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1. 发明申请

US20140248357A1 Respiratory Disease Treatment 有权
标题翻译：呼吸系统疾病治疗
公开(公告)号：US20140248357A1
公开(公告)日：2014-09-04
申请号：US14246695
申请日：2014-04-07
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED
发明人： Harry Finch , Craig Fox , Mohammed Sajad , Monique Bondil Van Niel , Andrew Forrest
IPC分类号： A61K31/4439 , A61K31/58 , A61K31/573 , A61K31/56 , A61K45/06
CPC分类号： A61K31/4439 , A61K9/0075 , A61K31/56 , A61K31/573 , A61K31/58 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.
摘要翻译：描述了适于通过吸入肺部施用的药物组合物，其中所述组合物包含格列酮和一种或多种药学上可接受的载体和/或赋形剂，其中所述组合物的格列酮含量由至少95重量％的5R对映体和小于5重量％的5S对映异构体，并且其中格列酮为吡格列酮或罗格列酮或其药学上可接受的盐，并且其中所述格列酮为微粒形式。

2. 发明授权

US09078885B2 Respiratory disease treatment 有权
标题翻译：呼吸系统疾病治疗
公开(公告)号：US09078885B2
公开(公告)日：2015-07-14
申请号：US14246695
申请日：2014-04-07
申请人： Pulmagen Therapeutics (Inflammation) Limited
发明人： Harry Finch , Craig Fox , Mohammed Sajad , Monique Bondil Van Niel , Andrew Forrest
IPC分类号： A01N43/00 , A61K31/33 , A61K31/4439 , A61K9/00 , A61K45/06 , A61K31/56 , A61K31/573 , A61K31/58
CPC分类号： A61K31/4439 , A61K9/0075 , A61K31/56 , A61K31/573 , A61K31/58 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.
摘要翻译：描述了适于通过吸入肺部施用的药物组合物，其中所述组合物包含格列酮和一种或多种药学上可接受的载体和/或赋形剂，其中所述组合物的格列酮含量由至少95重量％的5R对映体和小于5重量％的5S对映异构体，并且其中格列酮为吡格列酮或罗格列酮或其药学上可接受的盐，并且其中所述格列酮为微粒形式。

3. 发明申请

WO2011098801A1 INFLAMMATORY DISEASE TREATMENT 审中-公开
标题翻译：炎症性疾病治疗
公开(公告)号：WO2011098801A1
公开(公告)日：2011-08-18
申请号：PCT/GB2011/050226
申请日：2011-02-09
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , FINCH, Harry , FOX, Craig
发明人： FINCH, Harry , FOX, Craig
IPC分类号： A61K31/192 , A61P29/00
CPC分类号： A61K31/192 , A61K9/0073
摘要： Compounds of formula (I) are useful in the treatment of inflammatory disease wherein at least 95% by weight of the said compound of formula (I) is in the stereoconfiguration shown in formula (IA) and less than 5% by weight is in the stereoconfiguration shown in formula (IB) in which formulae (I), (IA) and (IB): R is CH 3 - or hydrogen; X 1 is -OR 1 , -S(O) n R 2 or -NR 3 R 4 and X 2 is-OH; or X 1 and X 2 taken together represent a radical *-OC(O)NH-** or *-C(O)N(H)O-** wherein the bond marked * is attached to the carbon to which W and R are attached, and the bond marked ** is attached to the carbonyl carbon; R 1 and R 2 are independently C 1-6 alkyl optionally substituted with one or more halogen atoms; C 1-6 alkoxyalkyl; or aryl R 3 and R 4 are independently hydrogen; C 1-6 alkyl; aryl; a group -C(R a )=C(R b )-C(=O)-Ar a wherein R a and R b are independently hydrogen or C 1-6 alkyl and Ar a is aryl; or a group -Ar b -C(=O)-Ar c wherein Ar b and Ar c are aryl; or -C(=O)O-R c wherein R c is an aryl or C 1-6 alkyl; or R 3 and R 4 taken together with the nitrogen to which they are attached form a saturated ring of 3 to 7 ring members or an unsaturated ring of 5 to 7 ring members; n is 0,1 or 2; W is a group which when linked to the -C(R)(X 1 )C(=O)X 2 results in a compound (I) having PPARγ agonist activity.
摘要翻译：式（I）化合物可用于治疗炎性疾病，其中至少95重量％的所述式（I）化合物为式（IA）所示的立体构型，小于5重量％为其中式（I），（IA）和（IB）：R是CH 3或氢的式（IB）所示的立体构型; X1为-OR1，-S（O）nR2或-NR3R4，X2为-OH; 或X 1和X 2一起表示基团* -OC（O）NH - **或* -C（O）N（H）O - **，其中标记*的键连接到W和R为并且标记为**的键连接到羰基碳上; R1和R2独立地为任选被一个或多个卤素原子取代的C 1-6烷基; C 1-6烷氧基烷基; 或芳基R 3和R 4独立地为氢; C 1-6烷基芳基; 基团-C（Ra）= C（Rb）-C（= O）-Ara，其中R a和R b独立地是氢或C 1-6烷基，Ara是芳基; 或Arb-C（= O）-Arc基团，其中Arb和Arc为芳基; 或-C（= O）O-Rc，其中R c是芳基或C 1-6烷基; 或者R 3和R 4与它们所连接的氮一起形成3至7个环成员的饱和环或5至7个环成员的不饱和环; n为0,1或2; W是与-C（R）（X1）C（= O）X2连接的基团，得到具有PPAR 3的化合物（I）激动剂活性。

