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1. 发明授权

US07670613B2 Androgen modulators 失效
标题翻译：雄激素调节剂
公开(公告)号：US07670613B2
公开(公告)日：2010-03-02
申请号：US11175097
申请日：2005-07-05
申请人： Lain-Yen Hu , Bruce A. Lefker , Daniel Y. Du , Yvonne Dorothy Smith , Huangshu Lei , William Glen Harter , Victoria Leigh Downs , Mark L. Boys , Donna Michele Iula
发明人： Lain-Yen Hu , Bruce A. Lefker , Daniel Y. Du , Yvonne Dorothy Smith , Huangshu Lei , William Glen Harter , Victoria Leigh Downs , Mark L. Boys , Donna Michele Iula
IPC分类号： A61K9/00
CPC分类号： C07C255/54 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42
摘要： The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
摘要翻译：本发明涉及一类新的4-环烷氧基苯并腈及其作为雄激素受体调节剂的用途。本发明的其它方面涉及这些化合物用于减少过量的皮脂分泌和刺激毛发生长的用途。

2. 发明授权

US07192979B2 EP4 receptor selective agonist in the treatment of osteoporosis 失效
标题翻译： EP4受体选择性激动剂治疗骨质疏松症
公开(公告)号：US07192979B2
公开(公告)日：2007-03-20
申请号：US10668633
申请日：2003-09-23
申请人： Kimberly O. Cameron , Bruce A. Lefker
发明人： Kimberly O. Cameron , Bruce A. Lefker
IPC分类号： A61K31/4015 , C07D207/04
CPC分类号： C07D403/06 , C07D207/20 , C07D405/10 , C07D409/06 , C07D409/14 , C07D417/06
摘要： This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.
摘要翻译：本发明涉及式I的EP4受体选择性前列腺素激动剂，其中R 2，X，Z和Q如说明书中所定义。本发明还涉及含有这些化合物的药物组合物。本发明还涉及治疗具有低骨量，特别是骨质疏松症，脆弱性，骨质疏松性骨折，骨缺损，儿童特发性骨丢失，牙槽骨丢失，下颌骨骨丢失，骨折，截骨术，骨丢失与哺乳动物中的牙周炎或假体向内生长相关，包括施用那些化合物。

3. 发明授权

US06649657B2 Prevention of loss and restoration of bone mass by certain prostaglandin agonists 失效
公开(公告)号：US06649657B2
公开(公告)日：2003-11-18
申请号：US10256985
申请日：2002-09-26
申请人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L. Rosati , David D. Thompson
发明人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L. Rosati , David D. Thompson
IPC分类号： A61K31235
CPC分类号： C07D207/263 , A61K45/06 , C07C235/34 , C07C311/04 , C07C311/06 , C07C323/49 , C07C2601/14 , C07C2602/08 , C07D209/14 , C07D213/42 , C07D215/18 , C07D239/26 , C07D241/12 , C07D249/06 , C07D257/04 , C07D271/12 , C07D277/28 , C07D277/56 , C07D307/24 , C07D307/52 , C07D307/68 , C07D307/81 , C07D317/58 , C07D319/18 , C07D333/20 , C07D333/24 , C07D333/34 , C07D333/38 , C07D409/12
摘要： Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

4. 发明授权

US6124264A Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US6124264A
公开(公告)日：2000-09-26
申请号：US259776
申请日：1999-03-01
申请人： Philip A Carpino , Paul A DaSilva-Jardine , Bruce A Lefker , John A Ragan
发明人： Philip A Carpino , Paul A DaSilva-Jardine , Bruce A Lefker , John A Ragan
IPC分类号： A61K38/00 , A61K31/415 , A61K31/565 , A61K31/66 , A61K38/04 , A61P5/06 , A61P9/00 , A61P19/10 , A61P43/00 , C07D231/54 , C07D471/04 , C07D487/02 , C07K20060101 , C07K5/02 , C07K5/06 , C07K5/062
CPC分类号： C07K5/06034 , C07D471/04 , C07K5/0202 , A61K38/00
摘要： ##STR1## This invention is directed to compounds of formula (I) and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretagogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGR-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其是生长激素促分泌素并且增加内源性生长激素的水平。本发明化合物可用于治疗和预防骨质疏松症，充血性心力衰竭，与衰老有关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。当与以下物质组合使用时，本发明的化合物也可用于治疗骨质疏松症：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGR-1，IGF-2或B-HT920。本发明还涉及可用于制备式（I）化合物的中间体。

5. 发明授权

US6110932A Growth hormone secretagogues 有权
标题翻译：生长激素促分泌素
公开(公告)号：US6110932A
公开(公告)日：2000-08-29
申请号：US258956
申请日：1999-03-01
申请人： Philip A Carpino , Paul A DaSilva-Jardine , Bruce A Lefker , John A Ragan
发明人： Philip A Carpino , Paul A DaSilva-Jardine , Bruce A Lefker , John A Ragan
IPC分类号： A61K38/00 , A61K31/415 , A61K31/565 , A61K31/66 , A61K38/04 , A61P5/06 , A61P9/00 , A61P19/10 , A61P43/00 , C07D231/54 , C07D471/04 , C07D487/02 , C07K20060101 , C07K5/02 , C07K5/06 , C07K5/062 , A61K31/435
CPC分类号： C07K5/06034 , C07D471/04 , C07K5/0202 , A61K38/00
摘要： This invention is directed to compounds of the formula ##STR1## and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating would healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2, or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula I.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其为生长激素分泌因子并且增加内源性生长激素的水平。本发明化合物可用于治疗和预防骨质疏松症，充血性心力衰竭，与衰老有关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速愈合，或加速烧伤患者或接受大手术的患者的恢复; 改善肌肉力量，流动性，皮肤厚度的维持，代谢稳态或肾动态平衡。当与以下物质组合使用时，本发明的化合物也可用于治疗骨质疏松症：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。本发明还涉及可用于制备式I化合物的中间体。

