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1. 发明授权

US11124475B2 Hydrogen sulfide donor in organic salt form and preparation method therefor 有权
公开(公告)号：US11124475B2
公开(公告)日：2021-09-21
申请号：US16625840
申请日：2018-03-15
申请人： CHENGDU KAOENSI SCIENCE AND TECHNOLOGY CO., LTD.
发明人： Hu Zheng , Lingling Weng
IPC分类号： C07C277/08 , C07C279/14 , C07C279/18 , C07C279/26 , C07C279/28 , C07D209/16 , C07D213/73 , C07D233/50 , C07D233/64 , C07D245/02 , C07D277/48 , C07D295/027 , C07D295/215 , C07D487/04
摘要： A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value.

2. 发明授权

US10588977B2 Preserved compositions containing hyaluronic acid or a pharmaceutically-acceptable salt thereof and related methods 有权
公开(公告)号：US10588977B2
公开(公告)日：2020-03-17
申请号：US16186866
申请日：2018-11-12
申请人： Johnson & Johnson Consumer Inc.
发明人： Uday Doshi , Kenneth T. Holeva
IPC分类号： A61K31/728 , C07C279/28 , C07C279/26 , A61K9/08 , A61K47/36 , C08B37/08 , A61K9/00 , A61K47/18 , A61K31/155
摘要： The invention provides a composition containing hyaluronic acid (HA) or a pharmaceutically-acceptable salt thereof preserved with a cationic preservative and related methods. In one embodiment, the pharmaceutically-acceptable salt is sodium hyaluronate. In another embodiment, the cationic preservative includes benzalkonium chloride (BAK).

3. 发明授权

US10266485B2 Compounds and compositions for intracellular delivery of therapeutic agents 有权
公开(公告)号：US10266485B2
公开(公告)日：2019-04-23
申请号：US16005286
申请日：2018-06-11
申请人： ModernaTX, Inc.
发明人： Kerry E. Benenato
IPC分类号： A61K48/00 , A61K9/127 , C07C229/12 , C07C271/20 , C07C279/12 , C07C279/28 , C07C279/32 , C07D233/72 , C07D249/04 , C07D263/20 , C07D265/33 , C07D271/06 , C07D271/10 , C07D207/27 , C07D277/38 , C07C275/14 , C07C279/24 , C07C311/05 , C07C229/16 , C07C335/08 , C07C233/36 , C07C235/10 , C07C255/24 , C07F9/09 , A61K9/16 , A61K38/18 , C07K14/505 , A61K9/00 , A61K47/54 , A61K47/69 , C07C227/16 , A61K9/51 , A61K31/7105 , A61K38/17 , C07C227/18
摘要： The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

4. 发明授权

US06881753B2 Potassium channel inhibitors and method 有权
标题翻译：钾通道抑制剂及方法
公开(公告)号：US06881753B2
公开(公告)日：2005-04-19
申请号：US10823987
申请日：2004-04-14
申请人： John Lloyd , Heather J. Finlay , Wayne Vaccaro , Karnail S. Atwal , Michael F. Gross , Kerry L. Spear
发明人： John Lloyd , Heather J. Finlay , Wayne Vaccaro , Karnail S. Atwal , Michael F. Gross , Kerry L. Spear
IPC分类号： A61K31/277 , A61K31/352 , A61K31/353 , A61K31/381 , A61K31/42 , A61K31/429 , A61K31/436 , A61K31/472 , A61K31/496 , A61K31/506 , A61P9/06 , C07C303/40 , C07C311/20 , C07D215/42 , C07D311/68 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D473/38 , C07D491/04 , C07D491/052 , C07D493/04 , C07D513/04 , C07C279/28 , A61K31/155 , C07C279/18
CPC分类号： C07D409/14 , C07C311/20 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D215/42 , C07D311/68 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/12 , C07D473/38 , C07D491/04 , C07D493/04 , C07D513/04
摘要： Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.
摘要翻译：茚，苯并吡喃及其类似物是IKur的钾通道抑制剂和阻断剂，并具有以下结构：其中A，B，D，Q，X 1，R 1，R 1， X 2和R 2如本文所定义。这些化合物可用作抗心律失常药。此外，提供了一种用于预防使用上述化合物的心律失常的方法。

