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1. 发明授权

US07910596B2 Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权
标题翻译：氨基四氢吡喃作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病
公开(公告)号：US07910596B2
公开(公告)日：2011-03-22
申请号：US12223143
申请日：2007-02-09
申请人： Tesfaye Biftu , Charles G Caldwell , Ann E. Weber , Ping P Chen , Xiaoxia Qian , Danqing Feng , Jason M. Cox
发明人： Tesfaye Biftu , Charles G Caldwell , Ann E. Weber , Ping P Chen , Xiaoxia Qian , Danqing Feng , Jason M. Cox
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D471/04 , C07D405/04 , C07D487/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

2. 发明授权

US5629322A Cyclic amidine analogs as inhibitors of nitric oxide synthase 失效
标题翻译：循环脒类似物作为一氧化氮合酶的抑制剂
公开(公告)号：US5629322A
公开(公告)日：1997-05-13
申请号：US468120
申请日：1995-06-06
申请人： Ravindra N. Guthikonda , Stephan K. Grant , Malcolm Maccoss , Shrenik K. Shah , Kothandaraman Shankaran , Charles G. Caldwell , Philippe L. Durette
发明人： Ravindra N. Guthikonda , Stephan K. Grant , Malcolm Maccoss , Shrenik K. Shah , Kothandaraman Shankaran , Charles G. Caldwell , Philippe L. Durette
IPC分类号： C07D215/36 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/435 , A61K31/445 , A61K31/4458 , A61K31/451 , A61K31/47 , A61K31/473 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/554 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D211/76 , C07D211/78 , C07D215/38 , C07D219/12 , C07D221/04 , C07D221/16 , C07D223/12 , C07D225/02 , C07D241/06 , C07D241/44 , C07D243/08 , C07D243/14 , C07D265/36 , C07D267/10 , C07D279/12 , C07D279/16 , C07D281/06 , C07D471/04 , C07D487/04 , C07D491/04
CPC分类号： C07D215/38 , C07D207/22 , C07D211/72 , C07D211/74 , C07D211/78 , C07D221/04 , C07D223/12 , C07D225/02 , C07D241/06 , C07D241/44 , C07D243/08 , C07D243/14 , C07D265/36 , C07D267/10 , C07D279/12 , C07D279/16 , C07D471/04 , C07D487/04 , C07D491/04
摘要： Disclosed herein are compounds of Formula I ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula I are also usful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, mulitple sclerosis, Korsakoff's disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.
摘要翻译：本文公开了式I的化合物及其药学上可接受的盐，其可用于治疗一氧化氮合酶介导的疾病和病症，包括神经变性疾病，胃肠蠕动和炎症的病症。这些疾病和病症包括低血压，脓毒性休克，中毒性休克综合征，血液透析，诸如癌症患者的IL-2治疗，恶病质，免疫抑制如移植治疗，自身免疫和/或炎性适应症，包括晒伤或牛皮癣和呼吸病症，例如支气管炎，哮喘和急性呼吸窘迫（ARDS），心肌炎，心力衰竭，动脉粥样硬化，关节炎，类风湿性关节炎，慢性或炎性肠病，溃疡性结肠炎，克罗恩病，系统性红斑狼疮（SLE），眼部疾病如眼高压和葡萄膜炎，1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。式I的化合物还可用于治疗缺氧，高压性氧惊厥和毒性，痴呆，Sydenham氏舞蹈病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，多发性硬化症，柯萨科夫病，与脑血管障碍有关的不育症，缺血性脑水肿，睡眠障碍，精神分裂症，抑郁症，PMS，焦虑，药物成瘾，疼痛，偏头痛，免疫复合物疾病，作为免疫抑制剂，以及用于预防或逆转对阿片剂和二氮杂类药物的耐受性。

