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1. 发明授权

US06239146B1 Neurotrophic difluoroamide agents 有权
标题翻译：神经营养性二氟酰胺药物
公开(公告)号：US06239146B1
公开(公告)日：2001-05-29
申请号：US09590808
申请日：2000-06-09
申请人： Vivekananda M. Vrudhula , Gene M. Dubowchik , Bireshwar Dasgupta , Dolatrai M. Vyas
发明人： Vivekananda M. Vrudhula , Gene M. Dubowchik , Bireshwar Dasgupta , Dolatrai M. Vyas
IPC分类号： A61K31444
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60
摘要： The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel &agr;,&agr;-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及作为神经营养剂（即能够刺激神经组织的生长或增殖的化合物）的新型α，α-二氟乙酰胺化合物的设计，合成和肽基 - 脯氨酰异构酶（PPIase或旋转异构酶）抑制活性，结合免疫亲和素如FKBP12并抑制它们的旋转异构酶活性。本发明还涉及含有这些化合物的药物组合物。

2. 发明授权

US6096762A Neurotrophic difluoroamide agents 有权
标题翻译：神经营养性二氟酰胺药物
公开(公告)号：US6096762A
公开(公告)日：2000-08-01
申请号：US316792
申请日：1999-05-21
申请人： Vivekananda M. Vrudhula , Gene M. Dubowchik , Bireshwar Dasgupta , Dolatrai M. Vyas
发明人： Vivekananda M. Vrudhula , Gene M. Dubowchik , Bireshwar Dasgupta , Dolatrai M. Vyas
IPC分类号： A61K31/401 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/4545 , A61P25/00 , A61P43/00 , C07D207/16 , C07D211/60 , C07D401/12 , A61K31/166 , C07C59/347 , C07C225/10
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60
摘要： The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及作为神经营养剂（即能够刺激神经组织的生长或增殖的化合物）的新型α，α-二氟乙酰氨基化合物的设计，合成和肽基脯氨酰异构酶（PPIase或旋转异构酶）抑制活性，结合免疫亲和素如FKBP12并抑制它们的旋转异构酶活性。本发明还涉及包含这些化合物的药物组合物。

3. 发明授权

US07238699B2 Imidazolyl derivatives as corticotropin releasing factor inhibitors 有权
标题翻译：咪唑衍生物作为促肾上腺皮质激素释放因子抑制剂
公开(公告)号：US07238699B2
公开(公告)日：2007-07-03
申请号：US10771766
申请日：2004-02-04
申请人： Vivekananda M. Vrudhula , Bireshwar Dasgupta , Gene M. Dubowchik , John E. Macor
发明人： Vivekananda M. Vrudhula , Bireshwar Dasgupta , Gene M. Dubowchik , John E. Macor
IPC分类号： A61K31/519 , C07D487/04 , C07D403/04 , C07D471/04 , C07D471/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
摘要翻译：本发明涉及式（I）的新型杂环拮抗剂和包含可用于治疗抑郁症，焦虑症，情感障碍，进食障碍，创伤后应激的促皮质激素释放因子受体（“CRF受体”）的所述拮抗剂的药物组合物疾病，头痛，药物成瘾，炎性疾病，药物或酒精戒断症状和其它治疗可由CRF-1受体拮抗作用的其他病症。

4. 发明授权

US06888004B2 Imidazolyl derivatives as corticotropin releasing factor inhibitors 有权
标题翻译：咪唑衍生物作为促肾上腺皮质激素释放因子抑制剂
公开(公告)号：US06888004B2
公开(公告)日：2005-05-03
申请号：US10044183
申请日：2002-01-11
申请人： Gene M. Dubowchik , Vivekananda M. Vrudhula , Dmitry Zuev , Bireshwar Dasgupta , John E. Macor
发明人： Gene M. Dubowchik , Vivekananda M. Vrudhula , Dmitry Zuev , Bireshwar Dasgupta , John E. Macor
IPC分类号： A61K31/53 , A61K31/41 , A61K31/415 , A61K31/4188 , A61K31/437 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/499 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/04 , A61P5/04 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P15/06 , A61P15/08 , A61P19/10 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/32 , A61P25/36 , A61P29/00 , A61P37/04 , C07D235/02 , C07D249/00 , C07D401/00 , C07D403/02 , C07D471/14 , C07D471/22 , C07D487/00 , C07D487/04 , A61K31/44 , C07D515/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
摘要翻译：本发明涉及式（I）的新型杂环拮抗剂和包含可用于治疗抑郁症，焦虑症，情感障碍，进食障碍，创伤后应激的促皮质激素释放因子受体（“CRF受体”）的所述拮抗剂的药物组合物疾病，头痛，药物成瘾，炎性疾病，药物或酒精戒断症状和其它治疗可由CRF-1受体拮抗作用的其他病症。

