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1. 发明授权

US07521448B2 N-substituted benzimidazolyl c-Kit inhibitors 失效
标题翻译： N-取代苯并咪唑c-Kit抑制剂
公开(公告)号：US07521448B2
公开(公告)日：2009-04-21
申请号：US10921414
申请日：2004-08-16
申请人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Ayako Honda , Radoslaw Laufer , An-Hu Li , Kristen Mulvihill , Li Qiu , Colin Peter Sambrook Smith , Yingchaun Sun , Graham Michael Wynne , Tao Zhang
发明人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Ayako Honda , Radoslaw Laufer , An-Hu Li , Kristen Mulvihill , Li Qiu , Colin Peter Sambrook Smith , Yingchaun Sun , Graham Michael Wynne , Tao Zhang
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D235/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

2. 发明授权

US07696225B2 (2-carboxamido)(3-Amino) thiophene compounds 失效
标题翻译：（2-甲酰氨基）（3-氨基）噻吩化合物
公开(公告)号：US07696225B2
公开(公告)日：2010-04-13
申请号：US10973870
申请日：2004-10-26
申请人： Jason Bloxham , Andrew Phillip Crew , Ayako Honda , An-Hu Li , Bijoy Panicker , Graham Michael Wynne , Lawrence Tardibono, Jr.
发明人： Jason Bloxham , Andrew Phillip Crew , Ayako Honda , An-Hu Li , Bijoy Panicker , Graham Michael Wynne , Lawrence Tardibono, Jr.
IPC分类号： A61K31/4745 , A61K31/4709 , A61K31/4436
CPC分类号： A61K31/381 , A61K31/437 , A61K31/4436 , A61K31/4709 , A61K31/4745 , A61K45/06 , C07D409/12 , C07D409/14 , C07D471/04 , A61K2300/00
摘要： Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
摘要翻译：进一步被杂芳基甲基氨基取代的酰胺芳基/酰胺基芳基取代的噻吩可用于治疗癌症。

3. 发明授权

US06949563B2 (2-carboxamido)(3-amino)thiophene compounds 有权
标题翻译：（2-甲酰氨基）（3-氨基）噻吩化合物
公开(公告)号：US06949563B2
公开(公告)日：2005-09-27
申请号：US10752342
申请日：2004-01-06
申请人： Graham Michael Wynne , Kevin Doyle , Saleh Ahmed , An-Hu Li , John Fraser Keily , Chrystelle Marie Rasamison , Neil Anthony Pegg , Imaad Saba , Claire Thomas , Don Smyth , Shazia Sadiq , Gary Newton , Graham Dawson , Andrew Phillip Crew , Arlindo Lucas Castelhano
发明人： Graham Michael Wynne , Kevin Doyle , Saleh Ahmed , An-Hu Li , John Fraser Keily , Chrystelle Marie Rasamison , Neil Anthony Pegg , Imaad Saba , Claire Thomas , Don Smyth , Shazia Sadiq , Gary Newton , Graham Dawson , Andrew Phillip Crew , Arlindo Lucas Castelhano
IPC分类号： A61K31/381 , A61K31/437 , A61K31/4436 , A61K31/4709 , A61K31/4745 , A61K45/06 , C07D409/12 , C07D409/14 , C07D471/04 , C07D49/02
CPC分类号： C07D409/12 , A61K31/165 , A61K31/22 , A61K31/277 , A61K31/381 , A61K31/437 , A61K31/4436 , A61K31/444 , A61K31/4709 , A61K31/4745 , A61K45/06 , C07D409/14 , C07D471/04 , A61K2300/00
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C0-4alkyl, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物，其中R1是R2，R3是C0-4-4烷基，可用于治疗癌症。

4. 发明申请

US20110142855A1 Compounds Having CRTH2 Antagonist Activity 有权
标题翻译：具有CRTH2拮抗作用的化合物
公开(公告)号：US20110142855A1
公开(公告)日：2011-06-16
申请号：US13014314
申请日：2011-01-26
申请人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
发明人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
IPC分类号： A61K39/395 , A61K31/4439 , A61K31/47 , A61K31/573 , A61K31/519 , A61K31/58 , A61K31/7135 , A61K33/24 , A61P31/12 , A61P31/00 , A61P37/02 , A61P11/06
CPC分类号： A61K31/4439 , A61K31/47 , A61K45/06 , C07D401/06
摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

5. 发明授权

US07919512B2 Compounds having CRTH2 antagonist activity 有权
标题翻译：具有CRTH2拮抗活性的化合物
公开(公告)号：US07919512B2
公开(公告)日：2011-04-05
申请号：US12828800
申请日：2010-07-01
申请人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
发明人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
IPC分类号： A61K31/44 , C07D401/00
CPC分类号： A61K31/4439 , A61K31/47 , A61K45/06 , C07D401/06
摘要： Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（II）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