3. 发明授权

US4999436A Aryl-substituted thiophene 3-ols, derivatives and analogs useful as lipoxgenase inhibitors 失效
标题翻译：芳基取代的噻吩3-ols，可用作脂氧合酶抑制剂的衍生物和类似物
公开(公告)号：US4999436A
公开(公告)日：1991-03-12
申请号：US397325
申请日：1989-08-22
申请人： Bruce E. Witzel , Debra L. Allison , Charles G. Caldwell , Kathleen Rupprecht
发明人： Bruce E. Witzel , Debra L. Allison , Charles G. Caldwell , Kathleen Rupprecht
IPC分类号： C07D333/32 , C07D333/50 , C07D333/64 , C07D333/78 , C07D333/80 , C07D409/04
CPC分类号： C07D409/04 , C07D333/32 , C07D333/50 , C07D333/64 , C07D333/78 , C07D333/80
摘要： Aryl substituted thiophenes 3-ols, its dihydro derivatives, 1-oxide and 1,1-dioxide analogs, as well as aryl substituted furans, are 5-lipoxygenase inhibitors useful in the treatment of inflammation and other leukotriene-mediated diseases.
摘要翻译：芳基取代的噻吩3-ols，其二氢衍生物，1-氧化物和1,1-二氧化物类似物以及芳基取代的呋喃是可用于治疗炎症和其它白三烯介导的疾病的5-脂氧合酶抑制剂。

4. 发明申请

US20090105210A1 Bicyclic Pyrimidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes 有权
标题翻译：双环嘧啶作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病
公开(公告)号：US20090105210A1
公开(公告)日：2009-04-23
申请号：US11793093
申请日：2006-01-18
申请人： Wallace T. Ashton , Charles G. Caldwell , Hong Dong , Ying-Duo Gao , Giovanna Scapin , Ann E. Weber
发明人： Wallace T. Ashton , Charles G. Caldwell , Hong Dong , Ying-Duo Gao , Giovanna Scapin , Ann E. Weber
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , C07D495/14
摘要： The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新型取代的双环嘧啶，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，如糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

5. 发明授权

US07388019B2 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 有权
标题翻译： 3-氨基-4-苯基丁酸衍生物作为二肽基肽酶抑制剂，用于治疗或预防糖尿病
公开(公告)号：US07388019B2
公开(公告)日：2008-06-17
申请号：US10542694
申请日：2004-01-27
申请人： Wallace T. Ashton , Charles G. Caldwell , Joseph L. Duffy , Robert J. Mathvink , Liping Wang , Ann E. Weber
发明人： Wallace T. Ashton , Charles G. Caldwell , Joseph L. Duffy , Robert J. Mathvink , Liping Wang , Ann E. Weber
IPC分类号： C07D471/04 , A61K31/4375 , A61P3/10 , C07D487/04 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/53
CPC分类号： C07D471/04 , C07D217/06 , C07D217/26
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）的抑制剂的3-氨基-4-苯基丁酸衍生物，其可用于治疗或预防其中二肽基肽酶 - 涉及IV酶，如糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

6. 发明授权

US06372733B1 Hexahydro-5-imino-1,4-1,4-thiazepine derivatives as inhibitors of nitric oxide synthases 失效
标题翻译：六氢-5-亚氨基-1,4-1,4-硫杂衍生物作为一氧化氮合酶的抑制剂
公开(公告)号：US06372733B1
公开(公告)日：2002-04-16
申请号：US09477246
申请日：2000-01-04
申请人： Charles G. Caldwell , Malcolm Maccoss , William K. Hagmann , Shrenik K. Shah , Kothandaraman Shankaran , Karla L. Furman
发明人： Charles G. Caldwell , Malcolm Maccoss , William K. Hagmann , Shrenik K. Shah , Kothandaraman Shankaran , Karla L. Furman
IPC分类号： C07D2806
CPC分类号： C07D281/06 , C07D243/08 , C07D267/16 , C07D337/04
摘要： Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
摘要翻译：本发明公开了已发现可用于治疗一氧化氮合酶介导的疾病和病症（包括神经退行性疾病，胃肠蠕动和炎症病症）的式I化合物及其药学上可接受的盐。这些疾病和障碍包括低血压，脓毒性休克，中毒性休克综合征，血液透析，诸如癌症患者中的IL-2治疗，恶病质，免疫抑制如移植治疗，自身免疫和/或炎性指征，包括晒伤，湿疹或银屑病和呼吸诸如支气管炎，哮喘，氧化剂诱发的肺损伤和急性呼吸窘迫（ARDS），肾小球性肾炎，再狭窄，病毒感染的炎症后遗症，心肌炎，心力衰竭，动脉粥样硬化，骨关节炎，类风湿性关节炎，脓毒性关节炎，慢性或炎性肠病溃疡性结肠炎，克罗恩病，系统性红斑狼疮（SLE），眼部疾病如眼高压，视网膜炎和葡萄膜炎，1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。

