公开(公告)号：EP4424371A2

公开(公告)日：2024-09-04

申请号：EP24173326.0

申请日：2016-02-29

申请人： Theaprin Pharmaceuticals Inc. ,  Brittain, Harry, G. ,  Felice, Philip, V.

发明人： Brittain, Harry, G. ,  Felice, Philip, V.

IPC分类号： A61P31/14

CPC分类号： A61K31/4453 ,  C07D401/14 ,  C07D215/22 ,  C07D233/94 ,  C07D405/12 ,  C07H15/252 ,  C07H17/08 ,  C07H19/06 ,  C07C229/36 ,  C07D249/08 ,  C07D457/04 ,  C07D457/06 ,  C07D473/18 ,  C07D473/30 ,  C07D261/16 ,  C07D265/18 ,  C07D491/22 ,  C07D499/00 ,  C07D277/56 ,  C07D209/14 ,  C07D499/24 ,  C07D209/24 ,  C07D501/22 ,  C07C255/41 ,  C07D519/00 ,  C07D519/02 ,  C07K7/08 ,  C07D285/28 ,  C07D211/22 ,  C07D307/52 ,  A61P31/00 ,  C07C69/157 ,  C07C57/30 ,  C07C59/105 ,  C07B2200/1320130101 ,  C07C211/38 ,  C07C215/58 ,  C07C2603/7420170501 ,  C07J5/0053 ,  A61K31/704 ,  A61K31/13 ,  A61K31/137 ,  A61K31/192 ,  A61K31/198 ,  A61K31/277 ,  A61K31/4045 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/426 ,  A61K31/43 ,  A61K31/445 ,  A61K31/4745 ,  A61K31/48 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/522 ,  A61K31/536 ,  A61K31/545 ,  A61K31/546 ,  A61K31/549 ,  A61K31/573 ,  A61K31/635 ,  A61K31/7048 ,  A61K31/7072 ,  A61K38/12 ,  A61K31/34 ,  A61K31/431 ,  A61K31/4709 ,  A61K31/603 ,  Y02A50/30

摘要： A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

公开(公告)号：EP3269699A1

公开(公告)日：2018-01-17

申请号：EP16382336.2

申请日：2016-07-15

申请人： Fundació Institut Català d'investigació Quimica ,  ICREA, Institució Catalana de Recerca I Estudis Avançats

发明人： MARTÍN ROMO, Rubén ,  JULIÁ HERNÁNDEZ, Francisco ,  CORNELLA, Josep

IPC分类号： C07C51/15 ,  C07C53/126 ,  C07C53/128 ,  C07C53/134 ,  C07C57/30 ,  C07C61/08 ,  C07C67/29 ,  C07C67/313 ,  C07C69/24 ,  C07C69/34 ,  C07C69/46 ,  C07C69/92

CPC分类号： C07C67/313 ,  C07C51/15 ,  C07C67/29 ,  C07C2601/14 ,  C07C53/128 ,  C07C53/126 ,  C07C69/46 ,  C07C69/34 ,  C07C69/92 ,  C07C69/24 ,  C07C53/134 ,  C07C61/08 ,  C07C57/30

摘要： The present invention relates to a method of reacting starting materials with an activating group, namely alkanes carrying a leaving group and/or olefins, with carbon dioxide under transition metal catalysis to give carboxyl group-containing products. It is a special feature of the method of the present invention that the carboxylation predominantly takes place at a preferred position of the molecule irrespective of the position of the activating group. The carboxylation position is either an aliphatic terminus of the molecule or it is a carbon atom adjacent to a carbon carrying an electron withdrawing group. The course of the reaction can be controlled by appropriately choosing the reaction conditions to yield the desired regioisomer.

摘要翻译： 本发明涉及在过渡金属催化作用下使起始原料与活化基团（即带有离去基团和/或烯烃的烷烃）与二氧化碳反应以产生含羧基产物的方法。 本发明方法的一个特殊特征是羧化主要发生在分子的优选位置，而与活化基团的位置无关。 羧化位置是分子的脂族末端或是与携带吸电子基团的碳相邻的碳原子。 反应的过程可以通过适当选择反应条件来控制以产生期望的区域异构体。

