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1. 发明授权

US5336796A Diastereomeric mono- and di-substituted diamino cyclohexane compounds and the method of preparation thereof 失效
标题翻译：非对映体单和二取代二氨基环己烷化合物及其制备方法
公开(公告)号：US5336796A
公开(公告)日：1994-08-09
申请号：US49672
申请日：1993-04-16
申请人： Donald T. Witiak , David P. Rotella
发明人： Donald T. Witiak , David P. Rotella
IPC分类号： C07C215/42 , C07F15/00
CPC分类号： C07C215/42 , C07F15/0093 , C07C2101/14
摘要： One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro- synthetic analysis. In another aspect, the present invention relates to novel antineoplasic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility. In a composition aspect, the present invention encompasses novel pharmaceutical compositions comprising the novel Pt(II) complexes in an amount sufficient to have an antineoplastic effect in an animal or patient.
摘要翻译：本发明的一个方面涉及可用作各种非对映体药物体系的合成子的环己烷-1,2-二（O）-4,5-二（N）非对映异构体的方法。本发明还涉及衍生自逆合成分析的立体异构体化合物。另一方面，本发明涉及衍生自立体异构体的新型抗磷酸化Pt（II）配合物和制备这种Pt（II）络合物的方法。环己烷环上的单羟基和二羟基取代使得有机铂复合物相对更易溶于水，从而便于静脉内给药。本发明的Pt（II）配合物与顺铂相比肾毒性较低，由于其水溶性增强，容易通过肾脏排出。在组合物方面，本发明包括新颖的药物组合物，其包含新颖的Pt（II）配合物，其量足以在动物或患者中具有抗肿瘤作用。

2. 发明授权

US5206400A Diastereomeric mono- and di-substituted diamino cyclohexane compounds and the method of preparation thereof 失效
标题翻译：非对映体单和二取代二氨基环己烷化合物及其制备方法
公开(公告)号：US5206400A
公开(公告)日：1993-04-27
申请号：US882258
申请日：1986-07-07
申请人： Donald T. Witiak , David P. Rotella
发明人： Donald T. Witiak , David P. Rotella
IPC分类号： C07C215/42 , C07F15/00
CPC分类号： C07C215/42 , C07F15/0093 , C07C2101/14
摘要： One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro-synthetic analysis. In another aspect, the present invention relates to novel antineoplastic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility. In a composition aspect, the present invention encompasses novel pharmaceutical compositions comprising the novel Pt(II) complexes in an amount sufficient to have an antineoplastic effect in an animal or patient.
摘要翻译：本发明的一个方面涉及可用作各种非对映体药物体系的合成子的环己烷-1,2-二（O）-4,5-二（N）非对映异构体的方法。本发明还涉及衍生自复合分析的立体异构体化合物。另一方面，本发明涉及衍生自立体异构体的新型抗肿瘤性Pt（II）络合物和制备这种Pt（II）络合物的方法。环己烷环上的单羟基和二羟基取代使得有机铂复合物相对更易溶于水，从而便于静脉内给药。本发明的Pt（II）配合物与顺铂相比肾毒性较低，由于其水溶性增强，容易通过肾脏排出。在组合物方面，本发明包括新颖的药物组合物，其包含新颖的Pt（II）配合物，其量足以在动物或患者中具有抗肿瘤作用。

3. 发明授权

US07384958B2 Quinoline inhibitors of cGMP phosphodiesterase 有权
公开(公告)号：US07384958B2
公开(公告)日：2008-06-10
申请号：US11680662
申请日：2007-03-01
申请人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
发明人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D405/12 , A61K31/47 , A61K31/4709 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D417/12 , C07D491/10
摘要： Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.

4. 发明授权

US07105537B2 2-substituted cyclic amines as calcium sensing receptor modulators 有权
标题翻译： 2-取代的环胺作为钙敏感受体调节剂
公开(公告)号：US07105537B2
公开(公告)日：2006-09-12
申请号：US10766086
申请日：2004-01-27
申请人： Ashvinikumar V. Gavai , Roy J. Vaz , John K. Dickson, Jr. , Jacques Y. Roberge , Wu Yang , Timur Gungor , James R. Corte , David P. Rotella , Yufeng Wang
发明人： Ashvinikumar V. Gavai , Roy J. Vaz , John K. Dickson, Jr. , Jacques Y. Roberge , Wu Yang , Timur Gungor , James R. Corte , David P. Rotella , Yufeng Wang
IPC分类号： A61K31/4439 , A61K31/4709 , C07D215/18 , C07D215/20 , C07D401/06
CPC分类号： C07D409/06 , C07D205/04 , C07D207/09 , C07D207/34 , C07D207/48 , C07D211/26 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/06 , C07D417/14
摘要： The present invention relates to modulators of the calcium sensing receptor having the formula I wherein Ar1, X, n, R1, R2, R3 and Q are as defined herein.
摘要翻译：本发明涉及具有式I的钙感应受体的调节剂，其中Ar 1，X，n，R 1，R 2， R 3和Q如本文所定义。

