体拮抗剂。本发明还提供使用式（1）和（2）的化合物的药物组合物和治疗方法。

3. 发明申请

US20050075328A1 Biphenyl vasopressin agonists 失效
标题翻译：联苯加压素激动剂
公开(公告)号：US20050075328A1
公开(公告)日：2005-04-07
申请号：US10980939
申请日：2004-11-04
申请人： Amedeo Failli , John Dusza , Thomas Caggiano , Jay Shumsky , Kevin Memoli , Eugene Trybulski
发明人： Amedeo Failli , John Dusza , Thomas Caggiano , Jay Shumsky , Kevin Memoli , Eugene Trybulski
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 , C07D487/12
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; R 1是下式的部分，R 2，R 3，R 7，R 8和R 9独立地选自氢

4. 发明授权

US4351828A N-Substituted cyclopeptide derivatives 失效
标题翻译： N-取代的环肽衍生物
公开(公告)号：US4351828A
公开(公告)日：1982-09-28
申请号：US164663
申请日：1980-06-30
申请人： Amedeo Failli , Hans U. Immer , Manfred K. Gotz
发明人： Amedeo Failli , Hans U. Immer , Manfred K. Gotz
IPC分类号： A61K38/00 , C07K7/64 , A61K37/00
CPC分类号： C07K7/64 , A61K38/00 , Y10S930/19 , Y10S930/27 , Y10S930/29
摘要： The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.
摘要翻译：式I的N-取代的环肽衍生物，其中R 1是低级烷基，R 2是低级烷基或环（低级）烷基，R 3是中性氨基酸侧链，Y是一个肽残基，公开了9个氨基酸残基和制备式I化合物的方法。式I的化合物是有用的抗菌和抗真菌剂。也公开了药物组合物。

5. 发明授权

US4033974A Pyridylmethyl esters of N-(phenoxyalkanoyl)peptide derivatives 失效
标题翻译： N-（苯氧基烷酰基）肽衍生物的吡啶基甲基酯
公开(公告)号：US4033974A
公开(公告)日：1977-07-05
申请号：US657118
申请日：1976-02-11
申请人： Jean-Marie Ferland , Amedeo Failli , Hans U. Immer , Manfred K. Gotz
发明人： Jean-Marie Ferland , Amedeo Failli , Hans U. Immer , Manfred K. Gotz
IPC分类号： A61K38/00 , C07D213/30 , C07D213/55
CPC分类号： C07D213/30 , A61K38/00
摘要： Pyridylmethyl esters of N-(phenoxyalkanoyl)peptide derivatives are disclosed. The derivatives are characterized by having a phenoxyalkanoyl group and a pyridylmethyloxy group-joined together by a peptide group. They possess antihyperlipoproteinemic activity. In addition, methods for their preparation and use are disclosed.
摘要翻译：公开了N-（苯氧基烷酰基）肽衍生物的吡啶基甲基酯。该衍生物的特征在于具有通过肽基团连接在一起的苯氧基烷酰基和吡啶基甲氧基。它们具有抗高脂蛋白血症活性。另外，公开了其制备和使用的方法。

6. 发明授权

US4000284A Phenoxyisobutyric acid salts 失效
标题翻译：酚氧基酸
公开(公告)号：US4000284A
公开(公告)日：1976-12-28
申请号：US611092
申请日：1975-09-08
申请人： Amedeo Failli , William T. Robinson , Dushan Dvornik
发明人： Amedeo Failli , William T. Robinson , Dushan Dvornik
IPC分类号： C07C59/68 , C07D213/30 , A61K31/395 , C07D213/55
CPC分类号： C07D213/30 , C07C59/68
摘要： Salts of phenoxyisobutyric acids with amino acid pyridylmethyl esters are disclosed. The salts possess antihyperlipoproteinemic activity. In addition, methods for their preparation and use, as well as pharmaceutical compositions thereof, are disclosed.

