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11. 发明授权

US6133282A Certain pyrrolopyridine derivatives; novel CRF1 specific ligands 失效
标题翻译：某些吡咯并吡啶衍生物; 新型CRF1特异性配体
公开(公告)号：US6133282A
公开(公告)日：2000-10-17
申请号：US368541
申请日：1999-08-05
申请人： Raymond F. Horvath , Alan Hutchison
发明人： Raymond F. Horvath , Alan Hutchison
IPC分类号： A61P25/24 , C07D471/04 , C07D471/14 , A61K31/437
CPC分类号： C07D471/04 , C07D471/14
摘要： Disclosed are compounds of the formula: ##STR1## wherein Ar is optionally substituted aryl or heteroarylR.sub.1 is hydrogen or alkyl;R.sub.7 is hydrogen or alkyl;R.sub.2 is hydrogen, halogen, alkyl or alkoxy; orR.sub.1 and R.sub.2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; andR.sub.5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms,which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：公开了下式的化合物：其中Ar是任选取代的芳基或杂芳基R 1是氢或烷基; R7是氢或烷基; R2是氢，卤素，烷基或烷氧基; 或者R 1和R 2与它们所连接的环一起形成任选具有选自氧，硫或氮的杂原子的5-9元饱和或芳环; R3和R4独立地是氢，烷基，环烷基，芳基或杂芳基; 或R 3和R 4与它们所连接的氮原子一起形成5-8元环; R5为氢，卤素，具有1-6个碳原子的直链或支链低级烷基，或具有1-6个碳原子的直链或支链低级烷氧基或硫代烷氧基，该化合物是人促皮素激素释放的高度选择性部分激动剂或拮抗剂因子1（CRF1）受体，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，头痛和焦虑。

12. 发明授权

US07179807B2 5-substituted-2-arylpyrazines 失效
标题翻译： 5-取代-2-芳基吡嗪
公开(公告)号：US07179807B2
公开(公告)日：2007-02-20
申请号：US10645312
申请日：2003-08-20
申请人： Taeyoung Yoon , Ping Ge , Stéphane De Lombaert , Raymond F. Horvath , Dario Doller , Kevin J. Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Yasuchika Yamaguchi , Cunyu Zhang , Jim Darrow
发明人： Taeyoung Yoon , Ping Ge , Stéphane De Lombaert , Raymond F. Horvath , Dario Doller , Kevin J. Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Yasuchika Yamaguchi , Cunyu Zhang , Jim Darrow
IPC分类号： A61K31/535 , A61K31/497 , A61K31/4965 , C07D413/00 , C07D403/00
CPC分类号： C07D241/12 , C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal 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-芳基吡嗪化合物。这些化合物可以作为选择性调节剂或CRF受体。本发明化合物由下式提供：本文提供的5-取代-2-芳基吡嗪化合物可用于治疗多种CNS和外周疾病，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。

13. 发明授权

US5712392A Certain 4-piperidine- and piperazinoalkyl-2-phenyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译：某些4-哌啶和哌嗪基烷基-2-苯基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5712392A
公开(公告)日：1998-01-27
申请号：US464548
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/04 , A61K31/415 , C07D403/06
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了式IMA的化合物，其中R 1表示任选取代的芳基，杂芳基，芳基烷基或环烷基; X，Z和Y是任选取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

14. 发明授权

US5656762A 4-piperidino-and piperazinomethyl-2-phenylimidazole derivatives, dopamine receptor subtype specific ligands 失效
标题翻译： 4-哌啶子基和哌嗪基甲基-2-苯基咪唑衍生物，多巴胺受体亚型特异性配体
公开(公告)号：US5656762A
公开(公告)日：1997-08-12
申请号：US461858
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/06 , C07D403/04
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substitutents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

15. 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。

16. 发明授权

US06670371B2 Certain pyrrolopyridine derivatives: novel CRF1 specific ligands 失效
标题翻译：某些吡咯并吡啶衍生物：新型CRF1特异性配体
公开(公告)号：US06670371B2
公开(公告)日：2003-12-30
申请号：US10096239
申请日：2002-03-12
申请人： Raymond F. Horvath , Alan Hutchison
发明人： Raymond F. Horvath , Alan Hutchison
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07D471/14
摘要： Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：公开了下式的化合物：其中Ar是任选取代的芳基或杂芳基R 1是氢或烷基; R 7是氢或烷基; R 2是氢，卤素，烷基或烷氧基; 或者R 1和R 2与它们所连接的环一起形成任选具有选自氧，硫或氮的杂原子的5-9元饱和或芳环; R 3和R 4独立地是氢，烷基，环烷基，芳基或杂芳基团体或R 3和R 4与它们所连接的氮原子一起形成5-8元环; 和R 5是氢，卤素，具有1-6个碳原子的直链或支链低级烷基，或具有1-6个碳原子的直链或支链低级烷氧基或硫代烷氧基，该化合物是人促皮激素释放因子的高选择性部分激动剂或拮抗剂 1（CRF1）受体，可用于诊断和治疗应激相关疾病如后遗传性应激障碍（PTSD）以及抑郁，头痛和焦虑。

17. 发明授权

US6156751A Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives 失效
标题翻译：某些三环取代的二氮杂双环（3.2.1）辛烷衍生物
公开(公告)号：US6156751A
公开(公告)日：2000-12-05
申请号：US393789
申请日：1999-09-10
申请人： Alan Hutchison , Jun Yuan , Raymond F. Horvath
发明人： Alan Hutchison , Jun Yuan , Raymond F. Horvath
IPC分类号： C07D487/08 , A61K31/495 , C07D247/00
CPC分类号： C07D487/08
摘要： This invention encompasses compounds of the formula: ##STR1## where either R.sub.1 or R.sub.2 represents ##STR2## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organic substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lowere alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neurolepticagents. These compounds show unexpectedly atypical antipsychotic profiles (clozapine-like) in the animal models described in this patent.
摘要翻译：本发明包括下式的化合物：其中R 1或R 2表示，另一个表示氢或具有1-6个碳原子的直链或支链低级烷基; X为氧，亚甲基或NH; Y代表各种无机和有机取代基; Z是氢，氨基或NHR 6，其中R6是具有1-6个碳原子的低级烷基; T是氢，卤素，羟基或具有1-6个碳原子的低级烷氧基; A是亚甲基，羰基或CHOH。这些化合物是脑单胺受体亚型或其前药的选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。这些化合物在本专利描述的动物模型中显示出意想不到的非典型抗精神病药谱（氯氮平样）。

18. 发明授权

US5646281A Certain 4-piperidino- and piperazinomethyl-2-phenyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译：某些4-哌啶子基和哌嗪基甲基-2-苯基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5646281A
公开(公告)日：1997-07-08
申请号：US461135
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/06 , A61K31/415 , C07D403/04
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

19. 发明授权

US5633377A 4-piperidino- and piperazinomethyl-2-cyclohexyl imidazole derivatives; dopamine receptor subtype specific ligands 失效
标题翻译： 4-哌啶子基和哌嗪基甲基-2-环己基咪唑衍生物; 多巴胺受体亚型特异性配体
公开(公告)号：US5633377A
公开(公告)日：1997-05-27
申请号：US462833
申请日：1995-06-05
申请人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/06 , C07D403/04
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substitutents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof,which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

20. 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。

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