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51. 发明授权

US4182897A Amino- or guanidino-phenylpropionic acid derivatives 失效
标题翻译：氨基或胍基 - 苯基丙酸衍生物
公开(公告)号：US4182897A
公开(公告)日：1980-01-08
申请号：US917232
申请日：1978-06-20
申请人： Setsuro Fujii , Hiroyuki Kawamura , Seizo Taira , Ryoji Matsui , Yojiro Sakurai , Toshiyuki Okutome
发明人： Setsuro Fujii , Hiroyuki Kawamura , Seizo Taira , Ryoji Matsui , Yojiro Sakurai , Toshiyuki Okutome
IPC分类号： C07C205/56 , C07C279/18 , A61K31/24 , C07C101/447 , C07C129/12
CPC分类号： C07C279/18 , C07C205/56 , Y10S514/822
摘要： Amino- or guanidino-phenylpropionic ester derivatives represented by the formula: ##STR1## wherein R is --NH.sub.2 or ##STR2## R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is an unsubstituted or a lower-alkyl-, carboxyalkyl-, lower-alkoxy-, lower-alkoxycarbonyl- or halogen-substituted phenyl group or an unsubstituted or a halogen-substituted naphthyl group, and acid addition salts thereof are novel compounds exhibiting a specific enzyme-inhibitory activity to proteolytic enzymes and, therefore, they are useful as the therapeutic agent of diseases induced by abnormal activation of these enzymes. The above-mentioned compounds can be produced by subjecting a nitrocinnamic acid derivative represented by the formula: ##STR3## and a phenol derivative or a naphthol derivative represented by the formula:HO--R.sup.2to an esterification in the conventional manner to obtain a nitrocinnamic ester derivative, then reducing the latter compound to obtain an aminophenylpropionic ester derivative and, if desired, reacting it with cyanamide to obtain a guanidino-phenylpropionic ester derivative and, if desired, further converting the reaction product to an acid addition salt.
摘要翻译：由下式表示的氨基或胍基 - 苯基丙酸酯衍生物：其中R是-NH 2或R 1是氢或低级烷基，R 2是未取代的或低级烷基 - 羧基烷基 - 低级 - 烷氧基 - ，低级烷氧基羰基或卤素取代的苯基或未取代的或卤素取代的萘基，其酸加成盐是对蛋白水解酶具有特异性酶抑制活性的新化合物，因此它们是有用的作为由这些酶的异常活化引起的疾病的治疗剂。上述化合物可以通过将下式所示的硝基肉桂酸衍生物和由式HO-R2表示的酚衍生物或萘酚衍生物以常规方式进行酯化而制得，得到硝基肌氨酸酯衍生物，然后还原后一种化合物以获得氨基苯基丙酸酯衍生物，并且如果需要，可与氰酰胺反应，得到胍基 - 苯基丙酸酯衍生物，如果需要，将反应产物进一步转化成酸加成盐。

52. 发明授权

US4096276A Thiourea derivatives for treating hypertension 失效
标题翻译：用于治疗高血压的硫脲衍生物
公开(公告)号：US4096276A
公开(公告)日：1978-06-20
申请号：US763172
申请日：1977-01-27
申请人： Michael Robert Cohen , Richard Wightman Kierstead , Jefferson Wright Tilley
发明人： Michael Robert Cohen , Richard Wightman Kierstead , Jefferson Wright Tilley
IPC分类号： A61K31/18 , A61K31/445 , A61P9/12 , C07C67/00 , C07C279/18 , C07C325/00 , C07C335/16 , C07C335/32 , C07D295/13 , A61K31/17
CPC分类号： C07D295/13 , C07C279/18 , C07C335/16 , C07C335/32
摘要： Antihypertensively active thiourea derivatives of the formulas ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and X are as hereinafter described,As well as a method of using a compound of the formula ##STR2## wherein R.sub.1 ', R.sub.2 ', R.sub.3 and X are as previously described,Or a compound of formula II as an anti-hypertensive agent, is described.

