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81. 发明授权

US3057866A Process for the production of a salt of the laevulinic acid derivative of cyanacetic acid hydrazide 失效
标题翻译：制备氰乙酸酰肼的laevulinic acid衍生物的盐的方法
公开(公告)号：US3057866A
公开(公告)日：1962-10-09
申请号：US6500460
申请日：1960-10-26
申请人： BAYER AG
发明人： ALBERT OFFE HANS , MANFRED FEDERMANN
IPC分类号： C07D295/02
CPC分类号： C07D295/02

82. 发明公开

US20240158360A1 Synthesis of a Monoacylglycerol Lipase Inhibitor 审中-公开
公开(公告)号：US20240158360A1
公开(公告)日：2024-05-16
申请号：US18325798
申请日：2023-05-30
申请人： H. Lundbeck A/S
发明人： Cheryl A. GRICE , Kurt G. GRIMM , Todd K. JONES , Giuseppe GUERCIO
IPC分类号： C07D295/02 , C07D295/023
CPC分类号： C07D295/02 , C07D295/023 , C07B2200/13
摘要： Described herein is the manufacture of MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate including salts thereof.

83. 发明授权

US09707551B2 Reaction catalyst for cross-coupling and method for manufacturing aromatic compound 有权
公开(公告)号：US09707551B2
公开(公告)日：2017-07-18
申请号：US14762456
申请日：2014-01-23
申请人： HOKKO CHEMICAL INDUSTRY CO., LTD.
发明人： Nobumichi Kumamoto , Kenta Suzuki
IPC分类号： C07D209/82 , C07C209/10 , B01J31/24 , C07D295/02 , C07F9/50 , C07F9/54 , C07C1/32 , C07C41/30 , C07C253/30 , C07D295/033
CPC分类号： B01J31/24 , B01J2231/4283 , B01J2531/824 , C07C1/321 , C07C41/30 , C07C209/10 , C07C253/30 , C07C2531/24 , C07D209/82 , C07D295/02 , C07D295/033 , C07F9/5013 , C07F9/5428 , C07C211/54 , C07C211/56 , C07C15/14 , C07C43/205 , C07C211/55 , C07C255/50
摘要： The object of the present invention is to provide a new organic phosphorus ligand that can efficiently promote cross-coupling reaction to obtain the target substance at high yield, as well as a method of manufacturing such ligand whose steric characteristics and electronic characteristics can be fine-tuned and which can be used to cause cross-coupling reaction at high yield. As a means for achieving the aforementioned object, a phosphine compound expressed by General Formula (1) below is provided. (In the formula, R1 and R2 are each independently a secondary alkyl group, tertiary alkyl group, or cycloalkyl group, while R3 and R4 are each independently a hydrogen, aliphatic group, heteroaliphatic group, aromatic group, alicyclic group, or heterocyclic group. Note that R3 and R4 have no phosphorus atom and that R3 and R4 are not both hydrogen at the same time).

84. 发明申请

US20160031840A1 1,4-Disubstituted Piperidines, 1,4-Disubstituted Piperazines, 1,4-Disubstituted Diazepines, and 1,3-Disubstituted Pyrrolidine Compounds 审中-公开
标题翻译： 1,4-二取代哌啶，1,4-二取代哌嗪，1,4-二取代二氮杂和1,3-二取代吡咯烷化合物
公开(公告)号：US20160031840A1
公开(公告)日：2016-02-04
申请号：US14776306
申请日：2014-03-14
申请人： UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
发明人： Peter A. CROOKS , Linda P. DWOSKIN , John CULVER , Justin R. NICKELL , Guangrong ZHENG
IPC分类号： C07D295/03 , C07D211/08
CPC分类号： C07D295/096 , C07D211/08 , C07D211/14 , C07D211/18 , C07D211/22 , C07D295/02 , C07D295/03 , C07D295/073
摘要： The present invention is directed to 1,4-disubstituted piperidines, 1,4-disubstituted piperazines, 1,4-disubstituted diazepanes, and 1,3-disubstituted pyrrolidine compounds and their use.
摘要翻译：本发明涉及1,4-二取代的哌啶，1,4-二取代的哌嗪，1,4-二取代的二氮杂环庚烷和1,3-二取代的吡咯烷化合物及其用途。

