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41. 发明申请

WO2006066436A1 CYCLOPROPANATION PROCESS 审中-公开
标题翻译：循环过程
公开(公告)号：WO2006066436A1
公开(公告)日：2006-06-29
申请号：PCT/CH2005/000763
申请日：2005-12-20
申请人： GIVAUDAN SA , SCHRÖDER, Fridtjof
发明人： SCHRÖDER, Fridtjof
IPC分类号： C07C29/32 , C07C41/30 , C07C253/30 , C07D313/00 , C07C43/115 , C07C43/162 , C07C2/42 , C07C67/347
CPC分类号： C07C29/36 , C07C2/861 , C07C29/32 , C07C41/16 , C07C41/30 , C07C67/347 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2602/18 , C07D313/00 , C07C13/32 , C07C69/608 , C07C255/31 , C07C43/23 , C07C43/115 , C07C43/162 , C07C31/137 , C07C33/05 , C07C33/12 , C07C31/1333
摘要： A process for the cyclopropanation of a substituted alkene, comprising the reaction of the alkene with a carbenoide, generated from dibromomethane and a tri-(C2 - C8)-alkyl aluminium compound, in the presence of a catalytic amount of a metal compound selected from the group consisting of Lewis acids, metallocenes and metal carbonyl complexes. The process advantageously uses transition metal compounds as catalysts and the dibromomethane can be recovered. The process is especially useful for the preparation of ingredients for the flavour and fragrance industry.
摘要翻译：在催化量的金属化合物的存在下，由二溴甲烷和三（C 2 -C 8） - 烷基铝化合物产生的包含烯烃与碳氰酸酯的反应的取代烯烃的环丙烷化方法，由路易斯酸，金属茂和金属羰基络合物组成的组。该方法有利地使用过渡金属化合物作为催化剂，并且可以回收二溴甲烷。该方法对于制备风味和香料工业的成分特别有用。

42. 发明申请

WO2003057661A1 PRODRUGS OF EXCITATORY AMINO ACIDS 审中-公开
标题翻译：激素氨基酸的产物
公开(公告)号：WO2003057661A1
公开(公告)日：2003-07-17
申请号：PCT/US2002/036145
申请日：2002-12-05
申请人： ELI LILLY AND COMPANY , BUENO MELENDO, Ana, Belen , DE DIOS, Alfonso , DOMINGUEZ-FERNANDEZ, Carmen , FERRITTO CRESPO, Rafael , HERIN, Marc , MARTIN, Jose, Alfredo , MARTINEZ-GRAU, Maria, Angeles , MASSEY, Steven, Marc , MONN, James, Allen , PEDREGAL-TERCERO, Concepcion , VALLI, Matthew, John
发明人： BUENO MELENDO, Ana, Belen , DE DIOS, Alfonso , DOMINGUEZ-FERNANDEZ, Carmen , FERRITTO CRESPO, Rafael , HERIN, Marc , MARTIN, Jose, Alfredo , MARTINEZ-GRAU, Maria, Angeles , MASSEY, Steven, Marc , MONN, James, Allen , PEDREGAL-TERCERO, Concepcion , VALLI, Matthew, John
IPC分类号： C07C229/50
CPC分类号： C07C229/50 , C07C2602/08 , C07C2602/18 , C07D263/52 , C07D333/16 , C07D333/56
摘要： This invention relates to synthetic excitatory amino acid prodrugs of formula (I) wherein the residue R 11 , R 12 and R 13 are aas defined in claim 1. The invention further relates to processes for the preparation of the compounds of formula (I), and to pharmaceutical compositions for the treatment of neurological and psychiatric disorders comprising said compounds.
摘要翻译：本发明涉及式（I）的合成兴奋性氨基酸前药，其中残基R 11，R 12和R 13是权利要求1中定义的。本发明还涉及制备化合物的方法式（I）的化合物，以及用于治疗包含所述化合物的神经和精神疾病的药物组合物。

