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1. 发明申请

WO03097633A8 2-THIO-SUBSTITUTED IMIDAZOLE DERIVATIVES AND THEIR USE IN PHARMACEUTICS 审中-公开
标题翻译： 2-硫代取代的咪唑衍生物及其在药店
公开(公告)号：WO03097633A8
公开(公告)日：2004-04-01
申请号：PCT/EP0305172
申请日：2003-05-16
申请人： MERCKLE GMBH , LAUFER STEFAN , STRIEGEL HANS-GUENTER , ALBRECHT WOLFGANG , TOLLMANN KAROLA
发明人： LAUFER STEFAN , STRIEGEL HANS-GUENTER , ALBRECHT WOLFGANG , TOLLMANN KAROLA
IPC分类号： A61K31/4439 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/06 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , A61K31/4164
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14
摘要： The invention relates to 2-thio-substituted imidazole derivatives of formula (I), wherein radicals R1, R2, R3, R4 and p have the meanings as cited in the description. The inventive compounds comprise an immunomodulating effect and/or an action that inhibits the release of cytokine, and are thus suited for treating diseases associated with a disorder of the immune system.
摘要翻译：本发明涉及式（I）到其中的基团RI，R2，R3，R4和p具有在说明书中给出的含义2-硫代 - 取代的咪唑衍生物。本发明的化合物具有免疫调节和/或细胞因子释放的抑制效果，因此用于治疗与免疫相关系统病症相关的疾病是有用的。

2. 发明申请

WO0105792A9 ANTI-INFLAMMATORY OXO DERIVATIVES AND HYDROXY DERIVATIVES OF PYRROLIZINES, AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：作者羟基衍生物PYRROLIZINEN抗炎氧代和及其在药学应用
公开(公告)号：WO0105792A9
公开(公告)日：2002-08-29
申请号：PCT/EP9909057
申请日：1999-11-23
申请人： MERCKLE GMBH , LAUFER STEFAN , NEHER KAROLA , STRIEGEL HANS-GUENTER
发明人： LAUFER STEFAN , NEHER KAROLA , STRIEGEL HANS-GUENTER
IPC分类号： A61K31/00 , A61K31/407 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I), wherein one of the radicals R8 and R9 represents a hydrogen atom or an alkyl group and the other represents hydroxyl, alkoxy or acyloxy or whereby, R8 and R9, together with the carbon atom, on which they are bound, represent a carbonyl group, and the radicals R1 to R7 have the meanings as cited in the description. The compounds inhibit the release of different mediators of the arachidonic acid cascade and are thus useful for preventing allergically induced illnesses or for treating illnesses of the rheumatic form circle.
摘要翻译：本发明涉及式（I）其中基团R 8和R 9中的一个表示氢原子或烷基而另一个是羟基，烷氧基或酰氧基或其中R8和R9与相连碳原子一起与它们所连接的化合物代表羰基和基团R1至R7具有说明书中给出的含义。化合物抑制花生四烯酸级联的各种介质的释放并因此用于预防allergically诱导的疾病或用于的风湿性类型可用的疾病的治疗。

