公开(公告)号：US20060172989A1

公开(公告)日：2006-08-03

申请号：US11049591

申请日：2005-02-02

Applicant: Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Upendra Topiwala ,  Hermogenes Jimenez ,  Jamie Talisman

Inventor： Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Upendra Topiwala ,  Hermogenes Jimenez ,  Jamie Talisman

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/404 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07D209/34 ,  C07D403/12 ,  C07D405/12

Abstract: This invention is directed to aminoalkoxyphenyl indolone derivatives which are ligands at the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/ or anxiety which comprises administering to the subject an amount of a compound of the subject invention.

Abstract translation: 本发明涉及作为GAL 3受体的配体的氨基烷氧基苯基吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。

公开(公告)号：US20070259942A1

公开(公告)日：2007-11-08

申请号：US11517589

申请日：2006-09-06

Applicant: Thomas Blackburn ,  Michael Konkel ,  Lakmal Boteju ,  Ian Talisman ,  John Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

Inventor： Thomas Blackburn ,  Michael Konkel ,  Lakmal Boteju ,  Ian Talisman ,  John Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

IPC: A61K31/403 ,  A61P25/22 ,  A61P25/24 ,  C07D409/06

CPC classification number: C07D401/06 ,  A61K31/404 ,  A61K31/407 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Abstract translation: 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的有效治疗受试者的抑郁症和/或焦虑症的本发明化合物。 本发明还提供了治疗受试者的抑郁症和/或焦虑的方法，其包括向受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：US20110092475A1

公开(公告)日：2011-04-21

申请号：US12908588

申请日：2010-10-20

Applicant: Allen Hopper ,  Anette Graven Sams ,  Gitte Kobberoee Mikkelsen ,  Mathivanan Packiarajan ,  Michel Grenon

Inventor： Allen Hopper ,  Anette Graven Sams ,  Gitte Kobberoee Mikkelsen ,  Mathivanan Packiarajan ,  Michel Grenon

IPC: A61K31/397 ,  C07D401/06 ,  A61K31/454 ,  C07D417/06 ,  A61K31/427 ,  C07D413/06 ,  A61K31/5377 ,  C07D277/56 ,  A61K31/426 ,  A61K31/496 ,  C07D403/06 ,  A61K31/55 ,  C07D471/04 ,  A61K31/437 ,  C07D491/10 ,  A61K31/438 ,  A61K31/538 ,  A61P25/00

CPC classification number: C07D277/24 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/435 ,  A61K31/496 ,  A61K31/5377 ,  C07D277/56 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/10 ,  C07D491/107 ,  C07D495/04

Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.

Abstract translation: 本发明提供式（I）的2-取代的乙炔基噻唑衍生物：其中R1，R2和X如本文所定义，或其药学上可接受的盐; 和药物组合物及其使用方法。

公开(公告)号：US20060293341A1

公开(公告)日：2006-12-28

申请号：US11472826

申请日：2006-06-21

Applicant: Vrej Jubian ,  Mathivanan Packiarajan ,  Hermogenes Jimenez ,  Emily Reinhard

Inventor： Vrej Jubian ,  Mathivanan Packiarajan ,  Hermogenes Jimenez ,  Emily Reinhard

IPC: A61K31/497 ,  A61K31/4439 ,  C07D417/02

CPC classification number: C07D417/04

Abstract: This invention is directed to alkyl sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from anxiety which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention.

Abstract translation: 本发明涉及作为NPY Y5受体的配体的烷基磺酰胺衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症的受试者的方法，其包括给予受试者一定量的本发明化合物。 本发明还提供了治疗患有焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。 本发明还提供了治疗患有肥胖症的受试者的方法，其包括给予受试者一定量的本发明化合物。

公开(公告)号：US07465750B2

公开(公告)日：2008-12-16

申请号：US11517589

申请日：2006-09-06

Applicant: Thomas P. Blackburn ,  Michael J. Konkel ,  Lakmal W. Boteju ,  Ian Jamie Talisman ,  John M. Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

Inventor： Thomas P. Blackburn ,  Michael J. Konkel ,  Lakmal W. Boteju ,  Ian Jamie Talisman ,  John M. Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

IPC: C07D209/34 ,  A61K31/381 ,  C07D403/14

CPC classification number: C07D401/06 ,  A61K31/404 ,  A61K31/407 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Abstract translation: 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的有效治疗受试者的抑郁症和/或焦虑症的本发明化合物。 本发明还提供了治疗受试者的抑郁症和/或焦虑的方法，其包括向受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：US20060173192A1

公开(公告)日：2006-08-03

申请号：US11343989

申请日：2006-01-31

Applicant: Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen

Inventor： Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen

IPC: C07D403/02

CPC classification number: C07D209/40 ,  C07D403/10

Abstract: This invention is directed to aminoalkylphenyl indolone derivatives which are ligands at the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the subject invention.

