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11. 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。

12. 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

13. 发明授权

US07015227B2 Certain amino-substituted monocycles as kinase modulators 有权
标题翻译：某些氨基取代的单环作为激酶调节剂
公开(公告)号：US07015227B2
公开(公告)日：2006-03-21
申请号：US10602560
申请日：2003-06-23
申请人： James W. Darrow , Robert W. DeSimone , Douglas A. Pippin , Scott A. Mitchell
发明人： James W. Darrow , Robert W. DeSimone , Douglas A. Pippin , Scott A. Mitchell
IPC分类号： A61K31/4965 , C07D241/00 , C07D241/02
CPC分类号： C07D239/26 , C07D239/42 , C07D241/20
摘要： A composition comprises a compound of Formula 1: a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, prodrug, or mixture thereof, wherein W is a nitrogen-substituted 5- or 6-membered monocyclic ring. The compounds are of utility as modulators of kinase activity.
摘要翻译：组合物包含式1的化合物：其药学上可接受的盐，水合物，溶剂合物，结晶形式，非对映异构体，前药或其混合物，其中W是氮取代的5-或6-元单环。这些化合物可用作激酶活性的调节剂。

14. 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.

15. 发明授权

US07259164B2 Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity 有权
标题翻译：某些取代的咪唑并[1,2-a]吡嗪，作为激酶活性的调节剂
公开(公告)号：US07259164B2
公开(公告)日：2007-08-21
申请号：US10915696
申请日：2004-08-11
申请人： Scott A. Mitchell , Robert W. DeSimone , James W. Darrow , Douglas A. Pippin , M. Diana Danca
发明人： Scott A. Mitchell , Robert W. DeSimone , James W. Darrow , Douglas A. Pippin , M. Diana Danca
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00
CPC分类号： C07D487/04
摘要： Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed.Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents.A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了某些取代的咪唑并[1,2-a]吡嗪及其药学上可接受的盐。本文还提供了含有一种或多种式I化合物或这些化合物的药学上可接受的盐以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。公开了治疗患有某些对EphB4激酶调节作用的疾病和病症的患者的方法，其包括给予这样的患者一定量的有效降低疾病或病症体征或症状的式I化合物。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂联合给药。一种用于确定样品中血管生成激酶存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与式I化合物接触确定样品中存在或不存在血管生成激酶。

16. 发明授权

US06372743B1 Certain alkylene diamine-substituted pyrazlo (1,5-a)-1,5-pyrimidines and pyrazolo (1,5-a) 1,3,5-triazines 失效
标题翻译：某些亚烷基二胺取代的吡唑（1,5-a）-1,5-嘧啶和吡唑并（1,5-a）1,3,5-三嗪
公开(公告)号：US06372743B1
公开(公告)日：2002-04-16
申请号：US09676970
申请日：2000-09-29
申请人： James W. Darrow , Stephane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
发明人： James W. Darrow , Stephane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
IPC分类号： A61K3153
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。这些化合物是NPY1受体的选择性调节剂。这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。给出了在受体定位研究中使用化合物的方法。

17. 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。

18. 发明授权

US06476038B1 Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines 失效
标题翻译：氨基取代的吡唑并[1,5-a] -1,5-嘧啶和吡唑并[1,5-a] -1,3,5-三嗪
公开(公告)号：US06476038B1
公开(公告)日：2002-11-05
申请号：US09676972
申请日：2000-09-29
申请人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
发明人： James W. Darrow , Stéphane De Lombaert , Charles Blum , Jennifer Tran , Mark Giangiordano , David Andrew Griffith , Philip Albert Carpino
IPC分类号： C07D48704
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物：其中R1，R2，R3，R4，R5，R6和X如本文所定义。这些化合物是NPY1受体的选择性调节剂。这些化合物可用于治疗许多CNS疾病，代谢紊乱和外周疾病，特别是进食障碍和高血压。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物也可用作NPY1受体定位的探针和作为NPY1受体结合测定中的标准物的探针。给出了在受体定位研究中使用化合物的方法。

19. 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

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