7. 发明授权

US6140349A Cyclic amine modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的环胺调节剂
公开(公告)号：US6140349A
公开(公告)日：2000-10-31
申请号：US241486
申请日：1999-02-01
申请人： Charles G. Caldwell , Malcolm Maccoss , Paul E. Finke , Sander G. Mills , Bryan Oates , Shankaran Kothandaraman , Dooseop Kim , Liping Wang
发明人： Charles G. Caldwell , Malcolm Maccoss , Paul E. Finke , Sander G. Mills , Bryan Oates , Shankaran Kothandaraman , Dooseop Kim , Liping Wang
IPC分类号： C07D211/56 , C07D211/58 , C07D401/06 , C07D405/06 , C07D409/06 , C07D521/00 , A61K31/445 , C07D409/10
CPC分类号： C07D231/12 , C07D211/56 , C07D211/58 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06
摘要： The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
摘要翻译：本发明涉及式I的环胺（其中R1，R2，R3，m和n如本文所定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-1，CCR-2，CCR-2A，CCR-2B，CCR-3，CCR-4，CCR-5，CXCR-3和/或CXCR- 4。

8. 发明授权

US5932551A Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative active agents 失效
标题翻译：取代的N-羧基烷基肽基衍生物作为抗再生活性剂
公开(公告)号：US5932551A
公开(公告)日：1999-08-03
申请号：US848766
申请日：1997-05-01
申请人： Charles G. Caldwell , Kevin T. Chapman , Craig K. Esser , William K. Hagmann , Ihor E. Kopka , Scott A. Polo , Soumya P. Sahoo , Philippe L. Durette
发明人： Charles G. Caldwell , Kevin T. Chapman , Craig K. Esser , William K. Hagmann , Ihor E. Kopka , Scott A. Polo , Soumya P. Sahoo , Philippe L. Durette
IPC分类号： A61K38/00 , C07K5/02 , A61K38/05
CPC分类号： C07K5/022 , A61K38/00
摘要： Novel N-carboxyalkylpeptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##
摘要翻译：发现式I的新型N-羧基烷基肽基化合物是有用的基质金属蛋白酶介导的疾病的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解性大疱性和冠状动脉血栓形成与动脉粥样硬化斑块破裂有关。基质金属蛋白酶是含有蛋白酶的家族，其包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。这些化合物也可以通过预防排卵或植入作为避孕的手段。

9. 发明授权

US5877191A Phenyl spiroethercycloalkyl tachykinin receptor antagonists 失效
标题翻译：苯基螺醚醚环烷基速激肽受体拮抗剂
公开(公告)号：US5877191A
公开(公告)日：1999-03-02
申请号：US955898
申请日：1997-10-22
申请人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
发明人： Charles G. Caldwell , Yuan-Ching Chiang , Conrad Dorn , Paul Finke , Jeffrey Hale , Malcolm Maccoss , Sander Mills , Albert Robichaud
IPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , A61K31/36 , C07D285/04 , C07D311/96
CPC分类号： C07D307/94 , C07D405/10 , C07D405/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译：本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，m，n和虚线在本文中定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

10. 发明授权

US5750549A Cycloalkyl tachykinin receptor antagonists 失效
标题翻译：环烷基速激肽受体拮抗剂
公开(公告)号：US5750549A
公开(公告)日：1998-05-12
申请号：US730277
申请日：1996-10-15
申请人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
发明人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
IPC分类号： C07C69/757 , C07C217/52 , C07C237/06 , C07C255/59 , C07D207/08 , C07D207/16 , C07D207/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07D521/00 , A61K31/41
CPC分类号： C07D207/26 , C07C217/52 , C07C237/06 , C07C255/59 , C07C69/757 , C07D207/08 , C07D207/16 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D231/12 , C07D233/56 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07C2101/08 , C07C2101/14
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译：本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，A，Q，W，X，Y，Z和n如本文所定义。本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。

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