公开(公告)号：US20060058284A1

公开(公告)日：2006-03-16

申请号：US10538134

申请日：2003-12-12

Applicant: Hanbiao Yang ,  Wieslaw Kazmierski ,  Christopher Aquino

Inventor： Hanbiao Yang ,  Wieslaw Kazmierski ,  Christopher Aquino

IPC: A61K31/4747 ,  C07D471/10

CPC classification number: C07D471/10

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).

Abstract translation: 本发明涉及可用于治疗CCR5相关疾病和病症的式（I）化合物或其药学上可接受的衍生物，例如可用于抑制HIV复制，预防或治疗HIV感染， 以及治疗所得的获得性免疫缺陷综合征（AIDS）。

公开(公告)号：US20060009471A1

公开(公告)日：2006-01-12

申请号：US11159724

申请日：2005-06-23

Applicant: Wenqing Yao ,  Meizhong Xu ,  Colin Zhang ,  Konstantinos Agrios ,  Brian Metcalf ,  Jincong Zhuo

Inventor： Wenqing Yao ,  Meizhong Xu ,  Colin Zhang ,  Konstantinos Agrios ,  Brian Metcalf ,  Jincong Zhuo

IPC: A61K31/495 ,  A61K31/4747 ,  A61K31/407 ,  C07D471/10 ,  C07D491/10

CPC classification number: C07D207/08 ,  C07D207/06 ,  C07D209/54 ,  C07D211/16 ,  C07D211/22 ,  C07D211/52 ,  C07D217/06 ,  C07D217/16 ,  C07D221/20 ,  C07D241/04 ,  C07D295/108 ,  C07D295/185 ,  C07D401/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

Abstract: The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

公开(公告)号：US20050288213A1

公开(公告)日：2005-12-29

申请号：US10520566

申请日：2003-07-14

Applicant: Douglas MacNeil ,  James McIntyre ,  Leonardus Van Der Ploeg ,  Akane Ishihara

Inventor： Douglas MacNeil ,  James McIntyre ,  Leonardus Van Der Ploeg ,  Akane Ishihara

IPC: C07D491/107 ,  A01N43/16 ,  A61K31/137 ,  A61K31/155 ,  A61K31/352 ,  A61K31/353 ,  A61K31/438 ,  A61K31/4747 ,  A61K31/485 ,  A61K31/497 ,  A61K31/506 ,  A61K38/17 ,  A61K45/00 ,  A61P3/04 ,  C07D311/82

CPC classification number: A61K31/155 ,  A61K31/353 ,  A61K31/438 ,  A61K31/4747 ,  A61K31/506

Abstract: The present invention relates to compositions comprising a NPY5 antagonist of formula I or II and an anti-obesity agent, useful for the treatment and prevention of diabetes, obesity and obesity-related disorders. The present invention further relates to methods of treating or preventing obesity and obesity-related disorder in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.

Abstract translation: 本发明涉及包含式I或II的NPY5拮抗剂和抗肥胖剂的组合物，其可用于治疗和预防糖尿病，肥胖症和肥胖相关疾病。 本发明还涉及通过给予本发明的组合物来治疗或预防有需要的受试者中的肥胖和肥胖相关疾病的方法。 本发明进一步提供可用于实施这些方法的药物组合物，药物和试剂盒。

公开(公告)号：US20050261327A1

公开(公告)日：2005-11-24

申请号：US11131642

申请日：2005-05-18

Applicant: Mark Bock ,  Scott Kuduk ,  Dai-Shi Su ,  Michael Wood

Inventor： Mark Bock ,  Scott Kuduk ,  Dai-Shi Su ,  Michael Wood

IPC: A61K31/4747 ,  C07D487/10

CPC classification number: C07D239/42 ,  C07D213/75 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

Abstract: Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Abstract translation: 本文公开的化合物是缓激肽B1拮抗剂化合物，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

公开(公告)号：US20050250802A1

公开(公告)日：2005-11-10

申请号：US11181098

申请日：2005-07-14

Applicant: James Loch ,  George Mullen ,  Eifion Phillips

Inventor： James Loch ,  George Mullen ,  Eifion Phillips

IPC: C07D491/20 ,  A61K20060101 ,  A61K31/439 ,  A61K31/4747 ,  A61P20060101 ,  A61P1/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P43/00 ,  C07B61/00 ,  C07D20060101 ,  C07D471/14 ,  C07D491/22

CPC classification number: C07D491/22

Abstract: Methods for the treatment of psychotic or intellectual impairment disorders with compounds of formula I, wherein A, R and R1 are as defined in the specification.

