公开(公告)号：US08133908B2

公开(公告)日：2012-03-13

申请号：US12627283

申请日：2009-11-30

Applicant: Giuseppe Alvaro ,  David Amantini ,  Emiliano Castiglioni ,  Romano Di Fabio ,  Francesca Pavone

Inventor： Giuseppe Alvaro ,  David Amantini ,  Emiliano Castiglioni ,  Romano Di Fabio ,  Francesca Pavone

IPC: A61K31/44

CPC classification number: C07D401/06 ,  C07D401/14

Abstract: Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R1, R2 and R3 are as defined herein, and their use as orexin antagonists.

Abstract translation: 公开了具有下式的N - {[（1S，4S，6S）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物，其中m ，n，Het，R 1，R 2和R 3如本文所定义，以及它们作为食欲素拮抗剂的用途。

公开(公告)号：US20110172255A1

公开(公告)日：2011-07-14

申请号：US11931313

申请日：2007-10-31

Applicant: Daniele Andreotti ,  Giovanni Bernasconi ,  Emiliano Castiglioni ,  Stefania Anne Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Maria Sabbatini ,  Yves St-Denis

Inventor： Daniele Andreotti ,  Giovanni Bernasconi ,  Emiliano Castiglioni ,  Stefania Anne Contini ,  Romano Di Fabio ,  Elettra Fazzolari ,  Aldo Feriani ,  Gabriella Gentile ,  Mario Mattioli ,  Anna Mingardi ,  Fabio Maria Sabbatini ,  Yves St-Denis

IPC: A61K31/519 ,  C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61P25/24 ,  A61P25/22

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

Abstract translation: 本发明提供式（I）化合物，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）介导的病症中的用途。

公开(公告)号：US20100311734A1

公开(公告)日：2010-12-09

申请号：US12670704

申请日：2008-07-24

Applicant: Maurizio Botta ,  Emiliano Castiglioni ,  Romano Di Fabio ,  Raffaella Spinosa ,  Andrea Togninelli

Inventor： Maurizio Botta ,  Emiliano Castiglioni ,  Romano Di Fabio ,  Raffaella Spinosa ,  Andrea Togninelli

IPC: A61K31/5386 ,  C07D295/033 ,  C07D207/04 ,  C07D205/04 ,  C07D211/06 ,  C07D221/20 ,  C07D498/10 ,  C07D491/107 ,  A61K31/136 ,  A61K31/5375 ,  A61K31/40 ,  A61K31/495 ,  A61K31/54 ,  A61K31/451 ,  A61K31/438 ,  A61K31/403 ,  A61P25/00

CPC classification number: C07C211/42 ,  C07C2603/94 ,  C07D221/20 ,  C07D295/00 ,  C07D295/027 ,  C07D295/03 ,  C07D295/033 ,  C07D491/10 ,  C07D498/10

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.

Abstract translation: 本发明提供了用于治疗中枢神经系统（CNS）的疾病和病症的式（I）化合物或其药学上可接受的盐，特别是睡眠障碍。

公开(公告)号：US20100286151A1

公开(公告)日：2010-11-11

申请号：US12524080

申请日：2008-01-30

Applicant: Jonathan Bentley ,  Matteo Biagetti ,  Romano Di Fabio ,  Thorsten Genski ,  Sebastien Guery ,  Silvia Rosalia Kopf ,  Colin philip Leslie ,  Angelica Mazzali ,  Sergio Melotto ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

Inventor： Jonathan Bentley ,  Matteo Biagetti ,  Romano Di Fabio ,  Thorsten Genski ,  Sebastien Guery ,  Silvia Rosalia Kopf ,  Colin philip Leslie ,  Angelica Mazzali ,  Sergio Melotto ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

IPC: A61K31/423 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/505 ,  C07D413/14 ,  A61K31/501 ,  A61K31/444 ,  A61K31/497 ,  A61K31/433 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/4985 ,  C07D413/12 ,  A61P3/04 ,  A61P3/00

CPC classification number: C07D413/14

Abstract: The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 5 membered heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, Cl C4 haloalkoxy, cyano; B is hydrogen or is a 5-6 membered heteroaryl, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

Abstract translation: 本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是5元杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或是5-6元杂芳基或苯基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

