专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

EP3247700B1 PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND 有权
公开(公告)号：EP3247700B1
公开(公告)日：2019-03-20
申请号：EP16701488.5
申请日：2016-01-25
申请人： Avexxin AS
发明人： SANDBERG, Marcel , AUKRUST, Inger-Reidun
IPC分类号： C07C303/28 , C07C309/66 , C07C327/22 , C07C319/02 , C07C323/14 , C07C319/14 , C07C323/22

3. 发明授权

EP3024818B1 PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND 有权
公开(公告)号：EP3024818B1
公开(公告)日：2018-04-04
申请号：EP14742219.0
申请日：2014-07-23
申请人： Avexxin AS
发明人： SANDBERG, Marcel , AUKRUST, Inger Reidun
IPC分类号： C07C319/02 , C07C319/14 , C07C321/08 , C07C323/22 , C07C327/22
CPC分类号： C07C319/14 , C07C319/02 , C07C319/26 , C07C327/22 , C07C321/08 , C07C323/22
摘要： The invention relates to the manufacture of certain polyunsaturated compounds employing a particular application of the Mitsonobu reaction in the presence of at least one anti-oxidant. We have found a method of making a pharmaceutically-acceptable polyunsaturated ester or thioester compound directly, which can ultimately be converted to the advantageous ketone compounds, in which unwanted oxidation and cis/trans isomerization are substantially reduced or eliminated using particular Mitsonobu chemistry.

4. 发明公开

EP3024818A1 PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND 有权
标题翻译： PROCESS FOR产生多个不饱和酮化合物
公开(公告)号：EP3024818A1
公开(公告)日：2016-06-01
申请号：EP14742219.0
申请日：2014-07-23
申请人： Avexxin AS
发明人： SANDBERG, Marcel , AUKRUST, Inger Reidun
IPC分类号： C07C319/02 , C07C319/14 , C07C321/08 , C07C323/22 , C07C327/22
CPC分类号： C07C319/14 , C07C319/02 , C07C319/26 , C07C327/22 , C07C321/08 , C07C323/22
摘要： The invention relates to the manufacture of certain polyunsaturated compounds employing a particular application of the Mitsonobu reaction in the presence of at least one anti-oxidant. We have found a method of making a pharmaceutically-acceptable polyunsaturated ester or thioester compound directly, which can ultimately be converted to the advantageous ketone compounds, in which unwanted oxidation and cis/trans isomerization are substantially reduced or eliminated using particular Mitsonobu chemistry.

5. 发明公开

EP3174873A1 2-OXOTHIATOLE COMPOUNDS HAVING ACTIVITY AS CPLA2 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISORDERS AND HYPERPROLIFERATIVE DISORDERS 有权
标题翻译： 2- OXOTHIATOLE WITH ACTIVITY TIES AS的cPLA 2抑制剂用于炎性疾病和过度增殖性疾病的治疗
公开(公告)号：EP3174873A1
公开(公告)日：2017-06-07
申请号：EP15745206.1
申请日：2015-08-03
申请人： Avexxin AS
发明人： JOHANSEN, Berit , SANDBERG, Marcel , AUKRUST, Inger-Reidun , KOKOTOS, George , EVENÄS, Johan , BRIMERT, Thomas , KILDAHL-ANDERSEN, Geir
IPC分类号： C07D417/04 , C07D277/56 , C07D513/04 , A61K31/426 , A61K31/427 , A61K31/429 , A61P29/00 , A61P35/00
摘要： A compound of formula (I') wherein R6 is H, C1-6alkyl, -(CH2)pCOOH, -(CH2)pCOOC1-6alkyl, - (CH2)pCONH2, -(CH2)pCONHC1-6alkyl, -(CH2)pCON(C1-6alkyl)2, R7 is as defined for R6; or and R7 taken together with the atoms joining them can form a 6-membered aromatic or non aromatic, saturated or unsaturated, carbocyclic or heteroatom containing (e.g. O, N or S containing) ring optionally substituted by up to 4 groups R8; each R8 is defined as for R6 or is oxo; R10 is C1-6 alkyl Ar is a C6-14 aryl group, wherein the aryl group may be optionally substituted (preferably in the meta or para position relative to O) with one or more R9 groups; each R9 is halo, OH, CN, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, haloC1-6alkyl, C6-10 aryl group, C7-12 arylalkyl, a C1-10alkyl group, C2-10-mono or multiply unsaturated alkenyl group, OC1-10alkyl group, SC1-10alkyl group -OC1-10alkyl-O-C10alkyl, -C1-10alkyl-O-C1-10alkyl, -OC2-10-mono or multiply unsaturated alkenyl group, OAr2, O(CH2)qAr2, SAr2 or S(CH2)qAr2; wherein Ar2 is phenyl, optionally substituted with one or more of halo, trihalomethyl, C1-10-alkoxy, or C1-10 alkyl; each q is 1 to 3, preferably 1; each p is 0 to 3; or a salt, ester, solvate, N-oxide, or prodrug thereof.
摘要翻译：（CH 2）pCOOH， - - （CH 2）pCOOC1-6alkyl， - （CH2）pCONH2， - （CH2）pCONHC1-6alkyl， - （CH2）PCON式（I“）其中R 6是H，C 1-6烷基，所述的化合物（C 1-6烷基）2，R 7是作为R6所定义; 或和R 7与其连接的原子连接它们可一起形成截取的6元芳族或非芳族的，饱和或不饱和的，碳环或含杂原子的（例如O，N或S的含）substituiertem任选被最多4个基团R8振铃; 每个R 8被定义为对R 6或为氧代; R 10是C 1-6烷基，Ar是C 6-14芳基，worin芳基可以任选地被substituiertem（优选在相对的间位或对位O）与一个或多个R 9基团; 每个R 9是卤素，OH，CN，硝基，NH 2，NHC 1-6烷基，N（C 1-6烷基）2，haloC1-6alkyl，C 6-10芳基，C 7-12芳烷基，C 1-10烷基一组，C2-10- 单或多不饱和链烯基，OC1-10alkyl基，SC1-10alkyl组-OC1-10alkyl-O - C 10的烷基，-C1-10alkyl-OC1-10alkyl，-OC2-10 - 单或多不饱和链烯基，OAR2， O（CH2）qAr2，SAR2或S（CH 2）qAr2; worin Ar 2为苯基，其被一个或多个卤素，三卤代甲基的，C 1-10烷氧基，C 1-10或烷基，其任选substituiertem; 每个q为1至3，优选1; 每个p为0至3; 或其盐，酯，溶剂化物，N-氧化物或前药。

