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1. 发明申请

WO2016053767A1 NOVEL CRYSTALLINE FORMS OF A BACE INHIBITOR, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：一种新型的晶体形态抑制剂，组合物及其使用
公开(公告)号：WO2016053767A1
公开(公告)日：2016-04-07
申请号：PCT/US2015/052096
申请日：2015-09-25
申请人： MERCK SHARP & DOHME CORP. , TRZASKA, Scott , DANCE, Zachary, E. , LIU, Yong , VARSOLONA, Richard John , YORK, Gregory
发明人： TRZASKA, Scott , LIU, Yong , VARSOLONA, Richard John , YORK, Gregory
IPC分类号： A61P25/28 , C07D285/18 , C07D417/14
CPC分类号： C07D417/12 , C07B2200/13 , C07C309/30
摘要： The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
摘要翻译：本发明提供了四种结晶形式的止卵石，以及其药学上可接受的组合物，其各自可用于治疗，预防，改善和/或延迟Aβ病理学和/或其症状或症状的发作。这种Aβ病理学的非限制性实例，包括阿尔茨海默病，在此公开。

2. 发明申请

WO00047567A1 HETERODIAZINONE DERIVATIVES 审中-公开
标题翻译：异恶唑烷酮衍生物
公开(公告)号：WO00047567A1
公开(公告)日：2000-08-17
申请号：PCT/JP2000/000799
申请日：2000-02-15
IPC分类号： A61K31/53 , A61K31/5395 , A61K31/549 , A61P25/00 , C07D249/12 , C07D271/10 , C07D271/113 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D253/06 , C07D273/04 , C07D285/18
CPC分类号： C07D271/113 , A61K31/53 , A61K31/5395 , A61K31/549 , C07D249/12 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： Heterodiazinone derivatives represented by general formula (1 ), pharmacologically acceptable salts of the same, or hydrates of both, exhibiting 2-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonism wherein A is O, S or NR (wherein R is hydrogen or lower alkyl); R and R are each independently optionally substituted (hetero)aryl or the like; and R and R are each independently hydrogen, hydroxyl, halogeno, cyano, nitro, lower alkyl, (hetero)aryl, or the like.
摘要翻译：表示2-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗作用的由通式（1）表示的异二酮二酮衍生物，它们的药理学上可接受的盐或两者的水合物，其中A是O，S 或NR 3（其中R 3是氢或低级烷基）; R 1和R 2各自独立地是任选取代的（杂）芳基等; R 4和R 5各自独立地为氢，羟基，卤代，氰基，硝基，低级烷基，（杂）芳基等。

3. 发明申请

WO00012084A1 GEOMETRICALLY RESTRICTED 2-INDOLINONE DERIVATIVES AS MODULATORS OF PROTEIN KINASE ACTIVITY 审中-公开
标题翻译：作为蛋白激酶活性调节剂的几何限制性2-吲哚啉酮衍生物
公开(公告)号：WO00012084A1
公开(公告)日：2000-03-09
申请号：PCT/US1999/019948
申请日：1999-08-30
IPC分类号： A61K31/404 , A61K31/34 , A61K31/35 , A61K31/36 , A61K31/38 , A61K31/385 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/405 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/535 , A61K31/54 , A61P3/10 , A61P7/00 , A61P9/08 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D209/12 , C07D209/34 , C07D231/54 , C07D235/02 , C07D237/26 , C07D239/70 , C07D241/36 , C07D249/16 , C07D251/16 , C07D251/72 , C07D253/065 , C07D253/08 , C07D257/04 , C07D257/08 , C07D257/10 , C07D261/08 , C07D261/20 , C07D263/32 , C07D263/52 , C07D265/12 , C07D265/16 , C07D265/34 , C07D265/36 , C07D271/04 , C07D271/06 , C07D271/08 , C07D271/10 , C07D271/12 , C07D273/04 , C07D275/02 , C07D275/04 , C07D279/06 , C07D279/08 , C07D279/12 , C07D279/14 , C07D279/16 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/14 , C07D285/18 , C07D285/20 , C07D285/22 , C07D285/34 , C07D291/02 , C07D291/08 , C07D307/36 , C07D307/38 , C07D307/40 , C07D307/52 , C07D307/77 , C07D311/02 , C07D311/94 , C07D317/04 , C07D317/06 , C07D317/14 , C07D317/44 , C07D317/46 , C07D319/06 , C07D319/08 , C07D319/12 , C07D319/14 , C07D319/16 , C07D323/02 , C07D323/04 , C07D327/04 , C07D327/06 , C07D327/10 , C07D333/06 , C07D333/50 , C07D401/02 , C07D401/10 , C07D403/04 , C07D471/02 , C07D487/02
CPC分类号： C07D209/34
摘要： The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及调节蛋白激酶活性的新颖的几何限制性2-二氢吲哚酮及其生理上可接受的盐，因此预期可用于预防和治疗与蛋白激酶相关的细胞病症例如癌症。