5. 发明授权

US06875764B1 Urea and thiourea compounds useful for treatment of coccidiosis 失效
标题翻译：用于治疗球虫病的尿素和硫脲化合物
公开(公告)号：US06875764B1
公开(公告)日：2005-04-05
申请号：US10111376
申请日：2000-10-27
申请人： Sabrina Muzi , Shoaá Abdul Rahman
发明人： Sabrina Muzi , Shoaá Abdul Rahman
IPC分类号： A23K1/16 , A23K1/18 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C279/24 , C07C279/28 , C07C281/16 , C07C281/18 , C07C335/16 , C07C335/18 , C07C335/22 , C07C335/28 , C07C335/42 , C07D209/54 , C07D213/71 , C07D213/75 , C07D215/38 , C07D217/24 , C07D233/84 , C07D241/20 , C07D265/24 , C07D265/30 , C07D277/48 , C07D277/82 , C07D295/215 , C07D401/12 , C07D405/04 , C07D413/12 , C07D417/14 , C07D275/28 , A61K31/17 , A61K31/425 , C07D295/16
CPC分类号： C07D213/75 , A23K20/105 , A23K20/111 , A23K20/116 , A23K50/75 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C279/24 , C07C279/28 , C07C281/16 , C07C281/18 , C07C335/16 , C07C335/18 , C07C335/22 , C07C335/28 , C07C335/42 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2603/24 , C07C2603/74 , C07D209/54 , C07D213/71 , C07D215/38 , C07D217/24 , C07D233/84 , C07D241/20 , C07D265/24 , C07D265/30 , C07D277/48 , C07D277/82 , C07D295/215 , C07D401/12 , C07D405/04 , C07D413/12 , C07D417/14
摘要： The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.
摘要翻译：本发明涉及新化合物，含有该化合物的药物组合物以及治疗寄生虫病的方法，其中施用所述化合物。本发明化合物特别适用于治疗球虫病，特别是在家禽中，并且它们具有通式（I）：其中Y是S或O，R如说明书中所定义。

6. 发明授权

US5395853A Anti-atherosclerotic diaryl compounds 失效
标题翻译：抗动脉粥样硬化二芳基化合物
公开(公告)号：US5395853A
公开(公告)日：1995-03-07
申请号：US157685
申请日：1993-11-24
申请人： William P. Jackson , Clifford J. Harris , Richard J. Arrowsmith , John G. Dann , Kevin J. O'Connor , Robert F. G. Booth
发明人： William P. Jackson , Clifford J. Harris , Richard J. Arrowsmith , John G. Dann , Kevin J. O'Connor , Robert F. G. Booth
IPC分类号： C07C233/07 , C07C233/11 , C07C271/44 , C07C275/24 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , A61K31/155 , A61K31/17 , C07C279/18
CPC分类号： C07C233/07 , C07C233/11 , C07C271/44 , C07C275/24 , C07C275/28 , C07C275/30 , C07C279/28 , C07C327/44 , C07C2101/14
摘要： The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.1-6 alkyl group optionally substituted by one or more independently selected polar groups; andring A is optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen;provided said compound of formula (I) is not N-{2-[(4-methyl-phenyl)methyl]phenyl}acetamide or .alpha.-(p-tolyl)-o-cresol carbanilate; and salts, solvates and physiologically functional derivatives thereof, processes for the preparation of these compounds, pharmaceutical formulations containing them and their use in medicine.
摘要翻译：本发明涉及式（I）的化合物：其中m为0或1; W是氢，C1-16直链，支链或环状烷基或C2-16直链，支链或环状烯基或炔基或Ph（CH2）n-，其中Ph是苯基，n是整数 0至2，苯基任选被一个或多个独立地选自卤素，羟基，硝基，C 1-4烷氧基和C 1-4烷基的一个或多个原子或基团取代，其中所述烷基中的一个或多个氢原子是任选的被卤素取代，或R1NHCO-，其中R1是氢或C1-6烷基，或R2CONH-，其中R2是氢或C1-6烷基; Y是 - （CH 2）q，其中q是1至3的整数，或-CH = CH-（E或Z）; Z是任选被一个或多个独立选择的极性基团取代的C 1-6烷基; 并且环A任选被一个或多个独立地选自卤素，羟基，硝基，C 1-4烷氧基和C 1-4烷基的原子或基团取代，其中所述烷基中的一个或多个氢原子任选被卤素取代; 所述式（I）化合物不是N- {2 - [（4-甲基 - 苯基）甲基]苯基}乙酰胺或α-（对甲苯基） - 邻甲酚氨基苯甲酸酯; 及其盐，溶剂合物及其生理功能衍生物，制备这些化合物的方法，含有它们的药物制剂及其在药物中的用途。

