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1. 发明授权

US4847282A Mucolytic acetylcysteine salts 失效
标题翻译：粘液溶解乙酰半胱氨酸盐
公开(公告)号：US4847282A
公开(公告)日：1989-07-11
申请号：US106005
申请日：1987-10-07
申请人： Arthur M. Deboeck
发明人： Arthur M. Deboeck
IPC分类号： A61K20060101 , A61K31/205 , A61K31/405 , C07C20060101 , C07C229/04 , C07C323/02 , C07D233/64
CPC分类号： C07C229/26 , C07C279/14 , C07C323/59
摘要： Water-soluble acetylcysteine salts, useful as mucolytic agents, consisting of reaction products of acetylcysteine with at least one basic amino-acid, the latter being preferably selected from the group comprising arginine, lysine, histidine, ornithine and glycine.
摘要翻译：由乙酰半胱氨酸与至少一种碱性氨基酸的反应产物组成的水溶性乙酰半胱氨酸盐，其可用作粘液溶解剂，后者优选选自精氨酸，赖氨酸，组氨酸，鸟氨酸和甘氨酸。

2. 发明授权

US5155133A Antiarrhythmic compounds and pharmaceutical compositions and methods thereof 失效
标题翻译：抗心律失常化合物及其药物组合物及其方法
公开(公告)号：US5155133A
公开(公告)日：1992-10-13
申请号：US643161
申请日：1991-01-18
申请人： Olle K. S. Almgren , Goran B. D. Duker , Gert C. Strandlund
发明人： Olle K. S. Almgren , Goran B. D. Duker , Gert C. Strandlund
IPC分类号： A61K31/275 , A61K20060101 , A61K31/10 , A61K31/13 , A61K31/54 , A61K31/55 , A61K31/554 , A61P9/06 , C07C255/53 , C07C255/54 , C07C255/56 , C07C255/58 , C07C315/02 , C07C315/04 , C07C317/02 , C07C317/18 , C07C317/26 , C07C317/28 , C07C317/32 , C07C317/44 , C07C319/20 , C07C323/02 , C07C323/13 , C07C323/25 , C07C323/26 , C07C323/29 , C07C323/32 , C07C323/36 , C07C323/41 , C07C323/58 , C07C323/62 , C07D20060101 , C07D207/08 , C07D207/12 , C07D211/18 , C07D211/24 , C07D223/04 , C07D223/06 , C07D279/00 , C07D279/12 , C07D281/06 , C07D295/00 , C07D295/04 , C07D295/08 , C07D295/22
CPC分类号： C07C323/25 , C07C317/32 , C07C323/32 , C07C323/41
摘要： A compound of the formula ##STR1## and when appropriate in the form of a racemic mixture or in the form of a stereoisomeric component and the pharmaceutically acceptable salts thereof, in which formulan is an integer 0, 1 or 2Y is [CH.sub.2 ].sub.m, CHOH, CHOCH.sub.3, CHNHR or CHF,m is an integer 0 or 1 andR is hydrogen, methyl or ethyl,Z is hydrogen or a saturated or unsaturated, straight or branched alkyl group containing 1-3 carbon atoms,A is a group ##STR2## wherein R.sub.a is a straight or branched hydroxyalkyl or an alkyl group containing 1-5 carbon atoms and optionally substituted by one or more fluoro atoms,R.sub.c is a saturated or unsaturated, straight or branched alkyl group containing 1-4 carbon atoms and optionally substituted by one or more fluoro atoms,R.sub.a' is the same as Ra and independently of R.sub.a",R.sub.a" is the same as Ra and independently of R.sub.a',p is an integer 0, 1 or 2,s is an integer 2, 3, 4, 5useful for the treatment of cardiac arrhythmia, pharmaceutical compositions containing such compounds as active ingredients, processes for preparation of such compounds as well as intermediates for their preparation.
摘要翻译：式I的化合物，适当时为外消旋混合物形式或其立体异构体形式及其药学上可接受的盐，其中式n为整数0,1或2，Y为[CH 2 m，CHOH，CHOCH 3，CHNHR或CHF，m为整数0或1，R为氢，甲基或乙基，Z为氢或含有1-3个碳原子的饱和或不饱和的直链或支链烷基，A为其中R a是直链或支链羟烷基或含有1-5个碳原子并任选被一个或多个氟原子取代的烷基，R c是含有1-4个碳原子的饱和或不饱和的直链或支链烷基原子并且任选地被一个或多个氟原子取代，Ra'与Ra相同且独立于Ra“，Ra”与Ra相同且独立于Ra'，p是整数0,1或2，s 是用于治疗心律失常的整数2,3,4,5，含有s的药物组合物这些化合物作为活性成分，制备这些化合物的方法以及其制备中间体。

