公开(公告)号：US07250519B2

公开(公告)日：2007-07-31

申请号：US10494081

申请日：2002-10-25

Applicant: Philipp Stössel ,  Hubert Spreitzer ,  Heinrich Becker

Inventor： Philipp Stössel ,  Hubert Spreitzer ,  Heinrich Becker

IPC: C07D211/05 ,  C07D43/02 ,  C07D29/10

CPC classification number: C07C209/10 ,  C07C2603/97 ,  H01L51/0059 ,  C07C211/61

Abstract: The invention relates to a method for the production of tertiary amines by reaction of secondary amines with aromatics or heteroaromatics in the presence of a base, a nickel or palladium compound and one or several phosphines, dialkoxy-, and/or diaryloxyphosphines in an inert solvent.Aromatic or heteroaromatics of this type play an important role in industry as reagents or intermediates for pharmaceuticals and agrochemicals and in diverse fine and electronics chemicals, above all in the rapidly growing field of organic semi-conductors, in particular in organic or polymeric light diodes, organic solar cells and organic ICs.

Abstract translation: 本发明涉及通过仲胺与芳族化合物或杂芳族化合物在碱，镍或钯化合物和一种或多种膦，二烷氧基和/或二芳氧基膦在惰性溶剂中的存在下反应生产叔胺的方法 。 这种类型的芳族或杂芳族化合物在工业中作为药物和农用化学品的试剂或中间体以及各种精细和电子化学品，尤其是在有机半导体，特别是有机或聚合物光二极管的快速增长的领域中尤其重要， 有机太阳能电池和有机IC。

公开(公告)号：US07241777B2

公开(公告)日：2007-07-10

申请号：US10508185

申请日：2003-03-18

Applicant: Patrick René Angibaud ,  Marc Gaston Venet ,  Christophe Meyer ,  Henry Joseph Breslin

Inventor： Patrick René Angibaud ,  Marc Gaston Venet ,  Christophe Meyer ,  Henry Joseph Breslin

IPC: A01N43/42 ,  A61K31/47 ,  C07D215/00 ,  A61K31/498 ,  C07D43/02

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D471/04

Abstract: This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract translation: 本发明包括式（I）的新化合物，其中r，t，Y 1，Y 2，R 1，R 2， 2，R 3，R 5，R 6和R 7具有定义的含义，具有 法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US07214681B2

公开(公告)日：2007-05-08

申请号：US10776584

申请日：2004-02-10

Applicant: Matthew Colin Thor Fyfe ,  Lisa Sarah Gardner ,  Maseo Nawano ,  Martin James Procter ,  Chrystelle Marie Rasamison ,  Karen Lesley Schofield ,  Vilasben Kanji Shah ,  Kosuke Yasuda

Inventor： Matthew Colin Thor Fyfe ,  Lisa Sarah Gardner ,  Maseo Nawano ,  Martin James Procter ,  Chrystelle Marie Rasamison ,  Karen Lesley Schofield ,  Vilasben Kanji Shah ,  Kosuke Yasuda

IPC: A61K31/502 ,  C07D43/02

CPC classification number: C07D231/12 ,  C07D211/34 ,  C07D213/55 ,  C07D233/56 ,  C07D249/08 ,  C07D277/30 ,  C07D277/40 ,  C07D277/46 ,  C07D307/54 ,  C07D309/04 ,  C07D309/08 ,  C07D333/24 ,  C07D333/28 ,  C07D335/02 ,  C07D405/10 ,  C07D405/12 ,  C07D407/12 ,  C07D409/10 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08

Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.

Abstract translation: 式（I）化合物或其药学上可接受的盐可用于预防和治疗高血糖症和糖尿病。

公开(公告)号：US20070027159A1

公开(公告)日：2007-02-01

申请号：US10867546

申请日：2004-06-14

Applicant: Donald Kyle ,  Qun Sun ,  Laykea Tafesse

Inventor： Donald Kyle ,  Qun Sun ,  Laykea Tafesse

IPC: C07D417/02 ,  C07D43/02 ,  C07D41/02

CPC classification number: C07D211/78 ,  C07D213/02 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.

Abstract translation: 下式的化合物：其中Ar 1，Ar 2，V，X，R 3，R 4， 和m如本文所公开或其药学上可接受的盐（“环（杂）烯基化合物”）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

公开(公告)号：US07087614B2

公开(公告)日：2006-08-08

申请号：US10173442

申请日：2002-06-17

Applicant: Junqing Guo ,  Joseph Barbosa ,  William John Pitts ,  Marianne Carlsen ,  Claude Quesnelle ,  Marco Dodier

Inventor： Junqing Guo ,  Joseph Barbosa ,  William John Pitts ,  Marianne Carlsen ,  Claude Quesnelle ,  Marco Dodier

IPC: A61K31/513 ,  A61K31/506 ,  A61K31/505 ,  C07D43/02 ,  C07D277/42

CPC classification number: C07D417/14 ,  A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/522 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/16 ,  C07D487/04 ,  C07D491/10

Abstract: Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, Z, J and L are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.

