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1. 发明申请

US20220009883A1 THIOAMIDE-CONTAINING COMPOSITIONS AND METHODS OF USE THEREOF 有权
公开(公告)号：US20220009883A1
公开(公告)日：2022-01-13
申请号：US17293671
申请日：2019-11-13
申请人： NORIA THERAPEUTICS, INC.
发明人： Stephen DIMAGNO
IPC分类号： C07C327/44 , A61K47/54 , A61K47/62
摘要： Provided herein are compositions and methods for preparing albumin-targeting moieties that feature a thioamide linkage. Methods to use the albumin targeting molecules to generate drugs with improved in vivo pharmacodynamics and biodistribution are described. Therapeutic compounds incorporating these thioamide linked albumin-targeting moieties are disclosed.

2. 发明授权

US09051240B2 Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators 有权
标题翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物及其作为钠和/或钙通道调节剂的用途
公开(公告)号：US09051240B2
公开(公告)日：2015-06-09
申请号：US13794555
申请日：2013-03-11
申请人： Newron Pharmaceuticals S.P.A.
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/165 , C07C237/08 , C07C233/05 , C07C233/65 , A61P25/00 , C07C237/20 , C07C317/28 , C07C323/25 , C07C327/42 , C07D295/182 , A61K31/381 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07D207/16 , C07D333/20 , C07C321/26 , C07C327/44
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
摘要翻译：取代的2- [2-（苯基）乙基氨基]烷酰胺衍生物，其药学上可接受的盐和含有它们的药物组合物可用作用于预防，减轻和治愈其中上述机制发挥病理作用的病症的钠和/或钙通道调节剂。这些化合物可能特别可用于预防，减轻和治愈例如神经，认知，精神，炎症，泌尿生殖和胃肠道疾病。

3. 发明申请

US20130231478A1 Novel Intermediate for Preparing Tapentadol or Analogues Thereof 有权
标题翻译：制备他喷他多或其类似物的新型中间体
公开(公告)号：US20130231478A1
公开(公告)日：2013-09-05
申请号：US13884810
申请日：2011-07-29
申请人： Ziao Xu , Yuanhai Zhao , Degang Li , Xiaoxiang Li
发明人： Ziao Xu , Yuanhai Zhao , Degang Li , Xiaoxiang Li
IPC分类号： C07D295/192 , C07C69/734 , C07C327/28 , C07C69/732 , C07C327/44 , C07C235/34 , C07C51/60 , C07C255/36 , C07C253/14 , C07D211/16 , C07C67/08 , C07C231/02 , C07C233/11 , C07C237/20 , C07C255/37 , C07C213/02 , C07C59/48
CPC分类号： C07D295/192 , C07C41/22 , C07C41/26 , C07C51/367 , C07C51/60 , C07C59/48 , C07C59/64 , C07C67/08 , C07C69/732 , C07C69/734 , C07C213/00 , C07C213/02 , C07C213/10 , C07C231/02 , C07C233/11 , C07C235/34 , C07C237/20 , C07C253/14 , C07C255/36 , C07C255/37 , C07C327/22 , C07C327/28 , C07C327/44 , C07D211/16 , C07D295/185 , C07C59/60 , C07C43/23 , C07C43/225 , C07C215/54
摘要： The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
摘要翻译：本发明公开了一种制备他喷他多及其类似物的新型中间体，其结构式如式I或II所示，其定义为说明书。本发明进一步公开了一种制备新型中间体的方法以及用于制备他喷他多和其类似物的中间体。本发明可显着提高他喷他多的产品产量和质量，降低生产成本，简化生产工艺。制备工艺环保，更适合工业生产要求。

4. 发明授权

US06890932B2 Anthranilic acid derivative 失效
标题翻译：邻氨基苯甲酸衍生物
公开(公告)号：US06890932B2
公开(公告)日：2005-05-10
申请号：US10355125
申请日：2003-01-31
申请人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
发明人： Naoki Tsuchiya , Susumu Takeuchi , Takumi Takeyasu , Naoki Hase , Takao Yamori , Takashi Tsuruo
IPC分类号： C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07D207/08 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/092 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12 , A61K31/435 , A01N43/40 , C07D213/00 , C07D213/63
CPC分类号： C07D207/08 , C07C235/38 , C07C235/56 , C07C271/16 , C07C271/26 , C07C307/08 , C07C311/07 , C07C311/20 , C07C311/29 , C07C323/25 , C07C323/30 , C07C323/41 , C07C323/42 , C07C323/43 , C07C323/60 , C07C323/62 , C07C327/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/28 , C07D211/02 , C07D211/46 , C07D213/30 , C07D213/64 , C07D213/643 , C07D213/70 , C07D213/82 , C07D213/89 , C07D295/088 , C07D295/185 , C07D307/42 , C07D307/58 , C07D309/10 , C07D405/12
摘要： The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要翻译：本发明涉及由下式（1）或下式（2）表示的邻氨基苯甲酸衍生物或其药理学上允许的盐或溶剂合物。

