-
公开(公告)号：US20180099920A1
公开(公告)日：2018-04-12
申请号：US15736756
申请日：2016-06-15
申请人： NMD PHARMA APS
发明人： Thomas HOLM PEDERSEN , Martin BROCH-LIPS , Claus ELSBORG OLESEN , Marc LABELLE , Ole BÆKGAARD NIELSEN
IPC分类号： C07C59/135 , C07C229/22 , C07C233/48 , C07C311/06 , C07C229/18 , C07C323/52
CPC分类号： C07C59/135 , A61K31/192 , A61K31/216 , A61K31/44 , C07C229/18 , C07C229/22 , C07C233/48 , C07C311/06 , C07C323/52 , C07C2601/02 , C07C2601/04 , Y02A50/465
摘要： The present invention relates to compositions comprising compounds for use in treating, ameliorating and/or preventing neuromuscular disorders. The compounds as defined herein preferably inhibit the ClC-1 ion channel. The invention further relates to methods of treating, preventing and/or ameliorating neuromuscular disorders, by administering said composition to a person in need thereof.
-
22.发明申请NOVEL CARBOXYLIC ACID ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS 审中-公开新型羧酸类似物作为GLYCOGEN SYNTHASE ACTIVATORS公开(公告)号：US20110136792A1
公开(公告)日：2011-06-09
申请号：US12908199
申请日：2010-10-20
IPC分类号： A61K31/198 , C07C233/48 , C07D295/185 , C07C271/22 , C07C311/19 , C07D233/90 , C07D213/82 , C07D213/81 , C07D307/24 , C07D279/02 , A61K31/5377 , A61K31/27 , A61K31/4164 , A61K31/455 , A61K31/4458 , A61K31/341 , A61P3/00 , A61K31/54 , A61P3/10
CPC分类号： C07C233/47 , C07C229/14 , C07C233/48 , C07C233/51 , C07C233/63 , C07C233/83 , C07C235/12 , C07C271/22 , C07C311/06 , C07C311/14 , C07C311/19 , C07C2601/02 , C07C2601/04 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D275/02 , C07D277/56 , C07D279/02 , C07D295/215 , C07D307/24 , C07D417/06
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
-
公开(公告)号：US06972300B2
公开(公告)日：2005-12-06
申请号：US10623142
申请日：2003-07-18
IPC分类号： C07D295/20 , A61K9/00 , A61K9/08 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/197 , A61K31/198 , A61K31/40 , A61K31/44 , A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/12 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C53/126 , C07C53/134 , C07C229/08 , C07C229/10 , C07C229/42 , C07C231/12 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/62 , C07C235/64 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C239/06 , C07C239/08 , C07C259/06 , C07C271/22 , C07C303/22 , C07C303/40 , C07C309/59 , C07C311/19 , C07D207/34 , C07D207/416 , C07D213/75 , C07D213/81 , C07D295/215 , C07D317/68 , C07D333/38 , A61K31/195 , C07C229/00
CPC分类号： C07D333/38 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D213/81 , C07D295/215 , C07D317/68
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 活性剂可以是肽，例如rhGH。 提供口服，皮下，舌下和鼻内给药的给药方法，提供修饰的氨基酸化合物的制备方法。
-
公开(公告)号：US06960355B2
公开(公告)日：2005-11-01
申请号：US10005511
申请日：2001-11-07
IPC分类号： A01N37/00 , A61K9/00 , A61K9/16 , A61K9/48 , A61K38/00 , A61K38/20 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C229/42 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/69 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C235/82 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D209/48 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K9/14 , A61K9/20
CPC分类号： C07D209/48 , A61K9/0019 , A61K9/0043 , A61K9/0056 , A61K9/1617 , A61K9/4858 , A61K31/727 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/541 , C07C229/42 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/69 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C235/82 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30
摘要： Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 也提供给药和制备方法。
-
公开(公告)号：US5650386A
公开(公告)日：1997-07-22
申请号：US414654
申请日：1995-03-31
IPC分类号： C07D295/20 , A61K9/00 , A61K9/08 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/197 , A61K31/198 , A61K31/40 , A61K31/44 , A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/12 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/48 , C07C53/126 , C07C53/134 , C07C229/08 , C07C229/10 , C07C229/42 , C07C231/12 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/62 , C07C235/64 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C239/06 , C07C239/08 , C07C259/06 , C07C271/22 , C07C303/22 , C07C303/40 , C07C309/59 , C07C311/19 , C07D207/34 , C07D207/416 , C07D213/75 , C07D213/81 , C07D295/215 , C07D317/68 , C07D333/38 , A61K38/17 , A61K31/725 , C07C229/14
CPC分类号： C07D213/81 , A61K38/212 , A61K38/23 , A61K38/27 , A61K38/29 , A61K47/18 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/4803 , A61K9/0019 , A61K9/1617 , A61K9/4858 , C07C233/34 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C233/83 , C07C233/84 , C07C233/87 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/40 , C07C235/52 , C07C235/60 , C07C235/64 , C07C235/82 , C07C237/22 , C07C237/40 , C07C237/42 , C07C259/06 , C07C271/22 , C07C309/59 , C07C311/19 , C07D207/34 , C07D295/215 , C07D317/68 , C07D333/38 , A61K9/0043 , A61K9/0056 , C07C2101/14 , C07C2101/18 , C07C2103/74
摘要： Modified amino acid compounds useful for the delivery of active agents are provided. The amino acids, non-alpha-amino acids, have been modified by acylation on the amino group particularly with phenyl or cyclohexyl groups. These groups have a variety of substituents including but not limited to hydroxy, methyl, fluoro, chloro, and the like. The compounds of the invention can be combined with numerous active agents including but not limited to heparin, peptides, and parathyroid hormone, and can then be used for effective administration of the active agent. Administration can be, for example, oral or parenteral.
