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1. 发明专利

IL260366A Quinolin-2-one derivatives, their preparation and use 未知
公开(公告)号：IL260366A
公开(公告)日：2020-08-31
申请号：IL26036618
申请日：2018-07-02
申请人： DORSCH DIETER , MERCK PATENT GMBH , MUZERELLE MATHILDE , BURGDORF LARS , WUCHERER PLIETKER MARGARITA , CZODROWSKI PAUL , ESDAR CHRISTINA , TSAKLAKIDIS CHRISTOS
发明人： ESDAR CHRISTINA , TSAKLAKIDIS CHRISTOS , DORSCH DIETER , MUZERELLE MATHILDE , BURGDORF LARS , WUCHERER-PLIETKER MARGARITA , CZODROWSKI PAUL
IPC分类号： A61K31/4704 , A61K31/436 , A61K31/5377 , A61K31/5513 , A61P35/00
摘要： Compounds of the formula Iin which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in claim 1,are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

2. 发明申请

WO2004087646A2 CARBONYLVERBINDUNGEN 审中-公开
标题翻译：羰基
公开(公告)号：WO2004087646A2
公开(公告)日：2004-10-14
申请号：PCT/EP2004/002350
申请日：2004-03-08
申请人： MERCK PATENT GMBH , TSAKLAKIDIS, Christos , DORSCH, Dieter , MEDERSKI, Werner , CEZANNE, Bertram , GLEITZ, Johannes
发明人： TSAKLAKIDIS, Christos , DORSCH, Dieter , MEDERSKI, Werner , CEZANNE, Bertram , GLEITZ, Johannes
IPC分类号： C07D
CPC分类号： C07D413/12 , C07D207/16 , C07D207/27 , C07D211/60 , C07D211/76 , C07D213/64 , C07D213/68 , C07D223/10 , C07D241/18 , C07D265/08 , C07D265/32 , C07D267/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/02 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08
摘要： Neue Verbindungen der Formel (I), worin D, E, G, W, X, Y, T, R 1 und R 2 die in Patentanspruch 1 angegebene Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und können zur Prophylaxe und/oder Therapie von thromboembolischen Erkrankungen und zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：新的式（I）化合物，其中D，E，G，W，X，Y，T，R <1>和R <2>的权利要求1中所示的含义，是凝血因子Xa的抑制剂，可用于预防和 /或血栓栓塞性疾病和用于治疗肿瘤的治疗可以使用。

3. 发明申请

WO2003093254A1 SEMICARBAZIDDERIVATE ZUR BEKÄMPUNG VON THROMBOEMBOLISCHEN KRANKHEITEN 审中-公开
标题翻译： SEMICARBAZIDDERIVATE用于疾病血栓栓塞BEKÄMPUNG
公开(公告)号：WO2003093254A1
公开(公告)日：2003-11-13
申请号：PCT/EP2003/003581
申请日：2003-04-07
申请人： MERCK PATENT GMBH , MEDERSKI, Werner , TSAKLAKIDIS, Christos , CEZANNE, Bertram , DORSCH, Dieter , BARNES, Christopher , GLEITZ, Johannes
发明人： MEDERSKI, Werner , TSAKLAKIDIS, Christos , CEZANNE, Bertram , DORSCH, Dieter , BARNES, Christopher , GLEITZ, Johannes
IPC分类号： C07D295/135
CPC分类号： C07D207/26 , C07D211/76 , C07D213/64 , C07D223/10 , C07D237/14 , C07D241/08 , C07D263/22 , C07D265/32 , C07D295/135 , C07D453/06
摘要： Neue Verbindungen der Formel I worin R, R 1 , R 1 , X die in Patentanspruch 1 angegebenen Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und können zur Prophylaxe und/oder Therapie von thromboembolischen Erkrankungen und zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：新的式I化合物，其中R，R <1>，R <1>中，X具有权利要求1中给出的含义，是凝血因子Xa的抑制剂，可用于预防和/或血栓栓塞性疾病的治疗和用于治疗肿瘤，

