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1. 发明授权

US06809200B2 Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-one compounds and intermediates thereof 失效
标题翻译：吡唑并[4,3-d]嘧啶-7-酮化合物及其中间体的制备方法
公开(公告)号：US06809200B2
公开(公告)日：2004-10-26
申请号：US09916099
申请日：2001-07-26
申请人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , Joanna Teresa Negri , David James Rawson , Albert Shaw Wood
发明人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , Joanna Teresa Negri , David James Rawson , Albert Shaw Wood
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： A process is provide for the preparation of compounds of formula (I) herein comprising reacting a compound of formula (III), (IV) or (V) wherein the variables are as defined in the specification. The reaction is conducted in the presence of −OR3 and a hydroxide trapping agent or in the case of compounds of formula (IV) reacting in the presence of an auxiliary base and a hydroxide trapping agent.
摘要翻译：一种制备式（I）化合物的方法，其包括使式（III），（IV）或（V）化合物与变量如说明书中所定义的反应。反应在< - > OR 3和氢氧化物捕获剂的存在下进行，或在式（Ⅳ）化合物的情况下，在辅助碱和氢氧化物捕获剂的存在下反应。

2. 发明授权

US06806272B2 Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions 有权
标题翻译：二氢蝶啶酮，其制备方法及其作为药物组合物的用途
公开(公告)号：US06806272B2
公开(公告)日：2004-10-19
申请号：US10226710
申请日：2002-08-23
申请人： Eckhart Bauer , Steffen Breitfelder , Christian Eickmeier , Matthias Grauert , Matthias Hoffmann , Thorsten Lehmann-Lintz , Gerald Pohl , Jens Quant , Norbert Redemann , Gisela Schnapp , Martin Steegmaier
发明人： Eckhart Bauer , Steffen Breitfelder , Christian Eickmeier , Matthias Grauert , Matthias Hoffmann , Thorsten Lehmann-Lintz , Gerald Pohl , Jens Quant , Norbert Redemann , Gisela Schnapp , Martin Steegmaier
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D475/00
摘要： The present invention relates to new dihydropteridinones of the formula (I) wherein the groups X, R1, R2, R3, R4, R5 and R7 have the meanings given in the claims and the specification, the isomers thereof, processes and intermediates for preparing these dihydropteridinones as well as the use thereof as pharmaceutical compositions.
摘要翻译：本发明涉及式（I）的新的二氢蝶啶酮，其中基团X，R 1，R 2，R 3，R 4，R 5和R 7具有如下含义：权利要求书和说明书中给出的其异构体，用于制备这些二氢蝶啶烷酮的方法和中间体以及其作为药物组合物的用途。

3. 发明授权

US06794387B2 Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：US06794387B2
公开(公告)日：2004-09-21
申请号：US10099264
申请日：2002-03-14
申请人： Charlotte Moira Norfor Allerton , Kevin Neil Dack , Mark Ian Kemp
发明人： Charlotte Moira Norfor Allerton , Kevin Neil Dack , Mark Ian Kemp
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X, Y and A have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：通式（I）的化合物：其中R 1，R 2，R 3，R 4，X，Y和A具有本文给出的用于治疗和预防性治疗需要抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（如cGMP PDE5）的医疗条件。

4. 发明授权

US06762185B1 Compounds useful for treatment of cancer, compositions containing the same, and methods of their use 有权
标题翻译：可用于治疗癌症的化合物，含有它们的组合物及其使用方法
公开(公告)号：US06762185B1
公开(公告)日：2004-07-13
申请号：US10087005
申请日：2002-03-01
申请人： Michael Kahn , Masakatsu Eguchi , Sung Hwan Moon , Jae Uk Chung , Kwang Won Jeong
发明人： Michael Kahn , Masakatsu Eguchi , Sung Hwan Moon , Jae Uk Chung , Kwang Won Jeong
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/513 , A61K2300/00
摘要： The invention involves compounds having the general formula (I) as described in the claims and pharmaceutical compositions comprising such compounds. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer.
摘要翻译：本发明涉及如权利要求中所述的具有通式（I）的化合物和包含这些化合物的药物组合物。本发明还涉及这种化合物用于抑制或治疗由Wnt信号传导途径调节的疾病如癌症，特别是结肠直肠癌的用途。

5. 发明授权

US06747033B2 Fungicidal triazolopyrimid-7-ylideneamines 失效
标题翻译：杀真菌三唑并嘧啶-7-亚胺
公开(公告)号：US06747033B2
公开(公告)日：2004-06-08
申请号：US09879258
申请日：2001-06-12
申请人： Waldemar Pfrengle
发明人： Waldemar Pfrengle
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A01N43/90
摘要： Compounds of formula I in which R1 is alkyl, alkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, trihydrocarbylsilyl, formyl, alkanoyl or alkoxycarbonyl group being attached either to the nitrogen in the 3- or 4-position; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic groups containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R3 is phenyl, cycloalkyl or 5- or 6-membered heteroaryl containing besides carbon atoms one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R4 is halogen, amino, alkoxy, haloalkoxy, alkylamino or dialkylamino; wherein the bent line indicates that the double Bond may be located between the 3- and 9-position or the 4- and 9-Position; and the zigzag line indicates that the groups connected may have the (E)- or (Z)-configuration; R1 to R4 groups may be unsubstituted or substituted as defined in the description; processes for preparing these compounds, constituents comprising them and their use for controlling harmful fungi are described.
摘要翻译：式Iin的化合物，其中R 1是烷基，烷氧基烷基，环烷基烷基，烯基，炔基，链烯基，卤代烷基，三烃基甲硅烷基，甲酰基，烷酰基或烷氧基羰基，其连接在3-或4-位的氮上; R 2，含有1至4个氮原子或1至3个氮原子和1个硫或氧原子的5或6元杂芳基或杂环基，可以是氢，烷基，烯基，炔基，链烯基，卤代烷基，环烷基， R 3是苯基，环烷基或除了碳原子一至四个氮原子或一至三个氮原子以及一个硫或氧原子作为环成员的5-或6-元杂芳基; R 4是卤素，氨基，烷氧基，卤代烷氧基，烷基氨基或二烷基氨基;其中所述弯曲线表示双键可位于3-和9-位之间或4-和9-位; 和之字形线表示组可以具有（E） - 或（Z） - 构型; R 1至R 4基团可以是未被描述的或如说明书中所定义的取代基;制备这些化合物的方法，包含它们的组分及其用于控制描述有害真菌。

