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公开(公告)号:US20180002724A1
公开(公告)日:2018-01-04
申请号:US15707740
申请日:2017-09-18
发明人: Joel Jessee , Gulilat Gebeyehu
IPC分类号: C12N15/88 , A61K31/195 , A61K31/713 , C07C217/08 , C07D233/64 , A61K9/127 , C07C237/10 , C07C237/12 , C12N15/113
CPC分类号: C12N15/88 , A61K9/1272 , A61K31/195 , A61K31/713 , C07C217/08 , C07C237/10 , C07C237/12 , C07D233/64 , C12N15/1137 , C12N2310/14 , C12N2310/3515 , C12N2320/32
摘要: New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes.
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公开(公告)号:US09796666B2
公开(公告)日:2017-10-24
申请号:US14385178
申请日:2013-03-11
申请人: Merck Patent GmbH
发明人: Michael Wilhelm Platscher , Raymond Behrendt , Viola Groehn , Simone Rachel Hoertner , Marco Silvio Passafaro , Finn Bauer
IPC分类号: C07C237/30 , C07C271/22 , C07C237/08 , C07C237/10 , A61K9/127 , C07C59/185 , C07C237/06 , C07C237/22
CPC分类号: C07C237/30 , A61K9/1272 , C07C59/185 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/22 , C07C271/22 , C07C2603/18 , Y02P20/55
摘要: The present invention is directed to a new class of lipids, more specifically ether-lipids having a polar headgroup, as well as vesicles comprising these lipids, methods of their preparation as well as their uses in medical applications, wherein the ether-lipids are represented by general formula I
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公开(公告)号:US20170144969A1
公开(公告)日:2017-05-25
申请号:US15125214
申请日:2015-03-13
IPC分类号: C07D209/18 , C07C237/10 , A61K31/16 , A61K31/404 , A61K31/40 , A61K31/165 , C07C237/20 , C07D207/16
CPC分类号: C07D209/18 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/404 , A61K47/543 , C07C237/10 , C07C237/20 , C07D207/16 , Y02A50/473
摘要: The present disclosure relates to polyamine conjugates, its isomers, prodrugs and pharmaceutically acceptable salts thereof. The present disclosure also relates to process of preparation of polyamine conjugates, its stereoisomers, prodrugs, pharmaceutically acceptable salts thereof, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases mediated by microbes.
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公开(公告)号:US09505707B2
公开(公告)日:2016-11-29
申请号:US13326910
申请日:2011-12-15
IPC分类号: C07C229/26 , C07C237/10 , C07C237/06 , C10L3/10 , C10L10/18
CPC分类号: C07C237/06 , C10L3/107 , C10L10/18 , C10L2200/0259 , C10L2200/029 , C10L2230/14
摘要: Disclosed and claimed is a composition and method of inhibiting the formation of hydrate agglomerates in a fluid comprising water, gas, and optionally liquid hydrocarbon. The composition comprises the following formula and the method comprises adding to the fluid an effective anti-agglomerant amount of any of the following formula and optionally salts thereof. R1, R2, and R3 are each independently CnH2n+1 or benzyl. R4 is C4-C20 alkyl or alkenyl. n is an integer from 0 to 10. X− is a counterion.
