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1. 发明申请

WO2011098746A1 CRYSTALLINE ACID ADDITION SALTS OF ( 5R) -ENANTI0MER OF PIOGLITAZONE 审中-公开
标题翻译：（5R） - PIOGLITAZONE内含物的结晶酸添加剂
公开(公告)号：WO2011098746A1
公开(公告)日：2011-08-18
申请号：PCT/GB2010/050200
申请日：2010-02-09
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , VAN NIEL, Monique Bodil , FORREST, Andrew , FOX, Craig , SAJAD, Mohammed , FINCH, Harry
发明人： VAN NIEL, Monique Bodil , FORREST, Andrew , FOX, Craig , SAJAD, Mohammed , FINCH, Harry
IPC分类号： C07D417/12 , A61K31/427 , A61P11/00
CPC分类号： C07D417/12
摘要： A crystalline acid addition salt of 5R-pioglitazone, said salt being selected from the hydrochloride, hydrobromide, (-)-O,O'-dibenzoyl-L-tartrate, phosphate, hydroxy-ethanesulfonic acid and the naphthalene-1,5-disulfonic acid (2:1 ) salts thereof, wherein the naphthalene-1,5-disulfonic acid salt contains 2 molecules of (5R)-5-{4-[2- (5-ethylpyrϊdin-2-yl)ethoxy]benzyI}-1,3-thiazoIidine-2,4-dione for each molecule of naphthalene-1,5-disulfonic acid.
摘要翻译：所述盐选自盐酸盐，氢溴酸盐，（ - ） - O，O-二苯甲酰基-L-酒石酸盐，磷酸盐，羟基 - 乙磺酸和萘-1,5-二磺酸盐的结晶酸加成盐其中1,5-二磺酸盐包含2分子的（5R）-5- {4- [2-（5-乙基吡啶-2-基）乙氧基]苄基 } -1,3-噻唑烷-2,4-二酮，每个分子萘-1,5-二磺酸。

2. 发明申请

WO2010150014A1 5R- 5 -DEUTERATED GLITAZONES FOR RESPIRATORY DISEASE TREATMENT 审中-公开
标题翻译：用于呼吸道疾病治疗的5R-5-灭菌玻璃制品
公开(公告)号：WO2010150014A1
公开(公告)日：2010-12-29
申请号：PCT/GB2010/051044
申请日：2010-06-24
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , FINCH, Harry , SAJAD, Mohammed , FORREST, Andrew , VAN NIEL, Monique Bodil
发明人： FINCH, Harry , SAJAD, Mohammed , FORREST, Andrew , VAN NIEL, Monique Bodil
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/506 , A61K31/513 , A61K45/06 , A61P11/06 , A61P11/08 , A61P29/00 , C07D417/12
CPC分类号： A61K31/4439 , A61K9/0043 , A61K31/426 , A61K31/427 , A61K31/506 , A61K31/513 , A61K2300/00
摘要： A composition comprising a 5R-5-deuterated glitazone or a salt thereof, in which composition the 5R-5 deuterated glitazone component includes less than 5% by weight in total of 5R-5-protonated glitazone, 5S-5-protonated glitazone and 5S-5- deuterated glitazone. The glitazone may be rosiglitazone or pioglitazone. Compositions may be for pulmonary inhalation for treatment of Pulmonary inflammatory disease.
摘要翻译：包含5R-5-氘代格列酮或其盐的组合物，其中5R-5氘化格列酮酮组分的组合物包含总共5R-5质子化格列酮，5S-5质子化格列酮和5S -5-氘代格列酮。格列酮可以是罗格列酮或吡格列酮。组合物可用于肺部吸入治疗肺炎性疾病。