4. 发明申请

WO2003074479A1 SEMICARBAZIDDERIVATE UND IHRE VERWENDUNG ALS ANTITHROMBOTIKA 审中-公开
标题翻译： SEMICARBAZIDDERIVATE及其作为抗血栓药的使用
公开(公告)号：WO2003074479A1
公开(公告)日：2003-09-12
申请号：PCT/EP2003/001177
申请日：2003-02-06
申请人： MERCK PATENT GMBH , MEDERSKI, Werner , CEZANNE, Bertram , TSAKLAKIDIS, Christos , DORSCH, Dieter , BARNES, Christopher , GLEITZ, Johannes
发明人： MEDERSKI, Werner , CEZANNE, Bertram , TSAKLAKIDIS, Christos , DORSCH, Dieter , BARNES, Christopher , GLEITZ, Johannes
IPC分类号： C07C317/42
CPC分类号： C07C317/32 , C07C311/47
摘要： Neue Verbindungen der Formel I worin R, R 1 , R 2 und R 3 die in Patentanspruch 1 angegebene Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und können zur Prophylaxe und/oder Therapie von thromboembolischen Erkrankungen und zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：新的式I化合物，其中R，R1，R2和R3具有如权利要求1中所示的含义，是凝血因子Xa的抑制剂，可用于预防和/或血栓栓塞性疾病的治疗和用于治疗肿瘤。

5. 发明申请

WO2003013531A1 PHENYLDERIVATE ALS FAKTOR XA INHIBITOREN 审中-公开
标题翻译：苯基衍生物作为Xa因子抑制剂
公开(公告)号：WO2003013531A1
公开(公告)日：2003-02-20
申请号：PCT/EP2002/007798
申请日：2002-07-12
申请人： MERCK PATENT GMBH , DORSCH, Dieter , CEZANNE, Bertram , TSAKLAKIDIS, Christos , MEDERSKI, Werner , GLEITZ, Johannes , BARNES, Christopher
发明人： DORSCH, Dieter , CEZANNE, Bertram , TSAKLAKIDIS, Christos , MEDERSKI, Werner , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： A61K31/4725
CPC分类号： C07D401/12 , C07D211/76 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Neue Verbindungen der Formel (I), worin D, W, X, Y, T und R 1 die in Patentanspruch 1 angegebene Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und können zur Prophylaxe und/oder Therapie von thromboembolischen Erkrankungen und zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：式（I）的新化合物：其中D，W，X，Y，T和R <1>的权利要求1中所示的含义，是凝血因子Xa的抑制剂，可用于预防和/或血栓栓塞性疾病的治疗和用于治疗由肿瘤被使用。

6. 发明申请

WO1995000522A1 PHOSPHOSUCCINIC ACID DERIVATIVES AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译： PHOSPHONOBERNSTEINSÄUREDERIVATE及其作为药物
公开(公告)号：WO1995000522A1
公开(公告)日：1995-01-05
申请号：PCT/EP1994001980
申请日：1994-06-17
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , ESSWEIN, Angelika , ZIMMERMANN, Gerd , BAUSS, Frieder
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07F09/38
CPC分类号： C07F9/655345 , C07F9/3808 , C07F9/3826 , C07F9/383 , C07F9/3882 , C07F9/572 , C07F9/59 , C07F9/6533 , C07F9/65515 , C07F9/6552
摘要： Compounds have formula (I), in which R , R may represent independently from each other hydrogen, lower alkyl, cycloalkyl or arylmethyl; R , R may represent independently from each other hydrogen, lower alkyl, or one of the groups -OR or -NR R , or they may form together with the atoms to which they are bound a five- to seven-membered carbocyclic ring or an heterocyclic ring containing one or two heteroatoms; R stands for lower alkenyl, cycloalkyl, cycloalkenyl, monocyclic arylalkyl, bicyclic aryl, biaryl or a group having formulae (a): R -X-alk- or (b), or forms together with R and the carbon atom to which it is bound a possibly substituted five- to seven-membered carbocyclic or heterocyclic ring; R stands for hydrogen, lower alkyl or arylmethyl; R , R represent independently from each other hydrogen or lower alkyl or form together with the nitrogen atom to which they are bound a five- or six-membered heterocyclic ring; R stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, mono- or bicyclic aryl, biaryl; R stands for a group having formula (a); X stands for a valence dash, oxygen or sulphur; Q stands for oxygen, sulphur or nitrogen; alk stands for a valence dash, a methylene chain, a saturated or unsaturated alkylene chain with 2-6 carbon atoms; n equals 0-3, m equals 0-2 and p equals 0-5. Also disclosed is a process for preparing said compounds and medicaments containing the same used for treating calcium metabolism disturbances.
摘要翻译：式（I）的化合物，其中R <1>，R <2>可以是氢，低级烷基，环烷基或彼此独立地芳甲基; [R <3>，R <4>各自独立地是氢，低级烷基，或以下基团之一-OR <6>，或-NR可以是<7> - [R <8>，或连同原子它们所连接可形成五至七元碳环或含有一到两个杂原子的杂环; [R <5>低级链烯基，环烷基，环烯基，单环芳基烷基，二环芳基，联芳基或式的基团（一）：R <9> -X-烷 - 或（b）指，或者与R一起<4> 和的碳原子其所连接形成任选经取代的五到形成七元碳环或杂环; [R <6>是氢，低级烷基或芳基甲基; [R <7> - [R <8>各自独立地表示氢或低级烷基，或一起与氮原子到它们所连接，形成五至六元杂环; [R <9>是氢，低级烷基，低级烯基，环烷基，环烯基，单环或双环芳基，联芳基，R <10>为式（a）的装置; X的化合价键，代表氧或硫; Q是氧，硫或氮; alk是价键，亚甲基，一个饱和或不饱和的亚烷基链与2 - 6个碳原子的装置; N = 0-3; M = 0-2且p = 0-5的装置，其制备方法和含有这些化合物，钙代谢紊乱的治疗的药物组合物的方法。

