公开(公告)号：US20060063930A1

公开(公告)日：2006-03-23

申请号：US11208460

申请日：2005-08-19

Applicant: Gregory Agoston ,  Todd Hembrough ,  Theresa LaVallee ,  Jamshed Shah ,  Lita Suwandi ,  Anthony Treston

Inventor： Gregory Agoston ,  Todd Hembrough ,  Theresa LaVallee ,  Jamshed Shah ,  Lita Suwandi ,  Anthony Treston

IPC: C07D261/18 ,  C07D235/30 ,  C07D403/02

CPC classification number: C07D295/185 ,  C07D205/04 ,  C07D207/34 ,  C07D213/56 ,  C07D213/82 ,  C07D231/40 ,  C07D233/64 ,  C07D235/26 ,  C07D235/30 ,  C07D241/26 ,  C07D249/04 ,  C07D261/18 ,  C07D275/03 ,  C07D277/46 ,  C07D403/06 ,  C07D487/04

Abstract: Compositions and methods comprising proteinase activated receptor antagonists are provided. More particularly, the present invention relates to the use of proteins, peptides and molecules that bind to proteinase activated receptor 2, and inhibit the processes associated with the activation of that receptor. More specifically, the present invention provides novel compositions and methods for the treatment of disorders and diseases such as those associated with abnormal cellular proliferation, angiogenesis, inflammation and cancer.

Abstract translation: 提供了包含蛋白酶激活的受体拮抗剂的组合物和方法。 更具体地，本发明涉及结合蛋白酶活化受体2的蛋白质，肽和分子的用途，并且抑制与该受体活化相关的过程。 更具体地，本发明提供了用于治疗疾病和疾病的新型组合物和方法，例如与异常细胞增殖，血管生成，炎症和癌症相关的疾病和疾病。

公开(公告)号：US07002021B2

公开(公告)日：2006-02-21

申请号：US10520838

申请日：2003-06-06

Applicant: Felix W. Grimm ,  Hans Joachim Metz ,  Joachim Weber ,  Andreas Wacker

Inventor： Felix W. Grimm ,  Hans Joachim Metz ,  Joachim Weber ,  Andreas Wacker

IPC: C09B57/00 ,  C07D235/26 ,  C07D403/04 ,  C09D11/00 ,  C08K5/3447

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D487/04 ,  C09B57/004

Abstract: Diketopyrrolopyrroles of the formula (I): wherein R1, R2, R3 and R4 independently of one another are a C1–C4 alkyl radical or a substituted or unsubstituted phenyl radical, wherein the phenyl radical can be substituted by 1, 2, 3 or 4 substituents from the group C1–C4 alkyl, C1–C4 alkoxy, CN, F, Cl, Br, NO2, CF3, S—C1–C4 alkyl, phenyl or (C1–C2)alkylenephenyl, with the proviso that at least one of the radicals, R1, R2, R3, or R4, is one of the stated substituted or unsubstituted phenyl radicals.

Abstract translation: 式（I）的二酮吡咯并吡咯：<化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US20050272765A1

公开(公告)日：2005-12-08

申请号：US11145579

申请日：2005-06-03

Applicant: Jun Feng ,  Stephen Gwaltney ,  Michael Wallace ,  Zhiyuan Zhang

Inventor： Jun Feng ,  Stephen Gwaltney ,  Michael Wallace ,  Zhiyuan Zhang

IPC: A61K31/4184 ,  A61K31/4192 ,  A61K31/4745 ,  A61P3/10 ,  C07C255/58 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/18 ,  C07D235/26 ,  C07D249/18 ,  C07D401/04 ,  C07D471/02

CPC classification number: C07D235/06 ,  C07C255/58 ,  C07D235/08 ,  C07D235/12 ,  C07D235/18 ,  C07D235/26 ,  C07D249/18 ,  C07D401/04

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined herein.

Abstract translation: 提供化合物，药物组合物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含下式化合物：其中取代基如本文所定义。

公开(公告)号：US06960579B1

公开(公告)日：2005-11-01

申请号：US09674403

申请日：1999-05-10

Applicant: Jesse A. May ,  Thomas R. Dean ,  Najam A. Sharif ,  Hwang-Hsing Chen

Inventor： Jesse A. May ,  Thomas R. Dean ,  Najam A. Sharif ,  Hwang-Hsing Chen

IPC: C07D209/08 ,  C07D295/088 ,  C07D295/13 ,  C07D513/04 ,  A61K31/443 ,  A61K31/4965 ,  C07D241/02 ,  C07D279/02 ,  C07D401/12

CPC classification number: C07D295/088 ,  C07D209/08 ,  C07D217/04 ,  C07D235/26 ,  C07D295/13 ,  C07D401/12 ,  C07D513/04

Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.

公开(公告)号：US06943149B2

公开(公告)日：2005-09-13

申请号：US10390098

申请日：2003-03-17

Applicant: Han-Cheng Zhang ,  Bruce E. Maryanoff ,  David F. McComsey ,  Kimberly B. White

Inventor： Han-Cheng Zhang ,  Bruce E. Maryanoff ,  David F. McComsey ,  Kimberly B. White

IPC: A61K38/00 ,  C07D235/26 ,  C07K5/06 ,  G01R1/067 ,  G01R1/073 ,  G01R3/00 ,  H05K3/40

CPC classification number: C07K5/06191 ,  A61K38/00 ,  C07D235/26 ,  H01L2924/01013 ,  H01L2924/01023 ,  H01L2924/01024 ,  H01L2924/01027 ,  H01L2924/01029 ,  H01L2924/0104 ,  H01L2924/01042 ,  H01L2924/01044 ,  H01L2924/01045 ,  H01L2924/01046 ,  H01L2924/01047 ,  H01L2924/01074 ,  H01L2924/01076 ,  H01L2924/01077 ,  H01L2924/01078 ,  H01L2924/01079 ,  H05K3/4092

Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

Abstract translation: 本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂的新型苯并咪唑酮肽模拟化合物 ，和神经变性疾病。 还公开了包含本发明的取代的苯并咪唑酮肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

公开(公告)号：US20050131039A1

公开(公告)日：2005-06-16

申请号：US10991861

申请日：2004-11-19

Applicant: Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

Inventor： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

IPC: A61P9/12 ,  C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  A61K31/4184 ,  C07D43/02

CPC classification number: C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

Abstract: A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m- or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.