公开(公告)号：EP2970088A4

公开(公告)日：2016-10-19

申请号：EP14762607

申请日：2014-03-14

申请人： PROMETIC PHARMA SMT LTD

发明人： GAGNON LYNE ,  LAURIN PIERRE ,  GROUIX BRIGITTE ,  GEERTS LILIANNE ,  SARRA-BOURNET FRANÇOIS ,  LEDUC MARTIN ,  ABBOTT SHAUN ,  ZACHARIE BOULOS ,  BIENVENU JEAN-FRANÇOIS ,  PERRON VALÉRIE

IPC分类号： C07C59/52 ,  A61K31/192 ,  A61K31/4418 ,  A61P11/00 ,  A61P19/04 ,  C07C57/30 ,  C07C57/58

CPC分类号： C07C57/30 ,  A61K31/192 ,  A61K31/4418 ,  A61K45/06 ,  C07C57/42 ,  C07C57/58 ,  C07C57/60 ,  C07C59/52 ,  C07C59/84

摘要： The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, OH or F; R2 is H, OH, F or CH2—OH; R3 is H, OH, F or CH2Ph; R4 is H, OH or F; Q is 1) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)OH.

公开(公告)号：EP2928599A4

公开(公告)日：2016-09-07

申请号：EP13859775

申请日：2013-12-06

申请人： UNIV CENTRAL FLORIDA RES FOUND

发明人： BLAIR RICHARD G

IPC分类号： B01J35/00 ,  B01J31/12 ,  B01J37/00 ,  B01J37/34 ,  C07F17/00

CPC分类号： C07C51/36 ,  B01J27/24 ,  B01J35/02 ,  B01J37/00 ,  B01J37/0036 ,  B01J37/343 ,  B01J2231/643 ,  B01J2231/645 ,  C01B21/0648 ,  C01P2002/85 ,  C01P2004/03 ,  C07C5/03 ,  C07C45/62 ,  C07C231/00 ,  C07C253/00 ,  C07C2527/24 ,  C07C9/08 ,  C07C9/22 ,  C07C15/18 ,  C07C15/16 ,  C07C255/03 ,  C07C255/07 ,  C07C233/11 ,  C07C57/30 ,  C07C49/784

摘要： The inventive concepts disclosed and/or claimed herein relate generally to catalysts and, more particularly, but not by way of limitation, to a heterogeneous, metal-free hydrogenation catalyst containing frustrated Lewis pairs. In one non-limiting embodiment, the heterogeneous, metal-free catalyst comprises hexagonal boron nitride (h-BN) having frustrated Lewis pairs therein.

摘要翻译： 本文公开和/或要求保护的发明概念通常涉及含有沮丧的路易斯对的非均相不含金属的氢化催化剂，更具体地但不限于此。 在一个非限制性实施方案中，非均相无金属催化剂包含其中具有沮丧的Lewis对的六方氮化硼（h-BN）。

公开(公告)号：EP2275398B1

公开(公告)日：2016-05-04

申请号：EP09733969.1

申请日：2009-01-20

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： ZHOU, Qilin ,  LI, Shen ,  ZHU, Shoufei ,  ZHANG, Canming ,  WANG, Lixin

IPC分类号： C07C51/347 ,  C07C57/04 ,  C07F9/653 ,  B01J31/18 ,  B01J31/22 ,  B01J31/24 ,  C07B53/00 ,  C07C51/36 ,  C07C201/12 ,  C07D263/12 ,  C07D307/54 ,  C07F15/00 ,  C07F17/02

CPC分类号： C07F9/653 ,  B01J31/189 ,  B01J31/2295 ,  B01J2231/645 ,  B01J2531/827 ,  C07B53/00 ,  C07B2200/07 ,  C07C51/36 ,  C07D263/12 ,  C07D307/54 ,  C07F15/0033 ,  C07F17/02 ,  C07C57/30 ,  C07C59/64

公开(公告)号：EP2752419A4

公开(公告)日：2015-04-29

申请号：EP12828043

申请日：2012-07-27

申请人： ZHEJIANG JIUZHOU PHARM CO LTD

发明人： ZHOU QILIN ,  ZHU SHOUFEI ,  YU YANBO ,  LI KUN ,  WANG LIXIN

IPC分类号： C07F9/50 ,  B01J31/24 ,  C07B35/02 ,  C07C51/36 ,  C07C53/128 ,  C07C57/30 ,  C07C57/58 ,  C07C59/125 ,  C07C59/13 ,  C07C59/64 ,  C07C67/303 ,  C07C69/42 ,  C07F19/00

CPC分类号： C07F15/004 ,  B01J31/189 ,  B01J2231/645 ,  B01J2531/827 ,  C07B35/02 ,  C07B53/00 ,  C07B2200/07 ,  C07C51/36 ,  C07F9/5022 ,  C07F9/505 ,  C07F15/0033 ,  C07C53/128 ,  C07C57/30 ,  C07C57/58 ,  C07C59/125 ,  C07C59/13 ,  C07C59/64

摘要： The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7'-diarylphosphino-1, 1'-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.