4. 发明申请

WO2011110859A1 PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF RESPIRATORY DISEASES SUCH AS COPD 审中-公开
标题翻译：吡嗪衍生物及其在治疗呼吸道疾病如COPD中的应用
公开(公告)号：WO2011110859A1
公开(公告)日：2011-09-15
申请号：PCT/GB2011/050478
申请日：2011-03-10
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
IPC分类号： C07D487/04 , A61K31/519 , A61P1/00 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C-R 1 or N; -X 1 -X 2 - is CR 15 =N- or -NR 19 -CO-; and R 1 -R 6 , R 15 and R 16 are as defined in the claims.
摘要翻译：式（I）化合物是中性粒细胞弹性蛋白酶抑制剂，其中A是C-R1或N; -X1-X2-是CR15 = N-或-NR19-CO-; 和R 1 -R 6，R 15和R 16如权利要求中所定义。

5. 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。

6. 发明申请

WO2010094955A1 PYRIMIDOPYRIDAZINE DERIVATIVES USEFUL AS P38 MAPK INHIBITORS 审中-公开
标题翻译： P38 MAPK抑制剂有用的吡咯烷酮衍生物
公开(公告)号：WO2010094955A1
公开(公告)日：2010-08-26
申请号：PCT/GB2010/050256
申请日：2010-02-16
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , BESWICK, Amanda , WASZKOWYCZ, Bohdan
发明人： BESWICK, Amanda , WASZKOWYCZ, Bohdan
IPC分类号： C07D237/14 , C07D237/18 , C07D403/12 , C07D487/04
CPC分类号： C07D487/04 , C07D237/14 , C07D237/18 , C07D403/12
摘要： A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.
摘要翻译：化合物式（IA）或（IB），或其药学上可接受的; 其中取代基如权利要求中所定义，及其用作P38 MAP激酶。

7. 发明申请

WO2011110858A1 PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF RESPIRATORY DISEASES SUCH AS COPD 审中-公开
标题翻译：吡嗪衍生物及其在治疗呼吸道疾病如COPD中的应用
公开(公告)号：WO2011110858A1
公开(公告)日：2011-09-15
申请号：PCT/GB2011/050477
申请日：2011-03-10
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
IPC分类号： C07D487/04 , A61K31/519 , A61P1/00 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C-R 1 or N; -X 1 -X 2 - is CR 15 =N- or -NR 19 -CO-; and R 1 -R 6 , R 15 , R 15 and R 19 are as defined in the claims.
摘要翻译：式（I）化合物是中性粒细胞弹性蛋白酶抑制剂，其中A是C-R1或N; -X1-X2-是CR15 = N-或-NR19-CO-; 并且R 1 -R 6，R 15，R 15和R 19如权利要求中所定义。