85. 发明授权

US09206111B1 Compositions and methods for the treatment of neurological diseases 有权
标题翻译：用于治疗神经系统疾病的组合物和方法
公开(公告)号：US09206111B1
公开(公告)日：2015-12-08
申请号：US14572812
申请日：2014-12-17
申请人： Mahesh Kandula
发明人： Mahesh Kandula
IPC分类号： C07C53/128 , C07D295/02 , C07C57/03 , C07C211/10
CPC分类号： C07C53/128 , C07C57/03 , C07C211/10 , C07C235/12 , C07C323/43 , C07C327/06 , C07D295/02
摘要： The compositions and compounds of formula I, formula II, formula III and formula IV which includes a salt of valproic acid or its polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III and formula IV and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, migraine, schizophrenia, depression, Alzheimer's disease, cancer, HIV and familial adenomatous polyposis.
摘要翻译：式I，式II，式III和式IV的组合物和化合物，其包含丙戊酸或其多晶型物的盐，对映异构体，立体异构体，溶剂合物及其水合物。这些盐可以配制成药物组合物。包含有效量的式I，式II，式III和式IV的化合物的药物组合物以及用于治疗或预防神经疾病的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射液。这样的组合物可用于治疗癫痫，双相情感障碍，偏头痛，精神分裂症，抑郁症，阿尔茨海默病，癌症，HIV和家族性腺瘤性息肉病。

86. 发明申请

US20140288040A1 SUBSTITUTED BENZYLAMINE COMPOUNDS, THEIR USE IN MEDICINE, AND IN PARTICULAR THE TREATMENT OF HEPATITIS C VIRUS (HCV) INFECTION 审中-公开
标题翻译：替代苄嘧啶化合物，其在医学中的使用，特别是治疗丙型肝炎病毒（HCV）感染的治疗
公开(公告)号：US20140288040A1
公开(公告)日：2014-09-25
申请号：US14355780
申请日：2012-10-31
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Andrew James Woodhead , Gianni Chessari , Gilbert Ebai Besong , Maria Grazia Carr , Steven Douglas Hiscock , Michael Alistair O'Brien , David Charles Rees , Susanne Maria Saalau-Bethell , Hendrika Maria Gerarda Willems , Neil Thomas Thompson
IPC分类号： A61K31/505 , A61K31/137 , A61K45/06 , C07C217/74 , A61K31/135 , C07D239/42 , C07C237/20 , A61K31/165 , C07D211/70 , A61K31/4409 , C07D295/027 , A61K31/4465 , A61K31/4462 , A61K31/397 , C07C217/58
CPC分类号： A61K31/505 , A61K31/135 , A61K31/137 , A61K31/165 , A61K31/397 , A61K31/4409 , A61K31/4462 , A61K31/4465 , A61K45/06 , C07B2200/05 , C07C217/58 , C07C217/60 , C07C217/62 , C07C217/74 , C07C217/90 , C07C225/12 , C07C233/18 , C07C233/25 , C07C235/46 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/20 , C07C243/34 , C07C251/48 , C07C255/24 , C07C255/29 , C07C255/37 , C07C255/46 , C07C255/54 , C07C259/06 , C07C271/12 , C07C275/36 , C07C311/04 , C07C311/08 , C07C311/29 , C07C313/06 , C07C317/22 , C07C323/25 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/04 , C07D207/14 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/44 , C07D211/26 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/84 , C07D217/02 , C07D231/12 , C07D233/24 , C07D233/64 , C07D237/14 , C07D239/34 , C07D239/42 , C07D241/18 , C07D241/20 , C07D241/24 , C07D243/14 , C07D263/32 , C07D265/36 , C07D271/10 , C07D277/68 , C07D285/13 , C07D295/02 , C07D295/027 , C07D295/185 , C07D295/192 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/22 , C07D307/79 , C07D309/06 , C07D309/12 , C07D309/14 , C07D319/18 , C07D513/04
摘要： The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0, 1, 2 or 3 heteroatom ring members selected from N, O and S; R4a is selected from halogen; cyano; C1-4 alkyl optionally substituted with one or more fluorine atoms; C1-4 alkoxy optionally substituted with one or more fluorine atoms; hydroxy-C1-4 alkyl; and C1-2 alkoxy-C1-4 alkyl; R5 is selected from hydrogen and a substituent R5a; and R5a is selected from C1-2 alkyl optionally substituted with one or more fluorine atoms; C1-3 alkoxy optionally substituted with one or more fluorine atoms; halogen; cyclopropyl; cyano; and amino. The compounds have activity against hepatitis C virus and can be used in the prevention or treatment of hepatitis C viral infections.
摘要翻译：本发明提供式（6）化合物或其盐，N-氧化物或互变异构体，其中A为CH，CF或氮; E是CH，CF或氮; 和R 0是氢或C 1-2烷基; R1a选自CONH2; CO2H; 任选取代的非环C 1-8烃基; 和3至7个环成员的任选取代的单环碳环或杂环基，其中0,1,2,3或4为选自O，N和S的杂原子环成员; R2选自氢和基团R 2a; R2a选自任选取代的无环C 1-8烃基; 3至7个环成员的任选取代的单环碳环或杂环基，其中0,1或2个环成员是选自O，N和S的杂原子环成员; 和9或10个环成员的任选取代的双环杂环基，其中1或2个环成员是氮原子; 其中R 1和R 2中的至少一个不是氢; R3是含有0,1,2或3个选自N，O和S的杂原子环成员的任选取代的3至10元单环或双环碳环或杂环; R4a选自卤素; 氰基; 任选被一个或多个氟原子取代的C 1-4烷基; 任选被一个或多个氟原子取代的C 1-4烷氧基; 羟基-C 1-4烷基; 和C 1-2烷氧基-C 1-4烷基; R5选自氢和取代基R5a; 并且R 5a选自任选被一个或多个氟原子取代的C 1-2烷基; 任选被一个或多个氟原子取代的C 1-3烷氧基; 卤素; 环丙基氰基; 和氨基。该化合物具有抗丙型肝炎病毒的活性，可用于预防或治疗丙型肝炎病毒感染。

