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1. 发明公开

EP1325008A1 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1325008A1
公开(公告)日：2003-07-09
申请号：EP01962869.2
申请日：2001-07-24
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： BENTLEY, Jonathan, Mark , HEBEISEN, Paul , MULLER, Marc , RICHTER, Hans , ROEVER, Stephan , MATTEI, Patrizio , TAYLOR, Sven
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10
CPC分类号： C07D487/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1. They can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnoea.

2. 发明授权

EP1370561B1 TETRAHYDRO-PYRAZINO[1,2-A]INDOLES FOR THE TREATMENT OF CENTRAL NERVOUS DISORDERS 有权
标题翻译： TETRA HYDRO吡嗪并[1,2-A]吲哚用于中央神经系统疾病的治疗
公开(公告)号：EP1370561B1
公开(公告)日：2009-02-11
申请号：EP02732459.9
申请日：2002-03-06
申请人： F. Hoffmann-La Roche AG , VERNALIS RESEARCH LIMITED
发明人： HEBEISEN, Paul , MATTEI, Patrizio , MULLER, Marc , RICHTER, Hans , ROEVER, Stephan , TAYLOR, Sven
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00
CPC分类号： C07D487/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R7 have the significance given in the description and the claims. The compounds can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, type II diabetes, obesity and sleep apnoea.

3. 发明授权

EP1325008B1 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1325008B1
公开(公告)日：2005-10-05
申请号：EP01962869.2
申请日：2001-07-24
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： BENTLEY, Jonathan, Mark , HEBEISEN, Paul , MULLER, Marc , RICHTER, Hans , ROEVER, Stephan , MATTEI, Patrizio , TAYLOR, Sven
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10
CPC分类号： C07D487/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1. They can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnoea.

4. 发明公开

EP1370561A2 TETRAHYDRO-PYRAZINO[1,2-A]INDOLES FOR THE TREATMENT OF CENTRAL NERVOUS DISORDERS 有权
标题翻译： TETRA HYDRO吡嗪并[1,2-A]吲哚用于中央神经系统疾病的治疗
公开(公告)号：EP1370561A2
公开(公告)日：2003-12-17
申请号：EP02732459.9
申请日：2002-03-06
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： HEBEISEN, Paul , MATTEI, Patrizio , MULLER, Marc , RICHTER, Hans , ROEVER, Stephan , TAYLOR, Sven
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00
CPC分类号： C07D487/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R7 have the significance given in the description and the claims. The compounds can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, type II diabetes, obesity and sleep apnoea.

5. 发明公开

EP1056716A1 CYCLOHEXANEDIOLE DERIVATIVES 有权
标题翻译： CYCLOHEXANDIOL衍
公开(公告)号：EP1056716A1
公开(公告)日：2000-12-06
申请号：EP99906250.8
申请日：1999-02-20
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BARBIER, Pierre , BAUER, Franz , MOHR, Peter , MULLER, Marc , PIRSON, Wolfgang
IPC分类号： C07C403/08 , C07F7/18 , A61K31/045
CPC分类号： C07F7/1852 , C07B2200/07 , C07B2200/09 , C07C17/00 , C07C45/29 , C07C45/292 , C07C47/19 , C07C47/263 , C07C47/273 , C07C403/08 , C07C2601/14 , C07C21/14 , C07C47/21 , C07C47/195
摘要： Compounds of formula (I) wherein X is C=CH2 or CH2; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is -C C-, -CH=CH- or -CH2-CH2-; R?1 and R2¿ are independently of each other alkyl or perfluoroalkyl; and R3 is lower alkyl; are useful in the treatment or prevention of hyperproliferative skin diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; or for reversing the conditions associated with photodamage.
摘要翻译：式I的化合物，其中X为C = CH 2或CH 2; Y和Z彼此独立地为氢，氟或羟基; A为-C = C - ， - CH = CH-或-CH 2 -CH 2 - ，R 1和R 2独立地为的其它烷基或全氟烷基; R 3为低级烷基，可用于治疗或预防过度增生性皮肤病，特别是牛皮癣，基底细胞癌，角质化和角化病症; 或用于逆转与光损伤相关的条件。

