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1. 发明授权

US06608203B2 Tetrahydroisoquinoline compounds as estrogen agonists/antagonists 失效
标题翻译：四氢异喹啉化合物作为雌激素激动剂/拮抗剂
公开(公告)号：US06608203B2
公开(公告)日：2003-08-19
申请号：US09745396
申请日：2000-12-21
申请人： Kimberly O. Cameron , Richard Chesworth , Paul A. DaSilva-Jardine , Robert F. Day , Bruce A. Lefker , Michael P. Zawistoski
发明人： Kimberly O. Cameron , Richard Chesworth , Paul A. DaSilva-Jardine , Robert F. Day , Bruce A. Lefker , Michael P. Zawistoski
IPC分类号： C07D21706
CPC分类号： C07D217/04 , C07D217/06 , C07D217/14 , C07D217/18
摘要： This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compounds.
摘要翻译：本发明涉及可用于治疗或预防肥胖，乳腺癌，骨质疏松症，子宫内膜异位症，心血管疾病，前列腺疾病等的化合物，以及包含这些化合物的药物组合物，方法和试剂盒。

2. 发明授权

US06482825B2 Growth-hormone secretagogues 有权
标题翻译：生长激素促分泌素
公开(公告)号：US06482825B2
公开(公告)日：2002-11-19
申请号：US09734274
申请日：2000-12-11
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： C07D47104
CPC分类号： C07K5/06034 , A61K38/00 , C07D471/04 , C07K5/0202
摘要： This invention provides compounds of formula I and pharmaceutically-acceptable salts thereof, where the substituents are defined in the specification, which are growth hormone secretogogues useful for 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 homeostatis or renal homeostasis. Compounds of formula I in combination with: a bisphosphonate such as alendronate; estrogen, estrogens, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions thereof are useful in treating osteoporosis. This invention also provides pharmaceutical compositions comprising a compound of formula I and GHRP-6, Hexarelin, GHRP-1, GRF, IGF-1, IFG-2 or B-HT920.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，其中取代基在说明书中定义，其是可用于治疗和预防骨质疏松症，充血性心力衰竭，与衰老相关的脆弱性，肥胖症的生长激素分泌元件; 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，代谢平衡或肾脏体内平衡。式I化合物与二膦酸盐如阿仑膦酸盐的组合：雌激素，雌激素和任选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素及其药物组合物可用于治疗骨质疏松症。本发明还提供包含式I化合物和GHRP-6，Hexarelin，GHRP-1，GRF，IGF-1，IFG-2或B-HT920的药物组合物。

3. 发明授权

US06441193B1 Estrogen agonists/antagonists 有权
标题翻译：雌激素激动剂/拮抗剂
公开(公告)号：US06441193B1
公开(公告)日：2002-08-27
申请号：US09466034
申请日：1999-12-17
申请人： Kimberly O. Cameron , Paul A. Dasilva-Jardine , Hua Zhu Ke , Robert L. Rosati
发明人： Kimberly O. Cameron , Paul A. Dasilva-Jardine , Hua Zhu Ke , Robert L. Rosati
IPC分类号： C07D20700
CPC分类号： C07D213/64 , A61K31/40 , C07D217/16 , C07D295/088 , C07D401/04
摘要： Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
摘要翻译：该化合物可用于治疗或预防，肥胖，乳腺癌，骨质疏松症，子宫内膜异位症，心血管疾病和前列腺疾病。

4. 发明授权

US06306875B1 Growth-hormone secretagogues 有权
标题翻译：生长激素促分泌素
公开(公告)号：US06306875B1
公开(公告)日：2001-10-23
申请号：US09593582
申请日：2000-06-13
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： A01N4342
CPC分类号： C07K5/06034 , A61K38/00 , C07D471/04 , C07K5/0202
摘要： This invention is directed to compounds of the formula 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 wound 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，其是生长激素分泌元素，并且其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，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。

5. 发明授权

US6107306A Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US6107306A
公开(公告)日：2000-08-22
申请号：US259691
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 wound 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，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，以及用于其的药物组合物。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

US06531485B2 Prostaglandin agonists 失效
标题翻译：前列腺素激动剂
公开(公告)号：US06531485B2
公开(公告)日：2003-03-11
申请号：US09446099
申请日：1999-12-16
申请人： Kimberly O. Cameron , Paul A. DaSilva-Jardine
发明人： Kimberly O. Cameron , Paul A. DaSilva-Jardine
IPC分类号： A61K315575
CPC分类号： C07D333/28 , C07C405/00 , C07D209/08 , C07D217/16 , C07D277/24 , C07D311/20 , C07D317/54
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。

7. 发明授权

US5936089A Dipeptides which promote release of growth hormone 失效
标题翻译：促进生长激素释放的二肽
公开(公告)号：US5936089A
公开(公告)日：1999-08-10
申请号：US973268
申请日：1997-11-26
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： C07D217/02 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/475 , A61K31/505 , A61K31/535 , A61K38/00 , A61K38/05 , A61K38/18 , A61P3/02 , A61P5/00 , A61P5/06 , A61P19/10 , A61P43/00 , C07D207/14 , C07D207/16 , C07D209/44 , C07D211/56 , C07D211/64 , C07D217/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07K20060101 , C07K5/02 , C07K5/027 , C07K5/03 , C07K5/033 , C07K5/06 , C07K5/065 , C07K5/078 , C07D217/06
CPC分类号： C07D413/06 , C07D207/14 , C07D209/44 , C07D211/56 , C07D211/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06034 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要： Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. ##STR1##
摘要翻译： PCT No.PCT / IB95 / 00410 Sec。 371日期：1997年11月26日 102（e）日期1997年11月26日PCT提交1995年5月29日PCT公布。公开号WO96 / 38471 日期1996年12月5日式（I）化合物是生长激素释放肽模拟物，其可用于治疗和预防骨质疏松症。

8. 发明申请

US20100317712A1 Estrogen Agonists/Antagonists For Preventing Breast Cancer 审中-公开
标题翻译：雌激素激动剂/预防乳腺癌的拮抗剂
公开(公告)号：US20100317712A1
公开(公告)日：2010-12-16
申请号：US12860099
申请日：2010-08-20
申请人： Kimberly O. Cameron , Paul A. Dasilva-Jardine , Hua Zhu Ke , Robert L. Rosati
发明人： Kimberly O. Cameron , Paul A. Dasilva-Jardine , Hua Zhu Ke , Robert L. Rosati
IPC分类号： A61K31/40 , C07D295/088 , A61P35/00
CPC分类号： C07D213/64 , A61K31/40 , C07D217/16 , C07D295/088 , C07D401/04
摘要： Compounds of this formula are useful for preventing breast cancer.
摘要翻译：该配方的化合物可用于预防乳腺癌。

9. 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。

10. 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。

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