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公开(公告)号：US08669249B2
公开(公告)日：2014-03-11
申请号：US13260680
申请日：2010-03-26
IPC分类号： C07D265/36 , C07D413/06 , A61K31/538
CPC分类号： C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/12
摘要： Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
摘要翻译： 提供下式的化合物用于抑制聚（ADP-核糖）聚合酶（PARP）：其中变量在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。
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公开(公告)号：US07741494B2
公开(公告)日：2010-06-22
申请号：US11932860
申请日：2007-10-31
申请人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
发明人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
IPC分类号： C07D231/56 , A01N43/56
CPC分类号： C07D231/12 , C07D209/18 , C07D209/44 , C07D231/14 , C07D231/20 , C07D231/38 , C07D231/56 , C07D249/18 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/06 , C07D409/12 , C07D471/04
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.
摘要翻译： 提供化合物，药物组合物，试剂盒和方法用于HDAC，其包含选自以下的化合物：其中取代基如本文所定义。
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公开(公告)号：US20080119648A1
公开(公告)日：2008-05-22
申请号：US11932995
申请日：2007-10-31
申请人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
发明人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
IPC分类号： C07D231/56 , C07D413/02 , C07D401/02 , C07D471/04 , C07D249/16 , C07D403/02 , C07D209/00
CPC分类号： C07D231/12 , C07D209/18 , C07D209/44 , C07D231/14 , C07D231/20 , C07D231/38 , C07D231/56 , C07D249/18 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/06 , C07D409/12 , C07D471/04
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.
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公开(公告)号：US20080114037A1
公开(公告)日：2008-05-15
申请号：US11932727
申请日：2007-10-31
申请人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
发明人： Jerome C. Bressi , Anthony R. Gangloff , Lily Kwok
IPC分类号： A61K31/4192 , A61K31/415 , A61K31/40 , C07D249/16 , C07D207/30
CPC分类号： C07D231/12 , C07D209/18 , C07D209/44 , C07D231/14 , C07D231/20 , C07D231/38 , C07D231/56 , C07D249/18 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/06 , C07D409/12 , C07D471/04
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.
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公开(公告)号：US06593322B1
公开(公告)日：2003-07-15
申请号：US09668893
申请日：2000-09-21
申请人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
发明人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
IPC分类号： C07D21718
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/10 , C07D417/12
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译： 公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。 在一个具体实施方案中，化合物对ER-β对ER-α是选择性的。 公开了用于在表达其中的细胞和/或组织中调节ER-β的方法，包括优先ER-β的细胞和/或组织。 还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失 ，尿失禁，脱发，白内障，自然激素失衡和与暴露于环境化学物质相关的不良生殖影响。
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公开(公告)号：US06562854B2
公开(公告)日：2003-05-13
申请号：US09874412
申请日：2001-06-04
申请人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
发明人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
IPC分类号： A61K314184
CPC分类号： C07D231/12 , A61F5/445 , C07D233/56 , C07D235/20 , C07D249/08 , C07D401/14 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07F7/0812
摘要： Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
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公开(公告)号：US08541417B2
公开(公告)日：2013-09-24
申请号：US13387342
申请日：2010-07-29
IPC分类号： A61K31/519
CPC分类号： C07D471/14
摘要： Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
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公开(公告)号：US20120094992A1
公开(公告)日：2012-04-19
申请号：US13260680
申请日：2010-03-26
IPC分类号： A61K31/538 , A61P3/00 , A61P25/28 , A61P9/00 , A61P9/10 , C07D265/36 , A61P35/00
CPC分类号： C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/12
摘要： Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
摘要翻译： 提供下式的化合物用于抑制聚（ADP-核糖）聚合酶（PARP）：其中变量在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。
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公开(公告)号：US20100190763A1
公开(公告)日：2010-07-29
申请号：US12691668
申请日：2010-01-21
IPC分类号： A61K31/397 , A61K31/551 , A61K31/542 , A61K31/5383 , A61K31/53 , A61K31/4985 , C07D471/16 , C07D417/14 , C07D498/14 , C07D403/14 , C07D471/14 , C07D401/04 , A61P25/28 , A61P3/00 , A61P9/10 , A61P7/08 , A61P29/00 , A61P35/00
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和t在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US07381825B2
公开(公告)日：2008-06-03
申请号：US10803575
申请日：2004-03-17
申请人： Jerome C. Bressi , Jason W. Brown , Sheldon X. Cao , Anthony R. Gangloff , Andrew J. Jennings , Jeffrey A. Stafford , Phong H. Vu , Xiao-Yi Xiao
发明人： Jerome C. Bressi , Jason W. Brown , Sheldon X. Cao , Anthony R. Gangloff , Andrew J. Jennings , Jeffrey A. Stafford , Phong H. Vu , Xiao-Yi Xiao
IPC分类号： C07D401/04
CPC分类号： C07D235/18 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/10
摘要： Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
摘要翻译： 可用于抑制组氨酸脱乙酰酶的化合物，其具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> ZQLM或ZLM <？in-line-formula description =“In-line 式“end =”tail“？>其中M是能够与脱乙酰酶催化部位和/或金属离子络合的取代基; L是在M取代基和化合物的其余部分之间分离0-10个原子之间的取代基; Z和Q如本文所定义。
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