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91. 发明申请

US20050171025A1 Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents 失效
标题翻译：二肽基肽酶IV抑制剂及其用途作为抗癌剂
公开(公告)号：US20050171025A1
公开(公告)日：2005-08-04
申请号：US11093991
申请日：2005-03-30
申请人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
发明人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
IPC分类号： A61K31/401 , A61K31/426 , A61K38/04 , A61K38/05 , A61K38/06
CPC分类号： A61K31/401 , A61K31/426 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55
摘要： The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.
摘要翻译：本发明提供本发明的DPIV-抑制剂及其相应的药学上可接受的酸加成盐形式的新用途，用于治疗由DPIV或DPIV样酶如癌和肿瘤介导的病症。在更优选的实施方案中，本发明的化合物可用于治疗转移和肿瘤定植。

92. 发明授权

US06849624B2 Aromatic and heteroaromatic substituted amides 失效
标题翻译：芳香族和杂芳香族取代的酰胺
公开(公告)号：US06849624B2
公开(公告)日：2005-02-01
申请号：US10196795
申请日：2002-07-17
申请人： Theresa Maria Ballard , Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
发明人： Theresa Maria Ballard , Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
IPC分类号： A61K31/541 , A61P1/00 , A61P1/08 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/02 , A61P13/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D213/75 , A61K31/54 , C07D279/10 , C07D279/12 , C07D295/00
CPC分类号： C07D213/75
摘要： The invention is the compounds 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide. Compounds of the invention are useful in pharmaceutical compositions for the treatment of migraine, rheumatoid arthritis, asthma, bronchial hyperreactivity, inflammatory bowel disease or for the treatment of disorders including Parkinson's disease, anxiety, depression, pain, headache, Alzheimer's disease, multiple sclerosis, edema, allergic rhinitis, Crohn's disease, ocular injury, ocular inflammatory diseases, psychosis, motion sickness, induced vomiting, emesis, urinary incontinence, psychoimmunologic or psychosomatic disorders, cancer, withdrawal symptoms of addictive drugs from opiates or nicotine, traumatic brain injury or benign prostatic hyperplasia.
摘要翻译：本发明是化合物2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1λ6 - 硫代吗啉-4-基）-4-邻甲苯基 - 吡啶-3-基] -N-甲基 - 异丁酰胺和2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1λ6-硫代吗啉-4-基）-4- （4-氟-2-甲基 - 苯基） - 吡啶-3-基] -N-甲基 - 异丁酰胺本发明的化合物可用于治疗偏头痛，类风湿性关节炎，哮喘，支气管高反应性，炎性肠的药物组合物疾病或治疗包括帕金森病，焦虑症，抑郁症，疼痛，头痛，阿尔茨海默病，多发性硬化，水肿，过敏性鼻炎，克罗恩病，眼部损伤，眼部炎性疾病，精神病，晕车症，诱发呕吐，呕吐，尿失禁，心理免疫或心身疾病，癌症，阿片剂或尼古丁成瘾药物的戒断症状，创伤性脑损伤或良性前列腺增生。

93. 发明授权

US06756380B1 5-phenyl-pyrimidine derivatives 失效
标题翻译： 5-苯基 - 嘧啶衍生物
公开(公告)号：US06756380B1
公开(公告)日：2004-06-29
申请号：US09575789
申请日：2000-05-22
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07D23932
CPC分类号： C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48
摘要： Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon ring atoms to which they are attached form a fused ring, with the proviso that n for R1 is 1; n is independently 0-2; and X is —C(O)N(R4″)— or —N(R4″)C(O)—; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：描述通式的化合物：其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 3是卤素，三氟甲基，低级烷氧基或低级烷基; R 4 R 5是氢或低级烷基; R 5是低级烷基，低级烷氧基，氨基，羟基，羟基 - 低级烷基， - （CH 2）n - 哌嗪基，任选被低级烷基取代，（CH2）n-吗啉基， - （CH2）n + 1-咪唑基，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基，低级烷基 - ，苄基氨基，-NH-（CH 2）n + 1N（R 4“）2， - （CH 2）n -NH-（CH 2）n + 1N（R 4”）2， - （CH 2） n + 1N（R 4“）2或-O-（CH 2）n + 1N（R 4”）2，其中R 4“是氢或低级烷基; R 6' R 2和R 6或R 1和R 6可以一起为-CH = CH-CH = CH-，其中R 2和R 6或R 1为氢; 和R 6分别与它们所连接的两个碳环原子一起形成稠合环，条件是R 1的n为1; n独立地为0-2; 和X是-C（O）N（R“”） - 或-N（R“”）C（O） - ;及其药学上可接受的酸加成盐。

