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1. 发明授权

US08877971B2 Method for preparing formamide compounds 有权
标题翻译：甲酰胺化合物的制备方法
公开(公告)号：US08877971B2
公开(公告)日：2014-11-04
申请号：US13805899
申请日：2012-04-04
申请人： Thibault Cantat , Christophe Gomes , Olivier Jacquet
发明人： Thibault Cantat , Christophe Gomes , Olivier Jacquet
IPC分类号： C07C231/10 , C07D265/30 , C07C249/02 , C07D231/12 , C07D233/58 , C07D251/28 , C07C249/16 , C07D243/28 , C07D233/06 , C07D249/16 , C07D249/08 , C07D249/02 , C07D241/04 , C07D295/185 , C07C241/04
CPC分类号： C07C231/10 , B01J31/0244 , B01J31/0245 , B01J31/0251 , B01J31/122 , B01J31/2409 , B01J2231/625 , B01J2531/0247 , B01J2531/842 , C07B59/00 , C07B2200/05 , C07C241/04 , C07C249/02 , C07C249/16 , C07D231/12 , C07D233/06 , C07D233/58 , C07D241/04 , C07D243/28 , C07D249/02 , C07D249/08 , C07D249/16 , C07D251/28 , C07D295/185 , C07C233/03 , C07C243/28 , C07C251/28 , C07C251/86
摘要： The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers which includes a step of preparing formamide compounds by the method according to the invention.
摘要翻译：本发明涉及使用二氧化碳制备甲酰胺化合物的方法，以及所述使用所述制造维生素，药物产品，粘合剂，丙烯酸纤维，合成革，农药和肥料的方法。本发明还涉及一种制造维生素，药物产品，粘合剂，丙烯酸纤维，合成皮革，农药和肥料的方法，其包括通过本发明的方法制备甲酰胺化合物的步骤。

2. 发明授权

US07851638B2 Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia 有权
标题翻译：环己磺酰基衍生物作为治疗精神分裂症的GLYT1抑制剂
公开(公告)号：US07851638B2
公开(公告)日：2010-12-14
申请号：US12571904
申请日：2009-10-01
申请人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Elizabeth Mary Naylor , Leslie Joseph Street
发明人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Elizabeth Mary Naylor , Leslie Joseph Street
IPC分类号： C07D249/02 , A61K31/4192
CPC分类号： C07D213/82 , C07C233/70 , C07C233/76 , C07C317/30 , C07C2601/02 , C07C2601/14 , C07D231/12 , C07D231/18 , C07D239/28 , C07D249/04 , C07D285/125 , C07D295/108 , C07D295/135 , C07D307/68 , C07D333/38 , C07D471/04 , C07D495/04
摘要： The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
摘要翻译：本发明提供式I化合物：其中R 1是烷基，苯基，杂环基，环烷基，烷氧基，酯，氨基或酰胺基; R2是苯基，杂环基，烷基，环烷基或环烷基烷基; R3是烷基，环烷基，环烷基烷基，氨基或杂环基; R4和R5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂，因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物，第一和第二医疗用途和治疗方法。

3. 发明授权

US5707978A Heteroaryl-substituted deoxy glycero-phosphoethanolamines 失效
标题翻译：杂芳基取代的脱氧甘油基 - 磷酸乙醇胺
公开(公告)号：US5707978A
公开(公告)日：1998-01-13
申请号：US485427
申请日：1995-06-07
申请人： Friedrich Paltauf , Albin Hermetter , Rudolf Franzmair
发明人： Friedrich Paltauf , Albin Hermetter , Rudolf Franzmair
IPC分类号： C07D249/02 , A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/675 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , C07D207/32 , C07D207/333 , C07D209/08 , C07D209/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D249/08 , C07D473/00 , C07F9/10 , C07F9/572 , C07F9/6503 , C07F9/6506 , C07F9/6515 , C07F9/6518
CPC分类号： C07F9/65188 , C07F9/10 , C07F9/5721 , C07F9/5728 , C07F9/65032 , C07F9/65061 , C07F9/65181
摘要： Therapeutically active, heteroaryl-substituted deoxy glycero-phosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of X, Y or Z is a fatty ether substituent, one is a heteroaryl ring substituent with 1-4 nitrogens as the only heteroatoms, one of which is bonded to a carbon of the glyceryl backbone, and one is a phosphoethanolamine substituent substituted at the nitrogen, provided that each of X, Y and Z is a different substituent, and the pharmaceutical compositions comprising the therapeutically active compounds and methods of using the therapetically active compounds to treat cancerous tumors, psoriasis and inflammation are also disclosed.
摘要翻译：公开了具有通式I：其中X，Y或Z之一是脂肪醚取代基的通式I的杂芳基取代的脱氧甘油基 - 磷酸乙醇胺，一个是具有1-4个氮原子的杂芳基环取代基杂原子，其中一个与甘油主链的碳键合，一个是在氮取代的磷酸乙醇胺取代基，条件是X，Y和Z各自为不同的取代基，并且药物组合物包含治疗活性化合物和还公开了使用治疗活性化合物治疗癌性肿瘤，牛皮癣和炎症的方法。

