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1. 发明授权

US06221875B1 Substituted 9H-pyridino [2,3-B]indole and 9H-pyrimidino [4,5-B]indole derivatives: selective neuropeptide Y receptor ligands 失效
标题翻译：取代的9H-吡啶并[2,3-b]吲哚和9H-嘧啶并[4,5-B]吲哚衍生物：选择性神经肽Y受体配体
公开(公告)号：US06221875B1
公开(公告)日：2001-04-24
申请号：US09283534
申请日：1999-04-01
申请人： James W. Darrow , George D. Maynard , Raymond F. Horvath , Jennifer Tran , Stephane De Lombaert
发明人： James W. Darrow , George D. Maynard , Raymond F. Horvath , Jennifer Tran , Stephane De Lombaert
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are effective neuropeptide Y1 receptor antagonists, and are therefore useful in the treatment of a wide variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.
摘要翻译：公开的是下式的化合物：其中Ar，R 1，W和X是如本文所定义的取代基，这些化合物是有效的神经肽Y1受体拮抗剂，因此可用于治疗各种临床病症，其特征在于存在的过量的神经肽Y.

2. 发明授权

US6147085A Aminoalkyl substituted 9H-pyridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives 失效
标题翻译：氨基烷基取代的9H-吡啶并[2,3-b]吲哚和9H-嘧啶并[4,5-b]吲哚衍生物
公开(公告)号：US6147085A
公开(公告)日：2000-11-14
申请号：US283409
申请日：1999-04-01
申请人： Raymond F. Horvath , James W. Darrow , George D. Maynard
发明人： Raymond F. Horvath , James W. Darrow , George D. Maynard
IPC分类号： A61P9/12 , A61P25/22 , C07D471/04 , C07D487/04 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: ##STR1## wherein Ar, R.sup.1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF.sub.1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y.sub.1 receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.
摘要翻译：公开了下式的化合物：其中Ar，R 1，W和X是如本文所定义的取代基，该化合物是（1）CRF1受体的拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后压力障碍（PTSD）以及抑郁，头痛和焦虑; 和（2）是神经肽Y1受体拮抗剂，因此可用于治疗以过量神经肽Y的存在为特征的各种临床病症。

3. 发明授权

US06472402B1 Aminoalkyl substituted 5,6,7,8-Tetrahydro-9H-Pyridino [2,3-B]indole derivatives 失效
标题翻译：氨基烷基取代的5,6,7,8-四氢-9H-吡啶并[2,3-b]吲哚衍生物
公开(公告)号：US06472402B1
公开(公告)日：2002-10-29
申请号：US09408613
申请日：1999-09-30
申请人： Raymond F. Horvath , James W. Darrow , George D. Maynard
发明人： Raymond F. Horvath , James W. Darrow , George D. Maynard
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis, hypoglycemia or a disorder the treatment of which can be effected or facilitated by antagonizing CRF, including but not limited to disorders induced or facilitated by CRF, in mammals, comprising: administering to the mammal a therapeutically effective amount of a compound of Formula I.
摘要翻译：公开了下式的化合物：其中Ar，R 1，W，X和m是如本文所定义的取代基。这些化合物是CRF受体的调节剂，因此可用于治疗情感障碍，焦虑症，抑郁症，头痛，肠易激综合征，创伤性应激障碍，核上性麻痹，免疫抑制，阿尔茨海默病，胃肠道疾病，神经性厌食症或其他进食障碍，药物成瘾，药物或酒精戒断症状，炎症性疾病，心血管或心脏相关疾病，生育问题，人类免疫缺陷病毒感染，出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡，肌萎缩性侧索硬化，低血糖或疾病，其治疗可以通过拮抗CRF来实现或促进，包括但不限于由 CRF，在哺乳动物中，包括：向哺乳动物施用治疗有效量的ac 一级方程式

