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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

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。

4. 发明授权

US07166725B2 Benzo[d]isoxazol-3-ol DAAO inhibitors 有权
标题翻译：苯并[d]异恶唑-3-醇DAAO抑制剂
公开(公告)号：US07166725B2
公开(公告)日：2007-01-23
申请号：US11024151
申请日：2004-12-28
申请人： Q Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil , Peter Wipf
发明人： Q Kevin Fang , Seth Hopkins , Michele Heffernan , Milan Chytil , Peter Wipf
IPC分类号： C07D261/20 , A61K31/42
CPC分类号： C07D261/20
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 therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein Z1 is N or CR3; Z2 is N or CR4; Z3is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.
摘要翻译：提高D-丝氨酸浓度和降低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，或防止神经功能丧失的方法神经变性疾病的特征包括向需要治疗的受试者施用治疗量的式I化合物或其药学上可接受的盐或溶剂合物：其中Z 1是N或CR 3 ; Z 2是N或CR 4; Z 3是O或S; A是氢，烷基或M + M是铝，钙，锂，镁，钾，钠，锌或它们的混合物; R 1，R 2，R 3和R 4独立地选自氢，烷基，羟基烷氧基，芳基，酰基，卤素，氰基，卤代烷基，NHCOOR 5和SO 2 NH 2。 R 5是芳基，芳基烷基，杂芳基或杂芳基烷基; R 1，R 2，R 3和R 4中的至少一个不是氢; 并且Z 1和Z 2中的至少一个不是N。

5. 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。

6. 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。

7. 发明授权

US4449231A Test signal generator for simulated speech 失效
标题翻译：用于模拟语音的测试信号发生器
公开(公告)号：US4449231A
公开(公告)日：1984-05-15
申请号：US305540
申请日：1981-09-25
申请人： Milan Chytil
发明人： Milan Chytil
IPC分类号： G10L11/00 , G10L1/10
CPC分类号： G10L25/00
摘要： A test signal generator for pseudo-simulated non-intelligible speech. The generator comprises first and second ROM's controlled by first and second address counters driven by a single clock. The first ROM generates digital samples which when decoded produce a random signal having a gaussian amplitude distribution. The second ROM also generates digital samples which when decoded produce a modulating signal having a power spectrum substantially equal to that of the modulation envelope of speech and a wave shape that results in a gamma amplitude distribution of a gaussian amplitude distributed signal. Each cycle of the modulating signal has an identical wave shape but a randomly varying wave period. The output of the second ROM is demodulated in a first digital-to-analog converter and the demodulated output is used to amplitude modulate the output of the first ROM in a second digital-to-analog converter to provide an output signal which is then passed through a band-shaping filter to provide the pseudo-simulated non-intelligible speech at its output.
摘要翻译：一种用于伪模拟不可理解语音的测试信号发生器。发生器包括由单个时钟驱动的第一和第二地址计数器控制的第一和第二ROM。第一个ROM产生数字样本，当解码时产生具有高斯幅度分布的随机信号。第二ROM还产生数字样本，当解码时产生具有与语音的调制包络的功率谱基本相等的功率谱的调制信号，以及导致高斯幅度分布信号的伽马幅度分布的波形。调制信号的每个周期具有相同的波形但随机变化的波周期。第二个ROM的输出在第一个数模转换器中进行解调，并且解调的输出用于对第二个数模转换器中的第一个ROM的输出进行幅度调制，以提供一个输出信号，然后通过该输出信号通过带形滤波器在其输出端提供伪模拟的不可理解的语音。

8. 发明授权

US08404670B2 Histamine H3 inverse agonists and antagonists and methods of use thereof 失效
标题翻译：组胺H3反向激动剂和拮抗剂及其使用方法
公开(公告)号：US08404670B2
公开(公告)日：2013-03-26
申请号：US13249166
申请日：2011-09-29
申请人： Milan Chytil , Sharon R. Engel , Qun Kevin Fang , Kerry L. Spear
发明人： Milan Chytil , Sharon R. Engel , Qun Kevin Fang , Kerry L. Spear
IPC分类号： A61K31/33 , A61K31/55
CPC分类号： C07D487/04 , C07D471/14
摘要： Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
摘要翻译：本文提供了稠合的咪唑基化合物，合成方法及其使用方法。本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍和代谢紊乱。本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触）的释放。本文还提供了含有化合物及其使用方法的药物制剂。

9. 发明授权

US08497278B2 Imidazo[1,2-a]pyridine compounds 有权
标题翻译：咪唑并[1,2-a]吡啶化合物
公开(公告)号：US08497278B2
公开(公告)日：2013-07-30
申请号：US12993679
申请日：2009-05-19
申请人： Qun Kevin Fang , Frank Xinhe Wu , Paul T. Grover , Seth C. Hopkins , Una Campbell , Milan Chytil , Kerry L. Spear
发明人： Qun Kevin Fang , Frank Xinhe Wu , Paul T. Grover , Seth C. Hopkins , Una Campbell , Milan Chytil , Kerry L. Spear
IPC分类号： C07D249/08 , C07D271/06 , C07D403/12 , A61K31/506 , A61K31/4245
CPC分类号： C07D471/04 , C07D487/04
摘要： Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. Many of the compounds disclosed herein may be represented by the following generic formula: in which Y is a direct bond or heteroatom and A3 is usually a nitrogenous heterocycle.
摘要翻译：公开了咪唑并[1,2-a]吡啶。本发明的化合物是有用的治疗剂，并且它们包括在药物制剂中并用于治疗方法。本文公开的许多化合物可以由以下通式表示：其中Y是直接键或杂原子，并且A3通常是含氮杂环。

10. 发明申请

US20120077802A1 HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF 审中-公开
标题翻译：组胺H3逆转激动剂和拮抗剂及其使用方法
公开(公告)号：US20120077802A1
公开(公告)日：2012-03-29
申请号：US13376368
申请日：2010-06-09
申请人： Milan Chytil , Sharon R. Engel , Qun Kevin Fang
发明人： Milan Chytil , Sharon R. Engel , Qun Kevin Fang
IPC分类号： A61K31/55 , C07D491/107 , A61K31/438 , A61K31/5377 , A61K31/513 , A61K31/497 , A61K31/496 , A61K31/4545 , A61P25/18 , A61P25/28 , A61P25/16 , A61P25/00 , A61P1/08 , A61P25/08 , A61P3/04 , A61P3/10 , A61P1/00 , A61P25/14 , A61P25/22 , A61P3/00 , A61P25/04 , A61P25/24 , C07D491/20
CPC分类号： C07D491/10 , C07D491/20
摘要： Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
摘要翻译：本文提供的是螺环化合物，合成方法及其使用方法。本文提供的化合物可用于治疗，预防和/或治疗各种疾病，包括例如神经障碍和代谢紊乱。本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质例如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触时）的释放。本文还提供了含有化合物及其使用方法的药物组合物。

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