专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

51. 发明授权

US08895733B2 Triazine-oxadiazoles 有权
标题翻译：三嗪 - 恶二唑
公开(公告)号：US08895733B2
公开(公告)日：2014-11-25
申请号：US14054221
申请日：2013-10-15
申请人： Oliver Barker , Jonathan Mark Bentley , Mark G. Bock , Thomas Cain , Praful Chovatia , Jennifer Ruth Dod , Florence Eustache , Laura Gleave , Jonathan Hargrave , Alexander Heifetz , Richard Law , Ali Raoof , David Willows
发明人： Oliver Barker , Jonathan Mark Bentley , Mark G. Bock , Thomas Cain , Praful Chovatia , Jennifer Ruth Dod , Florence Eustache , Laura Gleave , Jonathan Hargrave , Alexander Heifetz , Richard Law , Ali Raoof , David Willows
IPC分类号： C07D413/04 , C07D413/14 , A61K31/53 , A61P29/00 , A61K45/06 , C07D498/08 , C07D491/10 , C07D451/02 , C07D491/107 , C07D417/14 , C07D487/04
CPC分类号： C07D413/14 , A61K31/53 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D413/04 , C07D417/14 , C07D451/02 , C07D487/04 , C07D491/10 , C07D491/107 , C07D498/08
摘要： The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.
摘要翻译：本发明涉及式（I）的新衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 用于治疗慢性疼痛的衍生物。

52. 发明授权

US08828951B2 Glycoside derivatives and uses thereof 有权
标题翻译：糖苷衍生物及其用途
公开(公告)号：US08828951B2
公开(公告)日：2014-09-09
申请号：US13614534
申请日：2012-09-13
申请人： Gregory Raymond Bebernitz , Mark G. Bock , Dumbala Srinivas Reddy , Atul Kashinath Hajare , Vinod Vyavahare , Sandeep Bhausaheb Bhosale , Suresh Eknath Kurhade , Videsh Salunkhe , Nadim S. Shaikh , Debnath Bhuniya , P. Venkata Palle , Lili Feng , Jessica Liang
发明人： Gregory Raymond Bebernitz , Mark G. Bock , Dumbala Srinivas Reddy , Atul Kashinath Hajare , Vinod Vyavahare , Sandeep Bhausaheb Bhosale , Suresh Eknath Kurhade , Videsh Salunkhe , Nadim S. Shaikh , Debnath Bhuniya , P. Venkata Palle , Lili Feng , Jessica Liang
IPC分类号： A61K31/70
CPC分类号： A61K31/7052 , A61K31/7048 , A61K31/706 , C07D405/10 , C07D407/10 , C07D413/10 , C07H7/04
摘要： This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
摘要翻译：本发明涉及由式（I）表示的化合物：其中变量如上文所定义，其可用于治疗D-葡萄糖共转运体（SGLT）介导的疾病和病症，例如，糖尿病。本发明还提供了治疗这些疾病和病症以及组合物等的治疗方法。

53. 发明授权

US06919343B2 N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives 有权
标题翻译： N-联苯（取代甲基）氨基环烷基 - 甲酰胺衍生物
公开(公告)号：US06919343B2
公开(公告)日：2005-07-19
申请号：US10354674
申请日：2003-01-30
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
IPC分类号： A61K31/166 , A61K31/24 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/505 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , C07C237/24 , C07D213/82 , C07D239/28 , C07D257/04 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12 , A61K31/165
CPC分类号： C07D257/04 , C07D213/82 , C07D239/28 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