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公开(公告)号:US20130035296A1
公开(公告)日:2013-02-07
申请号:US13505625
申请日:2010-11-02
IPC分类号: C07C237/20 , A61K31/16 , C07C237/14 , A61K31/165 , A61P35/00 , A61K38/08 , A61K31/495 , C07D241/04 , A61P31/04 , A61P35/04 , C07C237/10 , C07K7/06
CPC分类号: C07K5/0202 , A61K38/00 , C07C237/20 , C07C2601/14 , C07D209/20 , C07D295/185 , C07K7/02
摘要: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
摘要翻译: 本发明提供具有至少+2的净正电荷并掺入二取代的bgr的肽,拟肽或氨基酸衍生物。 氨基酸,“bgr”中的每个取代基 氨基酸可以相同或不同,包含至少(7)个非氢原子,是亲脂性的并且具有至少一个环状基团,取代基团中的一个或多个环状基团可以连接或稠合至一个或多个 在另一个取代基中的环状基团,其中环状基团以这种方式融合,两个取代基团的非氢原子的合并总数至少为(12),用作细胞溶解治疗剂; 以及这些分子的非治疗用途和来自该定义内的某些定义的新化合物。
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公开(公告)号:US20120238747A1
公开(公告)日:2012-09-20
申请号:US13420091
申请日:2012-03-14
申请人: Yongliang CHU , Malek Masoud , Gulilat Gebeyehu
发明人: Yongliang CHU , Malek Masoud , Gulilat Gebeyehu
IPC分类号: C07C211/63 , C07D273/08 , C07C215/18 , C07C237/10 , C07J1/00
CPC分类号: A61K47/48046 , A61K9/16 , A61K31/14 , A61K38/28 , A61K38/40 , A61K47/543 , C07C211/21 , C07C211/63 , C07C211/64 , C07C229/26 , C07D209/48 , C07D241/12 , C12N15/88 , Y10S435/81
摘要: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L′-X2—Z or —Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and wherein at least one of R1, R3, R4 and R6 is a straight chain or branched, cyclic, alkyl, alkenyl, alkynyl or aryl group; and anyone of R1, R3, R4 and/or R6 may optionally be covalently linked with each other, with Y or with L when L is C or CH to form a cyclic moiety; Z is selected from the group consisting of amine, spermiyl, carboxyspermiyl, guanidyl, spermidinyl, putricinyl, diaminoalkyl, pyridyl, piperidinyl, pyrrolidinyl, polyamine, amino acid, peptide, and protein; X1 and X2, independently of one another, are selected from the group consisting of NH, O, S, alkylene, and arylene; U is selected from the group consisting of alkylene, alkenylene, alkynylene, arylene, alkylene ether, and polyether; D is Q or a bond; A1 and A2, independently of one another, are selected from the group consisting of CH2O, CH2S, CH2NH, C(O), C{NH), C(S) and (CH2)t; X is a physiologically acceptable anion; m, n, r, s, u, v, w and y are 0 or 1, with the proviso that when both m and n are 0 at least one of r, s, u and y is other than 0; i, j, k, l, p and are integers from 0 to about 100; q is an integer from 1 to about 1000; and a is the number of positive charge divided by the valence of the anion.
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17.
公开(公告)号:US20120027844A1
公开(公告)日:2012-02-02
申请号:US13148857
申请日:2010-02-09
IPC分类号: A61K31/16 , C07C231/08 , C07C211/27 , C07C209/60 , C07C251/24 , C07C249/02 , C07C233/18 , C07C237/10 , C07C237/20 , A61K9/127 , A61K31/133 , A61K31/137 , A61K31/165 , A61P35/00 , A61P35/02 , C07C233/60
CPC分类号: C07C233/60 , C07C215/24 , C07C233/21 , C07C237/06 , C07C251/24
摘要: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
摘要翻译: 本文公开了化合物及其合成。 还描述了包含化合物的组合物和药物组合物,并且包括还包含脂质体的组合物。 还描述了用于治疗动物中癌症的方法,包括给予化合物或包含化合物的组合物。
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公开(公告)号:US20050260597A1
公开(公告)日:2005-11-24
申请号:US10629522
申请日:2003-07-28
申请人: Yongliang Chu , Malek Masoud , Gulilat Gebeyehu
发明人: Yongliang Chu , Malek Masoud , Gulilat Gebeyehu
IPC分类号: C12N15/09 , A61K9/127 , A61K31/14 , A61K47/16 , A61K47/18 , A61K47/22 , C07C211/21 , C07C211/63 , C07C211/64 , C07C215/18 , C07C217/08 , C07C229/26 , C07C237/10 , C07C279/08 , C07D211/26 , C07D213/38 , C07D241/12 , C07D273/08 , C07D291/02 , C12N5/10 , C12Q1/68 , C07F9/06 , C07F9/28
CPC分类号: A61K47/48046 , A61K9/16 , A61K31/14 , A61K38/28 , A61K38/40 , A61K47/543 , C07C211/21 , C07C211/63 , C07C211/64 , C07C229/26 , C07D209/48 , C07D241/12 , C12N15/88 , Y10S435/81
摘要: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L′-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and wherein at least one of R1, R3, R4 and R6 is a straight chain or branched, cyclic, alkyl, alkenyl, alkynyl or aryl group; and anyone of R1, R3, R4 and/or R6 may optionally be covalently linked with each other, with Y or with L when L is C or CH to form a cyclic moiety; Z is selected from the group consisting of amine, spermiyl, carboxyspermiyl, guanidyl, spermidinyl, putricinyl, diaminoalkyl, pyridyl, piperidinyl, pyrrolidinyl, polyamine, amino acid, peptide, and protein; X1 and X2, independently of one another, are selected from the group consisting of NH, O, S, alkylene, and arylene; L′ is selected from the group consisting of alkylene, alkenylene, alkynylene, arylene, alkylene ether, and polyether; D is Q or a bond; A1 and A2, independently of one another, are selected from the group consisting of CH2O, CH2S, CH2NH, C(O), C{NH), C(S) and (CH2)t; X is a physiologically acceptable anion; m, n, r, s, u, v, w and y are 0 or 1, with the proviso that when both m and n are 0 at least one of r, s, u and y is other than 0; i, j, k, l, p and are integers from 0 to about 100; q is an integer from 1 to about 1000; and a is the number of positive charge divided by the valence of the anion.