53. 发明申请

US20190209548A1 LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：US20190209548A1
公开(公告)日：2019-07-11
申请号：US16195342
申请日：2018-11-19
申请人： University of Maryland, College Park , University of Maryland, Baltimore
发明人： Herman O. Sintim , Jie Zhou , Changhao Wang , Rena Lapidus
IPC分类号： A61K31/472 , C07D471/04 , A61K31/4725 , C07D413/12 , C07C245/24 , C07D217/22 , C07C257/18 , C07D417/12 , C07D401/12 , C07D401/04 , C07C279/18
CPC分类号： A61K31/472 , A61K31/4725 , C07C245/24 , C07C257/18 , C07C279/18 , C07D217/22 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

54. 发明授权

US09969709B2 Guanidinobenzoic acid ester compound 有权
公开(公告)号：US09969709B2
公开(公告)日：2018-05-15
申请号：US14775274
申请日：2014-03-13
申请人： Takeda Pharmaceutical Company Limited
发明人： Jiro Fujiyasu , Toru Asano , Susumu Yamaki , Osamu Kaneko , Yuka Koike , Tomoyoshi Imaizumi , Yasuharu Urano , Tomohki Satou , Satoshi Sasamura
IPC分类号： C07D333/70 , C07D279/18 , C07D333/24 , C07D333/68 , C07D217/26 , C07D333/40 , C07D307/81 , A61K31/24 , A61K31/343 , A61K31/381 , A61K31/472 , C07C279/18
CPC分类号： C07D333/70 , A61K31/24 , A61K31/343 , A61K31/381 , A61K31/472 , C07C279/18 , C07C2602/08 , C07C2602/10 , C07D217/26 , C07D307/81 , C07D333/24 , C07D333/40 , C07D333/68
摘要： [Problem]To provide a compound which is useful as an agent for preventing and/or treating kidney diseases.[Means for Solution]The present inventors have studied compounds having a trypsin inhibitory activity, and have confirmed that a guanidinobenzoic acid ester compound has a trypsin inhibitory activity, thereby completing the present invention. The guanidinobenzoic acid ester compound of the present invention can be used as an agent for preventing and/or treating kidney diseases (for example, chronic kidney disease, acute glomerulonephritis, acute kidney injury, and the like) as an agent which will substitute low-protein diet therapy, and/or as an agent for preventing and/or treating trypsin-related diseases (for example, chronic pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like).

55. 发明申请

US20180118668A1 NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF 审中-公开
公开(公告)号：US20180118668A1
公开(公告)日：2018-05-03
申请号：US15819758
申请日：2017-11-21
申请人： THE CATHOLIC UNIVERSITY OF KOREA INDUSTRY-ACADEMIC COOPERATION FOUNDATION
发明人： Mi-La CHO , Dong-Yun SHIN , Sung-Hwan PARK , Chul-Woo YANG , Jong-Young CHOI , Min-Jung PARK , Hye-Jin SON , Sung-Hee LEE , Seon-Yeong LEE , Eun-Kyung KIM , Jae-Kyung KIM , Seung-Hun LEE , Seong-Hyeok PARK
IPC分类号： C07C279/18
CPC分类号： C07C279/18 , C07C279/26
摘要： The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present invention has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune response

56. 发明申请

US20180072706A1 AZD9291 INTERMEDIATE AND PREPARATION METHOD THEREFOR 审中-公开
公开(公告)号：US20180072706A1
公开(公告)日：2018-03-15
申请号：US15822060
申请日：2017-11-24
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： C07D403/04 , C07C279/18 , C07C277/08
CPC分类号： C07D403/04 , C07C277/08 , C07C279/18
摘要： Disclosed are an intermediate, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II), applicable in preparing AZD9291 (I) and a preparation method for the intermediate. Preparation steps of the preparation method comprise: 2-fluoro-4-methoxyaniline, serving as a starting material, undergoes amidation, substitution, nitrification, reduction and guanidination reactions to prepare N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-formamidine]phenyl-2-propenamide (II). Also disclosed is a method for preparing AZD9291 (I) by means of a cyclization reaction between the compound of a formula II and (2E)-3-dimethylamino-1-(1-methyl-1H-indol-3-yl)-2-propen-1-one (III). The preparation method has readily available raw materials and a simple process and is economical, environmentally friendly, and suitable for industrialized production.