4. 发明申请

WO01053267A1 COMPOUNDS EXHIBITING THROMBOPOIETIN RECEPTOR AGONISM 审中-公开
标题翻译：化合物展示血栓素受体激动剂
公开(公告)号：WO01053267A1
公开(公告)日：2001-07-26
申请号：PCT/JP2001/000411
申请日：2001-01-23
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61P7/02 , A61P43/00 , C07D231/40 , C07D233/88 , C07D249/14 , C07D277/46 , C07D277/82 , C07D285/16 , C07D285/18 , C07D333/38 , C07D417/04 , C07D417/14 , A61K31/381 , A61K31/415 , A61K31/4168 , A61K31/4196 , A61K31/433 , C07D213/73 , C07D231/52 , C07D239/14 , C07D277/60 , C07D285/08 , C07D285/12 , C07D417/12
CPC分类号： C07D285/16 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/5377 , C07D231/40 , C07D249/14 , C07D277/46 , C07D277/82 , C07D285/18 , C07D333/38 , C07D417/04 , C07D417/14
摘要： Pharmaceutical compositions exhibiting thrombopoietin receptor agonism, which contain as the active ingredient compounds of the general formula (I): X -Y -Z -W prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them wherein X is optionally substituted aryl, optionally substituted heteroaryl, or the like; Y is -NR CO-(CH2)0-2- (wherein R is hydrogen or the like) or the like; Z is optionally substituted phenylene or the like; and W is a group of the general formula (II): (II) (wherein R , R , R and R are each independently hydrogen, optionally substituted lower alkyl, or the like; and the broken line represents the presence or absence of a bond), or the like.
摘要翻译：含有作为活性成分的通式（I）化合物：其中X 1 -Y 1 -Z 1 -W 1前药的药物组合物含有血小板生成素受体激动作用，其药学上可接受的盐其中X 1为任选取代的芳基，任选取代的杂芳基等; Y 1是-NR A CO - （CH 2）0-2-（其中R AA是氢等）等; Z 1是任选取代的亚苯基等; 和W 1是通式（II）的基团：（II）（其中R 1，R 2，R 3和R 4各自独立地为氢，任选取代的低级烷基，等等;虚线表示存在或不存在键）等。

5. 发明申请

WO01039762A2 METHODS OF TREATING TUMORS 审中-公开
标题翻译：治疗肿瘤的方法
公开(公告)号：WO01039762A2
公开(公告)日：2001-06-07
申请号：PCT/US2000/033103
申请日：2000-12-06
IPC分类号： C07D233/74 , A61K9/06 , A61K9/10 , A61K9/70 , A61K9/72 , A61K31/16 , A61K31/17 , A61K31/18 , A61K31/4166 , A61K31/505 , A61K31/522 , A61K31/54 , A61K31/549 , A61K45/00 , A61K45/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07D285/08 , C07D285/18 , A61K31/00
CPC分类号： A61K45/06 , A61K31/505 , A61K31/54 , A61K31/541 , A61K31/549 , Y10S514/885 , Y10S514/908 , A61K31/00 , A61K31/16 , A61K2300/00 , A61K31/17 , A61K31/18 , A61K31/4166 , A61K31/522
摘要： The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.
摘要翻译：本发明提供一种抑制哺乳动物肿瘤生长的方法，方法是给予含有taurolidine，taurultam或其生物活性衍生物的哺乳动物组合物。施用组合物以足以通过凋亡诱导细胞死亡的剂量直接接触肿瘤细胞。