8. 发明申请

WO2011098799A2 RESPIRATORY DISEASE TREATMENT 审中-公开
标题翻译：呼吸道疾病治疗
公开(公告)号：WO2011098799A2
公开(公告)日：2011-08-18
申请号：PCT/GB2011/050224
申请日：2011-02-09
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , FINCH, Harry , FOX, Craig
发明人： FINCH, Harry , FOX, Craig
IPC分类号： A61K9/00 , A61K31/427 , A61K31/4439 , C07D413/12
CPC分类号： C07D417/12 , A61K9/0075 , A61K9/008 , A61K31/427 , A61K31/4439
摘要： A pharmaceutical composition containing the compound 5-{4-[2-(5-ethyl-pyridin-2-yl)-2-hydroxy-ethoxy]-benzyl}-thiazolidine-2,4-dιone, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers and/or excipients, characterised in that at least 95% by weight of the 5-{4-[2-(5-ethyl-pyridin-2-yl)-2- hydroxy-ethoxy]-benzyl}-thiazolidine-2,4-dione content of the composition is the diastereomeric form 5(R)-{4-[2-(5-ethyl-pyridin-2-yI)=2(S)-hydroxy-ethoxy]=benzyl}- thiazolidιne-2,4-dione and less than 5% by weight is one or more of the other three diastereomeric forms.
摘要翻译：含有化合物5- {4- [2-（5-乙基 - 吡啶-2-基）-2-羟基 - 乙氧基] - 苄基} - 噻唑烷-2,4-d 1的药物组合物或药学上可接受的其盐和一种或多种药学上可接受的载体和/或赋形剂，其特征在于至少95重量％的5- {4- [2-（5-乙基 - 吡啶-2-基）-2-羟基 - 乙氧基] - 苄基} - 噻唑烷-2,4-二酮含量为非对映体形式5（R） - {4- [2-（5-乙基 - 吡啶-2-基）] = 2（S） - 羟基 - 乙氧基] =苄基} - 噻唑烷-2,4-二酮，并且小于5重量％是其它三种非对映体形式中的一种或多种。

9. 发明申请

WO2010076553A1 SULFONAMIDE COMPOUNDS FOR THE TREATMENT OF RESPIRATORY DISORDERS 审中-公开
标题翻译：用于治疗呼吸道疾病的磺酰胺化合物
公开(公告)号：WO2010076553A1
公开(公告)日：2010-07-08
申请号：PCT/GB2009/002951
申请日：2009-12-23
申请人： DR. REDDY'S LABORATORIES LTD , PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , RAMDOS, Vidya , FINCH, Harry , FOX, Craig
发明人： RAMDOS, Vidya , FINCH, Harry , FOX, Craig
IPC分类号： C07D231/18 , A61K31/415 , A61P11/00
CPC分类号： C07D231/18
摘要： Compounds of formula (I) are agonists of PPARγ, useful for the treatment of respiratory disease; formula (I): wherein R 1 , R 2 or R 3 each independently represents halo, cyano, nitro, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxylic acid or an ester or amide thereof; R 4 represents hydrogen or alkyl; m, n or p independently represents 0, 1, 2 or 3.
摘要翻译：式（I）化合物是PPARγ的激动剂，可用于治疗呼吸系统疾病; 式（I）：其中R 1，R 2或R 3各自独立地表示卤素，氰基，硝基，氨基，烷基，卤代烷基，烷氧基，卤代烷氧基，羧酸或其酯或酰胺; R4表示氢或烷基; m，n或p独立地表示0,1,2或3。

10. 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。

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