6. 发明授权

US06723719B1 Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction 失效
标题翻译：抑制5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP PDE5）治疗性功能障碍的吡唑并嘧啶酮
公开(公告)号：US06723719B1
公开(公告)日：2004-04-20
申请号：US09402229
申请日：1999-09-29
申请人： Mark Edward Bunnage , John Paul Mathias , Stephen Derek Albert Street , Anthony Wood
发明人： Mark Edward Bunnage , John Paul Mathias , Stephen Derek Albert Street , Anthony Wood
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D231/40
摘要： Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.
摘要翻译：式（IA）和（IB）化合物或其药学或兽医学上可接受的盐，或任一实体的药学上或兽医学上可接受的溶剂化物，其中R 1为被C 3至C 6环烷基取代的C 1至C 3烷基，CONR 5 R 6或N-连接的杂环基; （CH2）nHet或（CH2）nAr; R 2是C 1至C 6烷基; R 3是任选被C 1至C 4烷氧基取代的C 1至C 6烷基; R 4是SO 2 NR 7 R 8; R 5和R 6各自独立地选自H和任选被C 1至C 4烷氧基取代的C 1至C 4烷基，或与它们所连接的氮原子一起形成5-或6-元杂环组; R 7和R 8与它们所连接的氮原子一起形成4-R 10 - 哌嗪基; R 10是H或任选被OH，C 1至C 4烷氧基或CONH 2取代的C 1至C 4烷基; H是任选取代的C连接的5或6元杂环基; Ar是任选取代的苯基; 并且n为0或1; 是用于治疗男性勃起功能障碍和女性性功能障碍的有效和选择性的cGMP PDE5抑制剂。

7. 发明授权

US06699871B2 Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 有权
标题翻译： β-氨基杂环二肽基肽酶抑制剂，用于治疗或预防糖尿病
公开(公告)号：US06699871B2
公开(公告)日：2004-03-02
申请号：US10189603
申请日：2002-07-05
申请人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
发明人： Scott D. Edmondson , Michael H. Fisher , Dooseop Kim , Malcolm Maccoss , Emma R. Parmee , Ann E. Weber , Jinyou Xu
IPC分类号： C07D48704
CPC分类号： A61K31/4985 , A61K31/498 , A61K38/28 , A61K45/06 , C07D487/04 , Y10S514/866 , A61K2300/00
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

8. 发明授权

US06686366B1 Compounds specific to adenosine A3 receptor and uses thereof 失效
标题翻译：对腺苷A3受体特异性的化合物及其用途
公开(公告)号：US06686366B1
公开(公告)日：2004-02-03
申请号：US09454075
申请日：1999-12-02
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A3受体的化合物以及这些化合物用于治疗受试者中与A3腺苷受体有关的疾病的用途，其包括向受试者施用治疗有效量的化合物。

9. 发明授权

US06683081B2 Triazolotriazinones and the use thereof 失效
标题翻译：三唑并三嗪酮及其用途
公开(公告)号：US06683081B2
公开(公告)日：2004-01-27
申请号：US10149921
申请日：2002-10-21
申请人： Ulrich Niewöhner , Helmut Haning , Thomas Lampe , Mazen Es-Sayed , Gunter Schmidt , Erwin Bischoff , Klaus Dembowsky , Elisabeth Perzborn , Karl-Heinz Schlemmer
发明人： Ulrich Niewöhner , Helmut Haning , Thomas Lampe , Mazen Es-Sayed , Gunter Schmidt , Erwin Bischoff , Klaus Dembowsky , Elisabeth Perzborn , Karl-Heinz Schlemmer
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The invention relates to novel triazolotriazinones of the general formula (I), to a method for their production and to the pharmaceutical use thereof.
摘要翻译：本发明涉及通式（I）的新型三唑并三嗪酮及其制备方法及其药物用途。

10. 发明授权

US06670357B2 Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors 失效
标题翻译：治疗p38激酶相关病症的方法和可用作激酶抑制剂的吡咯并三嗪化合物
公开(公告)号：US06670357B2
公开(公告)日：2003-12-30
申请号：US10036293
申请日：2001-11-07
申请人： Katerina Leftheris , John Hynes , Stephen T. Wrobleski , Joel Barrish
发明人： Katerina Leftheris , John Hynes , Stephen T. Wrobleski , Joel Barrish
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups —ZR4R5 taken together comprise an —NH-substituted aryl.
摘要翻译：公开了治疗与p38激酶活性相关的一种或多种病症的方法，包括向有需要的患者施用至少一种具有式（I）的化合物或其药学上可接受的盐，前药或溶剂化物，其中R 3是氢，甲基，全氟甲基，甲氧基，卤素，氰基或NH 2，优选甲基，X，R 1至R 6和Z如说明书所述。有利的是基团-ZR 4 R 5一起包含-NH-取代的芳基。

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