94. 发明授权

US06624176B2 Heteroaromatic substituted amides with antagonistic activity to neurokinin 1 receptors 有权
公开(公告)号：US06624176B2
公开(公告)日：2003-09-23
申请号：US10282357
申请日：2002-10-29
申请人： Torsten Hoffmann , Patrick Schnider , Heinz Stadler
发明人： Torsten Hoffmann , Patrick Schnider , Heinz Stadler
IPC分类号： A61K31453
CPC分类号： C07D213/75 , C07D213/82 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D413/04
摘要： The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

95. 发明授权

US06576762B2 Heteroaromatic substituted amides with antagonistic activity to neurokinin 1 receptors 有权
公开(公告)号：US06576762B2
公开(公告)日：2003-06-10
申请号：US09901311
申请日：2001-07-09
申请人： Torsten Hoffmann , Patrick Schnider , Heinz Stadler
发明人： Torsten Hoffmann , Patrick Schnider , Heinz Stadler
IPC分类号： C07D26528
CPC分类号： C07D213/75 , C07D213/82 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D413/04
摘要： The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

96. 发明授权

US06512001B1 D-proline derivatives 有权
标题翻译： D-脯氨酸衍生物
公开(公告)号：US06512001B1
公开(公告)日：2003-01-28
申请号：US09636076
申请日：2000-08-10
申请人： Cornelia Hertel , Torsten Hoffmann , Roland Jakob-Roetne , Roger David Norcross
发明人： Cornelia Hertel , Torsten Hoffmann , Roland Jakob-Roetne , Roger David Norcross
IPC分类号： A61K314025
CPC分类号： C07D231/12 , C07D207/16 , C07D207/22 , C07D233/56 , C07D249/08 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
摘要翻译：新化合物具有下式：其中R，R 1，X和Y具有本文所述的含义。阐述了合成这些化合物和使用这些化合物治疗与淀粉样变性相关疾病如阿尔茨海默病，成熟发病的糖尿病，家族性淀粉样多发性神经病，瘙痒病和克雷伊兹费尔德 - 雅各布病的方法。

97. 发明授权

US06482829B2 Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor 失效
标题翻译：作为神经激肽1受体的拮抗剂活性的取代的杂环螺癸烷化合物
公开(公告)号：US06482829B2
公开(公告)日：2002-11-19
申请号：US09861795
申请日：2001-05-21
申请人： Guido Galley , Thierry Godel , Annick Goergler , Torsten Hoffmann , Sabine Kolczewski , Stephan Roever
发明人： Guido Galley , Thierry Godel , Annick Goergler , Torsten Hoffmann , Sabine Kolczewski , Stephan Roever
IPC分类号： A61K311454
CPC分类号： C07D471/10 , A61K9/0031 , A61K9/02 , A61K9/2018 , A61K9/4858
摘要： The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.
摘要翻译：本发明涉及本文所述的式的化合物及其药学上可接受的酸加成盐。所述化合物对NK1受体具有良好的亲和力。

98. 发明授权

US06407111B1 Phenyl substituted pyridine and benzene derivatives 失效
标题翻译：苯基取代吡啶和苯衍生物
公开(公告)号：US06407111B1
公开(公告)日：2002-06-18
申请号：US09505356
申请日：2000-02-16
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： A61K31496
CPC分类号： C07D213/75 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/40 , C07C323/41 , C07D295/135
摘要： The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.
摘要翻译：本发明是由苯基取代的吡啶或苯衍生物及其药学上可接受的盐形成的一系列化合物。这些化合物显示出高亲和力作为NK-1受体的拮抗剂。

99. 发明授权

US06291465B1 Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US06291465B1
公开(公告)日：2001-09-18
申请号：US09513147
申请日：2000-02-25
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07C23300
CPC分类号： C07D295/155 , C07C217/54 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42
摘要： The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.
摘要翻译：本发明涉及式的化合物，其中R是氢，低级烷基，低级烷氧基卤素，氨基，-N（R6）2或三氟甲基; R1是氢低级烷氧基或卤素，R和R1可以一起是-CH = CH-CH = CH-; R 2为卤素，低级烷基或三氟甲基; R 3为氢或低级烷基; R 4为氢或环状叔胺，任选被低级烷基取代; R 5为氢，硝基，氨基或-N（R 6） X是-C（O）N（R6） - ， - （CH2）nO-，（CH2）nN（R6） - ， - （R6）C（O） - 或-N ）（CH 2）n - 和n为1或2;及其药学上可接受的酸加成盐。式I化合物可用于治疗与NK-1受体有关的疾病。

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