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1. 发明申请

US20050143443A1 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：US20050143443A1
公开(公告)日：2005-06-30
申请号：US11023924
申请日：2004-12-28
申请人： Q. Fang , Seth Hopkins , Steven Jones
发明人： Q. Fang , Seth Hopkins , Steven Jones
IPC分类号： A61K31/401 , A61K31/405 , A61K31/415 , A61K31/416 , C07D207/34 , C07D209/42 , C07D209/44 , C07D231/14 , C07D231/16 , C07D231/54 , C07D231/56 , C07D491/04
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， SUP>独立地选自氢，卤素，硝基，烷基，酰基，烷基芳基和XYR 5。或R 1和R 2一起形成5,6或7元或8元的取代或未取代的碳环或杂环基; X和Y独立地选自O，S，NH和（CR 6）R 7）。 R 3是氢，烷基或M + H; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR 4; R 4选自氢，卤素，硝基，烷基，烷基芳基和XYR 5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R 6和R 7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）。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

2. 发明申请

US20050143434A1 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：US20050143434A1
公开(公告)日：2005-06-30
申请号：US11024151
申请日：2004-12-28
申请人： Q. Fang , Seth Hopkins , Steven Jones
发明人： Q. Fang , Seth Hopkins , Steven Jones
IPC分类号： A61K31/42 , C07D261/20
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。

3. 发明申请

US20080004327A1 FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE 有权
标题翻译： D-氨基酸氧化酶的荧光取代抑制剂
公开(公告)号：US20080004327A1
公开(公告)日：2008-01-03
申请号：US11772798
申请日：2007-07-02
申请人： Michele Heffernan , Robert Foglesong , Seth Hopkins , Mustapha Soukri , Steven Jones , Kerry Spear , Mark Varney
发明人： Michele Heffernan , Robert Foglesong , Seth Hopkins , Mustapha Soukri , Steven Jones , Kerry Spear , Mark Varney
IPC分类号： A61K31/407 , C07D491/02
CPC分类号： C07D495/04 , C07D491/04
摘要： This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O−X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
摘要翻译：本发明提供了D-氨基酸氧化酶酶的新型抑制剂以及包含本发明化合物的药物组合物。本发明还提供了治疗和预防神经系统疾病如神经精神和神经退行性疾病以及疼痛，共济失调和惊厥的方法。本发明的化合物具有以下一般结构：其中A是NH或S.Q是选自CR 1和N的成员.X和Y是独立地选自O，S，CR < > 2，N和NH。 R 1，R 2和R 4都是独立地选自H和F的成员，条件是选自R 1，R 2， R 1，R 2，R 4和R 4是F.R 6是选自O - >其中X + +为正离子，其为选自无机正离子和有机正离子的成员。

4. 发明申请

US20080058395A1 Fused heterocyclic inhibitors of D-amino acid oxidase 审中-公开
标题翻译： D-氨基酸氧化酶的融合杂环抑制剂
公开(公告)号：US20080058395A1
公开(公告)日：2008-03-06
申请号：US11825093
申请日：2007-07-02
申请人： Michele Heffernan , James Dorsey , Qun Fang , Robert Foglesong , Seth Hopkins , Michael Jones , Steven Jones , Cyprian Ogbu , Joe Perales , Mustapha Soukri , Kerry Spear , Mark Varney
发明人： Michele Heffernan , James Dorsey , Qun Fang , Robert Foglesong , Seth Hopkins , Michael Jones , Steven Jones , Cyprian Ogbu , Joe Perales , Mustapha Soukri , Kerry Spear , Mark Varney
IPC分类号： A61K31/40 , A61K31/415 , A61K31/425 , A61K31/48 , A61P43/00 , C07D231/02 , C07D303/02 , C07D487/02 , C07D513/00
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein Q is a member selected from O, S, CR1 and N, X and Y are members independently selected from CR2, O, S, N and NR3.
摘要翻译：本发明提供了D-氨基酸氧化酶酶的新型抑制剂以及包含本发明化合物的药物组合物。还提供了治疗和预防神经系统疾病如神经精神和神经退行性疾病以及疼痛，共济失调和惊厥的方法。本发明的化合物具有以下通式结构：其中Q是选自O，S，CR 1和N中的一个，X和Y是独立地选自CR 2，，O，S，N和NR 3。

5. 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.

6. 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。

7. 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。

8. 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。

9. 发明申请

US20080004328A1 FUSED HETEROCYCLES 失效
标题翻译：熔融杂环
公开(公告)号：US20080004328A1
公开(公告)日：2008-01-03
申请号：US11833903
申请日：2007-08-03
申请人： James Dorsey , Michele Heffernan , Qun Fang , Robert Foglesong , Seth Hopkins , Cyprian Ogbu , Mustapha Soukri , Kerry Spear
发明人： James Dorsey , Michele Heffernan , Qun Fang , Robert Foglesong , Seth Hopkins , Cyprian Ogbu , Mustapha Soukri , Kerry Spear
IPC分类号： A61K31/407
CPC分类号： A61K31/407 , C07D491/04 , C07D495/04
摘要： This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
摘要翻译：本发明提供具有下式的稠合杂环：其中R 1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R 2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R 3是选自H，C 1 -C 6取代或未取代的烷基，取代或未取代的芳基烷基和取代的或未取代的杂芳基烷基。 R 4是选自OH和O - O + X +的成员，其中X + +是正离子，其中是选自有机正离子和无机阳离子的成员。取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。索引n是从1到4的整数。

10. 发明申请

US20060281742A1 Amines that inhibit a mammalian anandamide transporter, and methods of use thereof 有权
公开(公告)号：US20060281742A1
公开(公告)日：2006-12-14
申请号：US11439529
申请日：2006-05-23
申请人： Brian Aquila , Seth Hopkins , Curtis Lockshin , Fengjiang Wang
发明人： Brian Aquila , Seth Hopkins , Curtis Lockshin , Fengjiang Wang
IPC分类号： A61K31/537 , A61K31/445 , C07D211/26 , C07D265/32
CPC分类号： C40B40/04 , C07C217/58 , C07C2601/02 , C07D307/14 , C40B20/08 , C40B30/04 , C40B40/00 , C40B50/14
摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

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