摘要翻译： 提供了可用于递送活性剂的改性氨基酸化合物。 氨基酸，非α-氨基酸已经通过氨基上的酰化，特别是用苯基或环己基进行改性。 这些基团具有多种取代基，包括但不限于羟基，甲基，氟，氯等。 本发明的化合物可以与许多活性剂组合，包括但不限于肝素，肽和甲状旁腺激素，然后可用于有效施用活性剂。 给药可以是例如口服或肠胃外。
-
公开(公告)号：US5266576A
公开(公告)日：1993-11-30
申请号：US833301
申请日：1992-02-10
IPC分类号： A61K31/195 , A61K31/198 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/435 , A61K31/675 , A61P31/12 , A61P31/16 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P37/04 , C07C233/48 , C07C233/51 , C07C233/87 , C07C235/06 , C07C235/12 , C07C323/60 , C07D207/16 , C07D207/26 , C07D207/277 , C07D209/26 , C07D209/44 , C07D211/60 , C07D211/78 , C07D217/22 , C07D217/26 , C07D233/54 , C07D233/64 , C07D317/24 , C07D453/06 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/14 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/48 , A61K31/44
CPC分类号： C07D207/277 , C07C233/48 , C07C233/51 , C07C233/87 , C07C235/12 , C07C323/60 , C07D209/26 , C07D209/44 , C07D211/60 , C07D217/26 , C07D233/64 , C07D317/24 , C07D453/06 , C07D471/04 , C07F9/3808 , C07F9/3882 , C07F9/4006 , C07F9/4021 , C07F9/4056 , C07F9/4465 , C07F9/4816 , C07C2101/14
摘要： The invention relates to a compound of formula (I): ##STR1## which can be used as N-myristoyltransferase inhibitors, in which R.sub.1 represents hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl, (C.sub.3 -C.sub.7) cycloalkyl methyl, substituted or unsubstituted (imidazolyl-2-yl)methyl, substituted or unsubstituted (indol-3-yl)methyl or (1-azaindolizin-2-yl)methyl,R.sub.2, R.sub.3, which are identical or different, represent hydrogen or (Cl-C6) alkyl,or when R.sub.1 represents hydrogen, R.sub.2 and R.sub.3 form with the carbon and nitrogen atoms to which they are attached, a mono-, bi- or tricyclic heterocycle,X represents --CO--, --SO.sub.2 --, --PO(OH)--,Y represents --COR.sub.5 or --POR.sub.6 R.sub.6 ',R.sub.4 represents substituted or unsubstituted, linear or branched (C.sub.6 -C.sub.21) alkyl in which, depending on the individual case, one or more methylene may be replaced by oxygen or sulfur or by a p-phenylene ring,their isomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.
摘要翻译： 本发明涉及可用作N-肉豆蔻酰转移酶抑制剂的式（I）化合物：其中R1表示氢，取代或未取代的（C1-C6）烷基，取代或未取代的苯基，（ C 3 -C 7）环烷基甲基，取代或未取代的（咪唑基-2-基）甲基，取代或未取代的（吲哚-3-基）甲基或（1-氮杂吲哚哩啶-2-基）甲基，R 2，R 3，其相同或 不同的，代表氢或（C 1 -C 6）烷基，或当R 1表示氢时，R 2和R 3与它们所连接的碳原子和氮原子一起形成单，双或三环杂环，X表示-CO-， -SO 2 - ， - PO（OH） - ，Y表示-COR 5或-POR 6 R 6'，R 4表示取代或未取代的直链或支链（C6-C21）烷基，其中根据个别情况，一个或多个亚甲基可以 由氧或硫或对亚苯基环，其异构体，非对映异构体和差向异构体代替，以及它们与药学上的加成盐 可溶性酸或碱。
-
27.发明授权Use of N-myristoyl-(S)-phenylalanine for the treatment of diseases involving myristoylation 失效使用N-马来酰基 - （S） - 苯乙胺治疗涉及脑血管病的疾病
公开(公告)号：US5164414A
公开(公告)日：1992-11-17
申请号：US645124
申请日：1991-01-24
IPC分类号： A61K31/195 , A61K31/198 , A61K31/20 , A61K38/00 , A61P31/12 , A61P31/18 , A61P35/00 , C07C233/48 , C12N9/99
CPC分类号： A61K38/005 , A61K31/195 , A61K31/20
摘要： The invention relates to the use of N-myristoyl-(S)-phenylalanine in the treatment of diseases involving myristoylation such as cancer or AIDS.Medicinal products including N-myristoyl-(S)-phenylalanine which are effective for such purpose.