4. 发明授权

US06291473B1 Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino [2, 3-B] indole and 5,6,7,8-tetrahydro-9H-pyrimidino [4, 5-B] indole derivatives: CRF1 specific ligands 失效
标题翻译：氨基烷基取代的5,6,7,8-四氢-9H-吡啶并[2,3-B]吲哚和5,6,7,8-四氢-9H-嘧啶并[4,5-B]吲哚衍生物：CRF1特异性配体
公开(公告)号：US06291473B1
公开(公告)日：2001-09-18
申请号：US09283723
申请日：1999-04-01
申请人： Raymond F. Horvath , James W. Darrow , George D. Maynard
发明人： Raymond F. Horvath , James W. Darrow , George D. Maynard
IPC分类号： A61K31405
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis, hypoglycemia or a disorder the treatment of which can be effected or facilitated by antagonizing CRF, including but not limited to disorders induced or facilitated by CRF, in mammals, comprising: administering to the mammal a therapeutically effective amount of a compound of Formula I.
摘要翻译：公开了下式的化合物：其中Ar，R 1，W，X和m是如本文所定义的取代基。这些化合物是CRF受体的调节剂，因此可用于治疗情感障碍，焦虑症，抑郁症，头痛，肠易激综合征，创伤性应激障碍，核上性麻痹，免疫抑制，阿尔茨海默病，胃肠道疾病，神经性厌食症或其他进食障碍，药物成瘾，药物或酒精戒断症状，炎症性疾病，心血管或心脏相关疾病，生育问题，人类免疫缺陷病毒感染，出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡，肌萎缩性侧索硬化，低血糖或疾病，其治疗可以通过拮抗CRF来实现或促进，包括但不限于由 CRF，在哺乳动物中，包括：向哺乳动物施用治疗有效量的ac 一级方程式

5. 发明授权

US06362186B1 Aminoalkyl substituted 9H-phridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives 失效
标题翻译：氨基烷基取代的9H-嘧啶并[2,3-b]吲哚和9H-嘧啶并[4,5-b]吲哚衍生物
公开(公告)号：US06362186B1
公开(公告)日：2002-03-26
申请号：US09707387
申请日：2000-11-06
申请人： Raymond F. Horvath , James W. Darrow , George D. Maynard
发明人： Raymond F. Horvath , James W. Darrow , George D. Maynard
IPC分类号： C07D23970
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y1, receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.
摘要翻译：公开了下式的化合物：其中Ar，R 1，W和X是如本文所定义的取代基，该化合物是（1）CRF1受体的拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后压力障碍（PTSD）以及抑郁，头痛和焦虑; 和（2）是神经肽Y1，受体拮抗剂，因此可用于治疗以过量神经肽Y的存在为特征的各种临床病症。

6. 发明授权

US08633193B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US08633193B2
公开(公告)日：2014-01-21
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

7. 发明授权

US08119665B2 Aryl imidazoles and related compounds as C5a receptor modulators 失效
标题翻译：芳基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US08119665B2
公开(公告)日：2012-02-21
申请号：US11680865
申请日：2007-03-01
申请人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
发明人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/4178
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供了芳基取代的咪唑，吡唑，吡啶并且其中变量在本文中定义的相关化合物的包装药物制剂。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

8. 发明授权

US06420365B1 Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors 失效
标题翻译：咪唑并吡啶类和相关衍生物作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06420365B1
公开(公告)日：2002-07-16
申请号：US09765159
申请日：2001-01-17
申请人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
发明人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
IPC分类号： A61K31435
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒性盐，其中A，B，C，D，Y，R 1，R 3，R 4，R 5和R 6是本文定义的变量，该化合物是缓激肽B2受体的调节剂。这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血脑屏障的渗透性，肿瘤屏障。

9. 发明授权

US06358949B1 Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors 失效
标题翻译：芳基和杂芳基稠合氨基烷基 - 咪唑衍生物：缓激肽B2受体的选择性调节剂
公开(公告)号：US06358949B1
公开(公告)日：2002-03-19
申请号：US09540580
申请日：2000-03-31
申请人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
发明人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
IPC分类号： A61K315377
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中：A，B，C和D是N或CH; X是一个或（un）取代的CH 2; R 1是低级烯基或（取代）低级烷基; R3是低级烷基; 和R2，R4，R5和R6是本文定义的变量;这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉成形术后再狭窄，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症或青光眼，或增加血脑屏障通透性，疼痛，哮喘和鼻炎。

10. 发明授权

US5648366A Substituted pyrrolidin-3-yl-alkyl-piperidines 失效
公开(公告)号：US5648366A
公开(公告)日：1997-07-15
申请号：US477167
申请日：1995-06-07
申请人： Timothy P. Burkholder , Tieu-Binh Le , Elizabeth M. Kudlacz , George D. Maynard
发明人： Timothy P. Burkholder , Tieu-Binh Le , Elizabeth M. Kudlacz , George D. Maynard
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.

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