6. 发明申请

US20100305120A1 COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY 审中-公开
标题翻译：用于治疗肌肉晶状体的化合物
公开(公告)号：US20100305120A1
公开(公告)日：2010-12-02
申请号：US12599963
申请日：2009-04-03
申请人： Graham Michael Wynne , Stephen Paul Wren , Renate Maria Van Well , Daniel Robert Chancellor , Frank Schroer , Francis Xavier Wilson
发明人： Graham Michael Wynne , Stephen Paul Wren , Renate Maria Van Well , Daniel Robert Chancellor , Frank Schroer , Francis Xavier Wilson
IPC分类号： A61K31/5377 , A61K31/498 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/4245 , A61K31/428 , A61K31/427 , A61K31/423 , A61K31/422 , A61K31/416 , C07D413/10 , C07D231/56 , A61P21/00
CPC分类号： A61K31/428 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/498 , A61K31/5377 , C07D231/56 , C07D405/12
摘要： Compounds of formula (I): wherein X, L1, R1, L2, R2, R3, and R4 are as defined herein, are useful in the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.
摘要翻译：式（I）化合物：其中X，L1，R1，L2，R2，R3和R4如本文所定义，可用于治疗或预防杜氏肌营养不良症，贝克肌营养不良症或恶病质。

7. 发明授权

US07750027B2 Compounds having CRTH2 antagonist activity 有权
标题翻译：具有CRTH2拮抗活性的化合物
公开(公告)号：US07750027B2
公开(公告)日：2010-07-06
申请号：US12625497
申请日：2009-11-24
申请人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
发明人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： A61K31/4439 , A61K31/47 , A61K45/06 , C07D401/06
摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

8. 发明申请

US20090075938A1 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY 有权
标题翻译：杜氏肌肉晶状体的治疗
公开(公告)号：US20090075938A1
公开(公告)日：2009-03-19
申请号：US12278769
申请日：2007-02-09
申请人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
发明人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
IPC分类号： A61K31/675 , C07D307/87 , A61K31/343 , A61K31/404 , C07D209/04 , A61K31/428 , C07D277/62 , C07D263/54 , A61K31/423 , A61P21/00 , A61K31/4184 , C07D235/04 , C07D413/02 , A61K31/4439 , A61K31/5383 , C07D498/04 , A61K31/5377
CPC分类号： C07F9/4003 , A61K31/343 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377
摘要： There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C═W, NR4, NC(═O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pair of A1-A4 each represent CR1, then the adjacent carbon atoms, together with their substituents may form a ring B, when X is CR6R7, R6 and R7, together with the carbon atom to which they are attached may form a ring C, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the therapeutic and/or prophylactic treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia.
摘要翻译：公开了式（1）的化合物：A1，A2，A3和A4可以相同或不同，表示N或CR1，X是选自O，S（O）n，CW，NR4，NC （-O）R 5和CR 6 R 7，W是O，S，NR 20，Y是N或CR 8，R 4，R 5，R 6，R 8，R 9和NR 20中的一个表示-L-R 3，其中L是单键或连接基团另外，可以相同或不同的R 1，R 3 -R 9独立地表示氢或取代基，R 20表示氢，羟基，任选被芳基取代的烷基，任选被芳基，芳基，CN任意取代的烷氧基，任选取代烷氧基，任选取代的芳氧基，任选取代的烷酰基，任选取代的芳酰基，NO 2，NR 30 R 31，其中R 30和R 31可以相同或不同，表示氢，任选取代的烷基或任选取代的芳基; 此外，R30和R31中的一个可以表示任选取代的烷酰基或任选取代的芳酰基，n表示0至2的整数，此外，当相邻的一对A1-A4各自表示CR1时，则相邻的碳原子连同它们取代基可以形成环B，当X是CR 6 R 7，R 6和R 7时，连同它们所连接的碳原子一起形成环C或其药学上可接受的盐在制备用于治疗和/ 或预防性治疗杜氏肌营养不良症，贝克肌营养不良症或恶病质。

9. 发明授权

US08268878B2 Compounds having CRTH2 antagonist activity 有权
标题翻译：具有CRTH2拮抗活性的化合物
公开(公告)号：US08268878B2
公开(公告)日：2012-09-18
申请号：US13180157
申请日：2011-07-11
申请人： Richard Edward Armer , Graham Michael Wynne , Colin Richard Dorgan , Peter David Johnson
发明人： Richard Edward Armer , Graham Michael Wynne , Colin Richard Dorgan , Peter David Johnson
IPC分类号： A61K31/40 , C07D209/04
CPC分类号： C07D407/10
摘要： Compounds of general formula (I) wherein R is phenyl optionally substituted with one or more halo substituents; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物，其中R是任选被一个或多个卤素取代基取代的苯基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

10. 发明申请

US20110195932A1 Drug Combinations for the Treatment of Duchenne Muscular Dystrophy 有权
标题翻译：药物组合治疗杜氏肌营养不良症
公开(公告)号：US20110195932A1
公开(公告)日：2011-08-11
申请号：US12600242
申请日：2008-08-01
申请人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
发明人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
IPC分类号： A61K31/675 , C07D307/79 , A61K31/343 , C07D209/08 , A61K31/4045 , C07D277/66 , A61K31/428 , C07D235/04 , A61K31/4184 , C07D263/58 , A61K31/423 , C07D413/02 , A61K31/5377 , C07F9/653 , A61K31/573 , A61K31/58 , A61P21/00
CPC分类号： A61K31/573 , A61K31/423 , A61K45/06 , C07D263/58 , A61K2300/00
摘要： Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.
摘要翻译：包含（或基本上由）一种或多种式（1）化合物与一种或多种辅助试剂组合的组合，以及组合的各种治疗用途。还提供了含有组合的药物组合物以及使用这些组合治疗杜氏肌营养不良症，贝克肌营养不良症或恶病质的方法。

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