公开(公告)号：EP2440530B1

公开(公告)日：2013-07-24

申请号：EP10727259.3

申请日：2010-06-08

申请人： Dow AgroSciences LLC

发明人： RENGA, James ,  WHITEKER, Gregory ,  ARNDT, Kim ,  LOWE, Christian

IPC分类号： C07D213/79 ,  C07D211/90

CPC分类号： C07D213/79 ,  C07D211/90

公开(公告)号：EP2114424A4

公开(公告)日：2012-07-18

申请号：EP08725107

申请日：2008-01-31

申请人： VDF FUTURECEUTICALS INC

发明人： PIETRZKOWSKI ZBIGNIEW ,  THRESHER WAYNE CARL

IPC分类号： A61K31/12 ,  A23L1/00 ,  A23L1/30 ,  A23L2/08 ,  A61K36/185 ,  A61P3/06

CPC分类号： C07H17/02 ,  A23L2/08 ,  A23L33/105 ,  A23P10/40 ,  A23V2002/00 ,  A61K9/1652 ,  A61K9/19 ,  A61K31/12 ,  A61K36/185 ,  C07D211/90 ,  C07H1/08 ,  A23V2200/3262

摘要： Solid, free-flowing, and substantially completely dissolvable preparations with high betalain content are presented. Most typically, the betalain profile of the preparations is near natural and includes betalains in an amount of between 10-40 wt %. As the preparations of the inventive subject matter maintain chemical stability and flowability over extended periods of time, it should be noted that the betalain preparations are now amenable to compounding in small and measured quantities. Furthermore, new biological activities of betalains are shown, and especially include significant induction of SIRT and reduction of serum triglyceride.

公开(公告)号：EP2440530A1

公开(公告)日：2012-04-18

申请号：EP10727259.3

申请日：2010-06-08

申请人： Dow AgroSciences LLC

发明人： RENGA, James ,  WHITEKER, Gregory ,  ARNDT, Kim ,  LOWE, Christian

IPC分类号： C07D213/79 ,  C07D211/90

CPC分类号： C07D213/79 ,  C07D211/90

摘要： 3-Halo-6-(aryl)-4-iminotetrahydropicolinic acid esters are heated with polar solvents to prepare 6-(aryl)-4-aminopicolinates.

摘要翻译： 用极性溶剂加热3-卤代-6-（芳基）-4-亚氨基四氢吡啶甲酸酯以制备6-（芳基）-4-氨基吡啶甲酸酯。

公开(公告)号：EP2311806A3

公开(公告)日：2011-08-10

申请号：EP10011436.2

申请日：1997-01-29

申请人： The United States of America, Represented by the Secretary, Department of Health and Human Services

发明人： Jacobson, Kenneth, A. ,  Kim, Yong-Chul ,  van Rhee, Albert Michiel ,  Jiang, Ji-Long ,  Karton, Yishai

IPC分类号： C07D211/90 ,  A61K31/4422 ,  A61P9/12 ,  A61P29/00

CPC分类号： C07D401/04 ,  C07D211/90 ,  C07D311/22 ,  C07D311/30 ,  C07D311/32 ,  C07D317/70 ,  C07D405/04 ,  C07D409/04 ,  C07D487/04 ,  C07D493/04 ,  C07F7/0812

摘要： The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R 1 to R 4 are as defined in the description, and M is -CH (OH) -CH (R 2 ) - or -C(OH)=C(R 2 )- and R 1 , R 2 are as defined in the description; or dihydropyridines of formula (III), wherein R 2 to R 6 are as defined in the description; or pyridines of formula (IV), wherein R 2 to R 6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R 1 and R 2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.