5. 发明授权

US07211669B2 Imidazolyl derivatives as corticotropin releasing factor inhibitors 有权
公开(公告)号：US07211669B2
公开(公告)日：2007-05-01
申请号：US10767645
申请日：2004-01-29
申请人： Vivekananda M. Vrudhula , Dmitry Zuev , Bireshwar Dasgupta
发明人： Vivekananda M. Vrudhula , Dmitry Zuev , Bireshwar Dasgupta
IPC分类号： C07D235/02 , C07D401/00 , C07D471/02 , C07D487/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

6. 发明授权

US06939968B2 Atropisomers of 3-substituted-4-arylquinolin-2-one derivatives 失效
标题翻译： 3-取代-4-芳基喹啉-2-酮衍生物的阻转异构体
公开(公告)号：US06939968B2
公开(公告)日：2005-09-06
申请号：US10739449
申请日：2003-12-17
申请人： Vivekananda M. Vrudhula , Valentin Kala Gribkoff , Bireshwar Dasgupta , Christopher G. Boissard
发明人： Vivekananda M. Vrudhula , Valentin Kala Gribkoff , Bireshwar Dasgupta , Christopher G. Boissard
IPC分类号： C07D215/22 , C07D215/227 , C07D215/16 , A61K31/47 , C07D215/20
CPC分类号： C07D215/227
摘要： Atropisomers of 3-substituted-4-arylquinolin-2-one derivatives having the general formula wherein R, R1, R2, R3, R4 and R5, are as defined herein, or a non-toxic pharmaceutically acceptable salt, solvate or prodrug thereof. The atropisomers can modulate the large conductance calcium-activated K+ channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels. In addition, the atropisomers can be stable, i.e., do not interconvert, for periods of up to one month, or more.
摘要翻译：具有以下通式的3-取代-4-芳基喹啉-2-酮衍生物的阻转异构体其中R，R 1，R 2，R 3， R 4，R 5和R 5如本文所定义，或其无毒的药学上可接受的盐，溶剂合物或前药。阻转异构体可以调节大电导钙激活的K + +通道，并且可用于治疗对钾通道开放有反应的病症。此外，阻转异构体可以是稳定的，即不会相互转化，持续一个月或更长时间。

7. 发明申请

US20110166160A1 Pyrazinone Modulator of Corticotropin-Releasing Factor Receptor Activity 有权
标题翻译：吡嗪酮调节剂促皮质激素释放因子受体活性
公开(公告)号：US20110166160A1
公开(公告)日：2011-07-07
申请号：US13052458
申请日：2011-03-21
申请人： Richard A. Hartz , Vijay T. Ahuja , Vivekananda M. Vrudhula , Joanne J. Bronson
发明人： Richard A. Hartz , Vijay T. Ahuja , Vivekananda M. Vrudhula , Joanne J. Bronson
IPC分类号： A61K31/4965 , A61P25/24 , A61P25/22
CPC分类号： C07D401/12
摘要： The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.
摘要翻译：本发明涉及化合物（S）-4-（1-环丙基-2-甲氧基乙基）-6-（6-（二氟甲氧基）-2,5-二甲基吡啶-3-基氨基）-5-氧代-4,5- 二氢吡嗪-2-腈，化合物的药物组合物，以及使用该化合物治疗精神疾病和神经疾病的方法，包括抑郁症，焦虑症，肠易激综合征，药物和酒精戒断的成瘾和消极方面等与CRF相关的条件。