57. 发明授权

US09745257B2 Phenyl-guanidine derivatives 有权
公开(公告)号：US09745257B2
公开(公告)日：2017-08-29
申请号：US14348577
申请日：2012-10-10
申请人： Universidad Nacional de Quilmes , Chemo Research, S.L.
发明人： Pablo Lorenzano Menna , Daniel Fernando Alonso , Daniel Eduardo Gómez , Julieta Comin
IPC分类号： A61K31/505 , A61K31/155 , C07D239/42 , C07C277/08 , C07C279/18 , C07D213/75 , C07D333/36 , C07D233/88 , C07D235/30 , C07D263/48 , C07D207/14 , C07D277/48 , C07D307/66
CPC分类号： C07C279/18 , A61K31/155 , A61K31/505 , C07C277/08 , C07D207/14 , C07D213/75 , C07D233/88 , C07D235/30 , C07D239/42 , C07D263/48 , C07D277/48 , C07D307/66 , C07D333/36
摘要： Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumors, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.

58. 发明申请

US20170114008A1 NOVEL COMPOUND HAVING IMMUNE DISEASE TREATMENT EFFECT AND USE THEREOF 审中-公开
公开(公告)号：US20170114008A1
公开(公告)日：2017-04-27
申请号：US15339410
申请日：2016-10-31
申请人： THE CATHOLIC UNIVERSITY OF KOREA INDUSTRY-ACADEMIC COOPERATION FOUNDATION
发明人： Mi-La CHO , Dong-Yun SHIN , Sung-Hwan PARK , Chul-Woo YANG , Jong-Young CHOI , Min-Jung PARK , Hye-Jin SON , Sung-Hee LEE , Seon-Yeong LEE , Eun-Kyung KIM , Jae-Kyung KIM , Seung-Hun LEE , Seong-Hyeok PARK
IPC分类号： C07C279/18
CPC分类号： C07C279/18 , C07C279/26
摘要： The present invention relates to a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present invention has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune response

59. 发明申请

US20160361279A1 NOVEL SIGMA RECEPTOR LIGANDS AND METHODS OF MODULATING CELLULAR PROTEIN HOMEOSTASIS USING SAME 审中-公开
标题翻译：新型SIGMA受体配体和使用相同方法调节细胞蛋白质的方法
公开(公告)号：US20160361279A1
公开(公告)日：2016-12-15
申请号：US15176812
申请日：2016-06-08
申请人： DREXEL UNIVERSITY
发明人： Felix J. KIM , Joseph M. Salvino
IPC分类号： A61K31/155 , C07C279/18 , A61K9/70 , A61K45/06 , A61K9/06
CPC分类号： A61K31/155 , A61K9/06 , A61K9/7023 , A61K31/138 , A61K31/366 , A61K31/4035 , A61K31/4706 , A61K31/496 , A61K31/69 , A61K45/06 , C07C279/18 , C07D209/48 , C07D311/16 , A61K2300/00
摘要： The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.
摘要翻译：本发明包括可用于预防，治疗或改善Sigma相关疾病或疾病的化合物。本发明的化合物可以调节细胞蛋白质内稳态，其包括蛋白质的翻译起始，折叠，加工，转运和降解（包括遍在蛋白选择性自噬）。本发明还包括在有需要的受试者中预防，治疗或改善与Sigma相关的病症或疾病的方法，所述方法包括向受试者施用有效量的Sigma-调节化合物。本发明还包括在有需要的受试者中预防，治疗或改善与Sigma相关的病症或疾病的方法，所述方法包括向受试者施用有效量的Sigma-调节化合物，其还包括给予有效量的一种抑制泛素蛋白酶体系统（UPS）和/或自噬存活途径的化合物。

60. 发明申请

US20160324880A1 4-DEDIMETHYLAMINO TETRACYCLINE COMPOUNDS 审中-公开
公开(公告)号：US20160324880A1
公开(公告)日：2016-11-10
申请号：US14962347
申请日：2015-12-08
申请人： Paratek Pharmaceuticals, Inc.
发明人： Mark L. Nelson , Kwasi Ohemeng
IPC分类号： A61K31/65
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

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