5. 发明授权

US6100263A Phenylacetic acid derivatives, preparation thereof and intermediates therefor, and compositions containing them 失效
标题翻译：苯乙酸衍生物，其制备方法及其中间体，以及含有它们的组合物
公开(公告)号：US6100263A
公开(公告)日：2000-08-08
申请号：US334385
申请日：1999-06-16
申请人： Herbert Bayer , Hubert Sauter , Ruth Muller , Wassilios Grammenos , Albrecht Harreus , Reinhard Kirstgen , Franz Rohl , Eberhard Ammermann , Gisela Lorenz
发明人： Herbert Bayer , Hubert Sauter , Ruth Muller , Wassilios Grammenos , Albrecht Harreus , Reinhard Kirstgen , Franz Rohl , Eberhard Ammermann , Gisela Lorenz
IPC分类号： C07D249/08 , A01N37/50 , A01N37/52 , A01N43/06 , A01N43/36 , A01N43/40 , A01N43/54 , A01N43/80 , A01N43/82 , A01N43/824 , A01P3/00 , A01P7/04 , C07C251/38 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/56 , C07C251/58 , C07C255/11 , C07C327/44 , C07C327/48 , C07C327/58 , C07D207/32 , C07D207/333 , C07D207/36 , C07D213/30 , C07D213/53 , C07D213/62 , C07D213/64 , C07D213/79 , C07D233/64 , C07D237/14 , C07D239/34 , C07D239/46 , C07D241/18 , C07D261/08 , C07D261/10 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/10 , C07D277/24 , C07D307/42 , C07D333/32 , C07D521/00 , C07D213/56 , C07D239/26
CPC分类号： C07D207/333 , A01N37/50 , A01N37/52 , A01N43/06 , A01N43/36 , A01N43/40 , A01N43/54 , A01N43/80 , A01N43/82 , C07C251/58 , C07C255/11 , C07C327/48 , C07C327/58 , C07D213/53 , C07D213/64 , C07D239/34 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D307/42
摘要： Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;and their salts, processes and intermediates for their preparation, and their use are described.
摘要翻译：式I的苯乙酸衍生物，其中取代基和指数具有以下含义：X是氧或硫; R是氢或烷基; R1是氢或烷基; R2是氰基，硝基，三氟甲基，卤素，烷基或烷氧基; m为0,1或2，如果m为2，则R2基团可能不同; 并描述了它们的盐，其制备方法和中间体及其用途。

6. 发明授权

US5723470A Fluoroalkenyl compounds and their use as pest control agents 失效
公开(公告)号：US5723470A
公开(公告)日：1998-03-03
申请号：US599827
申请日：1996-02-12
申请人： Dennis Paul Phillion , Peter Gerrard Ruminski , Gopichand Yalamanchili
发明人： Dennis Paul Phillion , Peter Gerrard Ruminski , Gopichand Yalamanchili
IPC分类号： C07D249/08 , A01N35/04 , A01N37/22 , A01N37/28 , A01N37/34 , A01N37/46 , A01N41/04 , A01N41/06 , A01N41/10 , A01N43/54 , A01N43/56 , A01N43/653 , A01N47/02 , A01N47/28 , A01N47/34 , A01N47/44 , A01N55/00 , A01N57/18 , A01N57/20 , C07C45/00 , C07C49/80 , C07C53/21 , C07C53/50 , C07C57/52 , C07C233/09 , C07C255/29 , C07C259/06 , C07C281/06 , C07C309/15 , C07C309/51 , C07C311/51 , C07C327/44 , C07D239/38 , C07D239/52 , C07D239/54 , C07D239/545 , C07D239/60 , C07D249/10 , C07D295/10 , C07D521/00 , C07F7/08 , C07F7/10 , C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , A61K31/505 , A61K31/41 , C07D239/47
CPC分类号： C07D239/545 , A01N35/04 , A01N37/22 , A01N37/28 , A01N37/46 , A01N41/04 , A01N41/06 , A01N43/54 , A01N43/56 , A01N43/653 , A01N47/02 , A01N47/34 , A01N55/00 , A01N57/20 , C07C233/09 , C07C255/29 , C07C259/06 , C07C281/06 , C07C309/15 , C07C309/51 , C07C311/51 , C07C45/004 , C07C49/80 , C07C53/21 , C07C53/50 , C07C57/52 , C07D231/12 , C07D233/56 , C07D239/38 , C07D239/52 , C07D249/08 , C07F7/0818 , C07F9/302 , C07F9/3808 , C07F9/3826 , C07F9/4015
摘要： Novel 3,4,4-trifluorobutenoic acid derivatives of the formula ##STR1## wherein Q is --(C.dbd.W)--R.sub.2 wherein W is O or S, and R.sub.2 is an aliphatic or aromatic group when W.dbd.O; --OR.sub.50 ; --SR.sub.50 ; or --NR.sub.50 R.sub.60 wherein R.sub.60 is hydrogen or R.sub.50 ; NR.sub.7 R.sub.8 ; a heterocyclic group; phenyl substituted by alkyl; or any agronomically acceptable salt thereof having usefulness as nematocides, insecticides and acaricides.