3. 发明申请

WO2011015868A1 ENANTIOMERIC RESOLUTION METHOD 审中-公开
标题翻译：完美解决方法
公开(公告)号：WO2011015868A1
公开(公告)日：2011-02-10
申请号：PCT/GB2010/051285
申请日：2010-08-04
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , VAN NIEL, Monique Bodil , SAJAD, Mohammed , FORREST, Andrew
发明人： VAN NIEL, Monique Bodil , SAJAD, Mohammed , FORREST, Andrew
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： A method for the preparation of pioglitazone O,O'-dibenzoyl-L-tartrate wherein the content by weight of pioglitazone consists of at least 95 % by weight of the 5R enantiomer and less than 5 % of the 5S enantiomer, which method comprises: (1a) adding seed crystals of 5R- pioglitazone O,O'-dibenzoyl-l-tartrate to a rnethanol-water solution of racemic pioglitazone hydrochloride and O,O'-dibenzoyI-L-tartaric acid, thereby precipitating pioglitazone O,O'- dibenzoyl-L-tartrate;(1b) recovering said precipitate from step (1a); (1c) forming a solution of the precipitate from step (1b) in a solvent mixture of methanol, acid and water and mixing into to the resultant solution seed crystals of 5R-pioglitazone O,O'-dibenzoyl-L-tartrate, thereby precipitating pioglitazone O,O'-dibenzoyl-L-tartrate; (1d) recovering said precipitate from step (1c); (1e) repeating steps (1c) and (1d), the recovered product being the desired pioglitazone O,O'-dibenzoy! tartrate wherein the content by weight of pioglitazone consists of at least 95 % by weight of the 5R enantiomer and less than 5 % of the 5S enantiomer. Also disclosed is a modification of the method in which step 1(e) is omitted.
摘要翻译：吡格列酮O，O-二苯甲酰基-L-酒石酸盐的制备方法，其中吡格列酮的重量含量为至少95重量％的5R对映异构体和小于5％的5S对映异构体，该方法包括：（1a）将5R-吡格列酮O，O-二苯甲酰基-1-酒石酸盐的晶体加入到外消旋吡格列酮盐酸盐和O，O-二苯并吡喃L-酒石酸的rnetanol-水溶液中，从而沉淀吡格列酮O，O' - 二苯甲酰基-L-酒石酸盐;（1b）从步骤（1a）回收所述沉淀物; （1c）将来自步骤（1b）的沉淀物的溶液形成在甲醇，酸和水的溶剂混合物中，并混合到得到的5R-吡格列酮O，O-二苯甲酰基-L-酒石酸盐的晶体中，从而沉淀吡格列酮O，O-二苯甲酰基-L-酒石酸盐; （1d）从步骤（1c）回收所述沉淀物; （1e）重复步骤（1c）和（1d），回收的产物是所需的吡格列酮O，酒石酸盐，其中吡格列酮的重量含量为至少95重量％的5R对映异构体和小于5％的5S对映异构体。还公开了省略步骤1（e）的方法的修改。

4. 发明申请

WO2010094956A1 TRIAZOLOPYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS 审中-公开
标题翻译：作为P38 MAP激酶抑制剂的三唑吡啶衍生物
公开(公告)号：WO2010094956A1
公开(公告)日：2010-08-26
申请号：PCT/GB2010/050257
申请日：2010-02-16
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED. , FINCH, Harry , MONTANA, John , VAN NIEL, Monique Bodil , WOO, Chi-Kit , KNIGHT, Jamie , WASZKOWYCZ, Bohdan
发明人： FINCH, Harry , MONTANA, John , VAN NIEL, Monique Bodil , WOO, Chi-Kit , KNIGHT, Jamie , WASZKOWYCZ, Bohdan
IPC分类号： C07D471/04 , A61P11/00 , A61P29/00 , A61K31/4162
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of, inter alia , diseases of the respiratory tract wherein; R 1 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R 3 and R 4 are independently H or C 1 -C 6 alkyl, or R 3 and R 4 taken together with the nitrogen to which they are attached form a 6- membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is -O- or -S(O) P - wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C 3 -C 6 divale nt cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R 2 NHC(=O)W-; W is a bond, -NH- or -C(R A )(R B ), wherein R A and R B are independently H, methyl, ethyl, amino, hydroxyl or halo; and R 2 is a radical as defined in the claims.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，其可用作治疗特别是呼吸道疾病的抗炎剂，其中： R 1是C 1 -C 6烷基，C 3 -C 6环烷基，任选取代的苯基，任选被取代的5-或6-元单环杂芳基，或其中n是1或2的式（II）基团，R 3和R 4是独立地是H或C 1 -C 6烷基，或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6-元杂环; Y是-O-或-S（O）P-，其中p是0,1或2; A是任选取代的二价亚芳基，或单环或双环亚杂芳基，或具有5或6个环原子的C 3 -C 6二烯基亚环烷基或其中环氮连接至R 2 NHC（= O）的哌啶子基， W-; W是键，-NH-或-C（RA）（RB），其中RA和RB独立地是H，甲基，乙基，氨基，羟基或卤素; 并且R 2是如权利要求中所定义的基团。

