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31. 发明授权

US06803381B1 Carbamic acid derivatives 失效
标题翻译：氨基甲酸衍生物
公开(公告)号：US06803381B1
公开(公告)日：2004-10-12
申请号：US10438361
申请日：2003-05-14
申请人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31352
CPC分类号： C07D295/088 , C07C233/91 , C07C271/64 , C07C333/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/30 , C07D213/61 , C07D263/48 , C07D271/07 , C07D271/113 , C07D311/84 , C07D333/16 , C07D335/14 , C07D413/12
摘要： The present invention relates to compounds of formula wherein R1 is hydrogen or lower alkyl; R2, R2′ are each independently hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X is O, S or two hydrogen atoms not forming a bridge; A1/A2 is phenyl; B is a group of formula wherein R3 is lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl; Y is —O—, —S— or a bond; and Z is —O—; or a pharmaceutically acceptable salt thereof. These compounds are useful for the control or prevention of acute and/or chronic neurological disorders.
摘要翻译：本发明涉及式I的化合物，R 1是氢或低级烷基; R 2，R 2各自独立地是氢，低级烷基，低级烷氧基，卤素或三氟甲基; X是O，S或两个氢不形成桥的原子; A 1 / A 2是苯基; B是一个亚烷基的基团R 3是低级烷基，低级烯基，低级炔基，苄基，低级烷基 - 环烷基，低级烷基 - 氰基，低级烷基 - 吡啶基，低级烷基 - 低级烷氧基 - 苯基，任选被低级烷氧基取代的低级烷基 - 苯基或任选被低级烷氧基取代的苯基或低级烷基 - 噻吩基，环烷基，低级烷基 - 三氟甲基或低级烷基吗啉基; Y是-O - ， - S-或键; 和Z是-O-; 或其药学上可接受的盐。这些化合物可用于控制或预防急性和/或慢性神经障碍。

32. 发明授权

US06462198B1 Carbamic acid derivatives 失效
公开(公告)号：US06462198B1
公开(公告)日：2002-10-08
申请号：US09545622
申请日：2000-04-10
申请人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D41312
CPC分类号： C07D213/30 , C07C233/91 , C07C271/64 , C07C333/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/61 , C07D263/48 , C07D271/07 , C07D271/113 , C07D295/088 , C07D311/84 , C07D333/16 , C07D335/14 , C07D413/12
摘要： The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas wherein R4 and R5 signifies hydrogen, lower alkyl, lower alkoxy, cyclohexyl, lower alkyl-cyclohexyl or trifluoromethyl, with the proviso that at least one of R4 or R5 has to be hydrogen; as well as to their pharmaceutically acceptable salts. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

33. 发明授权

US06596743B2 Carbamic acid derivatives 失效
标题翻译：氨基甲酸衍生物
公开(公告)号：US06596743B2
公开(公告)日：2003-07-22
申请号：US10008827
申请日：2001-12-10
申请人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31421
CPC分类号： C07D213/30 , C07C233/91 , C07C271/64 , C07C333/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/61 , C07D263/48 , C07D271/07 , C07D271/113 , C07D295/088 , C07D311/84 , C07D333/16 , C07D335/14 , C07D413/12
摘要： The present invention is a compound of formula: wherein R1, R2, R2′, X, A1/A2 and B are as defined in the specification. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.
摘要翻译：本发明是下式的化合物：其中R1，R2，R2'，X，A1 / A2和B如本说明书中所定义。这些化合物可用于控制或预防急性和/或慢性神经障碍，例如作为由旁路手术或移植引起的限制性脑功能，脑供血不足，脊髓损伤，头部损伤，怀孕引起的缺氧，心脏骤停，低血糖，阿尔茨海默病，亨廷顿舞蹈症，ALS，艾滋病引起的痴呆，眼睛损伤，视网膜病变，认知障碍，记忆缺陷，精神分裂症，由药物引起的特发性帕金森综合症或帕金森综合征以及导致谷氨酸缺乏功能的病症，例如肌肉痉挛，抽搐，偏头痛，尿失禁，尼古丁成瘾，精神病，鸦片成瘾，焦虑，呕吐，急性和慢性疼痛，运动障碍和抑郁症。

34. 发明申请

US20080261957A1 DIHYDRO-BENZO[B][1,4]DIAZEPIN-2-ONE SULFONAMIDE DERIVATIVES 失效
标题翻译：二氢苯并[B] [1,4]二氮杂-2-酮磺酰胺衍生物
公开(公告)号：US20080261957A1
公开(公告)日：2008-10-23
申请号：US12102140
申请日：2008-04-14
申请人： Silvia Gatti McArthur , Juergen Wichmann , Thomas Johannes Woltering
发明人： Silvia Gatti McArthur , Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31/551 , C07D243/12
CPC分类号： C07D243/24
摘要： The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) wherein R1, R2, R3 and R4 are defined as in the specification.
摘要翻译：本发明涉及式（I）化合物，其制备方法，其用于制备用于治疗CNS障碍的药物的用途和含有它们的药物组合物。式（I）化合物由通式（I）表示，其中R 1，R 2，R 3和R 4 如说明书中所定义。