摘要翻译： 本发明涉及N-肉豆蔻酰 - （S） - 苯丙氨酸在治疗涉及肉豆蔻酰化疾病如癌症或艾滋病的疾病中的应用。 药用产品，包括N-肉豆蔻酰 - （S） - 苯丙氨酸，对此目的有效。
-
28.发明授权Methods and compositions involving polyhydroxylated polyiodo non-ionic contrast media 失效涉及多羟基化多碘非离子造影剂的方法和组合物
公开(公告)号：US4584401A
公开(公告)日：1986-04-22
申请号：US544308
申请日：1983-10-20
IPC分类号： C07C233/65 , A61K49/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/08 , C07C233/00 , C07C233/48 , C07C237/30 , C07C237/46 , C07C103/24 , C07C103/76
CPC分类号： A61K49/04 , C07C233/00 , Y02P20/55
摘要： Methods and compositions are provided for preparing polyhydroxylated polyiodo non-ionic contrast media. Particularly, substituted polyiodobenzamides are prepared, wherein the benzamide nitrogen is polyhydroxylated by allylic substitution on the nitrogen and oxidation of the olefinic group to provide for polyhydroxyl substitution. Amino substituents on the benzamide may be polyhydroxylated by allyl substitution or acryl substitution. All of the olefins may be oxidized simultaneously to glycols to provide for water soluble relatively non-toxic contrast media in efficient economical processes. Alternatively, the same compounds can be synthesized by alkylating N-acylbenzamide with polyacetoxyalkyl or dioxolanylalkyl halides, followed by removal of the protective groups.
摘要翻译： 提供了用于制备多羟基化多碘非离子造影剂的方法和组合物。 特别地，制备了取代的聚碘苯甲酰胺，其中苯甲酰胺氮通过在氮上的烯丙取代和烯属基团的氧化进行多羟基化以提供多羟基取代。 苯甲酰胺上的氨基取代基可以通过烯丙基取代或丙烯基取代被多羟基化。 所有烯烃可以同时氧化成二醇，以在有效的经济过程中提供水溶性相对无毒的造影剂。 或者，可以通过用聚乙酰氧基烷基或二氧戊环烷基卤化物烷基化N-酰基苯甲酰胺，然后除去保护基来合成相同的化合物。
-
公开(公告)号：US09796660B2
公开(公告)日：2017-10-24
申请号：US15174306
申请日：2016-06-06
发明人： Samuel Helmer Gellman , Li Guo , Michael Giuliano
IPC分类号： A61K38/00 , C07C205/44 , C07C205/55 , C07C233/48 , C07C237/24 , C07C271/24 , C07D211/56 , C07D211/60 , C07K5/02 , C07C201/12 , C07C269/00 , C07C271/66 , C07K5/065 , C07K5/107 , C07K7/06
CPC分类号： C07C205/44 , C07C201/12 , C07C205/55 , C07C233/48 , C07C237/24 , C07C269/00 , C07C271/24 , C07C271/66 , C07C2601/08 , C07C2601/14 , C07D211/56 , C07D211/60 , C07K5/0205 , C07K5/06078 , C07K5/1016 , C07K7/06
摘要： The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.).The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.
-
公开(公告)号：US08791260B2
公开(公告)日：2014-07-29
申请号：US14047043
申请日：2013-10-07
申请人： Joerg Kley , Daniel Haerle , Guenter Linz , Sandra Stehle
发明人： Joerg Kley , Daniel Haerle , Guenter Linz , Sandra Stehle
IPC分类号： C07D403/12 , C07D241/06 , C07D241/40 , C07D241/44 , C07C233/11 , C07C233/48 , C07D241/28 , C07C231/14 , C07D233/48
CPC分类号： C07C231/14 , C07C231/00 , C07C231/10 , C07C233/11 , C07C235/28 , C07D233/48 , C07D241/06 , C07D241/28 , C07D241/40 , C07D241/44 , C07D261/08 , C07D403/12
摘要： The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译： 本发明涉及一种制备通式（I）化合物及其盐的新方法，特别是其与无机或有机酸和碱的生理上可接受的盐，其具有有价值的药理学性质，特别是对上皮的抑制作用 钠通道，其用于治疗疾病，特别是肺和气道疾病的用途。
-
-
-
-
-
-
-
-
-
搜索结果
38 条记录 (耗时 0.04 秒)