87. 发明申请

US20130281456A1 SYNTHESIS OF DEUTERATED MORPHOLINE DERIVATIVES 审中-公开
公开(公告)号：US20130281456A1
公开(公告)日：2013-10-24
申请号：US13678093
申请日：2012-11-15
申请人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
发明人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
IPC分类号： C07D263/06
CPC分类号： C07D413/10 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C215/12 , C07D263/06 , C07D295/02 , C07D295/033 , C07D295/06 , C07D295/12 , C07D295/135 , C07D413/14
摘要： The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.

88. 发明申请

US20130225594A1 DRUG DERIVATIVES 有权
标题翻译：药物衍生物
公开(公告)号：US20130225594A1
公开(公告)日：2013-08-29
申请号：US13883713
申请日：2011-11-11
申请人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
发明人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07C43/205 , C07C57/00 , C07C63/64 , C07C63/66 , C07C69/12 , C07C215/46 , C07C217/58 , C07C229/18 , C07C233/22 , C07C233/36 , C07C235/16 , C07C235/28 , C07C237/20 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/58 , C07C255/25 , C07C257/14 , C07C2601/16 , C07C2602/10 , C07C2603/74 , C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D407/06 , C07D411/10 , C07D413/04 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , C07D498/06 , C07D499/88 , C07D501/00 , C07D513/06 , C07D519/00 , C07H19/052 , C07H19/06 , C07H19/173 , C07J5/00 , C07J71/0031
摘要： The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
摘要翻译：本发明涉及已知的活性药物化合物的衍生物。由于活性化合物的氧化还原衍生物，这些衍生物与母体活性化合物不同。这意味着活性化合物中的一个或多个官能团已经在一个或多个反应中被转化为另一个基团，这可被认为代表氧化态的变化。我们通常将这些化合物称为氧化还原衍生物。本发明的衍生物可以仅通过单步转化与原始的母体活性药物化合物相关，或者可以通过包括氧化态的一个或多个变化的几个合成步骤相关。在某些情况下，两次或多次转化后获得的官能团可能与母体活性化合物处于相同的氧化态（我们在我们的氧化还原衍生物定义中包括这些化合物）。在其他情况下，本发明衍生物的氧化态可认为与母体化合物的氧化态不同。在许多情况下，本发明的化合物本身具有固有的治疗活性。在某些情况下，相对于母体化合物的相同靶标或靶标的此活性与母体化合物对靶点或靶标的活性相同或更好。