3. 发明申请

WO2008012110A3 ANNELLATED PYRROLE COMPOUNDS FOR CANCER MANAGEMENT 审中-公开
标题翻译：新型吡咯类化合物用于癌症治疗
公开(公告)号：WO2008012110A3
公开(公告)日：2008-04-10
申请号：PCT/EP2007006735
申请日：2007-07-30
申请人： MERCKLE GMBH , LAUFER STEFAN , GUARNIERI TIZIANA , TAVOLARI SIMONA , TOMASI VITTORIO , PALAZZINI ERNESTO , BARBANTI MIRIAM
发明人： LAUFER STEFAN , GUARNIERI TIZIANA , TAVOLARI SIMONA , TOMASI VITTORIO , PALAZZINI ERNESTO , BARBANTI MIRIAM
IPC分类号： A61K31/407 , A61P35/00
CPC分类号： A61K31/407
摘要： The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e. g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same. This treatment ameliorates, diminishes, actively treats, reverses or prevents any disease related to insufficient apoptosis, in particular neoplasia, and it may be combined with irradiation, heating and treatment with a cytotoxic agent for preventive and/or curative purposes.
摘要翻译：本发明涉及口服吡咯化合物，特别是ML3000（Licofelone），其盐或衍生物用于癌症治疗，并且一般涉及式（I）化合物的用途：其中变量具有给定的含义在本说明书中，用于预防和/或治疗瘤形成，特别是选自由乳头瘤，癌，腺瘤和腺癌组成的组的瘤形成， G。人气道或结直肠癌，优选快速生长，多药耐药性和/或COX-2阴性瘤形成。本发明进一步涉及用于上述目的的药物组合物，其包含螺化的吡咯化合物，特别是ML3000（Licofelone），其旋光异构体，盐或衍生物，以及治疗和/或预防瘤形成和/或恢复在失去细胞的细胞中发生细胞凋亡的能力。该治疗改善，减少，积极治疗，逆转或预防任何与细胞凋亡不足有关的疾病，特别是瘤形成，并且可以将其与辐射，加热和用细胞毒剂治疗组合用于预防和/或治疗目的。

4. 发明申请

WO0157042A3 4-PYRIDYL-AND 2,4-PYRIMIDINYL-SUBSTITUTED PYRROLE DERIVATIVES AND THEIR USE IN PHARMACY 审中-公开
标题翻译： 4-吡啶基和2,4-嘧啶基取代的吡咯衍生物及其在药学使用
公开(公告)号：WO0157042A3
公开(公告)日：2001-12-27
申请号：PCT/EP0101011
申请日：2001-01-31
申请人： MERCKLE GMBH , STRIEGEL HANS GUENTER , LAUFER STEFAN , TOLLMANN KAROLA , TRIES SUSANNE
发明人： STRIEGEL HANS-GUENTER , LAUFER STEFAN , TOLLMANN KAROLA , TRIES SUSANNE
IPC分类号： A61K31/4439 , A61K31/444 , A61K31/5365 , A61K31/542 , A61P1/00 , A61P11/16 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/395
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention concerns 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives of formula (1) and their use in pharmacy, wherein the variables have the meaning cited in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting effect and are hence useful for the treatment of diseases associated with disorders of the immune system.
摘要翻译：本发明是4-吡啶基和2,4-嘧啶基取代的吡咯衍生物及其在式（1）的药物的用途，其中各变量具有说明书中给出的含义。新化合物具有免疫调节和/或细胞因子释放炎症效果，因此用于治疗与免疫相关系统病症相关的疾病是有用的。

5. 发明申请

WO2006120010A3 DIBENZOCYCLOHEPTANE COMPOUNDS AND PHARMACEUTICALS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： DIBENZOCYCLOHEPTANVERBINDUNGEN与药品这些化合物
公开(公告)号：WO2006120010A3
公开(公告)日：2007-01-18
申请号：PCT/EP2006004488
申请日：2006-05-12
申请人： MERCKLE GMBH , LAUFER STEFAN , ALBRECHT WOLFGANG , GREIM CORNELIA , STRIEGEL HANS-GUENTER , TOLLMANN KAROLA
发明人： LAUFER STEFAN , ALBRECHT WOLFGANG , GREIM CORNELIA , STRIEGEL HANS-GUENTER , TOLLMANN KAROLA
IPC分类号： C07D313/12 , A61K31/335 , A61P29/00
CPC分类号： C07D313/12 , C07C225/22 , C07D337/12 , C07D491/044
摘要： The present invention relates to compounds of formula (I), in which R1, R2, R3, R4, X and Y have the meanings indicated in the description. These compounds have immuno-modulating effects, as well as an inhibiting or regulating effect on the release of IL-1ß and/or TNF-a. They can therefore be used for the treatment of diseases associated with a disturbance of the immune system.
摘要翻译：本发明涉及式（I）的化合物，其中R1，R2，R3，R4，X和Y具有在说明书中给出的含义。所述化合物具有免疫调节和IL-1β和/或TNF-α的抑制或调节活性的释放。因此，它们可用于治疗与免疫系统紊乱有关的疾病。

