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公开(公告)号：US20070142391A1
公开(公告)日：2007-06-21
申请号：US10545296
申请日：2004-02-06
IPC分类号： A61K31/496 , C07D403/14 , C07D405/14
CPC分类号： C07D231/12 , A61K31/16 , A61K31/495 , C07D233/56 , C07D241/04 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention is related to piperazine-2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R1 and R2 are as defined in the description.
摘要翻译： 本发明涉及式（I）的哌嗪-2-甲酰胺衍生物，其用于治疗和/或预防早产，早产，痛经和用于在剖宫产分娩前停止劳动。 其中A，X，Y，R 1和R 2如说明书中所定义。
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公开(公告)号：US20070203134A1
公开(公告)日：2007-08-30
申请号：US10571470
申请日：2004-09-10
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14 , C07D403/02
CPC分类号： C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.
摘要翻译： 本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。 所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）（I））。 本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。
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公开(公告)号：US20070185104A1
公开(公告)日：2007-08-09
申请号：US10571323
申请日：2004-09-10
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.
摘要翻译： 本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。 所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。 本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。 选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。
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4.发明申请Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists 审中-公开吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂公开(公告)号：US20060229343A1
公开(公告)日：2006-10-12
申请号：US11449802
申请日：2006-06-09
IPC分类号： A61K31/433 , A61K31/4245 , C07D413/14 , C07D417/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. B is a oxadiazole or thiadiazole group.
摘要翻译： 本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。 所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。 特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。 更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。 本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基。
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公开(公告)号：US20070060594A1
公开(公告)日：2007-03-15
申请号：US10555960
申请日：2004-05-03
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D401/06 , A61K31/505 , A61K31/53
摘要： The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.
摘要翻译： 本发明涉及吡啶基乙腈以及含有这种吡啶基乙腈的药物制剂。 所述吡啶基乙腈是蛋白激酶信号通路的调节剂，特别是涉及糖原激酶合成酶3或JNK的调节剂。 本发明还涉及制备吡啶基乙腈的方法。 X是取代或未取代的吡啶基。 G是未取代或取代的嘧啶基或三嗪基。
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公开(公告)号：US20050187275A1
公开(公告)日：2005-08-25
申请号：US10498356
申请日：2002-12-19
IPC分类号： A61K31/4196 , A61P1/16 , A61P9/04 , A61P9/12 , A61P13/12 , A61P15/06 , A61P15/12 , A61P15/14 , A61P27/02 , C07D249/10 , C07D249/12 , C07D249/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12
CPC分类号： C07D403/12 , C07D249/10 , C07D249/12 , C07D249/14 , C07D405/06 , C07D405/12
摘要： The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
摘要翻译： 本发明涉及特别用作药物活性化合物的式（I）的三唑衍生物以及含有这种三唑衍生物的药物制剂。 所述三唑可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。 特别地，本发明涉及显示催产素和/或加压素受体的显着调节，特别是拮抗活性的三唑衍生物。 更优选地，所述化合物可用于治疗和/或预防由催产素和/或加压素介导的疾病状态。 本发明还涉及新的三唑衍生物及其制备方法。
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公开(公告)号：US20060223813A1
公开(公告)日：2006-10-05
申请号：US10528437
申请日：2003-09-19
IPC分类号： A61K31/496
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds of formula I, R3. I N\′ N˜′ R2I(0)z- o R4 I wherein R′, R2, R3 and R4 are as defined in the claims and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译： 本发明提供式I R 3的2-甲酰胺哌嗪化合物。 其中R'，R 2，R“，R”，R“，R”，R“ 3和R 4如权利要求书和方法以及使用或包含一种或多种这样的化合物的药物组合物所定义。 本发明的化合物可用于治疗哺乳动物不育症。
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公开(公告)号：US20060074124A1
公开(公告)日：2006-04-06
申请号：US11077664
申请日：2005-03-11
申请人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
发明人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： A61K31/403 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D209/18 , C07D209/88 , C07D209/94 , C07D471/04
摘要： Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
摘要翻译： 本文描述式（I）化合物和通过施用式（I）化合物治疗病症的方法。 病症的实例包括肿瘤性疾病，脂肪细胞相关疾病，神经变性疾病和代谢紊乱。
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公开(公告)号：US20050261332A1
公开(公告)日：2005-11-24
申请号：US11098315
申请日：2005-04-04
申请人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Jean-Francois Pons , Russell Thomas , Manuel Navia , Thomas Coulter , Jeffrey Saunders , Bard Geesaman
发明人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Jean-Francois Pons , Russell Thomas , Manuel Navia , Thomas Coulter , Jeffrey Saunders , Bard Geesaman
IPC分类号： A61K31/422 , A61K31/4245 , A61K31/454 , A61K31/4745 , C07C311/32 , C07D413/02 , C07D471/02 , C07D471/10 , C07D43/02
CPC分类号： C07D471/10 , C07C311/32 , C07D401/12
摘要： Compounds of formulas (I), (II), (III), and (IV) and methods of treating disorders by administering a compound of formula (I), (II), (III), or (IV) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
摘要翻译： 本文描述式（I），（II），（III）和（IV）的化合物和通过施用式（I），（II），（III）或（IV）的化合物来治疗病症的方法。 病症的实例包括肿瘤性疾病，脂肪细胞相关疾病，神经变性疾病和代谢紊乱。
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公开(公告)号：US20050187237A1
公开(公告)日：2005-08-25
申请号：US10982997
申请日：2004-11-04
申请人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Manuel Navia , Russell Thomas , Jean-Francois Pons , Jeffrey Saunders
发明人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Manuel Navia , Russell Thomas , Jean-Francois Pons , Jeffrey Saunders
IPC分类号： A61K31/438 , A61K31/4747 , A61K31/5377 , C07D413/14 , C07D471/10
CPC分类号： C07D471/10 , C07D221/20 , C07D401/12
摘要： Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.
摘要翻译： 式（I）化合物在本文中描述。该化合物可用于例如调节生长激素促分泌素受体（GHS-R）。 在一些情况下，化合物可用于治疗肥胖症。
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