54. 发明授权

US5464788A Tocolytic oxytocin receptor antagonists 失效
标题翻译：溶血性催产素受体拮抗剂
公开(公告)号：US5464788A
公开(公告)日：1995-11-07
申请号：US217270
申请日：1994-03-24
申请人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
发明人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/495 , A61P7/02 , A61P7/10 , A61P9/08 , A61P9/12 , A61P43/00 , C07D211/46 , C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12 , C07D273/00 , C07D413/00 , C07D451/00
CPC分类号： C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl,--CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkylcarbonyl, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
摘要翻译：式X-Y-R化合物或其药学上可接受的盐和酯，其中X为Y是-SO 2 - ， - （CH 2）p - 或-CO-（CH 2）p - ; R是未取代或取代的苯基，其中所述取代基是R5，R6或R7中的一个或多个; R 1是氢，氰基，苯基，-CONHR 2，-CONR 2 R 2， - （CH 2）m OR 2， - （CH 2）pS（O）r -R 2， - （CH 2）m -CO 2 R 2， - （CH 2）m -N 3， - （CH 2）m -NH 2或 - （CH 2）m -NR 2 R 2; R2是氢，C3-8环烷基或C1-5烷基; R 5和R 6各自独立地选自氢，C 1-5烷氧基，卤素或 - （CH 2）n -N（R 2）-C（O）-R 18; R 7是氢或者R 11选自氢，C 1-5烷基羰基，或者被取代的C 1-5烷基，其中所述烷基取代基是未被取代的，一取代，二取代或三取代的吡啶基，其中所述吡啶基独立地选自卤素，C 1-5烷基或C 1-5烷氧基; R 13是未取代的或取代的C 1-10烷基，其中取代基选自-N（R 2）2，-NHR 2或咪唑基; R 14和R 15各自独立地选自C 1-5烷基，C 1-5烷氧基或卤素; R 16是氢或氧代; R 18为C 1-5烷氧基，未取代或取代的C 1-5烷基，其中所述取代基为Het，未取代或取代的C2-5烯基，其中所述取代基为Het或Het; Het是苯并咪唑基，羧甲基取代的苯并咪唑基或吲哚基; m为1〜5的整数， p为1〜3的整数，并且r是0至2的整数。用作催产素和加压素受体拮抗剂的这类化合物。

55. 发明授权

US4812442A Tripeptide renin inhibitors 失效
标题翻译：三肽肾素抑制剂
公开(公告)号：US4812442A
公开(公告)日：1989-03-14
申请号：US45941
申请日：1987-05-04
申请人： Joshua S. Boger , Ben E. Evans , Mark G. Bock
发明人： Joshua S. Boger , Ben E. Evans , Mark G. Bock
IPC分类号： A61K38/00 , C07D233/54 , C07F9/30 , C07F9/32 , C07F9/40 , C07F9/48 , C07F9/6506 , C07K5/02 , C07K5/065 , C07K7/02 , C07K5/06 , C07K5/08 , C07D241/04 , C07D265/30 , C07D211/30 , C07D211/70 , C07D263/02 , C07D207/04
CPC分类号： C07D233/64 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3217 , C07F9/3223 , C07F9/4006 , C07F9/4816 , C07F9/4833 , C07F9/65067 , C07K5/0227 , C07K5/06078 , C07K7/02 , A61K38/00 , Y10S530/86
摘要： Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.
摘要翻译：下式的酶三肽及其类似物抑制肾素，可用于治疗各种形式的肾素相关性高血压，醛固酮增多症和充血性心力衰竭; 含有这些肾素抑制肽的组合物，任选与其它抗高血压药物组合; 以及治疗高血压，醛固酮增多症或充血性心力衰竭的方法，或者在使用新型三肽的这些问题中建立肾素作为致病因素。

56. 发明授权

US4628084A Process for 3-acylamino benzodiazepines 失效
标题翻译： 3-酰基氨基苯并二氮杂卓的方法
公开(公告)号：US4628084A
公开(公告)日：1986-12-09
申请号：US815620
申请日：1986-01-02
申请人： Mark G. Bock , Daniel F. Veber , Robert M. DiPardo
发明人： Mark G. Bock , Daniel F. Veber , Robert M. DiPardo
IPC分类号： C07D243/24
CPC分类号： C07D243/24
摘要： The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl;R' is hydrogen, loweralkyl of from 1-6 carbon atoms, carboxymethyl or carbalkoxymethyl wherein the alkoxy groups contain from 1-4 carbon atoms;X is hydrogen or halogen;Y is hydrogen or halogen.These compounds are useful because of their activity as cholecystokinin (CCK) inhibitors.
摘要翻译：本发明提供了一种改进的下式的3-酰基氨基苯并二氮杂的方法：其中：R是1-6个碳原子的低级烷基，芳基如苯基和卤代苯基，芳烷基，烷氧基，芳烷氧基，吲哚基或取代的吲哚基 R'是氢，1-6个碳原子的低级烷基，羧甲基或烷氧基甲基，其中烷氧基含有1-4个碳原子; X是氢或卤素; Y是氢或卤素。由于它们作为胆囊收缩素（CCK）抑制剂的活性，这些化合物是有用的。