43. 发明申请

WO2003047568A1 N-ARYL-N'-ARYLCYCLOALKYL-UREA DERIVATIVES AS MCH ANTAGONISTS FOR THE TREATMENT OF OBESITY 审中-公开
标题翻译： N-ARYL-N'-ARYLCYCLOALKYL-UREA DERIVATIVES AS MCH ANTAGONISTS FOR OBETING OF OBESITY
公开(公告)号：WO2003047568A1
公开(公告)日：2003-06-12
申请号：PCT/US2002/038408
申请日：2002-12-03
申请人： SCHERING CORPORATION
发明人： CLADER, John, W. , PALANI, Anandan , XU, Ruo , MC BRIAR, Mark, D. , SU, Jing , TANG, Haiqun
IPC分类号： A61K31/40
CPC分类号： C07D207/08 , C07C275/30 , C07C2601/14 , C07C2602/18 , C07C2602/20 , C07D205/04 , C07D207/06 , C07D207/10 , C07D207/12 , C07D207/14 , C07D209/52 , C07D211/26 , C07D211/34 , C07D211/96 , C07D213/75 , C07D213/89 , C07D233/24 , C07D295/13 , C07D333/36 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/06
摘要： The present invention discloses compounds of the formula I which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明公开了式I化合物，它们是黑色素浓缩激素（MCH）的新型拮抗剂，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

44. 发明申请

WO02000605A1 NOVEL DICARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：新型二羧酸衍生物
公开(公告)号：WO02000605A1
公开(公告)日：2002-01-03
申请号：PCT/JP2001/005550
申请日：2001-06-28
IPC分类号： A61P9/10 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P43/00 , C07C229/50 , A61K31/198 , A61K31/223
CPC分类号： C07C229/50 , C07C2602/18
摘要： 2-Amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the following general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same. These compounds are useful as drugs, in particular, group 2 matabotropic glutamate receptor agonists having therapeutic and preventive effects on, for example, psychiatric diseases such as schizophrenia, anxiety and diseases associating the same, depression and bipolar disorder and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorder associating muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal disorder and head disorder.
摘要翻译：由以下通式（I）表示的2-氨基-6-氟双环[3.1.0]己烷-2,6-二羧酸衍生物，其药学上可接受的盐或其水合物。这些化合物可用作药物，特别是对具有治疗和预防作用的组2异构谷氨酸受体激动剂，例如精神疾病如精神分裂症，焦虑症和与之相关的疾病，抑郁症和双相情感障碍以及神经系统疾病如药物成瘾，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森病，运动障碍，肌肉僵硬，脑缺血，脑功能不全，脊柱障碍和头部疾病。

45. 发明申请

WO00037410A1 INTERMEDIATES AND PROCESS FOR PRODUCING FLUORINE-CONTAINING AMINO ACID COMPOUND BY USING THE SAME 审中-公开
标题翻译：含有含氟氨基酸化合物的中间体及其制备方法
公开(公告)号：WO00037410A1
公开(公告)日：2000-06-29
申请号：PCT/JP1999/007096
申请日：1999-12-17
IPC分类号： C07C62/38 , C07C51/363 , C07C67/307 , C07C69/757 , C07C227/18 , C07C227/24 , C07C227/26 , C07C229/50 , C07C231/12 , C07C235/82 , C07C255/47 , C07D235/02 , C07D303/42 , C07D303/46
CPC分类号： C07D235/02 , C07B2200/07 , C07C51/363 , C07C62/38 , C07C69/757 , C07C227/18 , C07C229/50 , C07C235/82 , C07C255/47 , C07C2602/18 , C07C2602/40 , C07D303/42 , C07D303/46
摘要： (1S,5R,6S)- or (1SR,5RS,6SR)-3-fluoro-2-oxobicylo[3.1.0]-hex-3-ene-6-carboxylic acid derivatives represented by general formula (1); a process for producing the same; and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptor which has therapeutic and preventive effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the above compound (1) and then further converting the same into hydantoin or amino cyanide followed by hydrolysis. In formula (1), R represents OR or NR R (wherein R and R are the same or different and each represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, (C3-6 cycloalkyl)(C1-6 alkyl), aryl, aryl(C1-6 alkyl), (C1-6 alkoxy)(C1-6 alkyl), C1-6 hydroxyalkyl, (C1-6 alkylthio)(C1-6 alkyl) or C1-6 mercaptoalkyl).
摘要翻译：（1）表示的（1S，5R，6S） - 或（1SR，5RS，6SR）-3-氟-2-氧代双[[3.1.0] - 己-3-烯-6-羧酸衍生物）其制造方法; 以及有效地制备作用于第2组代谢型谷氨酸受体的含氟氨基酸化合物的方法，其具有对精神病或神经疾病的治疗和预防作用，其特征在于氢化上述化合物（1），然后进一步将其转化为乙内酰脲或氨基氰化物接着水解。在式（1）中，R表示OR 1或NR 1 R 2（其中R 1和R 2相同或不同，各自表示氢，C 1-6烷基，C 3-6 环烷基，（C 3-6环烷基）（C 1-6烷基），芳基，芳基（C 1-6烷基），（C 1-6烷氧基）（C 1-6烷基），C 1-6羟烷基，（C 1-6烷硫基） C 1-6烷基）或C 1-6巯基烷基）。