Abstract translation: 用式I化合物治疗精神病或智力障碍障碍的方法，其中A，R和R 1如说明书中所定义。

公开(公告)号：US20050250800A1

公开(公告)日：2005-11-10

申请号：US10638742

申请日：2003-08-11

Applicant: Justin Bryans ,  David Horwell ,  Jean-Marie Receveur

Inventor： Justin Bryans ,  David Horwell ,  Jean-Marie Receveur

IPC: A61K31/195 ,  A61K31/403 ,  A61K31/4747

CPC classification number: C07D209/54 ,  C07D205/12 ,  C07D209/44

Abstract: Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract translation: 公开了新颖的取代的氨基酸，并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛和神经病理学障碍的药物。 还公开了用于制备的方法和可用于制备的中间体。

公开(公告)号：US06960600B2

公开(公告)日：2005-11-01

申请号：US10476942

申请日：2002-05-02

Applicant: Didier Babin ,  John Bernard Weston

Inventor： Didier Babin ,  John Bernard Weston

IPC: C07D249/08 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/4747 ,  A61P31/10 ,  C07D233/54 ,  C07D233/60 ,  C07D249/10 ,  C07D401/12 ,  C07D521/00 ,  A61K31/415 ,  A61K31/47 ,  C07D401/02

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.

Abstract translation: 本发明涉及式（I）的新型唑或三唑衍生物，其中：X，Ar 1，Ar 3，A，R 1， R 5，R 6，R 7和B如描述中所定义，它们的制备方法及其作为抗真菌药物的用途。

公开(公告)号：US20050215602A1

公开(公告)日：2005-09-29

申请号：US10511506

申请日：2003-04-24

Applicant: Alister Campbell ,  Mark Ridgill

Inventor： Alister Campbell ,  Mark Ridgill

IPC: A61P25/28 ,  C07D285/14 ,  C07D417/06 ,  A61K31/433 ,  A61K31/4747 ,  A61K31/497 ,  C07D498/10

CPC classification number: C07D285/14 ,  C07D417/06

Abstract: Compounds of formula (I) are disclosed. The compounds inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.

Abstract translation: 公开了式（I）的化合物。 该化合物抑制γ-分泌酶，因此可用于治疗阿尔茨海默病。

公开(公告)号：US20050165037A1

公开(公告)日：2005-07-28

申请号：US11006027

申请日：2004-12-06

Applicant: Hiroshi Tomori ,  Keijiro Kobayashi ,  Fumihiko Toriyama

Inventor： Hiroshi Tomori ,  Keijiro Kobayashi ,  Fumihiko Toriyama

IPC: C07D211/52 ,  C07D495/10 ,  A61K31/4747 ,  C07D498/10

CPC classification number: C07D495/10 ,  C07D211/52 ,  Y02P20/55

Abstract: A process for producing cyclic thioether compounds and their synthetic intermediates. The process produces a compound represented by formula (5): wherein G1 is an alkylene group, R1 is a thiol protecting group, R2 is hydrogen or an amino protecting group, and Ar is an aryl group or a 5- to 7-membered heteroaryl group.

Abstract translation: 一种制备环状硫醚化合物及其合成中间体的方法。 该方法产生由式（5）表示的化合物：其中G 1是亚烷基，R 1是巯基保护基，R 2 O >是氢或氨基保护基，Ar是芳基或5至7元杂芳基。

公开(公告)号：US20050154001A1

公开(公告)日：2005-07-14

申请号：US11028281

申请日：2005-01-03

Applicant: Simona Ceccarelli ,  Synese Jolidon ,  Emmanuel Pinard ,  Andrew Thomas

Inventor： Simona Ceccarelli ,  Synese Jolidon ,  Emmanuel Pinard ,  Andrew Thomas

IPC: C07D471/10 ,  A61K31/4747

CPC classification number: C07D471/10

Abstract: The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy; R1 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, cyano, CF3, —OCF3, lower alkoxy, —SO2-lower alkyl and heteroaryl; R2 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF3, and lower alkoxy; R3 is hydrogen or lower alkyl; n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders.

Abstract translation: 本发明涉及下式的化合物其中AB是-CH 2 -CH 2 - ， - CH 2 -O - 或-O- CH 2 - ; X是氢或羟基; R 1是芳基，任选被一个或两个选自卤素，低级烷基，氰基，CF 3，-OCF 3， 低级烷氧基，-SO 2 - 低级烷基和杂芳基; R 2是任选被一个或两个选自卤素，低级烷基，CF 3 N 3和低级烷氧基的取代基取代的芳基; R 3是氢或低级烷基; n为0,1或2; 或其药物活性盐。 本发明的化合物可用于治疗神经和神经精神障碍。