公开(公告)号：EP2562152A4

公开(公告)日：2014-08-06

申请号：EP11860849

申请日：2011-06-07

申请人： LIANHE CHEMICAL TECHNOLOGY CO LTD ,  JIANGSU LIANHE CHEMICAL TECHNOLOGY CO LTD

发明人： WANG PING ,  FAN XIAOBIN ,  LIN XINGJUN ,  HE ZHAOHUI

IPC分类号： C07C51/10 ,  C07C17/32 ,  C07C22/04 ,  C07C57/30

CPC分类号： C07C51/10 ,  C07C17/32 ,  Y02P20/542 ,  C07C57/30 ,  C07C22/04

公开(公告)号：EP2752419A1

公开(公告)日：2014-07-09

申请号：EP12828043.5

申请日：2012-07-27

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： ZHOU, Qilin ,  ZHU, Shoufei ,  YU, Yanbo ,  LI, Kun ,  WANG, Lixin

IPC分类号： C07F9/50 ,  C07F19/00 ,  B01J31/24 ,  C07B35/02 ,  C07C51/36 ,  C07C57/30 ,  C07C59/64 ,  C07C57/58 ,  C07C53/128 ,  C07C67/303 ,  C07C69/42 ,  C07C59/13 ,  C07C59/125

CPC分类号： C07F15/004 ,  B01J31/189 ,  B01J2231/645 ,  B01J2531/827 ,  C07B35/02 ,  C07B53/00 ,  C07B2200/07 ,  C07C51/36 ,  C07F9/5022 ,  C07F9/505 ,  C07F15/0033 ,  C07C53/128 ,  C07C57/30 ,  C07C57/58 ,  C07C59/125 ,  C07C59/13 ,  C07C59/64

摘要： The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7'-diarylphosphino-1, 1'-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.

摘要翻译： 本发明涉及螺苄胺 - 膦，其制备方法及其用途。 该化合物具有由式（I）表示的结构，其中n = 0至3; R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9具有如权利要求1所定义的值。从取代的7-三氟甲氧基-7'-二芳基膦基-1， 1'-螺二氢茚，该化合物以两步或三步反应合成。 新的螺苄胺 - 膦与铱前体络合并进行离子交换，得到包含各种阴离子的铱/螺苄基胺 - 膦配合物。 根据本发明的螺苄胺 - 膦/铱络合物可用于催化各种α-取代的丙烯酸的不对称氢化，具有高活性和对映选择性，并具有良好的工业化前景。

公开(公告)号：EP2651870A2

公开(公告)日：2013-10-23

申请号：EP11811095.6

申请日：2011-12-13

申请人： Aet Group

发明人： PILIA, Raimondo ,  TRANI, Alexandre ,  MARIE, Sabrina ,  DE PANTHOU, Fabrice

IPC分类号： C07C51/12 ,  C07C51/14 ,  C07C61/08

CPC分类号： C07C51/12 ,  C07C57/30 ,  C07C57/32 ,  C07C57/58 ,  C07C61/135

摘要： The invention relates to a continuous method for the carbonylation of an (R
1 R
3 )C - X alcohol in acid, where: R
1 and R
3 are radicals bonded to the carbon atom by means of a single covalent bond, or an aliphatic cyclic compound that integrates the central carbon atom and bonds to the latter on each side by means of a single covalent bond; and C - X is C(R) - OH, where R is (Z
1 Z
2 )HC- or (Z
1 Z
2 )C-, it being a given that said radical (Z
1 Z
2 )C- can be a substituted or unsubstituted unsaturated cyclic compound such as a benzene cyclic compound. Said method is carried out in a piston reactor provided with a mechanical axial agitation means, and in said method: a) at least one liquid phase comprising said raw alcohol is continuously added, optionally into an appropriate solvent, and a strong acid is also continuously added; b) said at least one liquid phase is subjected to mechanically axially agitated under the influence of a CO pressure of 2 to 250 bar during a transit time t of between 10 seconds and 10 minutes; and c) the liquid phase is removed from said reactor, and in said method, the temperature increase ΔT of the liquid, between the input thereof and removal thereof in/from the reactor, is controlled such that the ratio ΔΤ/AT
ad (where AT
ad is the adiabatic temperature increase) is between 0.02 and 0.6 when the ratio between the characteristic heat transfer time t
therm and the characteristic matter transfer time t
mat is between 1 and 50.