3. 发明授权

US5145611A Carboxylic acid derivatives, and pharmaceutical compositions containing them 失效
标题翻译：羧酸衍生物和含有它们的药物组合物
公开(公告)号：US5145611A
公开(公告)日：1992-09-08
申请号：US143456
申请日：1988-01-12
申请人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuehnle
发明人： Hans P. Wolff , Ernst-Christian Witte , Hans-Frieder Kuehnle
IPC分类号： C07C69/708 , A61K20060101 , A61K31/095 , A61K31/16 , A61K31/185 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/255 , A61P3/00 , A61P3/08 , A61P3/10 , C07C20060101 , C07C51/00 , C07C51/06 , C07C51/09 , C07C51/367 , C07C53/126 , C07C59/00 , C07C59/125 , C07C59/13 , C07C59/58 , C07C59/64 , C07C59/68 , C07C59/70 , C07C67/00 , C07C69/712 , C07C69/734 , C07C69/736 , C07C229/22 , C07C233/00 , C07C233/01 , C07C309/00 , C07C313/00 , C07C315/02 , C07C317/00 , C07C317/02 , C07C317/04 , C07C317/06 , C07C317/14 , C07C317/16 , C07C317/44 , C07C317/46 , C07C317/48 , C07C319/14 , C07C321/00 , C07C321/02 , C07C323/02 , C07C323/09 , C07C323/12 , C07C323/15 , C07C323/16 , C07C323/19 , C07C323/25 , C07C323/30 , C07C323/52 , C07C323/54 , C07C323/56 , C07C323/65
CPC分类号： C07C317/00 , Y10S514/866
摘要： Carboxylic acid derivatives of the formula ##STR1## R.sub.1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R.sub.2 is optionally substituted aryl or, when B is alkylene also a hydrogen atom. A is a straight-chained or branched, saturated or unsaturated alkylene containing 3 to 10 carbon atoms which is optionally interrupted by a heteratom attached to a saturated carbon and has a chain length of at least 3 atoms. Y is S(O).sub.n group or oxygen, n being 0, 1 or 2. B is a valency bond or a straight-chained or branched, saturated or unsaturated alkylene containing 1 to 18 carbon atoms. Physiologically acceptable salts, esters and amides thereof are also included. The compounds are useful in the treatment of metabolic diseases.
摘要翻译：式R1的羧酸衍生物是烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，环烷基或环烷氧基或任选取代的芳基，芳氧基，芳硫基，芳基亚磺酰基，芳基磺酰基或芳基氨基。 R2是任选取代的芳基，或当B是亚烷基也是氢原子时。 A是含有3至10个碳原子的直链或支链，饱和或不饱和的亚烷基，其任选被连接到饱和碳上的杂原子中断并具有至少3个原子的链长度。 Y是S（O）n基或氧，n是0,1或2.B是价键或含有1至18个碳原子的直链或支链，饱和或不饱和的亚烷基。还包括其生理上可接受的盐，酯和酰胺。该化合物可用于治疗代谢性疾病。