35. 发明授权

US07329662B2 Pyrazolo-pyridine 失效
公开(公告)号：US07329662B2
公开(公告)日：2008-02-12
申请号：US10948970
申请日：2004-09-24
申请人： Juergen Wichmann , Thomas Johannes Woltering
发明人： Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present invention also relates to a process for their preparation, a pharmaceutical composition containing said derivatives and a method of treating or preventing acute or chronic neurological disorder comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of at least one such derivatives. These disorders include acute and chronic disorders

36. 发明授权

US07514443B2 Substituted pyrazolo[1,5-a]pyrimidines as inhibitors of metabotropic glutamate receptors 失效
标题翻译：取代的吡唑并[1,5-a]嘧啶作为代谢型谷氨酸受体的抑制剂
公开(公告)号：US07514443B2
公开(公告)日：2009-04-07
申请号：US11707480
申请日：2007-02-16
申请人： Juergen Wichmann , Thomas Johannes Woltering
发明人： Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D487/04 , A61K31/519 , A61P25/16 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/30 , A61P25/06
CPC分类号： C07D487/04
摘要： The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present invention also relates to a process for their preparation, a pharmaceutical composition containing said derivatives and a method of treating or preventing acute or chronic neurological disorder comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of at least one such derivatives. These disorders include acute and chronic disorders.
摘要翻译：本发明涉及式I的新型吡唑并咪唑并嘧啶衍生物，其中A，D，E，L，M，Q，R 1，R 2和R 3如上所定义。本发明还涉及其制备方法，含有所述衍生物的药物组合物和治疗或预防急性或慢性神经障碍的方法，包括向需要这种治疗的患者施用药物组合物，其包含治疗有效量的至少一个此类衍生物。这些疾病包括急性和慢性疾病。

37. 发明授权

US07511033B2 Dihydro-benzo[B][1,4]diazepin-2-one sulfonamide derivatives 失效
标题翻译：二氢 - 苯并[b] [1,4]二氮杂-2-酮磺酰胺衍生物
公开(公告)号：US07511033B2
公开(公告)日：2009-03-31
申请号：US12102140
申请日：2008-04-14
申请人： Silvia Gatti McArthur , Juergen Wichmann , Thomas Johannes Woltering
发明人： Silvia Gatti McArthur , Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D243/24 , A61K31/5513 , A61P25/00
CPC分类号： C07D243/24
摘要： The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical compositions containing them. Compounds of formula (I) are represented by general formula (I) wherein R1, R2, R3 and R4 are defined as in the specification.
摘要翻译：本发明涉及式（I）化合物，其制备方法，其用于制备用于治疗CNS障碍的药物的用途和含有它们的药物组合物。式（I）的化合物由通式（I）表示，其中R1，R2，R3和R4如说明书中所定义。

38. 发明授权

US5869500A Pyridone compounds useful in treating Alzheimer's disease 失效
标题翻译：可用于治疗阿尔茨海默病的吡啶酮化合物
公开(公告)号：US5869500A
公开(公告)日：1999-02-09
申请号：US976541
申请日：1997-11-24
申请人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
发明人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
IPC分类号： C07D455/02 , C07D455/06 , C07D471/14 , C07D495/14 , A61K31/44 , A61K31/38 , A61K31/40 , A61K31/55
CPC分类号： C07D471/14 , C07D455/02 , C07D455/06 , C07D495/14
摘要： The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula ##STR1## where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及使用本文所述的式Ⅰ，R1，R3，R4和R7的式和其三价环吡啶酮化合物及其药学上可接受的盐，用于生产药物用于预防或治疗与抑制β-淀粉样蛋白肽活性相关的疾病，特别是用于治疗阿尔茨海默病。

39. 发明授权

US6030984A Pyridone compounds useful in treating Alzheimer's disease 失效
标题翻译：可用于治疗阿尔茨海默病的吡啶酮化合物
公开(公告)号：US6030984A
公开(公告)日：2000-02-29
申请号：US161853
申请日：1998-09-28
申请人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
发明人： Gerda Huber Trottmann , Roland Jakob-Roetne , Sabine Kolczewski , Roger David Norcross , Thomas Johannes Woltering
IPC分类号： C07D455/02 , C07D455/06 , C07D471/14 , C07D495/14 , A61K31/44 , A61K31/38 , A61K31/40 , A61K31/55 , C07D401/00
CPC分类号： C07D471/14 , C07D455/02 , C07D455/06 , C07D495/14
摘要： The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及使用下式的双和三环吡啶酮化合物，其中A，R 1，R 3，R 4和R 7在此描述及其药学上可接受的盐用于制备用于预防或治疗疾病的药物与β-淀粉样蛋白肽活性的抑制有关，特别是用于治疗阿尔茨海默氏病。

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