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21. 发明授权

US06696445B2 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：US06696445B2
公开(公告)日：2004-02-24
申请号：US10291446
申请日：2002-11-08
申请人： Raymond F. Horvath , Jennifer N Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
发明人： Raymond F. Horvath , Jennifer N Tran , Stéphane De Lombaert , Kevin J. Hodgetts , Philip A. Carpino , David A. Griffith
IPC分类号： C07D40112
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。包含的新化合物通过本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR 15; Y是N或CR 3; E，F和G各自独立地为CR 3或N; 当单键结合到两个相邻的环原子上时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15，当双键键合到相邻的环原子;当双键连接到L或J或O，S，C = O，CR 3 R 16或NR 15时，K是N或CR 3。当与相邻的环原子双键键合时，N或CR 3，当与其连接的所有原子单键键合时，L是N或CR 16，或当双键键合到K时，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至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NR 15。这些化合物抑制神经肽Y在那些受体上的活性可用于治疗与过量神经肽Y相关的生理障碍，包括进食障碍，例如肥胖和贪食症，以及某些心脏病高血压等疾病。

22. 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.

23. 发明授权

US06995161B2 Substituted arylpyrazines 有权
标题翻译：取代的芳基吡嗪
公开(公告)号：US06995161B2
公开(公告)日：2006-02-07
申请号：US09788315
申请日：2001-02-16
申请人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stephane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stephane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , C07D241/20
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译：提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。

24. 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

25. 发明授权

US06284766B1 9H-pyrimido [4,5-b] indole derivatives: CRF1 specific ligands 失效
标题翻译： 9H-嘧啶并[4,5-b]吲哚衍生物：CRF1特异性配体
公开(公告)号：US06284766B1
公开(公告)日：2001-09-04
申请号：US09561569
申请日：2000-04-28
申请人： Raymond F. Horvath
发明人： Raymond F. Horvath
IPC分类号： A01N4354
CPC分类号： C07D487/04 , G01N2333/5751 , G01N2333/726
摘要： Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, R4 and R5 are defined herein, which compounds are selective 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, anxiety, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
摘要翻译：公开了下式的化合物：其中Ar，R 1，R 2，R 3，R 4和R 5在本文中定义，这些化合物是CRF1受体的选择性拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁，头痛，焦虑，心血管疾病和饮食失调。还公开了治疗这种病症以及包装的药物组合物的方法。

26. 发明授权

US07223778B2 5-substituted-2-arylpyridines 失效
标题翻译： 5-取代-2-芳基吡啶
公开(公告)号：US07223778B2
公开(公告)日：2007-05-29
申请号：US10154396
申请日：2002-05-22
申请人： Ge Ping , Taeyoung Yoon , Lu Yan Zhang , Raymond F. Horvath
发明人： Ge Ping , Taeyoung Yoon , Lu Yan Zhang , Raymond F. Horvath
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07D213/68 , C07D213/65 , C07D213/69 , C07D213/74 , C07D213/82 , C07D413/04
摘要： Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Compounds provided 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：提供新的5-取代-2-芳基吡啶化合物。这些化合物可以作为CRF受体的选择性调节剂。本文提供的5-取代-2-芳基吡啶化合物可用于治疗许多CNS和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。提供的化合物也可用作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。

27. 发明授权

US07202250B2 Substituted arylpyrazines 失效
标题翻译：取代的芳基吡嗪
公开(公告)号：US07202250B2
公开(公告)日：2007-04-10
申请号：US11107148
申请日：2005-04-15
申请人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stėphane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
发明人： Taeyoung Yoon , Ping Ge , Raymond F. Horvath , Stėphane DeLombaert , Kevin J. Hodgetts , Dario Doller , Cunyu Zhang
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译：提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF 1受体（包括人CRF 1受体）的高选择性结合的芳基吡嗪。因此，本发明包括治疗与CRF 1受体相关的疾病和疾病的方法，包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。

28. 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

29. 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

30. 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。

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