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2. 发明申请

US20170349532A1 CATIONIC LIPID 审中-公开
公开(公告)号：US20170349532A1
公开(公告)日：2017-12-07
申请号：US15680578
申请日：2017-08-18
申请人： Kyowa Hakko Kirin Co., Ltd.
发明人： Takeshi KUBOYAMA , Tomohiro ERA , Tomoyuki NAOI , Nobuhiro YAGI
IPC分类号： C07C217/06 , A61K9/00 , C07D491/04 , C07D401/04 , C07D317/28 , C07D295/08 , C07D207/12 , C07D207/08 , C07C271/16 , C07C237/08 , C07C237/06 , C07C219/08 , C07C217/08 , A61K9/127 , C07D491/056 , C12N15/88
CPC分类号： C07C217/06 , A61K9/0019 , A61K9/1272 , C07C217/08 , C07C219/08 , C07C237/06 , C07C237/08 , C07C271/16 , C07D207/08 , C07D207/12 , C07D295/08 , C07D317/28 , C07D401/04 , C07D491/04 , C07D491/056 , C12N15/88
摘要： The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

3. 发明授权

US09783490B2 Antimicrobial compounds, their synthesis and applications thereof 有权
公开(公告)号：US09783490B2
公开(公告)日：2017-10-10
申请号：US14652714
申请日：2013-12-18
申请人： The Secretary of State for Health , Jawaharlal Nehru Center for Advanced Scientific Research
发明人： Jayanta Haldar , Chandradhish Ghosh , Goutham Belagula Manjunath , Padma Akkapeddi
IPC分类号： C07D215/00 , C07C237/06 , C07C231/12 , A61K38/05 , C07D215/12
CPC分类号： C07C237/06 , A61K38/05 , C07C231/12 , C07D215/12 , Y02A50/473
摘要： The present disclosure relates to the field of medicinal chemistry and more particularly to the development of antimicrobial compounds. The disclosure relates to the synthesis and characterization of compounds comprising aromatic radical or an aliphatic radical, an alkyl amine and amino acid moiety wherein said compounds exhibit antimicrobial activity against various drug-sensitive and drug-resistant pathogenic 10 microorganisms.

4. 发明授权

US09771317B2 Process for preparing lacosamide and related compounds 有权
公开(公告)号：US09771317B2
公开(公告)日：2017-09-26
申请号：US14439916
申请日：2013-11-01
申请人： CAMBREX KARLSKOGA AB , CAMBREX PROFARMACO MILANO
发明人： Stefano Radaelli , Giuseppe Zurlo , Lars Eklund , Margus Eek , Ants Maasalu , Malle Schmidt
IPC分类号： C07C231/12 , C07C237/06 , C07C231/24 , C07C233/47 , C07C231/22 , C07C233/46 , C07C247/12
CPC分类号： C07C231/12 , C07B2200/13 , C07C231/22 , C07C231/24 , C07C233/46 , C07C233/47 , C07C237/06 , C07C247/12
摘要： There is provided a process for the preparation of Lacosamide in a particular polymorphic form, which process involves the isolation of a salt of formula I: according to the methods defined in the application.

5. 发明申请

US20170260130A1 Benzimidazole Inhibitors of the Sodium Channel 审中-公开
公开(公告)号：US20170260130A1
公开(公告)日：2017-09-14
申请号：US15602089
申请日：2017-05-22
申请人： Mark G. DeGiacomo
发明人： Hassan Pajouhesh , Richard Holland , Lingyun Zhang , Hossein Pajouhesh , Jason Lamontagne , Brendan Whelan
IPC分类号： C07C237/06 , C07D207/16 , C07D211/60 , C07D235/14 , C07D401/04 , C07D403/04 , C07D403/06 , C07D413/04 , C07D205/04 , C07D401/12 , C07D413/06 , C07D241/08 , C07C237/04 , C07D231/14 , C07D265/30 , C07C237/22 , C07C237/24
CPC分类号： C07C237/06 , A61K31/401 , A61K31/454 , A61K31/5377 , C07C237/04 , C07C237/22 , C07C237/24 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/16 , C07D211/60 , C07D231/14 , C07D235/14 , C07D241/08 , C07D265/30 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04 , C07D413/06
摘要： The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.

