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1. 发明申请

US20130123230A1 2-Thiopyrimidinones 有权
公开(公告)号：US20130123230A1
公开(公告)日：2013-05-16
申请号：US13670852
申请日：2012-11-07
申请人： Philip A. Carpino , Edward L. Conn , Robert L. Dow , Matthew S. Dowling , David Hepworth , Daniel Wei-Shung Kung , Suvi Orr , Benjamin N. Rocke , Roger B. Ruggeri , Matthew F. Sammons , Joseph S. Warmus , Yan Zhang
发明人： Philip A. Carpino , Edward L. Conn , Robert L. Dow , Matthew S. Dowling , David Hepworth , Daniel Wei-Shung Kung , Suvi Orr , Benjamin N. Rocke , Roger B. Ruggeri , Matthew F. Sammons , Joseph S. Warmus , Yan Zhang
IPC分类号： C07D239/56 , C07D401/04 , C07D405/10 , C07D403/10 , C07D487/04 , C07D409/10 , C07D417/10 , C07D401/06 , C07D403/06 , C07D413/06 , A61K31/5377 , C07D405/04 , C07D403/04 , C07D409/04 , C07D401/10 , C07D403/12 , A61K31/352 , A61K45/06 , A61K31/513
CPC分类号： C07D239/56 , A61K31/352 , A61K31/37 , A61K31/513 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/10 , C07D413/06 , C07D417/04 , C07D417/10 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

2. 发明授权

US07074929B2 Certain alkylene diamine-substituted heterocycles 失效
标题翻译：某些亚烷基二胺取代的杂环
公开(公告)号：US07074929B2
公开(公告)日：2006-07-11
申请号：US10705446
申请日：2003-11-10
申请人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D471/04 , A61K31/4375 , A61P15/10 , A61P3/04
CPC分类号： C07D213/73 , C07D215/46 , C07D239/48 , C07D471/04 , C07D471/14 , C07D473/34 , C07D475/08 , C07D487/04 , C07D495/04 , G01N2333/5755 , G01N2333/70571
摘要： This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and XI
摘要翻译：本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。本发明包括的新化合物是式II，IV，V，VII-IX和XI的化合物

3. 发明授权

US06559150B2 Growth hormone secretagogues 失效
标题翻译：生长激素促分泌素
公开(公告)号：US06559150B2
公开(公告)日：2003-05-06
申请号：US09989040
申请日：2001-11-21
申请人： Philip A. Carpino
发明人： Philip A. Carpino
IPC分类号： C07D24186
CPC分类号： C07D471/04 , C07D487/04
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; a &bgr;3 adrenergic receptor agonist; 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.
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; β3肾上腺素能受体激动剂; 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。

4. 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。

5. 发明授权

US07232823B2 Cannabinoid receptor ligands and uses thereof 失效
标题翻译：大麻素受体配体及其用途
公开(公告)号：US07232823B2
公开(公告)日：2007-06-19
申请号：US10853993
申请日：2004-05-25
申请人： Philip A. Carpino , Subas M. Sakya
发明人： Philip A. Carpino , Subas M. Sakya
IPC分类号： A61K31/4985 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of Formula (I) or (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein
摘要翻译：本文描述了作为大麻素受体配体的式（I）或（II）化合物及其在治疗与动物中的大麻素受体的介导相关的疾病中的用途

6. 发明授权

US07151097B2 Bicyclic pyrazolyl and imidazolyl compounds and uses thereof 失效
标题翻译：双环吡唑基和咪唑基化合物及其用途
公开(公告)号：US07151097B2
公开(公告)日：2006-12-19
申请号：US10971599
申请日：2004-10-22
申请人： Philip A. Carpino , Robert L. Dow , David A. Griffith
发明人： Philip A. Carpino , Robert L. Dow , David A. Griffith
IPC分类号： C07D267/02 , C07D487/02 , C07D491/00 , A61K31/55 , A61P25/30
CPC分类号： C07D487/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.
摘要翻译：式（I）化合物在本文中描述。已经显示这些化合物作为大麻素受体配体，因此可用于治疗与动物中的大麻素受体的介导相关的疾病。