7. 发明申请

WO1991002732A1 NOVEL OPTICALLY ACTIVE BASIC ETHERS, PROCESS FOR PRODUCING THEM AND MEDICAMENTS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译：新的光学活性基础元素，生产它们的方法和含有这些化合物的药物
公开(公告)号：WO1991002732A1
公开(公告)日：1991-03-07
申请号：PCT/EP1990001372
申请日：1990-08-20
申请人： BOEHRINGER MANNHEIM GMBH , TSAKLAKIDIS, Christos , LEINERT, Herbert , FREUND, Peter
发明人： BOEHRINGER MANNHEIM GMBH
IPC分类号： C07D401/12
CPC分类号： C07D213/30 , C07D295/145
摘要： R- and S-isomers of the compounds of formula (I) in which R1 is an unsubstituted or a mono or multi-substituted monocyclic aromatic residue or an unsubstituted or substituted five or six-membered heteroaromatic residue, R2 is an unsubstituted or mono or multi-substituted monocyclic aromatic residue or an unsubstituted or substituted five or six-membered heteroaromatic residue, R3 is hydrogen, -C=N or (a), and R4 is hydrogen or a C1-C6-alkyl residue. Process for producing them and medicaments containing these compounds and their pharmacologically acceptable salts, process for producing the compounds, medicaments containing these compounds for the treatment of heart and circulatory conditions and intermediates products to manufacture the compounds of formula (I).

8. 发明专利

IL241513D0 Piperazine derivatives their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IL241513D0
公开(公告)日：2015-11-30
申请号：IL24151315
申请日：2015-09-10
申请人： MERCK PATENT GMBH , FRIESE HAMIM MANJA , STAEHLE WOLFGANG , WIENKE DIRK , TSAKLAKIDIS CHRISTOS , LEUTHNER BIRGITTA
IPC分类号： C07D20060101
摘要： in which R, X1, X2, X3, X4, R1, R2 and q have the meanings indicated in Claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

9. 发明专利

IL239874D0 Acylguanidine derivatives, their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IL239874D0
公开(公告)日：2015-08-31
申请号：IL23987415
申请日：2015-07-09
申请人： MERCK PATENT GMBH , KLEIN MARKUS , TSAKLAKIDIS CHRISTOS , CZODROWSKI PAUL
IPC分类号： C07C20060101
摘要： The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

10. 发明专利

IL263172D0 Tricyclic heterocyclic derivatives, their preparation and use 未知
公开(公告)号：IL263172D0
公开(公告)日：2018-12-31
申请号：IL26317218
申请日：2018-11-21
申请人： DORSCH DIETER , MERCK PATENT GMBH , BURGDORF LARS , TSAKLAKIDIS CHRISTOS
发明人： DORSCH DIETER , BURGDORF LARS , TSAKLAKIDIS CHRISTOS
IPC分类号： C07D20060101
摘要： in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of ATR, and can be employed for the treatment of diseases such as cancer.

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