6. 发明申请

US20170137409A1 Amine Cationic Lipids and Uses Thereof 审中-公开
公开(公告)号：US20170137409A1
公开(公告)日：2017-05-18
申请号：US15407512
申请日：2017-01-17
申请人： Dicerna Pharmaceuticals, Inc.
发明人： Bob Dale BROWN
IPC分类号： C07D403/06 , C07D295/13 , C07D243/08 , C07D401/04 , A61K31/713 , C12N15/113 , A61K9/127 , A61K9/107 , A61K9/14 , C07D295/03 , C07D403/04
CPC分类号： C07D403/06 , A61K9/107 , A61K9/127 , A61K9/1272 , A61K9/145 , A61K9/146 , A61K31/713 , A61K38/00 , A61K47/18 , A61K47/22 , C07C211/21 , C07C237/06 , C07D211/36 , C07D233/61 , C07D233/64 , C07D239/42 , C07D241/04 , C07D243/08 , C07D295/03 , C07D295/13 , C07D295/15 , C07D401/04 , C07D403/04 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2310/321 , C12N2320/32 , C12Y204/02008
摘要： The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).

7. 发明授权

US09556378B2 Chelating agent precursors, fluids containing them, and their use 有权
标题翻译：螯合剂前体，含有它们的流体及其用途
公开(公告)号：US09556378B2
公开(公告)日：2017-01-31
申请号：US14000675
申请日：2012-02-20
申请人： James N. Lepage , Cornelia Adriana De Wolf , Johanna Hendrika Bemelaar , Adrianus Maria Reichwein , Axel Carstens , Edwin Rudolf Antony Bang
发明人： James N. Lepage , Cornelia Adriana De Wolf , Johanna Hendrika Bemelaar , Adrianus Maria Reichwein , Axel Carstens , Edwin Rudolf Antony Bang
IPC分类号： C09K8/86 , C07C227/18 , C07C229/12 , C07C229/24 , C07C231/02 , C07C237/06 , C09K8/528
CPC分类号： C09K8/86 , C07C227/18 , C07C229/12 , C07C229/24 , C07C231/02 , C07C237/06 , C09K8/528
摘要： The present invention relates to a chelating agent precursor that contains glutamic acid N,N-diacetic acid (GLDA) and/or methylglycine N,N-diacetic acid (MGDA) wherein at least one of the carboxylic acid groups is present as a carboxylic acid derivative selected from the group of amides, anhydrides, and esters, combinations thereof, and salts thereof, provided that it is not the triethyl ester of GLDA, the triethyl mono-t-butyl ester of GLDA, the tri-t-butyl ester of GLDA, the monobenzyl tri-t-butyl ester of GLDA, any ester or amide that contains azacycloalkane groups, any amide that contains biotin groups, any amide that contains minoethylcarbamoyl based amide groups, (S)-diethyl 2,2′-(1-benzyloxy)-1,5-dioxo-5-(prop-2-ynylamino)pentan-2-ylazanediyl-diacetate, diethyl 2,2′-(5-(3-azidopropylamino)-1-(benzyloxy)-1,5-dioxo-pentan-2-ylazanediyl-diacetate, the trimethyl ester of MGDA, the monomethyl ester dimethylamide of MGDA, the dibenzyl ester of MGDA, the dibenzyl mono t-butyl ester of MGDA, the di t-butyl ester of MGDA, the di-t-butyl-monobenzyl ester of MGDA, N,N-bis(benzyloxycarbonylmethyl)-N′-methoxycarbonyl-methyl-alanine amide, or N,N-bis(tert-butoxycarbonyl)-N′-methoxycarbonylmethyl-alanine amide, and esters of GLDA immobilized on a gel, and that the amide is not the amide of ammonia, to a fluid containing the above chelating precursor and a liquid, and to the use of a chelating agent precursor of MGDA and GLDA and fluids containing them in an application wherein delayed acidity or the chelating capacity is useful, such as in descaling, bleaching, cleaning, and treating oil and/or gas-containing subterranean formations.
摘要翻译：本发明涉及含有谷氨酸N，N-二乙酸（GLDA）和/或甲基甘氨酸N，N-二乙酸（MGDA）的螯合剂前体，其中至少一个羧酸基团作为羧酸存在选自酰胺，酸酐和酯的组合的衍生物，其组合及其盐，条件是它不是GLDA的三乙基酯，GLDA的三乙基单叔丁基酯，三 GLDA，GLDA的单苄基三叔丁酯，含有氮杂环烷基的任何酯或酰胺，含有生物素基团的任何酰胺，含有最小乙基氨基甲酰基的酰胺基的任何酰胺，（S）-2,2' - （1 - 苄氧基）-1,5-二氧代-5-（丙-2-炔基氨基）戊-2-基二烷基二乙酸酯，2,2' - （5-（3-叠氮基丙基氨基）-1-（苄氧基） 5-二氧代戊烷-2-基二烷基二乙酸酯，MGDA的三甲基酯，MGDA的单甲基酯二甲基酰胺，MGDA的二苄基酯，二苄基单叔丁酯的MGDA的二叔丁基酯，MGDA的二叔丁基 - 单苄基酯，N，N-双（苄氧基羰基甲基）-N'-甲氧基羰基 - 甲基 - 丙氨酸酰胺或N，N-双叔丁氧基羰基）-N'-甲氧基羰基甲基 - 丙氨酸酰胺和固定在凝胶上的GLDA的酯，并且酰胺不是氨的酰胺，与含有上述螯合前体和液体的流体，以及使用在其中延迟酸度或螯合能力有用的应用中，例如在除垢，漂白，清洁和处理含油和/或含气体的地下地层中，MGDA和GLDA的螯合剂前体和含有它们的流体。