4. 发明授权

US6063807A Cyclo-oxygenase inhibitor and amidine derivatives salts, preparation method therefor, use thereof as drugs, and pharmaceutical compositions containing said salts 失效
标题翻译：环加氧酶抑制剂和脒衍生物盐，其制备方法，作为药物的用途，以及含有所述盐的药物组合物
公开(公告)号：US6063807A
公开(公告)日：2000-05-16
申请号：US981682
申请日：1998-01-06
申请人： Pierre Etienne Chabrier de Lassauniere , Colette Broquet
发明人： Pierre Etienne Chabrier de Lassauniere , Colette Broquet
IPC分类号： A61K45/00 , A61K31/155 , A61K31/19 , A61K31/195 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/60 , A61P9/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07C257/14 , C07C257/18 , C07C279/04 , C07C279/18 , C07C279/32 , C07C281/06 , C07D209/28 , A61K31/40 , C07C323/02 , C07D209/26 , C07D333/22
CPC分类号： A61K31/606 , A61K31/19 , A61K31/195 , A61K31/405 , A61K31/60
摘要： Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.
摘要翻译： PCT No.PCT / FR96 / 01095 Sec。 371日期：1998年1月6日 102（e）日期1998年1月6日PCT提交1996年7月15日PCT公布。出版物WO97 / 03678 日期：1997年2月6日公开了环加氧酶抑制剂和脒衍生物盐，其制备方法，含有所述盐的药物组合物及其用途，特别是NO合成酶和环加氧酶抑制剂。

5. 发明授权

US4621160A Process for the chlorination of aromatic derivatives 失效
标题翻译：芳香族衍生物氯化方法
公开(公告)号：US4621160A
公开(公告)日：1986-11-04
申请号：US623466
申请日：1984-06-22
申请人： Michel Desbois , Camille Disdier
发明人： Michel Desbois , Camille Disdier
IPC分类号： C07B31/00 , C07B39/00 , C07C17/00 , C07C17/12 , C07C17/14 , C07C25/02 , C07C25/13 , C07C25/22 , C07C37/62 , C07C39/27 , C07C41/00 , C07C41/22 , C07C43/225 , C07C43/29 , C07C45/00 , C07C45/63 , C07C49/80 , C07C49/813 , C07C51/00 , C07C51/363 , C07C63/70 , C07C65/03 , C07C67/00 , C07C201/00 , C07C201/12 , C07C205/12 , C07C209/00 , C07C209/74 , C07C211/52 , C07C313/00 , C07C319/20 , C07C323/02
CPC分类号： C07C323/00 , C07B39/00 , C07C17/12 , C07C201/12 , C07C37/62 , C07C41/22 , C07C45/63 , C07C49/80 , C07C49/813 , C07C51/363
摘要： A process for the chlorination of aromatic derivatives. The aromatic derivative is reacted with chlorine gas in liquid hydrofluoric acid. The products obtained are useful as intermediates for the synthesis of compounds having a plant-protecting or pharmaceutical activity.
摘要翻译：芳香族衍生物氯化方法。芳香族衍生物与液态氢氟酸中的氯气反应。获得的产物可用作合成具有植物保护或药物活性的化合物的中间体。

6. 发明授权

US4507500A Process for producing 2-mercaptoethylamine hydrohalides 失效
标题翻译： 2-巯基乙胺氢卤化物的制备方法
公开(公告)号：US4507500A
公开(公告)日：1985-03-26
申请号：US281091
申请日：1981-07-07
申请人： Shigenobu Nakayama , Eiichi Noda , Yoshiaki Noguchi , Isamu Yamamoto , Noboru Kawasaki
发明人： Shigenobu Nakayama , Eiichi Noda , Yoshiaki Noguchi , Isamu Yamamoto , Noboru Kawasaki
IPC分类号： C07C323/02 , A61K31/095 , A61K31/13 , A61K31/131 , C07C67/00 , C07C313/00 , C07C319/02 , C07C319/12 , C07C323/25 , C07C323/29 , C07C329/16 , C07C149/24
CPC分类号： C07C319/02 , C07C329/16
摘要： A process for producing 2-mercaptoethylamine hydrohalides of the general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are identical or different, and each represents a hydrogen atom, a lower alkyl group, a hydroxy-substituted lower alkyl group or a phenyl group, and X represents a halogen atom,which comprises reacting a 2-mercaptothiazoline of the general formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with a 2-halogenoethylamine hydrohalide of the general formula ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as defined above, in the presence of water.
摘要翻译：制备通式为（III）的2-巯基乙胺氢卤化物的方法，其中R 1，R 2，R 3和R 4相同或不同，各自表示氢原子，低级烷基，羟基取代的低级烷基或苯基，并且X表示卤素原子，其包括使通式为其中R 1，R 2，R 3和R 4如上定义的通式为其中R1，R2，R3和R4的2-巯基噻唑与2-卤代乙胺氢卤酸酯反应，在水的存在下，通式（II）其中R 1，R 2，R 3，R 4和X如上所定义。