6. 发明公开

EP3572398A1 PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND 审中-公开
公开(公告)号：EP3572398A1
公开(公告)日：2019-11-27
申请号：EP19163562.2
申请日：2016-01-25
申请人： Avexxin AS
发明人： AUKRUST, Inger-Reidun , SANDBERG, Marcel
IPC分类号： C07C303/28 , C07C309/66 , C07C327/22 , C07C321/08
摘要： A process for the preparation of a polyunsaturated thiol comprising:
(1) reacting a polyunsaturated alcohol in the presence of a compound of formula R 2 -SO 2 Hal wherein R 2 is a C 1-20 hydrocarbyl group, such an C 1-10 alkyl group, to form a polyunsaturated sulphonyl ester;
(2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula SC(=O)R 4 wherein R 4 is a C 1-20 hydrocarbyl group;
(3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate.

7. 发明授权

EP2951164B1 ANTIINFLAMMATORY AND ANTITUMOR 2-OXOTHIAZOLES COMPOUNDS 有权
公开(公告)号：EP2951164B1
公开(公告)日：2019-06-05
申请号：EP14702520.9
申请日：2014-01-28
申请人： Avexxin AS
发明人： JOHANSEN, Berit , SANDBERG, Marcel , AUKRUST, Inger-Reidun , KOKOTOS, George , BARBAYIANNI, Efrosini
IPC分类号： A61K45/06 , A61K31/381 , A61K31/428 , C07D333/38 , C07D277/26 , C07D277/64 , C07D277/24 , C07D277/56 , A61K31/426

8. 发明公开

EP3247700A1 PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND 审中-公开
标题翻译：制备多不饱和酮类化合物的方法
公开(公告)号：EP3247700A1
公开(公告)日：2017-11-29
申请号：EP16701488.5
申请日：2016-01-25
申请人： Avexxin AS
发明人： SANDBERG, Marcel , AUKRUST, Inger-Reidun
IPC分类号： C07C303/28 , C07C309/66 , C07C327/22 , C07C319/02 , C07C323/14 , C07C319/14 , C07C323/22
CPC分类号： C07C319/14 , C07C303/28 , C07C319/02 , C07C319/28 , C07C327/22 , C07C309/66 , C07C323/14 , C07C321/08
摘要： A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R2-SO2Hal wherein R2 is a C1-20 hydrocarbyl group, such an C1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula -SC(=O)R4 wherein R4 is a C1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R3COX wherein X is an electron withdrawing group and R3 is an alkylene group carrying a leaving group (LG), such as LG-CH2- forming (I) where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.

9. 发明公开

EP2951164A1 ANTIINFLAMMATORY AND ANTITUMOR 2-OXOTHIAZOLES AND 2-OXOTHIOPHENES COMPOUNDS 有权
标题翻译：抗坏血酸-2-氧代唑酮的化学发光二氧化钛 - 维生素D
公开(公告)号：EP2951164A1
公开(公告)日：2015-12-09
申请号：EP14702520.9
申请日：2014-01-28
申请人： Avexxin AS
发明人： JOHANSEN, Berit , SANDBERG, Marcel , AUKRUST, Inger-Reidun , KOKOTOS, George , BARBAYIANNI, Efrosini
IPC分类号： C07D277/24 , C07D277/56 , A61K31/426 , A61P1/00
CPC分类号： C07D333/38 , A61K31/381 , A61K31/426 , A61K31/428 , A61K45/06 , C07D277/24 , C07D277/26 , C07D277/56 , C07D277/64
摘要： A compound of formula (I) wherein X is O, C═O or S; Y is N or CH; R2 and R4 are each independently H, —(CH2)pCOOH, —(CH2)pCON(R5)2 or —(CH2)pCOOC1-6alkyl; or R2 and R4 together form a 6-membered phenyl ring fused to the five membered ring; each R1 is independently selected from H, halo (e.g. fluoro or chloro), C6-10aryl, C7-12arylalkyl, C2-12 alkenyl; OC1-12 alkyl, OC2-12 alkenyl or a C1-12 alkyl group; each R5 is H or C1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof
摘要翻译：式（I）的化合物，其中X为O，C = O或S; Y为N或CH; R2和R4各自独立地为H， - （CH2）pCOOH， - （CH2）pCON（R5）2或 - （CH2）pOCOC1-6烷基; 或者R 2和R 4一起形成与五元环稠合的6元苯环; 每个R 1独立地选自H，卤素（例如氟或氯），C 6-10芳基，C 7-12芳烷基，C 2- 12烯基; OC1-12烷基，OC2-12烯基或C1-12烷基; 每个R 5是H或C 1-6烷基; 每个p为0至3; n为1至4; 或其盐，酯，溶剂化物，N-氧化物或前药，例如。其盐

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式