46. 发明申请

WO1997001526A1 PREPARATION OF BICYCLOHEXANE DERIVATIVE 审中-公开
标题翻译：双酚衍生物的制备
公开(公告)号：WO1997001526A1
公开(公告)日：1997-01-16
申请号：PCT/US1996010847
申请日：1996-06-25
申请人： ELI LILLY AND COMPANY , ROBEY, Roger, L.
发明人： ELI LILLY AND COMPANY
IPC分类号： C07C61/12
CPC分类号： C07D235/02 , C07C62/24 , C07C227/24 , C07C229/50 , C07C2602/18
摘要： A process for the preparation of (+)-2-amino-bicyclo[3.1.0]-hexane-2-6-dicarboxylic acid, or a pharmaceutically acceptable salt thereof, which comprises hydrolysing (-)-2-spiro-5'-hydantoinbicyclo[3.1.0]hexane-6-carboxylic acid or a salt thereof, and optionally forming a pharmaceutically acceptable salt. Also disclosed are novel intermediates useful in the process.
摘要翻译：（+） - 2-氨基 - 双环[3.1.0] - 己烷-2,6-二羧酸或其药学上可接受的盐的制备方法，其包括水解（ - ） - 2-螺-5' - 乙内酰脲二环[3.1.0]己烷-6-羧酸或其盐，并任选地形成药学上可接受的盐。还公开了在该方法中有用的新型中间体。

47. 发明申请

WO2017024126A1 CYCLOPROPANATION OF SUBSTITUTED ALKENES 审中-公开
标题翻译：取代的碱的循环
公开(公告)号：WO2017024126A1
公开(公告)日：2017-02-09
申请号：PCT/US2016/045540
申请日：2016-08-04
申请人： INTERNATIONAL FLAVORS & FRAGRANCES INC.
发明人： GARA, Mohamad , BECKER, Yigal
IPC分类号： C07C2/86 , A23L27/20 , C07C13/28 , C07C13/04 , C11B9/00
CPC分类号： C07C2/861 , A23L27/203 , B01J23/06 , B01J23/72 , B01J35/0006 , B01J35/026 , C07C29/32 , C07C29/44 , C07C45/61 , C07C45/69 , C07C2523/06 , C07C2523/72 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2602/18 , C07C2602/20 , C07C2602/32 , C07C2602/40 , C07C2602/50 , C07C2603/08 , C07C2603/62 , C07C2603/96 , C11B9/00 , C11B9/0026 , C11B9/003 , C11B9/0042 , C11B9/0049 , C11B9/0057 , C07C13/605 , C07C13/38 , C07C13/40 , C07C49/427 , C07C31/1333 , C07C33/12 , C07C31/13
摘要： Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.
摘要翻译：公开了一种环丙烷化方法，其包括使具有至少一个碳 - 碳双键的烯烃化合物与至少一种二卤代烷反应的步骤。反应在（i）颗粒金属Zn存在下，（ii）催化有效量的颗粒状金属Cu或其盐，（iii）至少一种卤代烷基硅烷和（iv）至少一种溶剂的存在下进行。

48. 发明申请

WO2016094178A1 METHODS FOR PRODUCING ABIENOL 审中-公开
标题翻译：生产ABIENOL的方法
公开(公告)号：WO2016094178A1
公开(公告)日：2016-06-16
申请号：PCT/US2015/063656
申请日：2015-12-03
申请人： DSM IP ASSETS B.V. , ROYER, John
发明人： ROYER, John
IPC分类号： C12N9/88
CPC分类号： C12N9/88 , C07C13/38 , C07C2602/18 , C12N15/52 , C12N15/70 , C12N15/81 , C12Y205/01029 , C12Y402/01133 , C12Y402/0314
摘要： The present disclosure relates to a novel method, expression vectors, and host cells for producing abienol by converting geranylgeranyl diphosphate (GGPP) to abienol in the presence of a combination of a class II diterpene synthase and a bifunctional class I/II abienol synthase.
摘要翻译：本公开内容涉及在II类二萜合成酶和双功能I / II型二烯醇合酶的组合存在下将香叶基香叶基二磷酸酯（GGPP）转化为二烯醇的方法，表达载体和用于产生二烯酚的宿主细胞。