7. 发明授权

US5681835A Non-steroidal ligands for the estrogen receptor 失效
标题翻译：雌激素受体的非甾体配体
公开(公告)号：US5681835A
公开(公告)日：1997-10-28
申请号：US232910
申请日：1994-04-25
申请人： Timothy Mark Willson
发明人： Timothy Mark Willson
IPC分类号： C07D295/08 , A61K31/135 , A61K31/137 , A61K31/165 , A61K31/215 , A61K31/275 , A61K31/41 , A61K31/4245 , A61K31/5375 , A61K31/5377 , A61P9/00 , A61P19/02 , A61P19/10 , A61P35/00 , C07C20060101 , C07C33/28 , C07C45/45 , C07C45/59 , C07C47/548 , C07C49/796 , C07C57/42 , C07C57/48 , C07C69/618 , C07C211/28 , C07C233/10 , C07C233/11 , C07C233/22 , C07C233/40 , C07C233/44 , C07C233/58 , C07C251/40 , C07C255/07 , C07C255/34 , C07C327/44 , C07D271/06 , C07D295/185 , C07F9/40 , A61K31/42 , A61K31/535 , C07D265/30
CPC分类号： C07D271/06 , A61K31/135 , A61K31/165 , C07C211/28 , C07C233/11 , C07C233/22 , C07C233/40 , C07C233/58 , C07C251/40 , C07C255/34 , C07C327/44 , C07C327/48 , C07C33/28 , C07C45/45 , C07C45/59 , C07C47/548 , C07C49/796 , C07C57/42 , C07C57/48 , C07C69/618 , C07D295/185 , C07F9/4006 , C07B2200/07 , C07C2101/02 , C07C2101/14
摘要： Prescribed herein are novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.
摘要翻译：本文规定了具有组织依赖性雌激素和抗雌激素活性的雌激素受体的新型非甾体配体以及其制备方法及其在治疗各种疾病状态中的应用。

8. 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。

9. 发明授权

US5332833A .beta.-oxo-.beta.-benzenepropanethioamide compounds 失效
标题翻译： β-氧代-β-苯丙烷硫代酰胺化合物
公开(公告)号：US5332833A
公开(公告)日：1994-07-26
申请号：US996404
申请日：1992-12-23
申请人： Tetsuo Sekiya , Mikio Tsutsui , Tetsuro Shimpuku , Tatsuo Nagano , Junko Hayashi , Asami Seino
发明人： Tetsuo Sekiya , Mikio Tsutsui , Tetsuro Shimpuku , Tatsuo Nagano , Junko Hayashi , Asami Seino
IPC分类号： A61K31/16 , A61K31/18 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/496 , A61K31/50 , A61K31/505 , A61P1/00 , A61P9/08 , A61P9/12 , A61P11/00 , A61P11/08 , A61P29/00 , C07C327/42 , C07C327/44 , C07C327/46 , C07D207/327 , C07D213/59 , C07D231/12 , C07D233/54 , C07D233/58 , C07D233/60 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90 , C07D237/08 , C07D263/32 , C07D277/20 , C07D277/30 , C07C327/38 , A61K31/165 , C07C327/48 , C07D233/96
CPC分类号： C07C327/46 , C07C327/44 , C07C2101/02 , C07C2101/04 , C07C2101/08
摘要： The .beta.-oxo-.beta.-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome, and enteritis through pharmacological actions including blood vessel dilation, bronchial tract dilation, relaxation of gastrointestinal tract smooth muscle, and the like. The present invention also includes a pharmaceutical composition containing, as the active ingredient, the compound of the present invention and a method for producing the same.
摘要翻译：本发明的β-氧代-β-苯丙烷硫代酰胺衍生物具有钾通道开放作用，可用于治疗高血压，哮喘，过敏性结肠综合征和肠炎，包括血管扩张，支气管扩张，胃肠道松弛等药理作用平滑肌等。本发明还包括含有本发明化合物作为有效成分的药物组合物及其制造方法。

10. 发明授权

US5312964A Process and intermediates 失效
标题翻译：工艺和中间体
公开(公告)号：US5312964A
公开(公告)日：1994-05-17
申请号：US68251
申请日：1993-05-27
申请人： Didier Babin , Neerja Bhatnagar , Francis Brion , Colette Colladant
发明人： Didier Babin , Neerja Bhatnagar , Francis Brion , Colette Colladant
IPC分类号： A01N53/10 , A01N53/02 , A01N53/04 , A01N53/06 , A01P7/02 , A01P7/04 , C07B41/12 , C07C67/00 , C07C67/14 , C07C67/307 , C07C67/313 , C07C69/743 , C07C69/747 , C07C69/757 , C07C235/06 , C07C253/30 , C07C255/39 , C07C323/19 , C07C327/44 , C07D209/48 , C07D209/49 , C07D307/28 , C07D307/45 , C07C121/75
CPC分类号： C07D209/48 , C07C255/39 , C07C67/307 , C07C67/313 , C07C69/743
摘要： A novel process for the preparation of isomers or mixtures of isomers of compounds of the formula ##STR1## and novel intermediates therefore.
摘要翻译：用于制备式的化合物的异构体或异构体的混合物的新方法

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