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19.
公开(公告)号:US06962934B2
公开(公告)日:2005-11-08
申请号:US10337075
申请日:2003-01-06
IPC分类号: C12N9/99 , A61K31/166 , A61K38/00 , A61P25/16 , A61P25/28 , C07C237/06 , C07C237/10 , C07K1/08 , C07K5/06 , C07K5/062 , C07K7/06 , C07D43/02 , A61K31/44
CPC分类号: C07K7/06 , A61K38/00 , C07C237/06 , C07K5/06026 , C07K5/06191
摘要: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要翻译: 本发明涉及式(I)化合物:可用于治疗阿尔茨海默氏病和其他类似疾病。 这些化合物包括β-分泌酶的抑制剂,其可用于治疗阿尔茨海默病和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。
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20.
公开(公告)号:US06958352B2
公开(公告)日:2005-10-25
申请号:US10364292
申请日:2003-02-10
IPC分类号: C07D295/18 , A61K31/135 , A61K31/136 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/216 , A61K31/22 , A61K31/223 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/417 , A61K31/4184 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/5375 , A61K45/00 , A61P3/10 , A61P7/12 , A61P43/00 , C07C45/46 , C07C45/67 , C07C205/56 , C07C211/29 , C07C229/14 , C07C229/34 , C07C233/11 , C07C237/04 , C07C237/10 , C07C237/14 , C07C317/44 , C07C323/29 , C07C323/40 , C07C323/41 , C07C323/42 , C07C323/44 , C07C323/49 , C07C323/52 , C07C323/60 , C07C335/18 , C07D207/32 , C07D207/335 , C07D211/20 , C07D211/24 , C07D211/96 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/80 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/20 , C07D233/54 , C07D233/61 , C07D235/06 , C07D271/06 , C07D277/28 , C07D277/64 , C07D295/185 , C07D317/68 , C07D333/20 , C07D413/12 , C07D211/06
CPC分类号: C07D207/335 , C07C45/46 , C07C45/673 , C07C205/56 , C07C211/29 , C07C229/34 , C07C233/11 , C07C237/10 , C07C237/14 , C07C317/44 , C07C323/29 , C07C323/40 , C07C323/41 , C07C323/42 , C07C323/44 , C07C323/49 , C07C323/52 , C07C323/60 , C07C335/18 , C07C2601/02 , C07C2601/14 , C07D211/24 , C07D211/96 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/20 , C07D233/64 , C07D271/06 , C07D277/28 , C07D277/64 , C07D295/185 , C07D413/12 , C07C49/83
摘要: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein W1, W2, X, R1, R2, R3, R4, m and n are defined herein.
摘要翻译: 用于改变胰岛素分泌的化合物,组合物和方法,特别是在治疗具有或怀疑患有糖尿病风险的受试者的情况下。 该化合物具有以下结构(I):包括其立体异构体,前药和药学上可接受的盐,其中W 1,W 2,X,R 1, R 2,R 2,R 3,R 4,m和n在本文中定义。
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