7. 发明授权

US06337332B1 Neuropeptide Y receptor antagonists 失效
标题翻译：神经肽Y受体拮抗剂
公开(公告)号：US06337332B1
公开(公告)日：2002-01-08
申请号：US09382418
申请日：1999-08-24
申请人： Philip A. Carpino
发明人： Philip A. Carpino
IPC分类号： A01N4354
CPC分类号： C07D401/04 , C07D239/88 , C07D239/94
摘要： Compounds of the structures are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.
摘要翻译：该结构的化合物可用于治疗与过量神经肽Y相关的病症，包括肥胖症和循环系统疾病。

8. 发明授权

US07230024B2 Cannabinoid receptor ligands and uses thereof 失效
标题翻译：大麻素受体配体及其用途
公开(公告)号：US07230024B2
公开(公告)日：2007-06-12
申请号：US11433171
申请日：2006-05-12
申请人： Philip A. Carpino , Robert L. Dow
发明人： Philip A. Carpino , Robert L. Dow
IPC分类号： A61K31/4162 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
摘要翻译：本文描述了作为大麻素受体配体的式（I）和（II）的化合物及其用于治疗与动物中的大麻素受体的介导相关的疾病的用途。

9. 发明授权

US06506762B1 Certain alkylene diamine-substituted heterocycles 失效
标题翻译：某些亚烷基二胺取代的杂环
公开(公告)号：US06506762B1
公开(公告)日：2003-01-14
申请号：US09676941
申请日：2000-09-29
申请人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D48704
CPC分类号： C07D213/73 , C07D215/46 , C07D239/48 , C07D471/04 , C07D471/14 , C07D473/34 , C07D475/08 , C07D487/04 , C07D495/04 , G01N2333/5755 , G01N2333/70571
摘要： The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C═O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonded to L or J, or O, S, C═O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; the 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C═O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.
摘要翻译：本发明还提供了通用方法，其中单环，双环或三环杂环可以被修饰以在NPY1受体上获得有效的拮抗剂。本发明提供NPY受体的新型有效的非肽拮抗剂，特别是 NPY1受体由选自单，双或三环杂环核心设计。本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。包含的新化合物本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR15; Y为N或CR 3; E，F和G各自独立地为CR 3或N; 当双键连接到相邻的环原子时，当单键连接到两个相邻的环原子，或N或CR 3时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15;当双键键合时，K为N或CR 3 当与两个相邻的环原子单键键合时，或当与相邻环原子双键键合时为N或CR 3，L或J，或O，S，C = O，CR 3 R 16或NR 15;当单键连接到所有相邻环原子时，L为N或CR16 当与K键合时，其连接的原子或C（碳）;含有I，J，K和L的6-或7-元环可以含有1至3个双键，0至2个杂原子和0〜2个C = O基团，其中这些基团的碳原子是环的一部分，氧原子是环上的取代基; Q是O或NR15。这些化合物抑制神经肽Y在这些受体上的活性可用于治疗与过量神经肽Y相关的生理紊乱，包括进食障碍，例如肥胖症和贪食症，以及某些心血管疾病，例如高血压。

10. 发明授权

US07241788B2 Cannabinoid receptor ligands and uses thereof 失效
标题翻译：大麻素受体配体及其用途
公开(公告)号：US07241788B2
公开(公告)日：2007-07-10
申请号：US11433848
申请日：2006-05-12
申请人： Philip A. Carpino , Robert L. Dow
发明人： Philip A. Carpino , Robert L. Dow
IPC分类号： A61K31/415
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein
摘要翻译：本文描述了作为大麻素受体配体的式（I）和（II）化合物及其在治疗与动物中的大麻素受体的介导相关的疾病中的用途

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