公开(公告)号：EP1720857B1

公开(公告)日：2011-07-13

申请号：EP05701362.5

申请日：2005-02-05

申请人： Bayer Schering Pharma Aktiengesellschaft

发明人： GIELEN-HAERTWIG, Heike ,  ALBRECHT, Barbara ,  BAUSER, Marcus ,  KELDENICH, Jörg ,  LI, Volkhart ,  PERNERSTORFER, Josef ,  SCHLEMMER, Karl-Heinz ,  TELAN, Leila

IPC分类号： C07D401/06 ,  C07D211/76 ,  A61K31/4422

CPC分类号： C07D487/04 ,  C07D211/90 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12

摘要： The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

摘要翻译： 本发明涉及新的二氢吡啶酮衍生物，其制备方法及其在药物中的用途，特别是用于治疗慢性阻塞性肺病，急性冠状动脉综合征，急性心肌梗塞和心力衰竭发展。

公开(公告)号：EP2228365A1

公开(公告)日：2010-09-15

申请号：EP09173816.1

申请日：2009-10-22

申请人： Grindeks, a joint stock company

发明人： The designation of the inventor has not yet been filed

IPC分类号： C07D211/90 ,  A61K31/4422

CPC分类号： C07D211/90

摘要： New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I

wherein R is lower alkyl group, such as methyl or ethyl
R 1 and R 2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.

摘要翻译： 具有通式的2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸酯类型的新化合物，其中R是低级烷基，：如甲基乙基，或R 1和R 2是羧酸钠甲酯 中，具有协同细胞毒性作用与5-氟尿嘧啶组合。

公开(公告)号：EP1945614A4

公开(公告)日：2010-09-01

申请号：EP06799282

申请日：2006-10-17

申请人： SK CHEMICALS CO LTD

发明人： KIM JAE-SUN ,  KIM NAM HO ,  LEE NAM KYU

IPC分类号： C07D211/90 ,  C07D213/80 ,  C07D213/803

CPC分类号： C07D211/90

公开(公告)号：EP1435954B1

公开(公告)日：2010-01-13

申请号：EP02765135.5

申请日：2002-07-05

申请人： LEK Pharmaceuticals d.d.

发明人： FURLAN, Borut ,  RESNIK, Marijan

IPC分类号： A61K31/44 ,  C07D211/90 ,  A61P9/12 ,  A61P9/10

CPC分类号： C07D211/90 ,  A61K31/4422

摘要： 3-ethyl 5-methyl (+/-) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/-) 2-[2-(N-tritylamino)ethoxymethyl]-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20 °C and reflux temperature, followed by isolation and purification of 3-ethyl 5-mehyl (+/-) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4- dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent (Formula I).

公开(公告)号：EP1891009B1

公开(公告)日：2009-10-14

申请号：EP05760546.1

申请日：2005-06-15

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura Hetero Drugs Ltd.(R & D) ,  RAJI REDDY, Rapolu Hetero Drugs Ltd.(R & D) ,  MURALIDHARA REDDY, Dasari Hetero Drugs Ltd.(R & D) ,  SATISH KUMAR, Dandamudi, Hetero Drugs Limited (R & D)

IPC分类号： C07D211/02 ,  C07D211/90

CPC分类号： C07D211/90 ,  C07D211/82

摘要： The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropyl)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.

公开(公告)号：EP1831166A4

公开(公告)日：2009-09-02

申请号：EP05821317

申请日：2005-12-02

申请人： SK CHEMICALS CO LTD

发明人： KIM JAE-SUN ,  KIM NAM HO ,  LEE NAM KYU

IPC分类号： C07D211/90

CPC分类号： C07D211/90

摘要： The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O'-dibenzoyl tartaric acid as chiral reagent., More particularly, the present invention relates to a method comprising (a) obtaining (R)- or (S)-amlodipine dibenzoyl tartrate salt or solvate thereof by reacting (R,S)-amlodipines with optically active O,O'-dibenzoyl tartaric acid in isopropanol solvent, and (b) treating the (R)- or (S)-amlodipine salt with a base, thus obtaining optically active amlodipine.