6. 发明公开

EP0977734A2 ARYLSECOCHOLADIENE DERIVATIVES 失效
标题翻译：芳香族二茂铁衍生物
公开(公告)号：EP0977734A2
公开(公告)日：2000-02-09
申请号：EP98922685.7
申请日：1998-04-11
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BARBIER, Pierre , BAUER, Franz , MOHR, Peter , MULLER, Marc , PIRSON, Wolfgang
IPC分类号： C07C401/00
CPC分类号： C07C69/88 , C07C35/32 , C07C401/00 , C07F7/1856
摘要： 24-Nor-secochola-5,7-diene derivatives of formula (I) wherein A is a single or double bond, B is a group CH2CH2, CH=CH or C C, T is a group CH2 or CH2CH2, R?1 and R3¿ are H or OH, C(R,R) is CH¿2? or C=CH2, R?2¿ is CH¿3? and R?4¿ is H, or R2 is H and R4 is CH¿3?, L is phenyl and R?5¿ is OH or C(C¿1-4?-alkyl)2OH, or L-R?5¿ is 2-furyl which is 5-substituted by C(C¿1-4?-alkyl)2OH, with the proviso that when L is phenyl, A is a single bond, B is C C, T is CH2, each R?1 and R3¿ are OH, C(R,R) is C=CH¿2, R?2 is CH¿3, R?4 is H, and R5 is C(CH¿3?)2OH, then R?5¿ must be in position ortho or para, are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.
摘要翻译：其中A为单键或双键，B为基团CH 2 CH 2，CH = CH或CC，T为基团CH 2或CH 2 CH 2，R 1和R 2的式（I）的24-去乙酰基-5,7-二烯衍生物 R3是H或OH，C（R，R）是CH2- 或C = CH 2，R 2'是CH 3' R 4是H，或R 2是H，R 4是CH 3，L是苯基，R 5是OH或C（C 1-4 - 烷基）2 OH，或者LR 5是由C（C 1-4 - 烷基）2 OH 5-取代的2-呋喃基，条件是当L是苯基时，A是单键，B是CC，T是CH 2，各R 1和 R 3是OH，C（R，R）是C = CH 2，R 2是CH 3，R 4是H，并且R 5是C（CH 3）2 OH，则R 5必须位于原位或对位，可用于治疗或预防维生素D依赖性疾病，特别是牛皮癣，基底细胞癌，角化和角化病，白血病，骨质疏松症，伴随肾衰竭的甲状旁腺功能亢进，移植排斥和移植物抗宿主病。

7. 发明公开

EP0805682A1 DERMATOLOGICAL USE OF VITAMIN D DERIVATIVES 失效
标题翻译：维生素D衍生物的皮肤病学用途
公开(公告)号：EP0805682A1
公开(公告)日：1997-11-12
申请号：EP96901286.0
申请日：1996-01-17
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BARBIER, Pierre , MULLER, Marc , STADLWIESER, Josef
IPC分类号： A61K31 , A61P3 , A61P17 , A61P35 , C07C401
CPC分类号： A61K31/593 , C07C401/00
摘要： Vitamin D derivatives of formula (I), wherein: X is =CH2 or H,H; Y is a moiety (a) -CH(CH3)-(A)n-C(O)-OR1, (b) -CH(CH¿3?)-CH2-O-C(O)-R?2¿ or (c) -C(O)-OR1; A is -CH=CH- or CH¿2?-CH2-; R?1¿ is lower alkyl, cycloalkyl, cycloalkylmethyl, -CH¿2R?3 or -CH¿2?-CH2R?3; R2¿ is lower alkyl, cycloalkyl or R3; R3 is hydroxy-lower alkyl, hydroxy-cycloalkyl or trifluoromethyl-hydroxy-nieder-alkyl; n is 0 or 1; and the dotted bond in the five-membered ring is optional; can be used in the treatment of dermatological conditions, in particular keratinization disorders.

8. 发明公开

EP1230224A1 SUBSTITUIERTE 5-BENZYL-2,4-DIAMINOPYRIMIDINE 有权
标题翻译：取代的5-苄基-2,4-二氨基嘧啶
公开(公告)号：EP1230224A1
公开(公告)日：2002-08-14
申请号：EP00969149.4
申请日：2000-10-27
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GUERRY, Philippe , MOHR, Peter , MULLER, Marc , MUELLER, Werner , PFLIEGER, Philippe
IPC分类号： C07D239/49 , A61K31/505 , A61P31/04
CPC分类号： C07D239/49 , A61K31/505
摘要： The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A), wherein R1 is C2-C3 alkyl and R2 is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3 is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclylsulfonyl, heterocyclyalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alkenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R?2 and R3¿ can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations. The products have antibiotic properties and are useful for combating or preventing infectious diseases.

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