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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：US20070270473A1
公开(公告)日：2007-11-22
申请号：US11564815
申请日：2006-11-29
IPC分类号： A61K31/44 , A61K31/40 , C07D211/82 , C07D207/30
CPC分类号： C07D249/08 , C07D271/06 , C07D401/04
摘要： Compounds that modulate GHS-R are described, for examples compounds formula (I)
摘要翻译： 描述了调节GHS-R的化合物，例如化合物式（I）
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公开(公告)号：US20060293370A1
公开(公告)日：2006-12-28
申请号：US11451086
申请日：2006-06-12
IPC分类号： A61K31/4245 , A61K31/4196 , C07D271/06 , C07D249/12 , C07D249/14
CPC分类号： C07D249/08 , C07D271/06 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04
摘要： Compounds that modulate GHS-R are described, for examples compounds formula (I)
摘要翻译： 描述了调节GHS-R的化合物，例如化合物式（I）
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公开(公告)号：US20110152232A1
公开(公告)日：2011-06-23
申请号：US12912266
申请日：2010-10-26
IPC分类号： A61K31/4245 , C07D271/06 , C07D249/08 , C07D413/04 , C07D405/04 , C07D403/04 , C07D417/04 , C07D409/04 , C07D471/04 , C07D401/04 , A61K31/4196 , A61K31/4439 , A61K31/428 , A61K31/427 , A61K31/437 , A61K31/538 , A61P3/04 , A61P3/00 , A61P3/10
CPC分类号： C07D249/08 , C07D271/06 , C07D401/04
摘要： Compounds that modulate GHS-R are described, for examples compounds formula (I)
摘要翻译： 描述了调节GHS-R的化合物，例如化合物式（I）
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公开(公告)号：US07829589B2
公开(公告)日：2010-11-09
申请号：US11564815
申请日：2006-11-29
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08 , C07D271/06 , C07D401/04
摘要： Compounds that modulate GHS-R are described, for examples compounds formula (I)
摘要翻译： 描述了调节GHS-R的化合物，例如化合物式（I）
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公开(公告)号：US20060205697A1
公开(公告)日：2006-09-14
申请号：US11272019
申请日：2005-11-14
申请人： Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
发明人： Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
摘要： The present invention relates to novel synthetic derivatives of betulin and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译： 本发明涉及新颖的桦木素合成衍生物和药物衍生物的用途。 本发明涉及新的式I化合物：或其药学上可接受的盐或前药。
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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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8.发明申请Indole, azaindole and related heterocyclic N-substituted piperazine derivatives 审中-公开吲哚，氮杂吲哚和相关杂环N-取代的哌嗪衍生物公开(公告)号：US20050261296A1
公开(公告)日：2005-11-24
申请号：US11029673
申请日：2005-01-05
申请人： Kap-Sun Yeung , Michelle Farkas , John Kadow , Nicholas Meanwell , Malcolm Taylor , David Johnston , Thomas Coulter , J. Wright
发明人： Kap-Sun Yeung , Michelle Farkas , John Kadow , Nicholas Meanwell , Malcolm Taylor , David Johnston , Thomas Coulter , J. Wright
IPC分类号： A61K31/405 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/502 , A61K31/517 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D471/02 , C07D471/04 , C07D487/04 , C07D491/04 , C07D43/14
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D491/04
摘要： This invention provides compounds of Formula I, including pharmaceutically accceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is
摘要翻译： 本发明提供具有药物和生物影响性质的式I化合物，包括其药学上可接受的盐，其药物组合物和使用方法。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 式I的化合物具有下式：其中：Z为Q选自m为2; A选自噌啉基，萘啶基，喹喔啉基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹唑啉基，氮杂苯并呋喃基和酞嗪基，其各自可以任选被一个或两个独立地选自甲基，甲氧基，羟基，氨基 和卤素; 和-W-是
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公开(公告)号：US20050143426A1
公开(公告)日：2005-06-30
申请号：US11061084
申请日：2005-02-18
申请人： Michael Kelly , Shimin Xu , Ning Xi , Philip Miller , John Kincaid , Chiara Ghiron , Thomas Coulter
发明人： Michael Kelly , Shimin Xu , Ning Xi , Philip Miller , John Kincaid , Chiara Ghiron , Thomas Coulter
IPC分类号： A61K31/137 , A61K31/145 , A61K31/167 , A61K31/275 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/4045 , A61K31/417 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/4465 , A61K31/47 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/5377 , A61P3/14 , A61P5/18 , A61P5/20 , A61P19/10 , C07B53/00 , C07C209/28 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/55 , C07C215/46 , C07C217/54 , C07C217/58 , C07C229/38 , C07C233/43 , C07C235/20 , C07C237/30 , C07C255/58 , C07C255/59 , C07C275/40 , C07C311/08 , C07C317/32 , C07D207/26 , C07D207/32 , C07D207/325 , C07D209/08 , C07D209/10 , C07D209/44 , C07D211/22 , C07D211/26 , C07D211/70 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/62 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/82 , C07D215/12 , C07D231/56 , C07D233/22 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D237/14 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/47 , C07D241/12 , C07D241/42 , C07D249/18 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D271/12 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/66 , C07D277/78 , C07D285/00 , C07D285/01 , C07D295/096 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/42 , C07D307/52 , C07D307/68 , C07D317/46 , C07D317/54 , C07D317/58 , C07D319/18 , C07D321/10 , C07D333/16 , C07D333/20 , C07D333/56 , C07D401/12 , C07D405/12 , C07D471/04 , C07D473/00 , C07D487/04 , A61K31/138 , A61K31/44
CPC分类号： C07C233/36 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/55 , C07C215/46 , C07C217/54 , C07C217/58 , C07C229/38 , C07C233/43 , C07C233/46 , C07C235/20 , C07C237/30 , C07C255/58 , C07C255/59 , C07C275/40 , C07C311/08 , C07C317/32 , C07C2601/02 , C07D207/26 , C07D207/27 , C07D207/325 , C07D209/08 , C07D209/10 , C07D209/44 , C07D211/22 , C07D211/70 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/75 , C07D213/82 , C07D215/12 , C07D215/14 , C07D231/56 , C07D233/22 , C07D235/06 , C07D235/10 , C07D235/12 , C07D237/08 , C07D237/14 , C07D239/26 , C07D239/34 , C07D239/42 , C07D241/12 , C07D241/42 , C07D249/18 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/08 , C07D271/10 , C07D271/12 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/66 , C07D285/01 , C07D295/096 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/42 , C07D307/52 , C07D307/68 , C07D317/46 , C07D317/54 , C07D319/18 , C07D321/10 , C07D333/16 , C07D333/20 , C07D333/56 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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公开(公告)号：US20050075364A1
公开(公告)日：2005-04-07
申请号：US10871931
申请日：2004-06-18
申请人： Kap-Sun Yeung , Michelle Farkas , John Kadow , Nicholas Meanwell , Malcolm Taylor , David Johnston , Thomas Coulter , J. J. Wright
发明人： Kap-Sun Yeung , Michelle Farkas , John Kadow , Nicholas Meanwell , Malcolm Taylor , David Johnston , Thomas Coulter , J. J. Wright
IPC分类号： A61K31/405 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/502 , A61K31/517 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D471/02 , C07D471/04 , C07D487/04 , C07D491/04
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D491/04
摘要： This invention provides compounds of Formula I, including pharmaceutically accceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is
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