6. 发明申请

WO00035885A1 CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS 审中-公开
标题翻译：循环盐酸衍生物作为TNF-ALPHA抑制剂
公开(公告)号：WO00035885A1
公开(公告)日：2000-06-22
申请号：PCT/EP1999/009423
申请日：1999-12-02
IPC分类号： A61K31/4166 , A61K31/4184 , A61K31/433 , A61K31/438 , A61K31/4439 , A61K31/496 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/549 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07D233/34 , C07D233/38 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/96 , C07D235/02 , C07D239/22 , C07D239/54 , C07D239/96 , C07D241/08 , C07D249/12 , C07D251/34 , C07D253/06 , C07D285/10 , C07D285/18 , C07D401/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/04 , A61K31/395
CPC分类号： C07D235/02 , C07D233/34 , C07D233/80 , C07D233/84 , C07D233/96 , C07D239/54 , C07D239/96 , C07D241/08 , C07D249/12 , C07D251/34 , C07D285/10 , C07D285/18 , C07D401/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Hydrazine derivatives of formula (I) wherein W represents O, S, CO, NR , (CR R )m, or CR ; X represents CO, NR , (CH2)n, CR or CHR ; Y represents CO, NR , (CH2)p, or CHR ; Z represents CO, CS, SO2, or CH2; m stands for 0 or 1; n and p each individually stand for 0, 1, or 2; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula V-aryl, V-heterocyclyl or -(CH2)q-CH=CR R ; R , R , R , R and R each independently represent hydrogen, optionally substituted lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; or R and R together with the carbon atom to which they are attached form a 3- to 8-membered ring; or R and R or R and R together with the nitrogen atoms to which they are attached form a 3- to 8-membered ring; or R and R together with the sp carbon atoms to which they are attached form a fused lower cycloalkenyl, aryl or heteroaryl ring; or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or either R or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or R and R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; V represents a spacer group; R and R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; and q stands for 1 or 2; with the provisos that (i) at least one of W, X and Y represents one of the heteroatoms previously indicated for these substituents or CO, (ii) Z represents CO or SO2 or CS when W represents O; (iii) W, X, Y and Z are not all CO and (iv) W, X and Y are not all NR , NR and NR , respectively; and pharmaceutically acceptable salts thereof inhibit the release of tumour necrosis factor alpha (TNF- alpha ) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.
摘要翻译：式（I）的肼衍生物，其中W表示O，S，CO，NR 5，（CR 3 R 4）m或CR 11; X表示CO，NR 6，（CH 2）n，CR 12或CHR 13; Y表示CO，NR 7，（CH 2）p或CHR 14; Z表示CO，CS，SO2或CH2; m代表0或1; n和p各自分别代表0,1或2; R 1表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基或芳基 - 低级烷基; R 2表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基或式V-芳基，V-杂环基或 - （CH 2）q -CH = CR 8 R 9的基团。 R 3，R 4，R 5，R 6和R 7各自独立地表示氢，任选取代的低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基，芳基 - 低级烷基，杂环基或杂环基 - 低级烷基; 或R 3和R 4与它们所连接的碳原子一起形成3至8元环; 或R 5和R 6或R 5和R 7与它们所连接的氮原子一起形成3-至8-元环; 或R 11和R 12与它们所连接的sp 2碳原子一起形成稠合的低级环烯基，芳基或杂芳基环; 或R 5与R 13或R 14一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 6或R 7与R 3或R 4一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 3和R 4一起代表其中CH2基团任选被杂原子取代的低级亚烷基; V表示间隔基; R 8和R 9一起代表其中CH2基团任选被杂原子取代的低级亚烷基; q代表1或2; 条件是（i）W，X和Y中的至少一个表示先前对这些取代基或CO表示的杂原子之一，（ii）当W表示O时，Z表示CO或SO 2或CS; （iii）W，X，Y和Z不都是CO，（iv）W，X和Y不分别是NR 5，NR 6和NR 7; 和其药学上可接受的盐抑制肿瘤坏死因子α（TNF-α）从细胞的释放。它们可以用作药物，特别是用于治疗炎性和自身免疫疾病，骨关节炎，呼吸系统疾病，肿瘤，恶病质，心血管疾病，发热，出血和败血症。

7. 发明申请

WO9931074A3 ((CYCLO)ALKYL SUBSTITUTED)-.GAMMA.-AMINOBUTYRIC ACID DERIVATIVES (=GABA ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开
标题翻译：（（CYCLO）烷基取代） - 。氨基 - 氨基酸衍生物（= GABA类似物），其制备及其在治疗神经病症中的用途
公开(公告)号：WO9931074A3
公开(公告)日：1999-11-04
申请号：PCT/US9823917
申请日：1998-11-10
申请人： WARNER LAMBERT CO , BELLIOTTI THOMAS RICHARD , BRYANS JUSTIN STEPHEN , CAPIRIS THOMAS , HORWELL DAVID CHRISTOPHER , KNEEN CLARE OCTAVIA , WUSTROW DAVID JUERGEN
发明人： BELLIOTTI THOMAS RICHARD , BRYANS JUSTIN STEPHEN , CAPIRIS THOMAS , HORWELL DAVID CHRISTOPHER , KNEEN CLARE OCTAVIA , WUSTROW DAVID JUERGEN
IPC分类号： C07D285/08 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K31/66 , A61P1/00 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P43/00 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/32 , C07C311/33 , C07D211/26 , C07D257/04 , C07D271/06 , C07D271/07 , C07D285/18 , C07D291/04 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/38 , C07F9/59 , C07F9/655 , C07F9/6553
CPC分类号： C07C311/32 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/592 , C07F9/6552 , C07F9/655363
摘要： Novel amines of formulas (1A) and (1B) or a pharmaceutically acceptable salt thereof wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A is hydrogen or methyl; and B is (a), straight or branched alkyl of from 1 to 11 carbons, or -(CH2)1-4-Y-(CH2)0-4-phenyl wherein Y is -O-, -S-, -NR'3 wherein R'3 is alkyl of from 1 to 6 carbons, cycloalkyl of from 3 to 8 carbons, benzyl or phenyl wherein benzyl or phenyl can be unsubstituted or substituted with from 1 to 3 substituents each independently selected from alkyl, alkoxy, halogen, hydroxy, carboxy, carboalkoxy, trifluoromethyl, and nitro are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译：式（1A）和（1B）的新型胺或其药学上可接受的盐，其中：n为0-2的整数; R是磺酰胺，酰胺，膦酸，杂环，磺酸或异羟肟酸; A是氢或甲基; 和B是（a），1至11个碳的直链或支链烷基或 - （CH 2）1-4 -Y-（CH 2）0-4-苯基，其中Y是-O - ， - S - ， - NR '3其中R'3是1至6个碳的烷基，3至8个碳的环烷基，苄基或苯基，其中苄基或苯基可以是未取代的或被1至3个独立地选自烷基，烷氧基，卤素，羟基，羧基，烷氧羰基，三氟甲基和硝基，并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学疾病，炎性疾病和胃肠道疾病，尤其是IBS。还公开了用于制备的方法和可用于制备的中间体。

