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61. 发明授权

US5189050A Fermentation analogs of Virginiamycin M.sub.1 to treat panic and anxiety disorder 失效
标题翻译： VIRGINIAMYCIN M1的发酵模拟物治疗神经性和恶性疾病
公开(公告)号：US5189050A
公开(公告)日：1993-02-23
申请号：US709676
申请日：1991-06-03
申请人： Roger M. Freidinger , Mark G. Bock , Yiu-Kuen T. Lam , Raymond S. Chang , Otto D. Hensens , Cheryl D. Schwartz , Deborah L. Zink
发明人： Roger M. Freidinger , Mark G. Bock , Yiu-Kuen T. Lam , Raymond S. Chang , Otto D. Hensens , Cheryl D. Schwartz , Deborah L. Zink
IPC分类号： A61K31/42 , A61K38/00 , A61P25/00 , A61P25/20 , A61P25/30 , A61P27/02 , A61P35/00 , C07D498/18 , C07K5/078 , C12P17/18 , C12R1/58
CPC分类号： C07K5/06182 , A61K38/00
摘要： Pharmaceutical compositions containing Virginiamycin M.sub.1 having the Formula: ##STR1## and Virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

62. 发明授权

US4661473A Renin inhibitors containing peptide isosteres 失效
标题翻译：含有等位基因的肾素抑制剂
公开(公告)号：US4661473A
公开(公告)日：1987-04-28
申请号：US593758
申请日：1984-03-27
申请人： Joshua S. Boger , Mark G. Bock
发明人： Joshua S. Boger , Mark G. Bock
IPC分类号： C07D233/90 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/27 , A61K38/00 , A61P9/12 , A61P43/00 , C07C67/00 , C07C239/00 , C07C269/00 , C07D233/64 , C07F9/30 , C07F9/58 , C07K5/02 , C07K5/04 , C07K7/04 , C07K7/06 , C07K14/81 , A61K37/43 , C07K7/02
CPC分类号： C07K7/06 , C07K5/0227 , A61K38/00 , Y10S530/86
摘要： Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
摘要翻译：式（Ⅰ）及其类似物的肾素抑制肽抑制肾素，可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。

63. 发明授权

US4390703A Intermediates for the resolution of some interphenylene-9-thia-11-oxo-12-azaprostanoic acids 失效
标题翻译：一些亚氨基苯基-9-硫代-11-氧代-12-氮杂前列腺酸的分离中间体
公开(公告)号：US4390703A
公开(公告)日：1983-06-28
申请号：US276117
申请日：1981-06-22
申请人： Mark G. Bock , Robert M. Di Pardo
发明人： Mark G. Bock , Robert M. Di Pardo
IPC分类号： C07D277/14 , C07D417/12 , C07D277/04
CPC分类号： C07D417/12 , C07D277/14
摘要： Some derivatives of interphenylene-9-thia-11-oxo-12-azaprostanoic acid which are active renal vasodilator agents are resolved via diastereomeric camphanyl or camphorcarbonyl esters. Upon hydrolysis, the separated diastereoisomers yield optically pure enantiomers.
摘要翻译：作为活性肾血管扩张剂的间苯二甲酸-9-硫代-11-氧代-12-氮杂前列腺酸的一些衍生物通过非对映异亮氨酰樟脑基或樟脑羰基酯分解。水解后，分离的非对映异构体产生光学纯对映异构体。

64. 发明授权

US4362724A Method of treating edema and hypertension and pharmaceutical composition therefor in which the active ingredient comprises a novel substituted pyrazinyl-1,2,4-oxadiazole and a kaliuretic diuretic 失效
标题翻译：治疗水肿和高血压的方法及其药物组合物，其中活性成分包含新的取代的吡嗪基-1,2,4-恶二唑和卡利利特利尿剂
公开(公告)号：US4362724A
公开(公告)日：1982-12-07
申请号：US244509
申请日：1981-03-16
申请人： Mark G. Bock , Edward J. Cragoe, Jr. , Robert L. Smith
发明人： Mark G. Bock , Edward J. Cragoe, Jr. , Robert L. Smith
IPC分类号： C07D241/26 , A61K31/50
CPC分类号： C07D241/26
摘要： Novel pyrazinyl -1,2,4-oxadiazoles of the formulas: ##STR1## are useful in treating edema and hypertension, and particularly may be combined with kaliuretic diuretics such as hydrochlorothiazide and indacrinone.
摘要翻译：具有下式的新颖的吡嗪基-1,2,4-恶二唑可用于治疗水肿和高血压，特别是可以与卡利利特利尿剂如氢氯噻嗪和依卡柔酮组合。