5. 发明申请

WO2010131030A1 PYRIDYLUREA DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：吡啶衍生物及其治疗用途
公开(公告)号：WO2010131030A1
公开(公告)日：2010-11-18
申请号：PCT/GB2010/050767
申请日：2010-05-11
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , BESWICK, Amanda , WASZKOWYCZ, Bohdan , VAN NIEL, Monique Bodil
发明人： BESWICK, Amanda , WASZKOWYCZ, Bohdan , VAN NIEL, Monique Bodil
IPC分类号： C07D213/75 , C07D401/10
CPC分类号： C07D213/75 , C07D401/10
摘要： Compounds of formula (IA) are inhibitors of p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia , diseases of the respiratory tract formula (IA). wherein R 1 is a radical of formula (IIA), (IIB), or (IIC); wherein m is 0 or 1; T is N or CH; R 2a , R 2b , R 2c are independently selected from H, halogen and C 1 -C 6 alkyl; R 3 is H or F; R 4 is -CH 3 ; -C 2 H 5 ; -CH 2 OH, CH 2 SCH 3 ; - SCH 3 or -SC 2 H 5 ; R 5 is -CH 3 or -C 2 H 5 ; R 6 is H, or represents one or more 10 substituents, each independently selected from C 1 -C 6 alkyl, hydroxy, halogen, and radicals of formulae (IIIA), (IIIB) and (IIIC):IA)(IIIB)(IIIC); wherein R 61a and R 61b are independently H or C 1 -C 6 alkyl, or R 61a and R 61b taken together with the nitrogen to which they are attached to form a 6-membered 15 heterocyclic ring optionally containing a further heteroatom selected from N and O; n is 0, 1 or 2; p is 1 or 2; R 7 is H or F; and R 8 is H or CONH 2 .
摘要翻译：式（IA）化合物是p38MAPK抑制剂的抑制剂，其用作治疗特别是呼吸道配方（IA）的疾病的抗炎剂。其中R 1是式（IIA），（IIB）或（IIC）的基团; 其中m为0或1; T为N或CH; R 2a，R 2b，R 2c独立地选自H，卤素和C 1 -C 6烷基; R3为H或F; R4是-CH3; -C2 H5; -CH 2 OH，CH 2 SCH 3; - SCH3或-SC2H5; R5是-CH3或-C2H5; R6是H或代表一个或多个10个取代基，各自独立地选自C 1 -C 6烷基，羟基，卤素和式（IIIA），（IIIB）和（IIIC）的基团：IA）（IIIB）（IIIC）; 其中R61a和R61b独立地是H或C1-C6烷基，或者R61a和R61b与它们所连接的氮一起形成任选地含有另外选自N和O的杂原子的6元杂环; n为0,1或2; p为1或2; R7为H或F; R8为H或CONH 2。

6. 发明申请

WO2013083206A1 DERIVATIVES OF 4-HYDROXY-1,2,3,4-TETRAHYDRONAPHTALEN-1-YL UREA AND THEIR USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT 审中-公开
标题翻译： 4-羟基-1,2,3,4-四氢萘-1-炔酸的衍生物及其在治疗，相关性，呼吸道感染疾病中的应用
公开(公告)号：WO2013083206A1
公开(公告)日：2013-06-13
申请号：PCT/EP2011/072375
申请日：2011-12-09
申请人： CHIESI FARMACEUTICI S.p.A. , FINCH, Harry , VAN NIEL, Monique Bodil , WOO, Chi-Kit
发明人： FINCH, Harry , VAN NIEL, Monique Bodil , WOO, Chi-Kit
IPC分类号： C07D403/12 , C07D471/04 , A61K31/455 , A61K31/4196 , A61P11/06
CPC分类号： C07D471/04 , A61K9/007 , C07D401/12 , C07D403/12
摘要： Disclosed are compounds having [1,2,4]triazolo[4,3-a] pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
摘要翻译：公开了具有[1,2,4]三唑并[4,3-a]吡啶基团的化合物及其药学上可接受的盐。这些化合物是p38MAPK抑制剂，可用作治疗尤其是呼吸道疾病的抗炎药。

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