8. 发明授权

US5549883A Chemically defined polymeric carriers for release of covalently linked agents 失效
标题翻译：用于释放共价连接剂的化学定义的聚合物载体
公开(公告)号：US5549883A
公开(公告)日：1996-08-27
申请号：US71357
申请日：1993-06-03
申请人： Ananthachari Srinivasan , Vivekananda M. Vrudhula , Diana I. Brixner
发明人： Ananthachari Srinivasan , Vivekananda M. Vrudhula , Diana I. Brixner
IPC分类号： A61K47/48 , A61K51/10 , C07K7/02 , A61K51/08 , A61K49/00 , C07K1/00 , C07K2/00
CPC分类号： A61K47/48246 , A61K51/1093 , C07K7/02
摘要： A chemically defined polymeric carrier comprising a series of .alpha.-amino acids in any combination containing side chains to which diagnostic/therapeutic and chelating agents can be covalently joined through cleavable linkers either directly or covalently joined through cleavable linkers after chemical modification of the side chains. Hydrazone, disulfide, and ester linkages in any combination can be present in the polymeric carrier between the side chains of the .alpha.-amino acids and the agents. The presence of a particular covalent linkage between the side chain and the agent in the carrier is determined by the functional group present in the side chain of the .alpha.-amino acid and the functional group present in the agent. The .alpha.-amino acids with side chains to which agents do not covalently join can function as spacers to minimize interaction between bulky molecules attached to the polymeric carrier. In addition, those .alpha.-amino acids with charged or hydrophilic side chains to which agents do not covalently join can provide increased solubility to the polymeric carrier.
摘要翻译：一种化学上定义的聚合物载体，其包含任何组合的含有侧链的一系列α-氨基酸，诊断/治疗和螯合剂可以通过侧链化学修饰之后直接或共价连接在可切割接头上，通过可切割接头共价连接。任何组合中的腙，二硫化物和酯键可以存在于α-氨基酸的侧链与试剂之间的聚合物载体中。载体中侧链和试剂之间特定共价键的存在由存在于该α-氨基酸的侧链中的官能团和该试剂中存在的官能团来确定。具有不共价连接的侧链的α-氨基酸可以作为间隔物，以使连接到聚合物载体上的大体积分子之间的相互作用最小化。此外，具有带电荷或亲水侧链的α-氨基酸与试剂不共价连接的那些可以提供增加的对聚合物载体的溶解度。

9. 发明授权

US08372847B2 Pyrazinone modulator of corticotropin-releasing factor receptor activity 有权
标题翻译：吡嗪酮调节剂促肾上腺皮质激素释放因子受体活性
公开(公告)号：US08372847B2
公开(公告)日：2013-02-12
申请号：US13052458
申请日：2011-03-21
申请人： Richard A. Hartz , Vijay T. Ahuja , Vivekananda M. Vrudhula , Joanne J. Bronson
发明人： Richard A. Hartz , Vijay T. Ahuja , Vivekananda M. Vrudhula , Joanne J. Bronson
IPC分类号： A61K31/4965
CPC分类号： C07D401/12
摘要： The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.
摘要翻译：本发明涉及化合物（S）-4-（1-环丙基-2-甲氧基乙基）-6-（6-（二氟甲氧基）-2,5-二甲基吡啶-3-基氨基）-5-氧代-4,5- 二氢吡嗪-2-腈，化合物的药物组合物，以及使用该化合物治疗精神疾病和神经疾病的方法，包括抑郁症，焦虑症，肠易激综合征，药物和酒精戒断的成瘾和消极方面等与CRF相关的条件。

10. 发明授权

US5521290A Targeting substance-diagnostic/therapeutic agent conjugates having schiff base linkages and methods for their preparation 失效
标题翻译：具有希夫碱基键的靶向物质 - 诊断/治疗剂缀合物及其制备方法
公开(公告)号：US5521290A
公开(公告)日：1996-05-28
申请号：US342789
申请日：1994-11-21
申请人： Gowsala P. Sivam , A. Charles Morgan, Jr. , Vivekananda M. Vrudhula
发明人： Gowsala P. Sivam , A. Charles Morgan, Jr. , Vivekananda M. Vrudhula
IPC分类号： A61K47/48 , A61K51/10 , C07D207/40 , C07D207/404 , C07D207/44 , C07D207/452 , C07H15/203 , C07H15/252 , C07K16/00 , C07K16/46 , C07K19/00
CPC分类号： C07D207/404 , A61K47/48338 , A61K47/48715 , A61K51/1093 , C07D207/452 , C07H15/203 , C07H15/252 , A61K2123/00
摘要： Targeting substance-diagnostic/therapeutic agent conjugates joined by stabilized Schiff base or hydrazone linkages are disclosed. In addition, slow release carrier-drug pharmaceuticals are described. The diagnostic and therapeutic conjugates and pharmaceuticals of the present invention provide certain advantages relating to in vivo administration, including controlled release of the active agent at a target site.
摘要翻译：公开了通过稳定的席夫碱或腙键连接的靶向物质 - 诊断/治疗剂缀合物。此外，描述了缓释载体药物药物。本发明的诊断和治疗性缀合物和药物提供与体内施用有关的某些优点，包括活性剂在靶位点的受控释放。

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