57. 发明授权

US4309430A Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same 失效
标题翻译：吡嗪基-1,2,4-恶二唑-5-酮及其制备方法
公开(公告)号：US4309430A
公开(公告)日：1982-01-05
申请号：US163614
申请日：1980-06-27
申请人： Mark G. Bock , Robert L. Smith
发明人： Mark G. Bock , Robert L. Smith
IPC分类号： C07D413/04 , A61K20060101 , A61K31/42 , A61K31/495 , A61K31/54 , A61P9/12 , C07D20060101 , C07D241/08
CPC分类号： C07D413/04
摘要： The case concerns novel pyrazinyl-1,2,4-oxadiazole-5-ones and processes for preparing the same. The compounds are useful in the treatment of edema and hypertension.
摘要翻译：该案涉及新的吡嗪基-1,2,4-恶二唑-5-酮及其制备方法。该化合物可用于治疗水肿和高血压。

58. 发明授权

US08466114B2 Glycoside derivatives and uses thereof 有权
标题翻译：糖苷衍生物及其用途
公开(公告)号：US08466114B2
公开(公告)日：2013-06-18
申请号：US13425888
申请日：2012-03-21
申请人： Gregory Raymond Bebernitz , Mark G. Bock , Dumbala Srinivas Reddy , Atul Kashinath Hajare , Vinod Vyavahare , Sandeep Bhausaheb Bhosale , Suresh Eknath Kurhade , Videsh Salunkhe , Nadim S. Shaikh , Debnath Bhuniya , P. Venkata Palle , Lili Feng , Jessica Liang
发明人： Gregory Raymond Bebernitz , Mark G. Bock , Dumbala Srinivas Reddy , Atul Kashinath Hajare , Vinod Vyavahare , Sandeep Bhausaheb Bhosale , Suresh Eknath Kurhade , Videsh Salunkhe , Nadim S. Shaikh , Debnath Bhuniya , P. Venkata Palle , Lili Feng , Jessica Liang
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K31/7052 , A61K31/7048 , A61K31/706 , C07D405/10 , C07D407/10 , C07D413/10 , C07H7/04
摘要： This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
摘要翻译：本发明涉及由式（I）表示的化合物：其中变量如上文所定义，其可用于治疗D-葡萄糖共转运蛋白（SGLT）介导的疾病和病症，例如，糖尿病。本发明还提供了治疗这些疾病和病症以及组合物等的治疗方法。

59. 发明授权

US07790754B2 Alpha-hydroxy amides as bradykinin antagonists or inverse agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反向激动剂
公开(公告)号：US07790754B2
公开(公告)日：2010-09-07
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl.
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra。（5）（CH2）k-杂环，其任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）5元杂芳族环，其具有选自NO和S的环杂原子，并且任选地具有至多3个另外的环氮原子，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基。

60. 发明授权

US06908921B2 Quinoxalinone derivatives as bradykinin B1 antagonists 失效
标题翻译：喹喔啉酮衍生物作为缓激肽B1拮抗剂
公开(公告)号：US06908921B2
公开(公告)日：2005-06-21
申请号：US10614539
申请日：2003-07-07
申请人： Dai-Shi Su , Mark G. Bock
发明人： Dai-Shi Su , Mark G. Bock
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D409/14 , C07D471/04 , A01N43/58 , A01N43/60 , A61K31/495 , A61K31/50 , C07D241/36
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D409/14 , C07D471/04
摘要： 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： 2-喹喔啉酮衍生物是缓激肽B1拮抗剂或反激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

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