Abstract translation: 本发明涉及作为GAL 3受体的配体的氨基烷基苯基吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。

公开(公告)号：US20060173180A1

公开(公告)日：2006-08-03

申请号：US11343810

申请日：2006-01-31

Applicant: Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Upendra Topiwala ,  Hermogenes Jimenez ,  Jamie Talisman

Inventor： Michael Konkel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Upendra Topiwala ,  Hermogenes Jimenez ,  Jamie Talisman

IPC: C07D413/02 ,  C07D403/02

CPC classification number: C07D403/12 ,  C07D209/34 ,  C07D209/40 ,  C07D401/12

Abstract: This invention is directed to aminoalkoxyphenyl indolone derivatives, which are ligands at the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the subject invention.

Abstract translation: 本发明涉及作为GAL 3受体的配体的氨基烷氧基苯基吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。

公开(公告)号：US08440837B2

公开(公告)日：2013-05-14

申请号：US12908588

申请日：2010-10-20

Applicant: Allen Hopper ,  Anette Graven Sams ,  Gitte Kobberoee Mikkelsen ,  Mathivanan Packiarajan ,  Michel Grenon

Inventor： Allen Hopper ,  Anette Graven Sams ,  Gitte Kobberoee Mikkelsen ,  Mathivanan Packiarajan ,  Michel Grenon

IPC: C07D275/02 ,  C07D277/00 ,  C07D415/00 ,  C07D413/00 ,  C07D265/36 ,  C07D403/00 ,  C07D215/00 ,  C07D513/02 ,  C07D401/00 ,  A61K31/397 ,  A61K31/55 ,  A61K31/535 ,  A61K31/44 ,  A61K31/445 ,  A61K31/425

CPC classification number: C07D277/24 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/435 ,  A61K31/496 ,  A61K31/5377 ,  C07D277/56 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/10 ,  C07D491/107 ,  C07D495/04

Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.

Abstract translation: 本发明提供式（I）的2-取代的乙炔基噻唑衍生物：其中R1，R2和X如本文所定义，或其药学上可接受的盐; 和药物组合物及其使用方法。

公开(公告)号：US20090318504A1

公开(公告)日：2009-12-24

申请号：US12314675

申请日：2008-12-15

Applicant: Thomas P. Blackburn ,  Michael J. Konkel ,  Lakmal W. Boteju ,  Ian Jamie Talisman ,  John M. Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

Inventor： Thomas P. Blackburn ,  Michael J. Konkel ,  Lakmal W. Boteju ,  Ian Jamie Talisman ,  John M. Wetzel ,  Mathivanan Packiarajan ,  Heidi Chen ,  Hermo Jimenez

IPC: A61K31/404 ,  A61K31/4439 ,  C07D405/12

CPC classification number: C07D401/06 ,  A61K31/404 ,  A61K31/407 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Abstract translation: 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了一种治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的有效治疗受试者的抑郁症和/或焦虑症的本发明化合物。 本发明还提供了治疗受试者的抑郁症和/或焦虑的方法，其包括向受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：US20070213376A1

公开(公告)日：2007-09-13

申请号：US11714008

申请日：2007-03-05

Applicant: Vrej Jubian ,  Mathivanan Packiarajan ,  Emily Reinhard

Inventor： Vrej Jubian ,  Mathivanan Packiarajan ,  Emily Reinhard

IPC: A61K31/44

CPC classification number: C07D417/04

Abstract: This invention is directed to halogenated sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from anxiety which comprises administering to the subject an amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, the present invention is directed to use of a compound of the invention for the manufacture of a medicament for treating a subject suffering from depression, anxiety or obesity.

Abstract translation: 本发明涉及作为NPY Y5受体的配体的卤代磺酰胺衍生物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供通过混合治疗有效量的本发明化合物和药学上可接受的载体制备的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了治疗患有抑郁症的受试者的方法，其包括给予受试者一定量的本发明化合物。 本发明还提供了治疗患有焦虑症的受试者的方法，其包括给予受试者一定量的本发明化合物。 本发明还提供了治疗患有肥胖症的受试者的方法，其包括给予受试者一定量的本发明化合物。 此外，本发明涉及本发明化合物在制备用于治疗患有抑郁，焦虑或肥胖的受试者的药物中的用途。