5. 发明授权

US06087368A Quinazolinone inhibitors of cGMP phosphodiesterase 有权
标题翻译：喹唑啉酮抑制剂cGMP磷酸二酯酶
公开(公告)号：US06087368A
公开(公告)日：2000-07-11
申请号：US322678
申请日：1999-05-28
申请人： John E. Macor , David P. Rotella , Harold N. Weller, III , David W. Cushman , Joseph P. Yevich
发明人： John E. Macor , David P. Rotella , Harold N. Weller, III , David W. Cushman , Joseph P. Yevich
IPC分类号： A61K31/505 , A61K31/519 , A61K31/53 , A61K31/55 , A61P1/00 , A61P3/06 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P15/00 , A61P15/10 , A61P27/06 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel quinazolinone compounds, methods of using such compounds in the treatment of cGMP-associated conditions such as erectile dysfunction, and pharmaceutical compositions containing such compounds.
摘要翻译：新颖的喹唑啉酮化合物，使用这些化合物治疗cGMP相关病症如勃起功能障碍的方法，以及含有这些化合物的药物组合物。

6. 发明授权

US5468872A K-252a functional derivatives potentiate neurotrophin-3 for the treatment of neurological disorders 失效
标题翻译： K-252a功能衍生物增强神经营养因子-3活性，用于治疗神经系统疾病
公开(公告)号：US5468872A
公开(公告)日：1995-11-21
申请号：US122893
申请日：1993-09-16
申请人： Marcie A. Glicksman , David P. Rotella , Nicola Neff , Chikara Murakata
发明人： Marcie A. Glicksman , David P. Rotella , Nicola Neff , Chikara Murakata
IPC分类号： C07D487/22 , A61K31/40 , A61K31/407 , A61K31/55 , A61P21/02 , A61P25/00 , A61P25/16 , A61P25/28 , C07D487/14 , C07D498/22 , C07D487/12
CPC分类号： C07D487/14 , A61K31/40 , A61K31/55
摘要： Functional K-252a derivatives are used to enhance trk phosphorylation and to potentiate the activity of neurotrophin-3 (NT-3). These compounds can be used to treat neurological disorders, alone or in combination with NT-3.
摘要翻译：功能性K-252a衍生物用于增强trk磷酸化并增强神经营养因子-3（NT-3）的活性。这些化合物可用于单独或与NT-3组合治疗神经障碍。

7. 发明授权

US07265145B2 Substituted piperidines and pyrrolidines as calcium sensing receptor modulators and method 有权
公开(公告)号：US07265145B2
公开(公告)日：2007-09-04
申请号：US10854689
申请日：2004-05-26
申请人： John K. Dickson , R. Michael Lawrence , Jacques Y. Roberge , David P. Rotella , Wu Yang
发明人： John K. Dickson , R. Michael Lawrence , Jacques Y. Roberge , David P. Rotella , Wu Yang
IPC分类号： A61K41/40 , C07D207/18
CPC分类号： C07D207/06 , C07D207/08 , C07D207/10 , C07D211/18 , C07D211/22 , C07D333/28
摘要： Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R1O, R1R2N, R1OCO, R1CO, R1R2NCO, R1R2NCONR2a, R1OCONR2a, R1CONR2a, R1S, R1SO, R1SO2, R1R2NSO2, R1R2NSO2NR2a, and R1SO2NR2a; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R2 and R2a are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R3; R3 is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; Q is hydrogen, F, or hydroxyl. In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.

8. 发明授权

US06835737B2 Quinoline inhibitors of cGMP phosphodiesterase 有权
标题翻译： cGMP磷酸二酯酶的喹啉抑制剂
公开(公告)号：US06835737B2
公开(公告)日：2004-12-28
申请号：US10412969
申请日：2003-04-14
申请人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
发明人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
IPC分类号： A61K3147
CPC分类号： C07D405/12 , A61K31/47 , A61K31/4709 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D417/12 , C07D491/10
摘要： Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.
摘要翻译：式（I）的化合物可用作cGMP PDE特别是5型的抑制剂。

9. 发明授权

US06576644B2 Quinoline inhibitors of cGMP phosphodiesterase 有权
标题翻译： cGMP磷酸二酯酶的喹啉抑制剂
公开(公告)号：US06576644B2
公开(公告)日：2003-06-10
申请号：US09933066
申请日：2001-08-20
申请人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
发明人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
IPC分类号： A61K314706
CPC分类号： C07D405/12 , A61K31/47 , A61K31/4709 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D417/12 , C07D491/10
摘要： Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.
摘要翻译：式（I）的化合物可用作cGMP PDE特别是5型的抑制剂。

10. 发明授权

US07378430B2 Quinoline inhibitors of cGMP phosphodiesterase 有权
标题翻译： cGMP磷酸二酯酶的喹啉抑制剂
公开(公告)号：US07378430B2
公开(公告)日：2008-05-27
申请号：US11640732
申请日：2006-12-18
申请人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
发明人： Yingzhi Bi , Guixue Yu , David P. Rotella , John E. Macor
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D405/12 , A61K31/47 , A61K31/4709 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D417/12 , C07D491/10
摘要： Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.
摘要翻译：式（I）的化合物可用作cGMP PDE特别是5型的抑制剂。

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