4. 发明授权

US5622982A Acylated aminoalkanimidazoles and - triazoles 失效
标题翻译：酰化氨基链烷基咪唑和 - 三唑
公开(公告)号：US5622982A
公开(公告)日：1997-04-22
申请号：US442053
申请日：1995-05-16
申请人： Ingeborg Schuster , Helmut Egger
发明人： Ingeborg Schuster , Helmut Egger
IPC分类号： C12N9/99 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4196 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/08 , A61P29/00 , A61P43/00 , C07D233/54 , C07D233/60 , C07D233/61 , C07D249/02 , C07D249/08 , C07D401/06 , C07D409/06 , C07D521/00 , C07D401/12 , C07D409/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention concerns azole compounds of formula ##STR1## wherein the substituents have various significances, in free form or salt form.They can be prepared e.g. by acylation, or by aziridine or oxazole ring opening.The compounds can be used as pharmaceuticals, especially as selective inhibitors of the 25-hydroxyvitamin D3--hydroxylases in the treatment of disorders of proliferation and differentiation in vitamin D--responsive tissues.
摘要翻译：本发明涉及式I的唑类化合物，其含义为游离形式或盐形式。它们可以例如制备。通过酰化，或通过氮丙啶或恶唑环开环。该化合物可用作药物，特别是作为25-羟基维生素D3-羟化酶的选择性抑制剂，用于治疗维生素D反应性组织中增殖和分化紊乱。

5. 发明授权

US5607956A 1-heteroazolyl-1-heterocyclyl alkane derivatives and their use and their use as neuroprotective agents 失效
标题翻译： 1-杂唑基-1-杂环基烷烃衍生物及其用途及其作为神经保护剂的用途
公开(公告)号：US5607956A
公开(公告)日：1997-03-04
申请号：US459847
申请日：1995-06-02
申请人： Robin B. Boar , Alan J. Cross , Duncan A. Gray , Richard A. Green
发明人： Robin B. Boar , Alan J. Cross , Duncan A. Gray , Richard A. Green
IPC分类号： C07D277/24 , A61K20060101 , A61K31/395 , A61K31/41 , A61K31/415 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/443 , A61P9/10 , A61P25/00 , C07D20060101 , C07D207/00 , C07D207/32 , C07D207/33 , C07D231/12 , C07D233/58 , C07D233/64 , C07D249/02 , C07D261/06 , C07D263/30 , C07D263/32 , C07D271/02 , C07D273/00 , C07D275/02 , C07D277/20 , C07D277/22 , C07D277/26 , C07D277/28 , C07D285/01 , C07D291/04 , C07D293/04 , C07D293/06 , C07D307/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D421/06 , C07D421/14
CPC分类号： C07D405/06 , C07D413/06 , C07D417/06 , C07D417/14
摘要： The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## geometric and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof;having therapeutic activity, processes and intermediates for their preparation, pharmaceutical formulations containing said compounds and the medicinal use of said compounds.
摘要翻译：本发明涉及具有通式（1）的新型杂环化合物，其中存在这些异构体的几何和旋光异构体及其外消旋体，以及其药学上可接受的酸加成盐和溶剂合物; 具有治疗活性，其制备方法和中间体，含有所述化合物的药物制剂和所述化合物的医药用途。