8. 发明申请

US20170001948A1 DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS 审中-公开
标题翻译： DIAMINE交联剂，交联型酸性多糖和医用材料
公开(公告)号：US20170001948A1
公开(公告)日：2017-01-05
申请号：US15115331
申请日：2015-01-30
申请人： Seikagaku Corporation
发明人： Sho Funayama , Yosuke Yasuda , Akihiro Takezawa , Katsuya Takahashi
IPC分类号： C07C219/06 , C07C237/06 , A61L27/20 , C08B37/08 , C08B11/12 , A61L31/04 , C08B37/00 , C07C327/06
CPC分类号： C07C219/06 , A61L27/20 , A61L31/042 , C07C237/06 , C07C255/58 , C07C327/06 , C07C2601/02 , C08B11/12 , C08B15/005 , C08B37/0069 , C08B37/0072 , C08B37/0084 , C08K5/16 , C08L5/08 , C08L5/04 , C08L1/286
摘要： The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below: [the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
摘要翻译： [公式中的符号如说明书所述]; 通过二胺交联剂中的氨基与酸性多糖中的羧基之间的酰胺键形成交联而获得的交联酸性多糖; 以及包含交联产物的医疗材料。

9. 发明授权

US09422273B2 Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response 有权
公开(公告)号：US09422273B2
公开(公告)日：2016-08-23
申请号：US14792406
申请日：2015-07-06
申请人： Allergan, Inc.
发明人： Jose L. Martos , William R. Carling , David F. Woodward , Jenny W. Wang , Jussi J. Kangasmetsa
IPC分类号： C07D413/04 , A61K31/422 , C07D413/14 , C07C65/30 , C07C237/06 , C07C271/20 , C07C309/67 , C07D207/16 , C07D317/46
CPC分类号： C07D413/04 , C07C65/30 , C07C237/06 , C07C271/20 , C07C309/67 , C07D207/16 , C07D317/46 , C07D413/14
摘要： The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.

10. 发明授权

US09388123B2 LSD1-selective inhibitor having lysine structure 有权
标题翻译：具有赖氨酸结构的LSD1选择性抑制剂
公开(公告)号：US09388123B2
公开(公告)日：2016-07-12
申请号：US14648109
申请日：2013-11-28
申请人： KYOTO UNIVERSITY
发明人： Takayoshi Suzuki , Yukihiro Itoh , Daisuke Ogasawara , Naoki Miyata , Tamio Mizukami , Ryuzo Sasaki , Akifumi Takaori , Masahiro Kawahara
IPC分类号： C07C237/06 , C07C271/20 , C07D295/192 , A61K31/165 , A61K31/166 , A61K31/27 , A61K31/495
CPC分类号： C07C237/06 , A61K31/165 , A61K31/166 , A61K31/27 , A61K31/495 , C07C271/20 , C07C2601/02 , C07D295/192
摘要： Provided is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [in the formula, R1 to R5, A, and *1 to *3 are as defined in Description].
摘要翻译：提供由下式（I）表示的化合物或其药学上可接受的盐：[式中，R1〜R5，A，* 1〜* 3如说明书所述]。

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