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。

公开(公告)号：US20060258644A1

公开(公告)日：2006-11-16

申请号：US11432177

申请日：2006-05-11

申请人： Amedeo Failli ,  Arthur Santilli ,  Dominick Quagliato ,  Emily Shen

发明人： Amedeo Failli ,  Arthur Santilli ,  Dominick Quagliato ,  Emily Shen

IPC分类号： A61K31/551 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention provides compounds of formula or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, A, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.

摘要翻译： 本发明提供式或其药学上可接受的盐的化合物，其中R 1，R 2，R 2，R 3，A和B 如所附说明书中所定义。 还提供了制备这些化合物的方法。

公开(公告)号：US20060258645A1

公开(公告)日：2006-11-16

申请号：US11432200

申请日：2006-05-11

申请人： Amedeo Failli ,  Dominick Quagliato ,  Gavin Heffernan ,  Richard Coghlan ,  Emily Shen

发明人： Amedeo Failli ,  Dominick Quagliato ,  Gavin Heffernan ,  Richard Coghlan ,  Emily Shen

IPC分类号： A61K31/551 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention provides compounds of formula or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.

摘要翻译： 本发明提供了式或其药学上可接受的盐的化合物，其中R 1，R 2，R 2，R 3和B分别为 在所附说明书中定义。 还提供了制备这些化合物的方法。

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

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.

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。

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。

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

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。

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。