6. 发明申请

WO02066458A2 2-THIO-SUBSTITUTED IMIDAZOLE DERIVATIVES AND THE USE THEREOF IN THE PHARMACEUTICAL INDUSTRY 审中-公开
标题翻译： 2-硫代取代的咪唑衍生物及其在药店
公开(公告)号：WO02066458A2
公开(公告)日：2002-08-29
申请号：PCT/EP0201746
申请日：2002-02-19
申请人： MERCKLE GMBH , LAUFER STEFAN , KOTSCHENREUTHER DUNJA , MERCKLE PHILIPP , TOLLMANN KAROLA , STRIEGEL HANS-GUENTER
发明人： LAUFER STEFAN , KOTSCHENREUTHER DUNJA , MERCKLE PHILIPP , TOLLMANN KAROLA , STRIEGEL HANS-GUENTER
IPC分类号： A61K31/164 , A61K31/4164 , A61K31/4439 , A61K31/4545 , A61K31/5377 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P17/06 , A61P17/14 , A61P19/06 , A61P19/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention relates to 2-thio-substituted imidazole derivatives of formula I, wherein the groups R1, R2, R3 and R4 are defined as per the description. The inventive compounds have an immunomodulating action and/or an inhibitive action on the release of cytokine and are therefore suitable for treating diseases, which are related to the dysfunction of the immune system.
摘要翻译：本发明涉及式I的2-硫代 - 取代的咪唑衍生物，其中基团R1，R2，R3和R4具有在说明书中给出的含义。本发明的化合物具有免疫调节和/或细胞因子释放的抑制效果，因此用于治疗与免疫相关系统病症相关的疾病是有用的。

7. 发明专利

RS51877B METHOD FOR THE PRODUCTION OF 6-(4-CHLOROPHENYL)-2,2-DIMETHYL -7-PHENYL-2,3-DIHYDRO-1H-PYRROLIZIN-5-YLACETIC ACID 未知
公开(公告)号：RS51877B
公开(公告)日：2012-02-29
申请号：YUP14604
申请日：2002-08-21
申请人： MERCKLE GMBH
发明人： DANNHARDT GERD , KAMMERMEIER THOMAS , MERCKLE PHILIPP , STRIEGEL HANS-GUENTER , LAUFER STEFAN
IPC分类号： C07D487/04 , C07D207/20
摘要： The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with omega-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.

8. 发明专利

AU2003267000B2 2-thio-substituted imidazole derivatives and their use in pharmaceutics 未知
公开(公告)号：AU2003267000B2
公开(公告)日：2009-05-28
申请号：AU2003267000
申请日：2003-08-20
申请人： MERCKLE GMBH
发明人： STRIEGEL HANS-GUNTER , ALBRECHT WOLFGANG , TOLLMANN KAROLA , LAUFER STEFAN
IPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/06 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D493/04
摘要： The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3 and m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.

9. 发明专利

DK1419160T3 未知
公开(公告)号：DK1419160T3
公开(公告)日：2009-04-14
申请号：DK02767415
申请日：2002-08-21
申请人： MERCKLE GMBH
发明人： DANNHARDT GERD , KAMMERMEIER THOMAS , MERCKLE PHILIPP , STRIEGEL HANS-GUENTER , LAUFER STEFAN
IPC分类号： C07D487/04 , C07D207/20
摘要： The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with omega-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.

10. 发明专利

DE50213105D1 未知
公开(公告)号：DE50213105D1
公开(公告)日：2009-01-22
申请号：DE50213105
申请日：2002-08-21
申请人： MERCKLE GMBH
发明人： DANNHARDT GERD , KAMMERMEIER THOMAS , MERCKLE PHILIPP , STRIEGEL HANS-GUENTER , LAUFER STEFAN
IPC分类号： C07D487/04 , C07D207/20
摘要： The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with omega-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.

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