7. 发明授权

US5352831A Oligomeric cyanoguanidines 失效
标题翻译：低聚氰胍
公开(公告)号：US5352831A
公开(公告)日：1994-10-04
申请号：US914158
申请日：1992-07-14
申请人： Peter Flury , Martin Roth , Sameer H. Eldin
发明人： Peter Flury , Martin Roth , Sameer H. Eldin
IPC分类号： C07C279/28 , C08G18/02 , C08G59/40
CPC分类号： C07C279/28 , C08G18/025 , C08G59/4021
摘要： Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R.sup.1 and R.sup.2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in solvents suitable for the application of epoxy resins, and the cured products obtained therewith have a high glass transition temperature.
摘要翻译：式I的低聚氰基胍其中例如R1和R2各自为苯基，R为1,4-亚苯基，n为1至20的整数，为环氧树脂的合适的潜在硬化剂。它们易溶于适用于环氧树脂的溶剂中，由此获得的固化产物具有较高的玻璃化转变温度。

8. 发明授权

US5352796A Amino acids useful in making GnRH analogs 失效
标题翻译：用于制备GnRH类似物的氨基酸
公开(公告)号：US5352796A
公开(公告)日：1994-10-04
申请号：US78965
申请日：1993-06-17
申请人： Carl A. Hoeger , Jean E. F. Rivier , John S. Porter
发明人： Carl A. Hoeger , Jean E. F. Rivier , John S. Porter
IPC分类号： A61K38/04 , A61K38/00 , C07C277/08 , C07C279/18 , C07C279/24 , C07C279/28 , C07C313/30 , C07D249/14 , C07K1/00 , C07K7/02 , C07K7/06 , C07K7/23
CPC分类号： C07C279/24 , C07C277/08 , C07C279/28 , C07C313/30 , C07D249/14 , C07K1/006 , C07K7/02 , C07K7/23 , A61K38/00 , C07C2101/14 , Y02P20/55
摘要： Unnatural amino acids are provided which can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1,2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl; or the formula (b): ##STR3## where R.sub.11 is H or acyl and W is as defined in (a), and preferably R.sub.11 is H and W is ##STR4## Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.
摘要翻译：可以提供非天然氨基酸，其可以并入肽中，其抑制或促进垂体分泌促性腺激素并抑制性腺释放类固醇。这些非天然氨基酸可用于肽的合成并具有式（a）：其中W为（CH 2）n或 n为1至6的整数; j = 1,2或3，优选Y为N-CN，X为NH，R 2为烷基，改性烷基，烯基，炔基，芳基或甲基吡啶基; 或式（b）：其中R11为H或酰基，W为如（a）中所定义的式（b）：其中R 11为H且W为本文所公开的肽，其为存在十肽GnRH的类似物在3-，5-，6-和/或8-位的至少一个非天然氨基酸残基。

