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公开(公告)号：US06841671B2
公开(公告)日：2005-01-11
申请号：US10047592
申请日：2001-10-23
申请人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
发明人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
IPC分类号： C07D471/10 , C07D487/10
CPC分类号： C07D471/10 , C07D487/10
摘要： The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译： 本发明涉及式Ⅳ所示的5-螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂，所述“A”是本说明书中定义的5-7元杂环，以及治疗炎症的药物组合物和方法， 癌症等疾病。
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公开(公告)号：US06720351B2
公开(公告)日：2004-04-13
申请号：US10177858
申请日：2002-06-20
申请人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31405
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及制备该化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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3.发明授权公开(公告)号：US06649636B1
公开(公告)日：2003-11-18
申请号：US09723608
申请日：2000-11-28
申请人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
发明人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
IPC分类号： C07D40114
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译： 本发明涉及下式的化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地稠合于碳环或5至6个 杂芳基 R 2是任选被卤素，氨基或烷基氨基取代的（C 1 -C 4）烷基; R 3和R 4各自为氢，卤素，任选被卤素取代的（C 1 -C 4）烷基等; X 1至X 4各自为氢，卤素，羟基，任选被卤素取代的（C 1 -C 4）烷基等。 这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。
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公开(公告)号：US06194578B1
公开(公告)日：2001-02-27
申请号：US09348449
申请日：1999-07-07
申请人： David A. Griffith , Brian S. Bronk
发明人： David A. Griffith , Brian S. Bronk
IPC分类号： C07D48700
CPC分类号： C07K5/06034 , A61K38/05 , C07K5/0207 , C07K5/06191 , A61K2300/00
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 therapeutically effective in treating osteoporosis and/or frailty, 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 and/or frailty 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 therapeutically effective 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。 本发明的化合物在治疗骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症中具有治疗上的有效性; 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，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素，和孕激素; 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，本发明涉及治疗有效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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公开(公告)号：US6043227A
公开(公告)日：2000-03-28
申请号：US320352
申请日：1999-05-26
申请人： Hengmiao Cheng , Michael Letavic , Carl B. Ziegler, Jr. , Jason K. Dutra , Peter Bertinato , Brian S. Bronk
发明人： Hengmiao Cheng , Michael Letavic , Carl B. Ziegler, Jr. , Jason K. Dutra , Peter Bertinato , Brian S. Bronk
摘要： This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
摘要翻译： 本发明涉及式的化合物及其药学上可接受的盐。 式1的化合物是可用于治疗各种细菌感染和与这种感染有关的疾病的有效的抗菌剂。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗细菌感染的方法。本发明还涉及制备式1化合物的方法和用于此类制备的中间体。
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公开(公告)号：US06979692B2
公开(公告)日：2005-12-27
申请号：US10639854
申请日：2003-08-13
申请人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Alan E. Blize , Brian S. Bronk , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/44 , A61P3/00 , C07D213/28
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
摘要翻译： 本发明涉及式1的三酰胺MTP / ApoB抑制剂，其中R 1 -R 8如本说明书中所定义，以及其药物组合物及其用途，以及 制备化合物的方法。 本发明的化合物可用于治疗肥胖症和脂质疾病。
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公开(公告)号：US06949572B2
公开(公告)日：2005-09-27
申请号：US10639855
申请日：2003-08-13
申请人： Peter Bertinato , Brian S. Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
发明人： Peter Bertinato , Brian S. Bronk , Alan E. Blize , Hengmiao Cheng , Jin Li , Hiep Huatan , Clive Mason
IPC分类号： A61K31/341 , A61K31/343 , A61K31/397 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/4525 , A61K31/4709 , A61K31/501 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/42 , C07D307/85 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/44 , A61P3/00 , C07D40/00
CPC分类号： C07D401/12 , A61K31/343 , A61K31/381 , A61K31/405 , A61K31/4439 , A61K31/655 , C07D209/42 , C07D307/85 , C07D401/14 , C07D405/12 , C07D409/12
摘要： The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
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公开(公告)号：US06846818B2
公开(公告)日：2005-01-25
申请号：US10414856
申请日：2003-04-16
IPC分类号： A61K31/4439 , A61K31/497 , A61K31/728 , A61K31/737 , A61K45/00 , A61P19/02 , A61P29/00 , A61P43/00 , C07D401/06 , C07D403/06 , C07D401/12 , A61K31/5355 , A61K31/541 , C07D403/12 , C07D403/14
CPC分类号： C07D401/06 , C07D403/06
摘要： The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.
摘要翻译： 本发明涉及式I的环加氧酶-2（COX-2）选择性抑制剂：含有它们的药物组合物，其药用用途及其制剂。 本发明的化合物特别可用于治疗或减轻炎症和炎症相关疾病，例如类风湿性关节炎和骨关节炎，以及缓解疼痛，例如与手术或创伤相关的疼痛 ，哺乳动物，优选猫科动物和犬科动物。
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公开(公告)号：US6100240A
公开(公告)日：2000-08-08
申请号：US396876
申请日：1999-09-16
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61P31/04 , C07H17/00 , C07H17/08
摘要： The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, Q, X, Y and Z are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said 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R 1，R 2，R 3，Q，X，Y和Z如本文所定义。 本发明还涉及含有式I化合物的药物组合物，使用式I化合物治疗感染的方法，以及制备所述式I化合物的方法。
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