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1.SUBSTITUTED (ARYLALKOXYBENZYL)AMINOPROPANAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS ANTI-EPILEPTIC, NEUROPROTECTIVE AND ANTIDEPRESSANT AGENTS 审中-公开
Title translation: 取代(芳基烷氧基)氨基丙酰胺衍生物,其制备和用作抗真菌,神经保护和抗原剂公开(公告)号:WO1994022808A1
公开(公告)日:1994-10-13
申请号:PCT/EP1994000802
申请日:1994-03-15
Applicant: FARMITALIA CARLO ERBA Srl
Inventor: FARMITALIA CARLO ERBA Srl , VARASI, Mario , DOSTERT, Philippe , PEVARELLO, Paolo , BONSIGNORI, Alberto
IPC: C07C237/06
CPC classification number: C07C237/00
Abstract: The invention provides new compounds of formula (I) wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C1-C4 alkoxy; R2 is hydrogen or C1-C4 alkyl optionally substituted by hydroxy; each of R3 and R4 independently is hydrogen or C1-C4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA), wherein R5 is hydrogen, halogen, trifluoromethyl or C1-C4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.
Abstract translation: 本发明提供新的式(I)化合物,其中,条件是n为0或1至3的整数; R和R 1可以相同或不同,为氢,卤素,三氟甲基或C 1 -C 4烷氧基; R2是氢或任选被羟基取代的C 1 -C 4烷基; R 3和R 4各自独立地是氢或C 1 -C 4烷基; 或其药学上可接受的盐; 和式(IA)的化合物,其中R5是氢,卤素,三氟甲基或C1-C4烷氧基,或其药学上可接受的盐,它们在中枢神经系统(CNS)上有活性,可用作抗癫痫药, 抗帕金森,神经保护,抗抑郁药,抗痉挛和催眠药。
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2.INHIBITORS OF MCI-1 AS DRUGS TO OVERCOME RESISTANCE TO BRAF INHIBITORS AND MEK INHIBITORS 审中-公开
Title translation: MCI-1作为药物的抑制剂对BRAF抑制剂和MEK抑制剂的耐药性公开(公告)号:WO2016200726A1
公开(公告)日:2016-12-15
申请号:PCT/US2016/036002
申请日:2016-06-06
Applicant: TEXAS TECH UNIVERSITY SYSTEM
Inventor: SRIVASTAVA, Sanjay, K. , FOFARIA, Neel, M.
IPC: C07D211/16 , A61K31/445 , A61K38/16 , A61K39/395 , A61P35/00
CPC classification number: A61K31/4184 , A61K31/165 , A61K31/167 , A61K31/341 , A61K31/40 , A61K31/4025 , A61K31/405 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61K31/423 , A61K31/4245 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4525 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K45/06 , A61P35/00 , C07C233/87 , C07C237/00 , C07C237/52 , C07D207/337 , C07D209/08 , C07D209/42 , C07D211/34 , C07D215/48 , C07D217/06 , C07D233/60 , C07D235/10 , C07D235/12 , C07D235/16 , C07D235/28 , C07D249/12 , C07D263/34 , C07D265/36 , C07D279/02 , C07D295/108 , C07D307/54 , C07D317/60 , C07D401/06 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/14 , C07D413/06 , C07D417/12 , C07D487/04 , G01N33/5011 , G01N2333/4703 , A61K2300/00
Abstract: The present invention includes compositions and methods for inhibiting MCL-1, including novel inhibitors of MCL-1, and compositions and methods for treating a subject with cancer that is refractory to one or more MAPK pathway protein inhibitors.
Abstract translation: 本发明包括用于抑制MCL-1的组合物和方法,包括MCL-1的新型抑制剂,以及用于治疗患有对一种或多种MAPK通路蛋白抑制剂难治的癌症的受试者的组合物和方法。
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3.O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES 审中-公开
Title translation: O-环丙基胆碱二羧酸和它们作为杀真菌剂使用公开(公告)号:WO2011151383A1
公开(公告)日:2011-12-08
申请号:PCT/EP2011/059055
申请日:2011-06-01
Applicant: BAYER CROPSCIENCE AG , GREUL, Jörg Nico , BENTING, Jürgen , DAHMEN, Peter , WACHENDORFF-NEUMANN, Ulrike
Inventor: GREUL, Jörg Nico , BENTING, Jürgen , DAHMEN, Peter , WACHENDORFF-NEUMANN, Ulrike
IPC: C07D213/82 , C07D231/16 , C07D277/56 , A01N43/40 , A01N43/50 , A01N43/56
CPC classification number: C07D231/18 , A01N37/18 , A01N37/44 , A01N43/40 , A01N43/50 , A01N43/56 , A01N43/78 , A01N43/80 , C07C211/35 , C07C233/65 , C07C237/00 , C07C2601/02 , C07C2601/14 , C07D211/04 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/16 , C07D277/02 , C07D277/56
Abstract: The present invention relates to O-cyclopropylcyclohexyl-carboxanilides derivatives of formula (I), their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
Abstract translation: 本发明涉及式(I)的O-环丙基环己基 - 甲酰苯胺衍生物,其制备方法,它们作为杀真菌剂的用途,特别是杀真菌剂组合物的形式,以及使用这些方法控制植物病原真菌,特别是植物的方法 化合物或组合物。
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公开(公告)号:WO1992021648A1
公开(公告)日:1992-12-10
申请号:PCT/US1992004687
申请日:1992-06-04
Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.