7. 发明授权

US08067467B2 Thiosuccinic acid derivatives and the use thereof 有权
标题翻译：硫代琥珀酸衍生物及其用途
公开(公告)号：US08067467B2
公开(公告)日：2011-11-29
申请号：US11914426
申请日：2006-05-03
申请人： Rajendra Kumar Joshi , Hans-Peter Strebel , Jitka Ulrichová , Thomas J. Schmidt
发明人： Rajendra Kumar Joshi , Hans-Peter Strebel , Jitka Ulrichová , Thomas J. Schmidt
IPC分类号： A61K31/225 , C07C323/02
CPC分类号： C07K14/001 , C07C323/58 , C07K5/0215
摘要： The present invention relates to compounds of the formula (I) wherein X1 and X2 independently represent O, NH or S, R1 and R2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X1 or X2 in this case being NH, and hydrogen, both radicals R1 and R2 preferably not being H, wherein R3 is a residue selected from group consisting of —S—R6, wherein R6 is a C1-C30 hydrocarbyl group, at least one of R1 and R2 not being H when X1 and X2 are oxygen, —S—CH2—CH(NH2)(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group, and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug and drugs containing the same.
摘要翻译：本发明涉及式（I）化合物，其中X 1和X 2独立地表示O，NH或S，R 1和R 2独立地选自C 1 -C 30烃基，通过酰胺键键合的氨基酸或通过酰胺键键合的肽，其各自具有多达200个氨基酸，在这种情况下，缀合的残基X1或X2为NH，氢为自由基R1和R2优选不为H，其中R3为选自的-S-R 6，其中R 6是C 1 -C 30烃基，当X 1和X 2是氧时，R 1和R 2中的至少一个不是H，-S-CH 2 -CH（NH 2）（COOH）（半胱氨酸-S- （例如N-乙酰半胱氨酸-S-基），具有至多200个氨基酸的肽，其含有至少一个具有硫醇基的氨基酸基团，优选半胱氨酸基团，并通过硫硫，优选经由半胱氨酸硫（肽-S-基），辅酶A，其通过硫醇基或脆片键合通过硫醇基键合的酰基载体蛋白和通过硫醇基键合的二氢硫辛酸及其药学上可接受的盐。本发明还涉及这些化合物用于制备药物的用途和含有这些化合物的药物。

8. 发明申请

US20090232747A1 THIOESTER COMPOUNDS AND THEIR USE IN FRAGRANCE OR FLAVOR APPLICATIONS 有权
标题翻译：硫化物化合物及其在芳香或挥发油应用中的用途
公开(公告)号：US20090232747A1
公开(公告)日：2009-09-17
申请号：US12047095
申请日：2008-03-12
申请人： Kathryn Bardsley , David O. Agyemang , Tao Pei
发明人： Kathryn Bardsley , David O. Agyemang , Tao Pei
IPC分类号： A61K8/46 , C07C323/02 , A61K47/20 , A23L1/226 , A23G4/06
CPC分类号： A23L2/56 , A23L27/2022 , A23L27/204 , A23L27/29 , C07C323/52
摘要： The present invention relates to thioester compounds and the incorporation and use of the new chemical entities as flavor and fragrance chemicals.
摘要翻译：本发明涉及硫酯化合物以及新化学实体作为香料和香料化学品的掺入和使用。