6. 发明授权

US5567692A 9-[(substituted glycyl) amido)]-6-demethyl-6-deoxytetracyclines 失效
标题翻译： 9 - [（取代甘氨酰）酰氨基）] - 6-脱甲基-6-脱氧四环素
公开(公告)号：US5567692A
公开(公告)日：1996-10-22
申请号：US443612
申请日：1995-05-18
申请人： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
发明人： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC分类号： A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C239/20 , C07C255/50 , C07C271/22 , C07C323/29 , C07D207/06 , C07D207/14 , C07D207/16 , C07D207/30 , C07D209/02 , C07D211/14 , C07D211/56 , C07D213/40 , C07D213/74 , C07D221/22 , C07D231/12 , C07D231/14 , C07D241/04 , C07D241/14 , C07D249/02 , C07D249/04 , C07D249/08 , C07D265/28 , C07D279/04 , C07D295/14 , C07D295/15 , C07D295/215 , C07D295/24 , C07D307/33 , C07D333/20 , C07D333/36 , C07F15/00
CPC分类号： C07D213/40 , C07C237/26 , C07C239/18 , C07C239/20 , C07C271/22 , C07D295/15 , C07D295/215 , C07D295/24 , C07D333/20 , C07C2103/46
摘要： The invention provides a method for prevention, treatment or control of bacterial infections in warm blooded animals by administering a pharmacologically effect amount of a compound of the formula: ##STR1## wherein R, R.sup.1 and W are defined in the specification.
摘要翻译：本发明提供了一种通过施用药理作用量的下式化合物其中R，R 1和W在说明书中定义的方法来预防，治疗或控制温血动物细菌感染的方法。

7. 发明授权

US5397701A Azido-substituted fatty acid analog enzyme substrates 失效
标题翻译：叠氮取代的脂肪酸类似物酶底物
公开(公告)号：US5397701A
公开(公告)日：1995-03-14
申请号：US198717
申请日：1994-02-18
申请人： Balekudru Devadas , Jeffrey I. Gordon , Steven P. Adams
发明人： Balekudru Devadas , Jeffrey I. Gordon , Steven P. Adams
IPC分类号： A61K31/41 , A61K31/655 , A61P31/12 , C07C247/12 , C07C323/52 , C07D249/02 , C07D249/04 , C07D257/04 , C07D521/00 , C07K1/107 , C07K1/113 , C07K14/00 , C12N9/10 , C12P21/02 , C12P21/00
CPC分类号： C07D257/04 , C07C247/12 , C07C323/52 , C07D231/12 , C07D233/56 , C07D249/04 , C07D249/08 , C07K1/1077 , C12N9/1029
摘要： Azido-substituted fatty acid analogs which are useful in the fatty acid acylation of peptides and proteins and as antiviral agents are disclosed having the following chemical structure:Z--(CH.sub.2).sub.x COORwhereinZ=azido, tetrazolyl or triazolylR=H or C.sub.1 -C.sub.8 alkyl, andx=8-12.
摘要翻译：公开了可用于肽和蛋白质和抗病毒剂的脂肪酸酰化的叠氮取代的脂肪酸类似物，其具有以下化学结构：Z-（CH 2）x COOR其中Z =叠氮基，四唑基或三唑基R = H或C1- C8烷基，x = 8-12。