Abstract translation: 一种制备由下式表示的化合物的方法：其中环A是除R'基之外可被取代的苯环; R 1是氢或任选取代的烃残基; X是在亚苯基和苯基之间具有原子长度或者两个或更少的直接键或间隔子; Y是-O - ， - S（O）m - 或-N（R 4） - ，其中m是0,1或2的整数，R 4是 氢或任选取代的烷基; R'是羧基，其酯，其酰胺或能够形成阴离子的基团或可转化的基团; n为1或2的整数; 其包括使由下式表示的化合物脱保护：其中R是三苯甲基，2-四氢吡喃基，甲氧基甲基或乙氧基甲基，其它符号如上定义; 或其盐。

公开(公告)号：US20050043379A1

公开(公告)日：2005-02-24

申请号：US10900152

申请日：2004-07-27

Applicant: Frank Axe ,  Scott Bembenek ,  Christopher Butler ,  James Edwards ,  Anne Fourie ,  Cheryl Grice ,  Brad Savall ,  Kevin Tays ,  Jianmei Wei

Inventor： Frank Axe ,  Scott Bembenek ,  Christopher Butler ,  James Edwards ,  Anne Fourie ,  Cheryl Grice ,  Brad Savall ,  Kevin Tays ,  Jianmei Wei

IPC: A61P29/00 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/10 ,  A61K31/428 ,  A61K31/4184 ,  A61K31/423

CPC classification number: C04B35/632 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/10

Abstract: Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation.

Abstract translation: 白细胞三烯A4水解酶（LTA4H）抑制剂，含有它们的组合物，以及用于抑制LTA4H酶活性以及治疗，预防或抑制与炎症相关的炎症和/或病症的方法。

公开(公告)号：US20050014812A1

公开(公告)日：2005-01-20

申请号：US10860139

申请日：2004-06-04

Applicant: Hisashi Hayashida ,  Keiko Hatanaka ,  Takeshi Kato ,  Yoshiyuki Kido ,  Masaki Tomishima ,  Hiroshi Kayakiri ,  Ichiro Takase ,  Takahiro Hiramura

Inventor： Hisashi Hayashida ,  Keiko Hatanaka ,  Takeshi Kato ,  Yoshiyuki Kido ,  Masaki Tomishima ,  Hiroshi Kayakiri ,  Ichiro Takase ,  Takahiro Hiramura

IPC: C07D235/08 ,  C07D235/10 ,  C07D235/26 ,  C07D235/28 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D417/06 ,  A61K31/4184 ,  C07D235/20 ,  C07

CPC classification number: C07D401/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/26 ,  C07D235/28 ,  C07D401/12 ,  C07D413/06 ,  C07D417/06

Abstract: The present invention provides novel benzimidazole compounds of the formula (I): wherein each symbol is as defined in the specification, salts thereof and prodrugs thereof, which are useful in treating, for example, the diseases curable through decrease in blood sugar level.

Abstract translation: 本发明提供新的式（I）的苯并咪唑化合物：其中每个符号如本说明书中所定义，其盐和前药，其可用于治疗例如通过降低血糖水平可治愈的疾病。

公开(公告)号：US20040204409A1

公开(公告)日：2004-10-14

申请号：US10816700

申请日：2004-04-02

Inventor： Kazuo Ando ,  Makoto Kawai ,  Mitsuhiro Kawamura ,  Miyako Matsumizu ,  Asato Morita ,  Isao Sakurada

IPC: A61K031/537 ,  A61K031/495 ,  C07D265/30 ,  C07D211/26

CPC classification number: C07D239/94 ,  C07D209/08 ,  C07D215/12 ,  C07D215/26 ,  C07D231/56 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/26 ,  C07D261/20 ,  C07D263/56 ,  C07D471/04

Abstract: This invention provides a compound of the formula (I): 1 wherein R1 and R2 independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract translation: 本发明提供式（I）化合物：其中R 1和R 2独立地表示氢原子等; X表示共价键或类似物：A表示具有8至12个环原子的双环，芳族，饱和或部分不饱和的杂环或碳环基团; B表示苯基或具有5〜6个环原子的杂芳基等：这些化合物可用于治疗NMDA NR2B受体过度活化引起的疾病状况，例如哺乳动物的疼痛等 。 本发明还提供了包含上述化合物的药物组合物。

公开(公告)号：US06794402B2

公开(公告)日：2004-09-21

申请号：US10276054

申请日：2002-11-12

Applicant: Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

Inventor： Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

IPC: A61K31423

CPC classification number: C07D263/58 ,  C07D235/26 ,  C07D277/68 ,  C07D413/12 ,  C07D417/12

Abstract: Described are bicycle-substituted cyclohexylamines of Formula I and their pharmaceutically acceptable salts thereof: The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are defined in the specification.

Abstract translation: 描述了式I的自行车取代的环己胺及其药学上可接受的盐：该化合物是可用于治疗脑血管病症例如脑缺血，心脏停搏，中风和帕金森病的NMDA受体通道复合物的拮抗剂。 取代基在说明书中定义。