89. 发明授权

US08278489B2 Method for producing an amine 有权
标题翻译：胺的制备方法
公开(公告)号：US08278489B2
公开(公告)日：2012-10-02
申请号：US12809653
申请日：2008-12-10
申请人： Petr Kubanek , Wolfgang Mägerlein , Ekkehard Schwab , Johann-Peter Melder , Manfred Julius
发明人： Petr Kubanek , Wolfgang Mägerlein , Ekkehard Schwab , Johann-Peter Melder , Manfred Julius
IPC分类号： C07C209/16 , C07D265/30 , C07D295/03 , C07D241/04 , B01J23/835 , B01J37/03 , B01J37/18
CPC分类号： B01J23/835 , B01J23/002 , B01J37/03 , B01J37/18 , B01J2523/00 , C07C209/16 , C07C213/02 , C07D295/02 , C07D295/06 , C07C217/08
摘要： Processes for preparing an amine, which processes comprise: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, nickel and tin, and 0.5 to 8.0% by weight of an oxygen compound of cobalt, calculated as CoO, and wherein the catalytically active composition does not comprise any ruthenium.
摘要翻译：用于制备胺的方法，该方法包括：将选自伯醇，仲醇，醛，酮及其混合物的反应物与氢和选自以下的氮化合物反应：氨，伯胺，仲胺及其混合物，在二氧化锆，含铜和镍的催化剂存在下; 其中所述催化剂包含催化活性组合物，所述催化活性组合物在用氢还原之前包括锆，铜，镍和锡的氧化合物和0.5至8.0重量％的作为CoO计算的钴的氧化合物，并且其中催化活性组合物不包含任何钌。

90. 发明申请

US20110263862A1 PIPERIDINE DERIVATIVE, PIPERAZINE DERIVATIVE AND AGENT FOR TREATMENT OF DISEASE INVOLVING CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：哌啶衍生物，哌嗪衍生物和治疗涉及中枢神经系统疾病的疾病
公开(公告)号：US20110263862A1
公开(公告)日：2011-10-27
申请号：US13126158
申请日：2009-10-26
申请人： Shiro Mita , Naoyuki Kobayashi
发明人： Shiro Mita , Naoyuki Kobayashi
IPC分类号： C07D221/00
CPC分类号： C07D211/14 , C07D295/02 , C07D295/033
摘要： A novel piperidine derivative and a novel piperazine derivative which are useful as novel sigma receptor ligands, and an agent for treatment of diseases involving a central nervous system disorders, said agent containing one of the compound as an active ingredient. The agent contains a compound represented by general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: wherein X represents an alkylene group having 1 to 5 carbon atoms, and the alkylene group may be substituted by one or more alkyl groups each having 1 to 2 carbon atoms; Y represents a carbon atom or a nitrogen atom; and R1 and R2 each independently represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 2 carbon atoms or an alkoxy group having 1 to 2 carbon atoms.
摘要翻译：可用作新型σ受体配体的新型哌啶衍生物和新型哌嗪衍生物，以及用于治疗涉及中枢神经系统疾病的疾病的药剂，所述药剂含有该化合物之一作为活性成分。该试剂含有由通式（I）表示的化合物或其药学上可接受的盐作为活性成分：其中X表示碳原子数为1〜5的亚烷基，亚烷基可以各自被一个以上的烷基取代具有1至2个碳原子; Y表示碳原子或氮原子; R 1和R 2各自独立地表示氢原子，卤素原子，碳原子数1〜2的烷基或碳原子数1〜2的烷氧基。

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