9. 发明授权

US07011960B2 Substituted 2-amino-3-(2-amino-phenylsulfanyl)-propionic acids 有权
标题翻译：取代的2-氨基-3-（2-氨基 - 苯硫基） - 丙酸
公开(公告)号：US07011960B2
公开(公告)日：2006-03-14
申请号：US10252971
申请日：2002-09-23
申请人： Konrad Bleicher , Scott Borthwick , Hans Iding , Mark Rogers-Evans , Stefan Schmid , Han Min Tong , Beat Wirz
发明人： Konrad Bleicher , Scott Borthwick , Hans Iding , Mark Rogers-Evans , Stefan Schmid , Han Min Tong , Beat Wirz
IPC分类号： C12P13/04 , A61K38/17 , A01N43/10 , C07D291/06 , C07C323/02
CPC分类号： C12P13/04 , C07C323/59 , C07C323/63 , C07D285/36 , C12P11/00 , C12P41/005
摘要： The present invention relates to a new process for the preparation compounds of formula I wherein R1, R2, R3 and n are as described in the description which process comprises reacting compounds of formula II wherein R1, R2, R3, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent. The compound of formula I are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin converting enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor).
摘要翻译：本发明涉及制备式I化合物的新方法，其中R 1，R 2，R 3和n如上所述在描述中，该方法包括使式II化合物其中R 1，R 2，R 3，R 3，R 4和R 4， / SUP>如描述中所述，在含有有机共溶剂的水性体系中具有蛋白酶。式I化合物可用于制备可用作酶抑制剂的1,5-苯并硫氮杂，如蛋白酶，白细胞介素-1β转换酶，弹性蛋白酶或血管紧张素转换酶，GPCR拮抗剂（缩胆囊素，血管紧张素II受体）。

10. 发明申请

US20050261506A1 Process for producing spiroglycol 审中-公开
标题翻译：生产螺旋藻的方法
公开(公告)号：US20050261506A1
公开(公告)日：2005-11-24
申请号：US11130122
申请日：2005-05-17
申请人： Masafumi Watanabe , Junichi Amemiya , Ikutaro Kuzuhara
发明人： Masafumi Watanabe , Junichi Amemiya , Ikutaro Kuzuhara
IPC分类号： C07D493/10 , C07C323/02
CPC分类号： C07D493/10
摘要： In the production of spiroglycol by the reaction of pentaerythritol and hydroxypivalaldehyde in water in the presence of an acid catalyst, (A) a total content of amines and amine salts in hydroxypivalaldehyde is reduced to 1.5% by weight or lower; (B) seed crystals are added to the reaction system before initiating the reaction and/or during the reaction in an amount from 1.5 to 30% by weight on the basis of the total feed amount of pentaerythritol, hydroxypivalaldehyde, water, the acid catalyst and the seed crystals, each being fed into the reaction system; (C) the pH of the reaction system is kept from 0.1 to 4.0 from initiation of the reaction to completion of the reaction; and (D) the sum of a maximum theoretical amount of spiroglycol to be synthesized from pentaerythritol and hydroxypivalaldehyde to be fed into the reaction system and an amount of spiroglycol contained in the seed crystals to be added to the reaction system is controlled within a range from 5 to 35% by weight on the basis of the total feed amount. The spiroglycol produced has an increased particle size. By washing the spiroglycol with a basic solution, the heat stability is improved.
摘要翻译：在酸催化剂存在下，季戊四醇与羟基新戊醛在水中的反应生产中，（A）羟基新戊醛中胺和胺盐的总含量降低至1.5重量％以下; （B）基于季戊四醇，羟基新戊醛，水，酸催化剂的总进料量和基于季铵盐的总进料量，在开始反应和/或反应期间将晶种加入到反应体系中的量为1.5至30重量％种子晶体，各自被送入反应体系; （C）反应体系的pH从反应开始至反应完全为止保持在0.1〜4.0; 和（D）将从进料到反应体系中的季戊四醇和羟基新戊醛合成的螺旋体的最大理论量的总和和加入到反应体系中的晶种中所含的螺旋体的量控制在基于总进料量5至35重量％。所生产的螺旋体具有增加的粒度。通过用碱性溶液洗涤螺旋藻，热稳定性得到改善。

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