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1. 发明申请

US20090170916A1 Pyrrole and Pyrazole DAAO Inhibitors 有权
标题翻译：吡咯和吡唑DAAO抑制剂
公开(公告)号：US20090170916A1
公开(公告)日：2009-07-02
申请号：US12335250
申请日：2008-12-15
申请人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
发明人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
IPC分类号： A61K31/415 , A61K31/42 , A61P25/18
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.
摘要翻译：提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

2. 发明授权

US07488747B2 Pyrrole and pyrazole DAAO inhibitors 有权
公开(公告)号：US07488747B2
公开(公告)日：2009-02-10
申请号：US11023924
申请日：2004-12-28
申请人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
发明人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
IPC分类号： A61K31/416 , A61K31/405 , C07D231/56
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.

3. 发明授权

US07893098B2 Pyrrole and pyrazole DAAO inhibitors 有权
标题翻译：吡咯和吡唑DAAO抑制剂
公开(公告)号：US07893098B2
公开(公告)日：2011-02-22
申请号：US12566990
申请日：2009-09-25
申请人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
发明人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
IPC分类号： A61K31/415 , C07D231/14 , C07D231/54
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.
摘要翻译：提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

4. 发明申请

US20100016397A1 Pyrrole and Pyrazole DAAO Inhibitors 有权
标题翻译：吡咯和吡唑DAAO抑制剂
公开(公告)号：US20100016397A1
公开(公告)日：2010-01-21
申请号：US12566990
申请日：2009-09-25
申请人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
发明人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
IPC分类号： A61K31/415 , C07D231/54 , C07D231/14 , A61K31/416 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.
摘要翻译：提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

5. 发明授权

US07615572B2 Pyrrole and pyrazole DAAO inhibitors 有权
标题翻译：吡咯和吡唑DAAO抑制剂
公开(公告)号：US07615572B2
公开(公告)日：2009-11-10
申请号：US12335250
申请日：2008-12-15
申请人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
发明人： Q. Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D491/04
摘要： Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.
摘要翻译：提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

6. 发明授权

US08445470B2 Carbonate and carbamate modified forms of glucocorticoids in combination with B2 adrenergic agonists 有权
标题翻译：碳酸酯和氨基甲酸酯修饰形式的糖皮质激素与B2肾上腺素能激动剂组合
公开(公告)号：US08445470B2
公开(公告)日：2013-05-21
申请号：US12277004
申请日：2008-11-24
申请人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
发明人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
IPC分类号： A61K31/58 , A61K31/573
CPC分类号： A61K45/06 , A61K31/137 , A61K31/56 , A61K31/573 , A61K31/58 , Y10S514/87 , A61K2300/00
摘要： Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula. and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.
摘要翻译：含有β2肾上腺素能激动剂与下式的碳酸酯和氨基甲酸酯组合的组合物。并结合相关类固醇碳酸酯和氨基甲酸酯。该组合物可用于治疗支气管痉挛，用于诱发支气管扩张和治疗鼻炎，哮喘和慢性阻塞性肺疾病（COPD）和炎性疾病，特别是通过吸入治疗。

7. 发明授权

US07566725B2 Imidazo[1,2-A] pyridine anxiolytics 有权
标题翻译：咪唑并[1,2-A]吡啶抗焦虑药
公开(公告)号：US07566725B2
公开(公告)日：2009-07-28
申请号：US11532402
申请日：2006-09-15
申请人： Q. Kevin Fang , Paul Grover , Thomas P. Jerussi
发明人： Q. Kevin Fang , Paul Grover , Thomas P. Jerussi
IPC分类号： A01N43/42 , A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： A61K31/435 , C07D471/04
摘要： Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed. A representative compound of the invention is:
摘要翻译：公开了式I和II的咪唑并[1,2-a]吡啶。这些化合物可用于治疗焦虑和失眠。还公开了药物组合物和方法。本发明的代表性化合物是：

8. 发明授权

US07018995B2 Carbonate and carbamate modified forms of glucocorticoids 有权
公开(公告)号：US07018995B2
公开(公告)日：2006-03-28
申请号：US10369828
申请日：2003-02-20
申请人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
发明人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
IPC分类号： A61K31/573 , C07J5/00 , C07J71/00
CPC分类号： C07J71/0031 , A61K31/58 , C07J5/0076 , C07J5/0092 , C07J41/0033 , A61K2300/00
摘要： Carbonates and carbamates of the formula and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

9. 发明授权

US07723324B2 Imidazo[1,2-A]pyridine anxiolytics 有权
标题翻译：咪唑并[1,2-A]吡啶抗焦虑药
公开(公告)号：US07723324B2
公开(公告)日：2010-05-25
申请号：US10595592
申请日：2004-10-28
申请人： Q. Kevin Fang , Paul Grover , Thomas P. Jerussi
发明人： Q. Kevin Fang , Paul Grover , Thomas P. Jerussi
IPC分类号： A61K31/437 , A61K31/454 , A61K31/55 , A61P25/00 , A61P25/04 , A61P27/02 , C07D211/40 , C07D401/14 , C07D471/04
CPC分类号： A61K31/435 , C07D471/04
摘要： Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed. A representative compound of the invention is:
摘要翻译：公开了式I和II的咪唑并[1,2-a]吡啶。该化合物可用于治疗焦虑和失眠。还公开了药物组合物和方法。本发明的代表性化合物是：

10. 发明授权

US07253156B2 Carbonate and carbamate modified forms of glucocorticoids in combination with B2 adrenergic agonists 有权
标题翻译：碳酸酯和氨基甲酸酯修饰形式的糖皮质激素与B2肾上腺素能激动剂组合
公开(公告)号：US07253156B2
公开(公告)日：2007-08-07
申请号：US11364659
申请日：2006-02-28
申请人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
发明人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
IPC分类号： A61K31/56
CPC分类号： A61K45/06 , A61K31/137 , A61K31/56 , A61K31/573 , A61K31/58 , Y10S514/87 , A61K2300/00
摘要： Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.
摘要翻译：公开了含有β2肾上腺素能激动剂与下式的碳酸酯和氨基甲酸酯并与相关的类固醇碳酸酯和氨基甲酸酯组合的组合物。该组合物可用于治疗支气管痉挛，用于诱发支气管扩张和治疗鼻炎，哮喘和慢性阻塞性肺疾病（COPD）和炎性疾病，特别是通过吸入治疗。

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