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1. 发明申请

US20130225617A1 INDOLES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：吲哚及其治疗用途
公开(公告)号：US20130225617A1
公开(公告)日：2013-08-29
申请号：US13755727
申请日：2013-01-31
申请人： PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
发明人： George Hynd , John Gary Montana , Harry Finch , Rosa Arienzo , Barbara Avitabile-Woo , Mathias Domostoj
IPC分类号： C07D209/12 , C07D417/14 , C07D409/06 , C07D417/06 , C07D403/06 , C07D403/12 , C07D401/06
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
摘要翻译：本发明的化合物是CRTH2受体的配体，尤其用于治疗炎性病症。

2. 发明申请

US20190276405A1 CRYSTAL OF QUINOLINE DERIVATIVE 审中-公开
公开(公告)号：US20190276405A1
公开(公告)日：2019-09-12
申请号：US16302553
申请日：2017-05-15
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： Donald John Daley , John Gary Montana , George Hynd , Mitsuru Teramoto , Takahiro Ito , Taro Tameyama
IPC分类号： C07D215/22
摘要： Crystals of [8-chloro-3-(4-chlorobenzyl)-4-difluoromethoxy-2-ethylquinolin-5-yloxy]acetic acid L-lysine salt, i.e., a crystal A which has peaks at diffraction angles 2θ=6.0°, 10.0°, 10.7°, 12.1°, 18.4°, 19.2° and 20.1° in powder X-ray diffraction spectra and a crystal B which has peaks at diffraction angles 2θ=6.0°, 11.7°, 12.4°, 15.2°, 16.4°, 20.3° and 22.6° in powder X-ray diffraction spectra. These crystals are chemically stable and have excellent thermal stability and physical properties, and are therefore suitable as medicinal substances.

3. 发明申请

WO2010142934A1 INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS 审中-公开
标题翻译：作为CRTH2受体配体的衍生物
公开(公告)号：WO2010142934A1
公开(公告)日：2010-12-16
申请号：PCT/GB2009/050671
申请日：2009-06-12
申请人： PULMAGEN THERAPEUTICS (ASTHMA) LIMITED , HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
发明人： HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
IPC分类号： C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , A61P37/00 , A61K31/4439 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , A61K31/4178 , A61K31/422 , A61K31/404
CPC分类号： C07D417/14 , C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid, [3-(5-benzenesulfonyloxazol-4-ylmethyl)-5-fluoro-2-methylindol-1-yl]acetic acid, [3-(3-benzenesulfonyl-4-met ylthiophen-2-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {5-fluoro-2-methyl-3-[2-(pyridin-2-ylsulfamoyl)benzyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[4-methyl-3-(pyridine-2-sulfonyl)thiophen-2- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[3-methyl-5-(pyridine-2-sulfonyl)-3H-imidazol-4- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-3-[2-(3-fluorophenylsulfamoyl)pyridin-3-ylmethyl]-2-methylindol-1- yl}acetic acid, [3-(4-benzenesulfonyloxazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {3-[2-(3-cyanophenylsulfamoyl)benzyl]-5-fluoro-2-methylindol-1-yl}acetic acid, [3-(4-benzenesulfonylthiazol-5-ylmethyl)-5-chloro-2-methyl-indol-1-yl]acetic acid, [3-(4-benzenesulfonyl-2-methylthiazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, and [3-(4-benzenesulfonyl-3-methylisothiazol-5-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid.
摘要翻译：以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂：{3- [3-氯-4-（吡啶-2-磺酰基）异噻唑-5-基甲基] -5-氟-2-甲基吲哚-1-基} 乙酸，[3-（5-苯磺酰基-3-甲基-3H-咪唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸[3-（5-苯磺酰基恶唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸，[3-（3-苯磺酰基-4-甲基噻吩-2-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸， {5-氟-2-甲基-3- [2-（吡啶-2-基氨磺酰基）苄基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [4-甲基-3- （吡啶-2-磺酰基）噻吩-2-基甲基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [3-甲基-5-（吡啶-2-磺酰基）咪唑-4-基甲基]吲哚-1-基}乙酸，{5-氟-3- [2-（3-氟苯基氨磺酰基）吡啶-3-基甲基] -2-甲基吲哚-1-基}乙酸[3 - （4-苯磺酰氧基-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸{3- [2-（3-氰基苯基氨磺酰基）苄基] -5-氟-2-甲基吲哚-1-基] 乙酸，[3- （4-苯磺酰基噻唑-5-基甲基）-5-氯-2-甲基 - 吲哚-1-基]乙酸[3-（4-苯磺酰基-2-甲基噻唑-5-基甲基）-5-氟-2- 甲基吲哚-1-基]乙酸和[3-（4-苯磺酰基-3-甲基异噻唑-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸。

4. 发明授权

EP2229358B1 INDOLES AND THEIR THERAPEUTIC USE 有权
标题翻译：吲哚和治疗用途
公开(公告)号：EP2229358B1
公开(公告)日：2011-03-23
申请号：EP08862784.9
申请日：2008-12-12
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry , ARIENZO, Rosa , AVITABILE-WOO, Barbara , DOMOSTOJ, Mathias
IPC分类号： C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/404
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Compound of formula (I) are are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is -SO2- or *-SO2NR3- wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3- C7cycloalkyl, -O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3- C3- C7cycloalkyl, -O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.