Abstract translation: 其中R 1，R 2，Z，J和L的嘧啶磷酸二酯酶7（PDE 7）抑制剂其中R 1，R 2，Z，J和L如本文所述，并且提供其类似物是有用的 在治疗T细胞介导的疾病。

公开(公告)号：US20060135519A2

公开(公告)日：2006-06-22

申请号：US11030416

申请日：2005-01-06

Applicant: Alexander NIVOROZHKIN ,  John VAN DUZER ,  Garry SOUTHAN ,  Siya RAM ,  Qi ZENG

Inventor： Alexander NIVOROZHKIN ,  John VAN DUZER ,  Garry SOUTHAN ,  Siya RAM ,  Qi ZENG

IPC: A61K31/5377 ,  A61K31/454 ,  C07D413/02 ,  C07D43/02 ,  A61K31/41

CPC classification number: C07D257/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: Abstract of the DisclosureABSTRACT5-ARYLTETRAZOLES COMPOUNDS AND COMPOSITIONS THEREOFThe present invention relates to 5-Aryltetrazole Compounds, compositions comprising an effective amount of a 5-Arytetrazole Compound, and methods for treating an inflammation disease, a reperfusion disease, or hyperuricemia in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.

Abstract translation: 摘要摘要5-亚油酸酯化合物及其组合物本发明涉及5-芳基四唑化合物，包含有效量的5-三硝基吡唑化合物的组合物，以及用于治疗动物体内炎症疾病，再灌注疾病或高尿酸血症的方法 其需要包括向动物施用有效量的5-芳基四唑化合物。

公开(公告)号：US20060116364A1

公开(公告)日：2006-06-01

申请号：US11158245

申请日：2005-06-22

Applicant: Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

Inventor： Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

IPC: A61K31/55 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/405 ,  A61K31/4025 ,  C07D417/02 ,  C07D43/02

CPC classification number: C07C217/22 ,  C07C215/78 ,  C07C217/18 ,  C07C217/78 ,  C07C217/84 ,  C07C219/34 ,  C07C323/25 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/09 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/44 ,  C07D211/14 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D213/38 ,  C07D213/64 ,  C07D213/73 ,  C07D223/16 ,  C07D243/08 ,  C07D277/66 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D309/04 ,  C07D309/14 ,  C07D311/58 ,  C07D317/66 ,  C07D333/20 ,  C07D333/58 ,  C07D405/12 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07D491/10 ,  C07F5/025 ,  C07F7/1804 ,  C07F7/2208

Abstract: The present invention provides a compound represented by the following formula [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof

Abstract translation: 本发明提供由下式表示的化合物[其中T表示单键，可具有取代基的C 1 -C 4亚烷基等; 式（I-1）表示单键或双键; A表示单键，可以具有取代基的二价5〜14元杂环基等; Y表示单键等; Z表示亚甲基等; 环G表示可以用5-至6-元环缩合并可具有杂原子的亚苯基等; R a和R b彼此相同或不同，表示氢原子等; W代表单键等; R'表示1〜4个独立的氢原子等; R“表示1〜4个独立的氢原子等]或其盐或其水合物

公开(公告)号：US20060106062A1

公开(公告)日：2006-05-18

申请号：US11130359

申请日：2005-05-16

Applicant: Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

Inventor： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

IPC: A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

Abstract translation: 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

公开(公告)号：US20060009472A1

公开(公告)日：2006-01-12

申请号：US11158574

申请日：2005-06-20

Applicant: Weibo Wang ,  Paul Barsanti ,  Yi Xia ,  Rustum Boyce ,  Sabina Pecchi ,  Nathan Brammeier ,  Megan Phillips ,  Kris Mendenhall ,  Kelly Wayman ,  Liana Lagniton ,  Ryan Constantine ,  Hong Yang ,  Elizabeth Mieuli ,  Savithri Ramurthy ,  Elisa Jazan ,  Anu Sharma ,  Rama Jain ,  Sharadha Subramanian ,  Paul Renhowe ,  Kenneth Bair ,  David Duhl ,  Annette Walter ,  Tinya Abrams ,  Kay Huh ,  Eric Martin ,  Mark Knapp ,  Vincent Le

Inventor： Weibo Wang ,  Paul Barsanti ,  Yi Xia ,  Rustum Boyce ,  Sabina Pecchi ,  Nathan Brammeier ,  Megan Phillips ,  Kris Mendenhall ,  Kelly Wayman ,  Liana Lagniton ,  Ryan Constantine ,  Hong Yang ,  Elizabeth Mieuli ,  Savithri Ramurthy ,  Elisa Jazan ,  Anu Sharma ,  Rama Jain ,  Sharadha Subramanian ,  Paul Renhowe ,  Kenneth Bair ,  David Duhl ,  Annette Walter ,  Tinya Abrams ,  Kay Huh ,  Eric Martin ,  Mark Knapp ,  Vincent Le

IPC: A61K31/5377 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/4178 ,  C07D417/02 ,  C07D43/02

CPC classification number: C07D233/54 ,  C07D233/24 ,  C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D498/10

Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:

公开(公告)号：US20060004195A1

公开(公告)日：2006-01-05

申请号：US11168938

申请日：2005-06-28

Applicant: Xiaohu Deng ,  Neelakandha Mani ,  Christopher Mapes

Inventor： Xiaohu Deng ,  Neelakandha Mani ,  Christopher Mapes

IPC: C07D43/02 ,  C07D413/02 ,  C07D417/02

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14

Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators which have the general formula: wherein Ar is an aromatic or heteroaromatic group, X is a hydrocarbon linker, Y is a bond or hydrocarbon linker and R1, R2, R3, R4 and R5 are certain organic substituents, methods for making the same, and stereoselective dehydration methods for generally making α,β-unsaturated esters, acids and their derivatives.

Abstract translation: 本发明提供了具有以下通式的某些基于吡唑的CCK-1受体调节剂：其中Ar是芳族或杂芳族基团，X是烃连接基，Y是键或烃连接基，R 1， R 2，R 3，R 4，R 4和R 5是某些有机取代基，R 1，R 2，R 4， 制备与通常制备α，β-不饱和酯，酸及其衍生物的相同的立体选择性脱水方法。