65. 发明授权

US4145551A Pyrazine-2-carbonyloxyguanidines 失效
标题翻译：吡嗪-2-羰基氧基胍
公开(公告)号：US4145551A
公开(公告)日：1979-03-20
申请号：US868104
申请日：1978-01-09
申请人： Edward J. Cragoe, Jr. , Otto W. Woltersdorf, Jr. , Mark G. Bock
发明人： Edward J. Cragoe, Jr. , Otto W. Woltersdorf, Jr. , Mark G. Bock
IPC分类号： C07D241/26 , C07D241/28 , A61K31/495
CPC分类号： C07D241/26 , Y10S514/869
摘要： The case involves novel pyrazine-2-carbonyloxyguanidines and processes for preparing same. The pyrazine-2-carbonyloxyguanidines are eukalemic or antikaliuretic agents possessing diuretic and natriuretic properties.
摘要翻译：该案涉及新的吡嗪-2-羰基氧基胍及其制备方法。吡嗪-2-羰氧基胍是具有利尿和利尿钠特性的白血病或抗利尿剂。

66. 发明授权

US08466289B2 Heterocyclic sulfonamide derivatives 失效
标题翻译：杂环磺酰胺衍生物
公开(公告)号：US08466289B2
公开(公告)日：2013-06-18
申请号：US12938583
申请日：2010-11-03
申请人： Mark G. Bock , Dinesh Chikkanna , Clive McCarthy , Henrik Moebitz , Chetan Pandit
发明人： Mark G. Bock , Dinesh Chikkanna , Clive McCarthy , Henrik Moebitz , Chetan Pandit
IPC分类号： C07D513/04 , C07D471/04 , C07D498/04 , A61K31/437 , A61K31/4355 , A61K31/4365
CPC分类号： C07D471/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.
摘要翻译：本发明涉及其中R1a，R1b，X，R2a，R2b，W，R3，R4和R5如本文所定义的式I化合物及其药学上可接受的盐。已经显示这些化合物作为MEK抑制剂，其可用于治疗过度增殖性疾病，如癌症和炎症。

67. 发明授权

US08163704B2 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：US08163704B2
公开(公告)日：2012-04-24
申请号：US12906682
申请日：2010-10-18
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 , C07H1/00
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。

68. 发明申请

US20080318976A1 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激动剂
公开(公告)号：US20080318976A1
公开(公告)日：2008-12-25
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 , C07C229/36 , A61K31/505 , A61P25/00 , C07D239/24 , A61K31/24
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，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）具有选自NO和S的环杂原子并且任选具有至多3个另外的环氮原子的5元杂芳环，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;

69. 发明授权

US07163951B2 N-biarylmethyl aminocycloalkanecarboxamide derivatives 失效
标题翻译： N-二芳基甲基氨基环烷甲酰胺衍生物
公开(公告)号：US07163951B2
公开(公告)日：2007-01-16
申请号：US10523911
申请日：2003-08-25
申请人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
发明人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
IPC分类号： A61K31/4427 , C07D401/12
CPC分类号： C07D417/12 , C07D213/40 , C07D213/61 , C07D239/28 , C07D239/42 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/12
摘要： N-Biarylmethylaminocycloalkanecarboxamide 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-二芳基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。

70. 发明授权

US06319932B1 Oxazolidinones useful as alpha 1A adrenoceptor antagonists 失效
标题翻译：可用作α1A肾上腺素受体拮抗剂的恶唑烷酮
公开(公告)号：US06319932B1
公开(公告)日：2001-11-20
申请号：US09438006
申请日：1999-11-10
申请人： Jennie B. Nerenberg , Mark G. Bock , Harold G. Selnick , Linda Payne
发明人： Jennie B. Nerenberg , Mark G. Bock , Harold G. Selnick , Linda Payne
IPC分类号： A61K31445
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D413/12
摘要： Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
摘要翻译：公开了新的恶唑烷酮化合物及其药学上可接受的盐。还描述了这些化合物的合成及其作为α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人类5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

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