公开(公告)号：EP2629889A2

公开(公告)日：2013-08-28

申请号：EP11788587.1

申请日：2011-10-11

申请人： Yeda Research and Development Co. Ltd.

发明人： MILSTEIN, David ,  BALARAMAN, Ekambaram ,  GUNANATHAN, Chidambaram ,  GNANAPRAKASAM, Boopathy ,  ZHANG, Jing

IPC分类号： B01J31/18

CPC分类号： C07K5/12 ,  B01J31/18 ,  B01J31/189 ,  B01J31/2404 ,  B01J31/2409 ,  B01J31/248 ,  B01J31/2485 ,  B01J2231/40 ,  B01J2231/49 ,  B01J2231/643 ,  B01J2231/763 ,  B01J2531/0244 ,  B01J2531/821 ,  C07B41/02 ,  C07B41/08 ,  C07B41/12 ,  C07B43/04 ,  C07B43/06 ,  C07C29/136 ,  C07C29/149 ,  C07C29/177 ,  C07C41/16 ,  C07C41/26 ,  C07C45/002 ,  C07C45/006 ,  C07C51/00 ,  C07C51/02 ,  C07C51/23 ,  C07C51/295 ,  C07C67/00 ,  C07C67/03 ,  C07C67/297 ,  C07C209/00 ,  C07C209/62 ,  C07C213/00 ,  C07C213/02 ,  C07C231/02 ,  C07C231/10 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D207/06 ,  C07D207/08 ,  C07D211/12 ,  C07D213/38 ,  C07D241/08 ,  C07D241/12 ,  C07D295/023 ,  C07D295/027 ,  C07D295/185 ,  C07D305/06 ,  C07D307/14 ,  C07D307/33 ,  C07D307/44 ,  C07D307/52 ,  C07D307/83 ,  C07D309/30 ,  C07D487/14 ,  C07F9/58 ,  C07F9/65583 ,  C07F15/0046 ,  C07F15/0053 ,  C07K1/00 ,  C08G69/00 ,  Y02P20/52 ,  C07C233/05 ,  C07C235/06 ,  C07C233/07 ,  C07C235/16 ,  C07C235/14 ,  C07C235/10 ,  C07C211/27 ,  C07C211/07 ,  C07C211/35 ,  C07C211/46 ,  C07C211/10 ,  C07C215/28 ,  C07C217/58 ,  C07C69/14 ,  C07C69/24 ,  C07C31/125 ,  C07C31/12 ,  C07C49/78 ,  C07C49/04 ,  C07C49/10 ,  C07C49/08 ,  C07C49/403 ,  C07C31/205 ,  C07C31/202 ,  C07C31/04 ,  C07C31/08 ,  C07C33/20 ,  C07C33/22 ,  C07C31/1355 ,  C07C31/10 ,  C07C43/13 ,  C07C69/78 ,  C07C69/75 ,  C07C53/124 ,  C07C53/126 ,  C07C59/125 ,  C07C57/32 ,  C07C61/08 ,  C07C57/30 ,  C07C65/21 ,  C07C63/08 ,  C07C63/06

摘要： The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.

摘要翻译： 本发明涉及新的钌络合物和相关的硼氢化物，及对（1）酰胺（包括聚酰胺），以醇和cardamines的氢化使用; （2）制备的酰胺从醇与cardamines（包括通过使二元醇与二胺或由氨基醇的聚合制备聚酰胺（例如，多肽））; （3）酯的氢化，以醇（包括环状酯的氢化（内酯），环状二酯（二 - 内酯）或聚酯）; （4）的有机碳酸酯（包括聚碳酸酯）醇类和氨基甲酸酯类（包括聚氨基甲酸酯）或尿素衍生物为醇和cardamines的加氢; （5）的醇脱氢以酯的耦合; （6）仲醇到酮的加氢; （7）酯的酰胺化（从酯和cardamines酰胺的合成）; （8）使用酯醇的酰化; （9）与水的醇的偶联以形成羧酸; 和（10）的β-氨基醇的脱氢以形成吡嗪。 本发明还涉及某些吡啶钌配合物的新颖用途。