49. 发明申请

WO2015181182A1 CHIRAL DIAMINE COMPOUNDS FOR THE PREPARATION OF CHIRAL ALCOHOL AND CHIRAL AMINE 审中-公开
标题翻译：用于制备精制酒精和乳酸胺的化学键合物
公开(公告)号：WO2015181182A1
公开(公告)日：2015-12-03
申请号：PCT/EP2015/061610
申请日：2015-05-26
申请人： UNIVERSITY COLLEGE DUBLIN
发明人： GILHEANY, Declan , BIESZCZAD, Bartosz
IPC分类号： C07D311/76 , C07C29/40 , C07D235/12 , C07C211/36 , C07C211/53 , C07C215/50 , C07C215/64
CPC分类号： C07C45/69 , C07B2200/07 , C07C29/40 , C07C41/30 , C07C211/36 , C07C211/53 , C07C215/50 , C07C215/64 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2602/18 , C07D235/12 , C07D311/76 , C07C33/20 , C07C31/125 , C07C33/46 , C07C35/32 , C07C43/23 , C07C49/213 , C07C33/30 , C07C33/24 , C07C33/18 , C07C31/1355 , C07C35/23 , C07C35/36
摘要： A process for the stereoselective preparation of a chiral alcohol or a chiral amine, the process comprising reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an inline, with a second reactant comprising a Grignard reagent, in the presence of a chiral trans -diamim of formula (1) as defined herein. Also provided is the use of the chiral trans -diamine of formula (1) in a Grignard reaction and the chiral trans -diamines per se .
摘要翻译：用于手性醇或手性胺的立体选择性制备的方法，该方法包括将选自酮，醛和在线的第一前手性反应物与包含格利雅试剂的第二反应物反应，式（1）的手性反式二胺的存在如本文所定义。还提供了在格利雅反应中使用式（1）的手性反式二胺和手性反式二胺本身。

50. 发明申请

WO2013177224A1 N-SUBSTITUTED BENZAMIDES AND THEIR USE IN THE TREATMENT OF PAIN 审中-公开
标题翻译： N-取代苯甲酸及其在治疗疼痛中的应用
公开(公告)号：WO2013177224A1
公开(公告)日：2013-11-28
申请号：PCT/US2013/042111
申请日：2013-05-21
申请人： GENENTECH, INC. , XENON PHARMACEUTICALS INC. , ANDREZ, Jean-Christophe , CHOWDHURY, Sultan , DECKER, Shannon , DEHNHARDT, Christoph, Martin , FOCKEN, Thilo , GRIMWOOD, Michael, Edward , HEMEON, Ivan, William , JIA, Qi , LI, Jun , ORTWINE, Daniel, F. , SAFINA, Brian , SHENG, Tao , SUN, Shaoyi , SUTHERLIN, Daniel, P. , WILSON, Michael, Scott , ZENOVA, Alla, Yurevna
发明人： ANDREZ, Jean-Christophe , CHOWDHURY, Sultan , DECKER, Shannon , DEHNHARDT, Christoph, Martin , FOCKEN, Thilo , GRIMWOOD, Michael, Edward , HEMEON, Ivan, William , JIA, Qi , LI, Jun , ORTWINE, Daniel, F. , SAFINA, Brian , SHENG, Tao , SUN, Shaoyi , SUTHERLIN, Daniel, P. , WILSON, Michael, Scott , ZENOVA, Alla, Yurevna
IPC分类号： C07C311/51 , C07D207/08 , C07D213/82 , C07D307/12 , A61K31/44 , A61K31/445 , A61K31/18 , A61P25/04
CPC分类号： C07D491/107 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/44 , A61K31/5375 , C07B2200/05 , C07C307/06 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/18 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50 , C07C2603/66 , C07C2603/68 , C07C2603/74 , C07D205/04 , C07D207/46 , C07D207/48 , C07D209/52 , C07D211/22 , C07D211/96 , C07D213/64 , C07D213/82 , C07D233/84 , C07D257/04 , C07D265/30 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/18 , C07D309/08 , C07D311/58 , C07D311/70 , C07D311/72 , C07D403/12 , C07D405/12 , C07D413/12 , C07D451/02 , C07D471/08
摘要： The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables R A , subscript n, ring A, X 2 , L, subscript m, X 1 , B, R 1 , R 2 , R 3 , R 4 , R 5 and R N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
摘要翻译：本发明提供具有通式（I）及其药学上可接受的盐的新化合物，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和 RN具有本文所述的含义，含有这些化合物的组合物和使用这些化合物和组合物的方法。

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