IPC: C07C233/00
CPC classification number: C07D207/337 , A61K31/165 , A61K31/195 , A61K31/34 , A61K31/38 , A61K31/40 , C07C229/30 , C07C233/47 , C07C237/00 , C07C237/22 , C07C239/18 , C07C239/20 , C07C243/22 , C07C259/06 , C07C271/22 , C07C271/54 , C07C275/16 , C07C275/28 , C07C281/02 , C07C309/18 , C07C311/55 , C07C311/58 , C07C317/50 , C07C323/60 , C07C327/42 , C07C335/16 , C07D207/34 , C07D207/404 , C07D209/20 , C07D209/42 , C07D213/56 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/16 , C07D249/08 , C07D257/04 , C07D271/06 , C07D295/15 , C07D303/46 , C07D307/16 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/85 , C07D333/24 , C07D333/38 , C07D333/60 , C07D333/70 , C07D405/12
Abstract: The present invention relates to compounds of formula (I).
Abstract translation: 本发明涉及式(I)化合物。
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公开(公告)号:WO2016082934A1
公开(公告)日:2016-06-02
申请号:PCT/EP2015/002382
申请日:2015-11-26
Applicant: HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH , GOTTFRIED WILHELM LEIBNIZ UNIVERSITÄT HANNOVER
Inventor: BAUMANN, Sascha , HERRMANN, Jennifer , MOHR, Kathrin , STEINMETZ, Heinrich , GERTH, Klaus , RAJU, Ritesh , MÜLLER, Rolf , HARTMANN, Rolf , HAMED, Mostafa , ELGAHER, Walid, A., M. , MORENO, Marla , GILLE, Franziska , WANG, Liang Liang , KIRSCHNING, Andreas , HÜTTEL, Stephan
IPC: C07C237/44 , C12P13/02 , A61K31/196 , A61P31/04
CPC classification number: C07C237/44 , A61K31/196 , C07C237/00 , C12P13/02 , C12R1/00 , C12R1/01
Abstract: The present invention provides cystobactamides of formula (I) and the use thereof the treatment or prophylaxis of bacterial infections.
Abstract translation: 本发明提供式(I)的胱氨酰胺酰胺及其用于治疗或预防细菌感染的用途。
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6.DERIVATIVES OF (R) 5-PENTYLAMINO-5-OXOPENTANOIC ACID WITH ANTICHOLECYSTOKININ ACTIVITY 审中-公开
Title translation: (R)5-戊基氨基-5-氧代戊酸与抗转氨酶活性的衍生物公开(公告)号:WO1988005774A1
公开(公告)日:1988-08-11
申请号:PCT/EP1988000061
申请日:1988-01-28
Applicant: ROTTA RESEARCH LABORATORIUM S.P.A.
Inventor: ROTTA RESEARCH LABORATORIUM S.P.A. , MAKOVEC, Francesco , CHISTE', Rolando , PERIS, Walter , ROVATI, Luigi
IPC: C07C103/50
CPC classification number: A61K31/195 , C07C231/02 , C07C233/12 , C07C233/83 , C07C237/00
Abstract: Optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with formula (I), in which R1 is selected from the groups 2-naphthyl, 3,4-dichlorobenzoyl and 3,4-dimethylbenzoyl and R2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.
Abstract translation: (R)5-戊基氨基-5-氧代戊酸及其药学上可接受的盐,对缩胆囊素具有拮抗作用并且具有式(I)的光学活性衍生物,其中R 1选自2-萘基,3,4- 二氯苯甲酰基和3,4-二甲基苯甲酰基,R 2是具有4个碳原子的戊基或烷氧基烷基,其中中心手性基团上的取代基(在式(I)中用星号标记))具有R(直角) 构象。
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