7. 发明申请

US20060276456A1 Biphenyl vasopressin agonists 失效
公开(公告)号：US20060276456A1
公开(公告)日：2006-12-07
申请号：US11502982
申请日：2006-08-11
申请人： Kevin Memoli , Amedeo Failli , Thomas Caggiano , Jay Shumsky , Eugene Trybulski , John Dusza
发明人： Kevin Memoli , Amedeo Failli , Thomas Caggiano , Jay Shumsky , Eugene Trybulski , John Dusza
IPC分类号： A61K31/551 , C07D487/02
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.

8. 发明申请

US20060199806A1 Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists 失效
标题翻译：吡咯并苯并二氮杂芳基甲酰胺及其衍生物作为促卵泡激素受体拮抗剂
公开(公告)号：US20060199806A1
公开(公告)日：2006-09-07
申请号：US11365035
申请日：2006-03-01
申请人： Amedeo Failli , Dominick Quagliato , Patrick Andrae , Gavin Heffernan , Richard Coghlan , Emily Shen
发明人： Amedeo Failli , Dominick Quagliato , Patrick Andrae , Gavin Heffernan , Richard Coghlan , Emily Shen
IPC分类号： C07D487/12 , A61K31/551
CPC分类号： C07D487/04
摘要： This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment
摘要翻译：本发明提供了选自式（1）的吡咯并苯并二氮杂芳基羧酰胺，其作为促卵泡激素受体拮抗剂，以及药物组合物和治疗方法

9. 发明申请

US20050032873A1 3-Amino chroman and 2-amino tetralin derivatives 审中-公开
标题翻译： 3-氨基苯并二氢吡喃和2-氨基四氢化萘衍生物
公开(公告)号：US20050032873A1
公开(公告)日：2005-02-10
申请号：US10898866
申请日：2004-07-26
申请人： Nicole Hatzenbuhler , Deborah Evrard , Richard Mewshaw , Dahui Zhou , Uresh Shah , Jennifer Inghrim , Steven Lenicek , Reinhardt Baudy , John Butera , Annmarie Sabb , Amedeo Failli , Pudukkaraipudur Ramamoorthy
发明人： Nicole Hatzenbuhler , Deborah Evrard , Richard Mewshaw , Dahui Zhou , Uresh Shah , Jennifer Inghrim , Steven Lenicek , Reinhardt Baudy , John Butera , Annmarie Sabb , Amedeo Failli , Pudukkaraipudur Ramamoorthy
IPC分类号： C07C237/48 , C07D209/10 , C07D209/12 , C07D209/14 , C07D405/12 , C07D407/12 , C07D409/12 , A61K31/405 , A61K31/353 , A61K31/381 , C07D45/02 , C07D49/02
CPC分类号： C07D405/12 , C07C237/48 , C07D209/10 , C07D209/12 , C07D209/14 , C07D407/12 , C07D409/12
摘要： 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.
摘要翻译：公开了3-氨基苯并二氢吡喃和2-氨基四氢化萘衍生物和含有这些化合物的组合物。还公开了使用3-氨基苯并二氢吡喃和2-氨基四氢化萘化合物的方法和含有这些化合物的组合物在治疗5-羟色胺疾病如抑郁和焦虑中的方法。

10. 发明授权

US4235901A 1-Hydroxyalkanamine pyrano(3,4-b)indole compositions and use thereof 失效
标题翻译： 1-羟基烷胺吡喃酮（3,4-b）吲哚组合物及其用途
公开(公告)号：US4235901A
公开(公告)日：1980-11-25
申请号：US38994
申请日：1979-05-14
申请人： Andre A. Asselin , Leslie G. Humber , Gervais Dionne , Clara Revesz , Amedeo Failli
发明人： Andre A. Asselin , Leslie G. Humber , Gervais Dionne , Clara Revesz , Amedeo Failli
IPC分类号： C07D491/04 , C07D495/04 , A61K31/535 , A61K31/40
CPC分类号： C07D491/04 , C07D495/04 , Y10S514/869
摘要： Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano-[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.
摘要翻译：其特征在于具有1,3,4,9-四氢吡喃并[3,4-b]吲哚或1,3,4,9-四氢噻喃并[3,4-b]吲哚核与羟基卡胺或低级烷氧基烷胺取代基并且公开了位置1的低级烷基。核可任选地在9位和芳环上被进一步取代。衍生物是有用的利尿剂，并且还公开了它们的制备和使用方法。

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