5. 发明授权

EP1928457B1 QUINOLINES AND THEIR THERAPEUTIC USE 有权转让
标题翻译： CHINO LINE及其治疗应用
公开(公告)号：EP1928457B1
公开(公告)日：2012-12-12
申请号：EP06779591.4
申请日：2006-09-29
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
IPC分类号： A61K31/47 , A61P11/00 , A61P43/00
CPC分类号： C07D215/233 , A61K31/47 , C07D215/12 , C07D215/18 , C07D215/20 , C07D215/227 , C07D215/36 , C07D215/48 , C07D401/04 , C07D401/10 , C07D401/12

6. 发明授权

EP2327693B9 Indoles and their therapeutic use 有权
标题翻译：吲哚及其治疗用途
公开(公告)号：EP2327693B9
公开(公告)日：2012-10-24
申请号：EP10193389.3
申请日：2008-12-12
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： Hynd, George , Montana, John Gary , Finch, Harry , Arienzo, Rosa , Avitabile-Woo, Barbara , Domostoj, Mathias
IPC分类号： C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/404
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14

7. 发明授权

EP2139881B1 QUINOLINES AND THEIR THERAPEUTIC USE 失效转让
标题翻译： CHINO LINE及其治疗用途
公开(公告)号：EP2139881B1
公开(公告)日：2011-11-09
申请号：EP08736891.6
申请日：2008-04-03
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： MONTANA, John, Gary , FINCH, Harry , HYND, George , CRAMP, Michael, Colin , ARIENZO, Rosa , MCLEAN, Neville
IPC分类号： C07D401/10 , C07D413/10 , C07D417/10 , C07D215/227 , C07D215/233 , A61K31/4709 , A61P11/00
CPC分类号： C07D401/10 , C07D215/227 , C07D215/233 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently -OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6alkyl or C3-C6cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is -CH2-, -S-, or -O-; one of Y and Y1 is hydrogen and the other is OR6, -C(=O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.

8. 发明公开

EP2245010A1 INDOLES ACTIVE ON CRTH2 RECEPTOR 审中-公开
标题翻译：对受体CRTH2 ACTING吲哚
公开(公告)号：EP2245010A1
公开(公告)日：2010-11-03
申请号：EP09701632.3
申请日：2009-01-16
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry
IPC分类号： C07D209/22 , A61K31/405 , A61P29/00
CPC分类号： C07D209/22
摘要： Indole derivatives having therapeutic utility are of formula (I): X is -SO2- or *-SO2NR3- wherein the bond marked with an asterisk is attached to Ar1; R1 and R2 are, independently, hydrogen, fluoro, chloro, CN or CF3; R3 is hydrogen, C1-C8alkyl or C3-C7cycloalkyl; and Ar1 and Ar2 are, independently, phenyl or a 5- or 6-membered heteroaryl group, wherein the phenyl or heteroaryl group is optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, -O(C1-C4alkyl) or C1-C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.

9. 发明授权

EP2129661B1 QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS 有权
标题翻译：喹啉，CRTH2受体配体
公开(公告)号：EP2129661B1
公开(公告)日：2012-02-08
申请号：EP07732192.5
申请日：2007-03-29
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： RAY, Nicholas, Charles , FINCH, Harry , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , MONTANA, John, Gary
IPC分类号： C07D215/20 , C07D215/22 , A61K31/47 , A61P11/00 , A61P29/00
CPC分类号： C07D215/233 , C07D215/20 , C07D215/227
摘要： Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component.

10. 发明公开

EP2327693A1 Indoles and their therapeutic use 有权
标题翻译： Indole und ihre therapeutische Verwendung
公开(公告)号：EP2327693A1
公开(公告)日：2011-06-01
申请号：EP10193389.3
申请日：2008-12-12
申请人： Pulmagen Therapeutics (Asthma) Limited
发明人： Hynd, George , Montana, John Gary , Finch, Harry , Arienzo, Rosa , Avitabile-Woo, Barbara , Domostoj, Mathias
IPC分类号： C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/404
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Compound of formula (I) are are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions:

wherein X is -SO 2 - or *-SO 2 NR 3 - wherein the bond marked with an asterisk is attached to Ar 1 ; R 1 is hydrogen, fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; R 3 is hydrogen, C 1 -C 8 alkyl or C 3 -C 7 cycloalkyl; Ar 1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C 3 -C 7 cycloalkyl, -O(C 1 -C 4 alkyl) or C 1 -C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar 2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C 3 -C 7 cyCloalkyl, -O(C 1 -C 4 alkyl) or C 1 -C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
摘要翻译：式（I）化合物是CRTH2受体的配体，特别用于治疗炎性病症：其中X是-SO 2 - 或* -SO 2 NR 3 - ，其中标有星号的键连接到Ar 1 ; R 1是氢，氟，氯，CN或CF 3; R 2是氢，氟或氯; R 3是氢，C 1 -C 8烷基或C 3 -C 7环烷基; Ar 1是苯基或选自呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基的5-或6-元杂芳基，其中苯基或杂芳基任选被一个或多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选地被一个或多个氟原子; 并且Ar 2是苯基或选自吡咯基，呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基中的5-或6-元杂芳基，其中苯基或杂芳基是任选的被一个或多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基取代，后两个基团任选地被一个或多个更多的氟原子。

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