8. 发明授权

US4978672A Alpha-heterocyclc substituted tolunitriles 失效
标题翻译： α-杂环取代的亚苄基
公开(公告)号：US4978672A
公开(公告)日：1990-12-18
申请号：US240862
申请日：1988-09-06
申请人： Robert M. Bowman , Ronald E. Steele , Leslie Browne
发明人： Robert M. Bowman , Ronald E. Steele , Leslie Browne
IPC分类号： C07D213/57 , C07D233/61 , C07D249/02 , C07D249/08 , C07D521/00
CPC分类号： C07D231/12 , C07D213/57 , C07D233/56 , C07D249/02 , C07D249/08
摘要： The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4)-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, 1-(1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及芳香酶抑制化合物，其中R和R 4代表氢或低级烷基; 或R和Ro位于相邻的碳原子上并与它们所连接的苯环组合时形成萘或四氢萘环; R 1和R 2独立地表示氢，低级烷基，（低级烷基，芳基或芳基 - 低级烷基） - 硫代，低级链烯基，芳基，芳基 - 低级烷基，C 3 -C 6环烷基或C 3 -C 6环烷基 - 低级烷基。或R 1和R 2组合表示低级亚烷基，单 - 或二 - 芳基 - 低级亚烷基; R1和R2组合也表示C4-C6-直链亚烷基，低级烷基取代的直链亚烷基或邻 - 亚苯基桥连的C 2 -C 4 - 直链亚烷基，每个亚甲基与连接有相应的任选取代的或苯并 - 稠合的5,6或7元环; W表示1-咪唑基，1-（1,2,4-或1,3,4） - 三唑基或3-吡啶基; 或W表示1-咪唑基，1-（1,2,4或1,3,4） - 三唑基或被低级烷基取代的3-吡啶基; 及其药学上可接受的盐。

9. 发明授权

US4284584A Process for the preparation of acyl cyanides 失效
标题翻译：酰基氰的制备方法
公开(公告)号：US4284584A
公开(公告)日：1981-08-18
申请号：US967932
申请日：1978-12-08
申请人： Kurt Findeisen
发明人： Kurt Findeisen
IPC分类号： C07D249/02 , C07C20060101 , C07C51/54 , C07C63/04 , C07C67/00 , C07C253/00 , C07C253/04 , C07C255/17 , C07C255/31 , C07C255/40 , C07C255/45 , C07C255/56 , C07D235/04 , C07D247/00 , C07D253/06 , C07D261/08 , C07D263/32 , C07D269/00 , C07D285/08 , C07D295/18 , C07D307/46 , C07D307/54 , C07D521/00
CPC分类号： C07C253/16
摘要： Acyl cyanides of the formula ##STR1## in which R represents alkyl or substituted alkyl of from 1 to 8 carbon atoms, cycloalkyl or substituted cycloalkyl of from 3 to 12 carbon atoms, aryl or substituted aryl; or an optionally substituted 5-membered or 6-membered heterocyclic radical which can also be fused with a benzene ringare prepared by reacting the corresponding carboxylic acid anhydride in the presence of a carboxylic acid halide with an alkali metal cyanide or anhydrous acid, at a temperature of between 50.degree. and 300.degree. C.
摘要翻译：式（I）的酰基氰化物，其中R表示1至8个碳原子的烷基或取代的烷基，具有3至12个碳原子的环烷基或取代的环烷基，芳基或取代的芳基; 或者也可以与苯环稠合的任意取代的5元或6元杂环基通过在羧酸卤化物存在下与相应的羧酸酐与碱金属氰化物或无水酸反应来制备，温度在50°C到300°C之间

10. 发明授权

US4198406A Carbamoyl heterocyclicthio cephalosporins and pharmaceutical compositions formulated therewith 失效
标题翻译：氨基甲酰基杂环硫代头孢菌素及其配制的药物组合物
公开(公告)号：US4198406A
公开(公告)日：1980-04-15
申请号：US835218
申请日：1977-09-21
申请人： Kenneth D. Hardy , George Burton
发明人： Kenneth D. Hardy , George Burton
IPC分类号： C07D249/02 , C07D257/04 , C07D271/10 , C07D271/113 , C07D285/12 , C07D285/125 , C07D501/36 , A61K31/545
CPC分类号： C07D257/04 , C07D249/02 , C07D271/113 , C07D285/125 , C07D501/36
摘要： Novel cephalosporin compounds, process of preparation thereof, intermediates useful in the preparation of the cephalosporins, pharmaceutical compositions formulated therefrom for administration and combinations of the cephalosporins in pharmaceutical composition form with clavulanic acid. The cephalosporin compounds are characterized by a 5-membered nitrogen-containing ring in the group in the 3-position of the sulphur-containing ring.
摘要翻译：新型头孢菌素化合物，其制备方法，可用于制备头孢菌素的中间体，由其配制的药物组合物，以及药物组合物形式的头孢菌素与克拉维酸的组合。头孢菌素化合物的特征在于含硫环3位的5元含氮环。

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