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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

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。

3. 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。

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

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

6. 发明授权

US06436932B1 Aminoalkyl substituted pyrrolo[3,2-e] pyridine and pyrrolo[2,3-b]pyrimidine derivatives: modulators of CRF1 receptors 失效
标题翻译：氨基烷基取代的吡咯并[3,2-e]吡啶和吡咯并[2,3-b]嘧啶衍生物：CRF1受体的调节剂
公开(公告)号：US06436932B1
公开(公告)日：2002-08-20
申请号：US09947045
申请日：2001-09-04
申请人： Ping Ge , Raymond F. Horvath , Stephane De Lombaert
发明人： Ping Ge , Raymond F. Horvath , Stephane De Lombaert
IPC分类号： A61K31519
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, Q1, Q2, R1, W and X are substituents as defined herein, which compounds are water-soluble CRF1 receptor antagonists, and are therefore useful for the treatment of psychiatric disorders and neurological diseases, including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders, as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
摘要翻译：公开了下式的化合物：其中Ar，Q1，Q2，R1，W和X是本文定义的取代基，该化合物是水溶性CRF1受体拮抗剂，因此可用于治疗精神疾病和神经疾病，包括重症抑郁症，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍，以及治疗与精神病理学障碍和应激相关的免疫学，心血管或心脏相关疾病和结肠超敏反应。

7. 发明授权

US06310063B1 Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors 失效
标题翻译：氨基烷基取代的吡咯并[3,2-E]吡啶和pyrollo [2,3-b]嘧啶衍生物：CRF1受体的调节剂
公开(公告)号：US06310063B1
公开(公告)日：2001-10-30
申请号：US09283410
申请日：1999-04-01
申请人： Ping Ge , Raymond F. Horvath , Stephane De Lombaert
发明人： Ping Ge , Raymond F. Horvath , Stephane De Lombaert
IPC分类号： A61K31496
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula: wherein Ar, Q1, Q2, R1, W and X are substituents as defined herein, which compounds are water-soluble CRF1 receptor antagonists, and are therefore useful for the treatment of psychiatric disorders and neurological diseases, including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders, as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
摘要翻译：公开了下式的化合物：其中Ar，Q1，Q2，R1，W和X是本文定义的取代基，该化合物是水溶性CRF1受体拮抗剂，因此可用于治疗精神疾病和神经疾病，包括重症抑郁症，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍，以及治疗与精神病理学障碍和应激相关的免疫学，心血管或心脏相关疾病和结肠超敏反应。

8. 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。

9. 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

10. 发明授权

US06281237B1 N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives 失效
标题翻译： N-苯基苯并咪唑酰胺和N-苯基吲哚甲酰胺衍生物
公开(公告)号：US06281237B1
公开(公告)日：2001-08-28
申请号：US09540478
申请日：2000-03-31
申请人： Raymond F. Horvath , Ping Ge , Taeyoung Yoon , Alan Hutchison
发明人： Raymond F. Horvath , Ping Ge , Taeyoung Yoon , Alan Hutchison
IPC分类号： A61K314184
CPC分类号： C07D235/14 , C07D209/14 , G01N2333/726
摘要： Disclosed are compounds of the forumla: or the pharmaceutically acceptable non-toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. 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 CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了该论坛的化合物或其药学上可接受的无毒盐，其中：A是N或CH; R 1和R 2表示氢或低级烷基; G，R 3，R 4，R 5，R 6，R 7和R 8是本文定义的变量这些化合物是CRF受体的调节剂，因此可用于治疗人类和其他动物中的情感障碍，焦虑症，抑郁症，进食障碍和应激障碍。还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物还可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

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