公开(公告)号：US20100069416A1

公开(公告)日：2010-03-18

申请号：US12295304

申请日：2007-03-30

Applicant: Barbara Bertani ,  Anna Checchia ,  Romano Di Fabio ,  Gabriella Gentile ,  Alessandra Pasquarello ,  Silvia Terreni

Inventor： Barbara Bertani ,  Anna Checchia ,  Romano Di Fabio ,  Gabriella Gentile ,  Alessandra Pasquarello ,  Silvia Terreni

IPC: A61K31/506 ,  C07D403/06 ,  C07D401/14 ,  C07D417/14 ,  A61P25/00 ,  A61P25/30 ,  A61P15/12

CPC classification number: C07D401/14 ,  C07D403/06 ,  C07D405/14

Abstract: The present invention relates to certain azabicyclo compounds of formula (I)′: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.

Abstract translation: 本发明涉及某些式（I）'的氮杂二环化合物：其中各种基团在本文中定义，并且是多巴胺D3受体的调节剂，例如， 治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

公开(公告)号：US20080249108A1

公开(公告)日：2008-10-09

申请号：US11955847

申请日：2007-12-13

Applicant: Giuseppe Alvaro ,  Romano DI FABIO ,  Riccardo GIOVANNINI ,  Giuseppe GUERCIO ,  Yves ST-DENIS ,  Antonella URSINI

Inventor： Giuseppe Alvaro ,  Romano DI FABIO ,  Riccardo GIOVANNINI ,  Giuseppe GUERCIO ,  Yves ST-DENIS ,  Antonella URSINI

IPC: A61K31/495 ,  A61P25/00

CPC classification number: C07D401/06 ,  A61K31/135 ,  A61K31/196 ,  A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D403/06 ,  A61K2300/00

Abstract: The invention relates to methods for the treatment of medical conditions comprising administering an effective amount of a compound of formula (I): wherein all variables are as defined herein.

Abstract translation: 本发明涉及治疗医学病症的方法，包括施用有效量的式（I）化合物：其中所有变量如本文所定义。

公开(公告)号：US20080114049A1

公开(公告)日：2008-05-15

申请号：US11851459

申请日：2007-09-07

Applicant: Romano Di Fabio

Inventor： Romano Di Fabio

IPC: A61K31/403 ,  C07D209/02

CPC classification number: C07D221/04

Abstract: The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

Abstract translation: 本发明涉及（1S，6R）-6-（3,4-二氯苯基）-1 - [（甲氧基）甲基] -3-氮杂双环[4.1.0]庚烷，其药学上可接受的盐，前药或溶剂合物; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的应用。

公开(公告)号：US07329667B2

公开(公告)日：2008-02-12

申请号：US10476441

申请日：2002-04-30

Applicant: Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St. Denis

Inventor： Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St. Denis

IPC: A01N43/54 ,  C07D239/00

CPC classification number: C07D471/06 ,  C07D487/06

Abstract: The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

Abstract translation: 本发明涉及式（I）的三环嘧啶化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放介导的病症 因子（CRF）。

公开(公告)号：US07253284B2

公开(公告)日：2007-08-07

申请号：US10483792

申请日：2002-07-15

Applicant: Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

Inventor： Romano Di Fabio ,  Fabrizio Micheli ,  Yves St-Denis

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: Compounds of the formula I, Wherein X is N, n is 1 and R2and R3 together form a ring, R, R1 and R4 are as defined in the specifications.

Abstract translation: 式I化合物，其中X为N，n为1，R 2和R 3一起形成环，R，R 1和R 4如说明书中所定义。

公开(公告)号：US20070099914A1

公开(公告)日：2007-05-03

申请号：US11608853

申请日：2006-12-11

Applicant: Giuseppe Alvaro ,  Romano Di Fabio ,  Maria Tranquillini ,  Simone Spada

Inventor： Giuseppe Alvaro ,  Romano Di Fabio ,  Maria Tranquillini ,  Simone Spada

IPC: A61K31/5383 ,  A61K31/498

CPC classification number: C07D487/04 ,  A61K31/445

Abstract: The present invention relates to methods for treatment of inflammatory diseases of the bladder.

Abstract translation: 本发明涉及治疗膀胱炎性疾病的方法。