6. 发明授权

US5442044A Orally active renin inhibitors 失效
标题翻译：口服活性肾素抑制剂
公开(公告)号：US5442044A
公开(公告)日：1995-08-15
申请号：US28038
申请日：1993-03-08
申请人： Dennis J. Hoover , Bruce A. Lefker , Robert L. Rosati
发明人： Dennis J. Hoover , Bruce A. Lefker , Robert L. Rosati
IPC分类号： A61K38/00 , C07D211/58 , C07D401/12 , C07D409/12 , C07D417/12 , C07K5/02 , C07K5/065 , C07K5/06 , A61K38/05
CPC分类号： C07D401/12 , C07D211/58 , C07D409/12 , C07D417/12 , C07K5/0202 , C07K5/06078 , A61K38/00
摘要： This invention relates to compounds of the formula ##STR1## wherein Q, Z, D, E, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.
摘要翻译：本发明涉及下式的化合物，其中Q，Z，D，E，R 3，R 4，R 5和R 6如下定义，其药学上可接受的盐被公开。该化合物可用作抗高血压药。

7. 发明授权

US06552067B2 EP4 receptor selective agonists in the treatment of osteoporosis 失效
标题翻译： EP4受体选择性激动剂治疗骨质疏松症
公开(公告)号：US06552067B2
公开(公告)日：2003-04-22
申请号：US09990556
申请日：2001-11-21
申请人： Kimberly O. Cameron , Bruce A. Lefker
发明人： Kimberly O. Cameron , Bruce A. Lefker
IPC分类号： C07D20704
CPC分类号： C07D403/06 , C07D207/20 , C07D405/10 , C07D409/06 , C07D409/14 , C07D417/06
摘要： This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.
摘要翻译：本发明涉及式I的EP4受体选择性前列腺素激动剂，其中R2，X，Z和Q如说明书中所定义。本发明还涉及含有这些化合物的药物组合物。本发明还涉及治疗具有低骨量，特别是骨质疏松症，脆弱性，骨质疏松性骨折，骨缺损，儿童特发性骨丢失，牙槽骨丢失，下颌骨骨丢失，骨折，截骨术，骨丢失与哺乳动物中的牙周炎或假体向内生长相关，包括施用那些化合物。

8. 发明授权

US06492412B2 Prevention of loss and restoration of bone mass by certain prostaglandin agonists 失效
公开(公告)号：US06492412B2
公开(公告)日：2002-12-10
申请号：US09897824
申请日：2001-06-29
申请人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L. Rosati , David D. Thompson
发明人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L. Rosati , David D. Thompson
IPC分类号： A61K3140
CPC分类号： C07D207/263 , A61K45/06 , C07C235/34 , C07C311/04 , C07C311/06 , C07C323/49 , C07C2601/14 , C07C2602/08 , C07D209/14 , C07D213/42 , C07D215/18 , C07D239/26 , C07D241/12 , C07D249/06 , C07D257/04 , C07D271/12 , C07D277/28 , C07D277/56 , C07D307/24 , C07D307/52 , C07D307/68 , C07D307/81 , C07D317/58 , C07D319/18 , C07D333/20 , C07D333/24 , C07D333/34 , C07D333/38 , C07D409/12
摘要： Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

9. 发明授权

US06376502B1 Osteoporosis compounds 失效
标题翻译：骨质疏松症化合物
公开(公告)号：US06376502B1
公开(公告)日：2002-04-23
申请号：US09511128
申请日：2000-02-22
申请人： Kimberly O. Cameron , Bruce A. Lefker , Robert L. Rosati
发明人： Kimberly O. Cameron , Bruce A. Lefker , Robert L. Rosati
IPC分类号： C07D40112
CPC分类号： C07D213/70 , A61K45/06 , C07C311/06 , C07D277/56 , C07D307/68 , C07D333/40
摘要： This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
摘要翻译：本发明涉及前列腺素激动剂，使用这种前列腺素激动剂的方法，含有这种前列腺素激动剂的药物组合物和含有这种前列腺素激动剂的试剂盒。前列腺素激动剂可用于治疗包括骨质疏松症在内的骨疾病。

10. 发明授权

US06344485B1 Method for treating glaucoma 失效
标题翻译：治疗青光眼的方法
公开(公告)号：US06344485B1
公开(公告)日：2002-02-05
申请号：US09335630
申请日：1999-06-18
申请人： Kimberly O. Cameron , Bruce A. Lefker
发明人： Kimberly O. Cameron , Bruce A. Lefker
IPC分类号： A61K3118
CPC分类号： A61K31/496 , A61K31/192 , A61K31/197 , A61K31/381 , A61K31/41 , Y10S514/912 , Y10S514/913
摘要： Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.
摘要翻译：使用前列腺素激动剂降低眼内压的方法，因此使用青光眼。

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