9. 发明授权

US5053427A Guanidino-substituted benzopyrans and their use as pharmaceuticals 失效
标题翻译：甘氨酸取代苯并噻唑及其作为药物的用途
公开(公告)号：US5053427A
公开(公告)日：1991-10-01
申请号：US407227
申请日：1989-09-14
申请人： Geoffrey Stemp , Gordon Burrell , David G. Smith
发明人： Geoffrey Stemp , Gordon Burrell , David G. Smith
IPC分类号： A61K31/155 , A61K31/35 , A61K31/352 , A61K31/435 , A61P1/00 , A61P9/00 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , A61P15/04 , C07C255/59 , C07C255/67 , C07C279/16 , C07C279/28 , C07C335/32 , C07D311/58 , C07D311/68 , C07D405/04 , C07D491/04 , C07D491/052
CPC分类号： C07D405/04 , C07C255/59 , C07C255/67 , C07C279/28 , C07C335/32 , C07D311/68 , C07D491/04 , C07C2102/08
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;either Y is N and R.sub.2 is hydrogen; orY is C-R.sub.1whereineither one of R.sub.1 and R.sub.2 is hydrogen and the other is nitro, cyano, halo, CF.sub.3, formyl, aldoxime, CF.sub.3 O, NO.sub.2 --CH.dbd.CH--, NC--CH.dbd.CH--; a group R.sub.x X-- wherein R.sub.x and C.sub.1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, halo, CF.sub.3 and cyano; and X is C.dbd.O, O.C.dbd.O, C.dbd.0.0, CHOH, SO, SO.sub.2, 0.SO, 0.SO.sub.2, CONH, 0.CONH, C.dbd.S, 0.C.dbd.S, C.dbd.S.0, CH.SH, SONH, SO.sub.2 NH, 0.SONH, 0.SO.sub.2 NH, CO--CH.dbd.CH, C.dbd.NHOH, C.dbd.NNH.sub.2 ; or a group R.sub.y R.sub.z NZ-- wherein R.sub.y and R.sub.z are independently hydrogen or C.sub.1-6 alkyl and Z is C.dbd.O, SO or SO.sub.2 ; orR.sub.1 is a C.sub.3-8 cycloalkyl group or a C.sub.1-6 alkyl group optionally substituted by a group which is hydroxy, C.sub.1-6 alkoxy, amino optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-7 alkanoylamino, C.sub.3-8 cycloalkyloxy or C.sub.3-8 cycloalkylamino; and R.sub.2 is hydrogen; orone of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C.sub.1-3 alkylcarbonyl, methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;either one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl; orR.sub.3 and R.sub.4 together are C.sub.2-5 polymethylene;either R.sub.5 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy; andR.sub.6 is hydrogen; orR.sub.5 and R.sub.6 together are a bond;either R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; andR.sub.8 is hydrogen or C.sub.1-6 alkyl; orR.sub.7 and R.sub.8 together are C.sub.2-4 polymethylene;R.sub.9 is CN, NO.sub.2, COR.sub.10 or SO.sub.2 R.sub.10 wherein R.sub.10 is C.sub.1-3 alkyl, NH.sub.2, NH(C.sub.1-3 alkyl), CF.sub.3 or phenyl optionally substituted as defined for R.sub.x ; andthe R.sub.8 N(NR.sub.9)NHR.sub.7 moiety is trans to the R.sub.5 group when R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.

10. 发明授权

US5021429A Pharmacologically active aminoalkylphenyl compounds and their use 失效
标题翻译：药理活性氨基烷基苯基化合物及其用途
公开(公告)号：US5021429A
公开(公告)日：1991-06-04
申请号：US944217
申请日：1986-12-22
申请人： Michael Martin-Smith
发明人： Michael Martin-Smith
IPC分类号： A61K31/135 , A61K31/17 , C07C275/10 , C07C279/08 , C07C279/28 , C07C279/36 , C07C335/08 , C07D209/48 , C07D295/096
CPC分类号： C07D209/48 , C07C255/00 , C07C275/10 , C07C279/08 , C07C279/28 , C07C279/36 , C07C335/08 , C07D295/096
摘要： Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.7 represents nitro, lower alkylsulphonyl or arylsulphonyl; m is an integer from 2 to 4 inclusive; n is zero, 1 or 2; and Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms. The compounds have therapeutic activity.
摘要翻译：这些化合物的通式为：其中R 1和R 2可以相同或不同，表示氢或低级烷基，环烷基，环烷基，芳烷基或低级烯基，或被氧原子或其中R 4表示氢或低级烷基的基团< 或R 1和R 2可以与它们所连接的氮原子一起形成可含有杂官能团-O-和R 3代表氢，低级烷基，烯基或烷氧基烷基的杂环; X表示-O - ， - S-或-CH 2 - 或其中R 5是氢或低级烷基; Y表示= S，= O，= NR6或= CHR7; 其中R 6表示氢，硝基，氰基，低级烷基，芳基，芳基磺酰基或低级烷基磺酰基; R7表示硝基，低级烷基磺酰基或芳基磺酰基; m为2〜4的整数， n为零，1或2; 并且Alk表示1至6个碳原子的直链或支链亚烷基链。该化合物具有治疗活性。

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