8. 发明申请

WO99031074A2 NOVEL AMINES AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：作为药物代理商的新品
公开(公告)号：WO99031074A2
公开(公告)日：1999-06-24
申请号：PCT/US1998/023917
申请日：1998-11-10
IPC分类号： C07D285/08 , A61K20060101 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/454 , A61K31/66 , A61K31/665 , A61P1/00 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P43/00 , C07C20060101 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/32 , C07C311/33 , C07D20060101 , C07D211/26 , C07D211/28 , C07D211/54 , C07D257/04 , C07D271/06 , C07D271/07 , C07D285/18 , C07D291/04 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/38 , C07F9/59 , C07F9/655 , C07F9/6553 , C07D257/00
CPC分类号： C07C311/32 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/592 , C07F9/6552 , C07F9/655363
摘要： Novel amines of formulas (1A) and (1B) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译：公开了式（1A）和（1B）的新型胺，可用作治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性障碍，抑郁，焦虑，恐慌，疼痛，神经病理学障碍，炎性疾病和胃肠道疾病，尤其是IBS。还公开了用于制备的方法和可用于制备的中间体。

9. 发明申请

WO2014093190A1 BACE INHIBITORS OF IMINOTHIADIAZINE DIOXIDES 审中-公开
标题翻译：三氮嗪二氧化物的抑制剂
公开(公告)号：WO2014093190A1
公开(公告)日：2014-06-19
申请号：PCT/US2013/073781
申请日：2013-12-09
申请人： MERCK SHARP & DOHME CORP. , CUMMING, Jared, N. , SCOTT, Jack, D. , BIFTU, Tesfaye
发明人： CUMMING, Jared, N. , SCOTT, Jack, D. , BIFTU, Tesfaye
IPC分类号： A61K31/549 , A61P25/28 , C07D285/18
CPC分类号： C07D417/12 , C07D285/18
摘要： In its many embodiments, the present invention provides certain C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些C2-环取代的亚氨基二嗪化合物或其互变异构体，以及所述化合物和所述互变异构体的药学上可接受的盐。本发明的新化合物作为BACE抑制剂和/或用于治疗和预防与之相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

10. 发明申请

WO2007057092A1 SUBSTITUIERTE 5-PHENYL-3,6-DIHYDRO-2-OXO-6H-[1,3,4]THIADIAZINE 审中-公开
标题翻译：取代的5-苯基-3,6-二氢-2-氧代-6H- [1,3,4]噻二嗪
公开(公告)号：WO2007057092A1
公开(公告)日：2007-05-24
申请号：PCT/EP2006/010285
申请日：2006-10-25
申请人： MERCK PATENT GMBH , SCHADT, Oliver , DORSCH, Dieter , SCHULTZ, Melanie , BLAUKAT, Andree
发明人： SCHADT, Oliver , DORSCH, Dieter , SCHULTZ, Melanie , BLAUKAT, Andree
IPC分类号： C07D285/08 , C07D285/18 , C07D417/12 , A61K31/433 , A61K31/541 , A61K31/54 , A61P35/00
CPC分类号： C07D417/12 , C07D285/08 , C07D285/18
摘要： Verbindungen der Formel (I), worin R 1 , R 2 , m, Q und B die in Anspruch 1 angegebenen Bedeutungen haben, sind Inhibitoren der Tyrosinkinasen, insbesondere der Met-Kinase und können u.a. zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：式（I），其中R ^{1 ，R ^{2 ，M，Q和B具有权利要求1中给出的含义，是酪氨酸激酶的抑制剂，特别是Met的化合物激酶和CAN，除其他事项外用于肿瘤的治疗。}}

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