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1. 发明申请

US20190241566A1 HETEROCYCLIC AMIDE COMPOUND 审中-公开
公开(公告)号：US20190241566A1
公开(公告)日：2019-08-08
申请号：US16333296
申请日：2017-09-14
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Takaharu HIRAYAMA , Yasuhiro HIRATA , Yusuke TOMINARI , Naoki IWAMURA , Yusuke SASAKI , Moriteru ASANO , Terufumi TAKAGI , Masanori OKANIWA , Masato YOSHIDA , Takashi ICHIKAWA , Shinichi IMAMURA
IPC分类号： C07D473/28 , C07D473/40 , C07D519/00 , C07D471/04 , C07D417/14 , C07D413/14 , C07D401/14 , C07D409/14 , C07D405/14 , C07D401/04 , A61P35/00
摘要： Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): wherein a group represented by is a group represented by the following formula (II) or the following formula (III): and other symbols are as described in the DESCRIPTION, or a salt thereof.

2. 发明授权

US09284316B2 Substituted fused pyrimidine compounds 有权
标题翻译：取代的稠合嘧啶化合物
公开(公告)号：US09284316B2
公开(公告)日：2016-03-15
申请号：US14511847
申请日：2014-10-10
申请人： Advinus Therapeutics Private Limited
发明人： Venkata Palle , Vidya Ramdas , Dinesh Barawkar , Sujay Basu , Summon Koul , Yogesh Waman , Meena Patel , Anil Panmand
IPC分类号： A61K31/522 , C07D473/28 , C07D473/40 , C07D473/06 , C07D473/18 , C07D473/30 , A61K31/5377
CPC分类号： C07D473/40 , A61K31/522 , A61K31/5377 , C07D473/06 , C07D473/18 , C07D473/30
摘要： The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
摘要翻译：本发明公开了式（I）的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，溶剂合物，药学上可接受的盐或含有它们的药物组合物和治疗由腺苷受体（AR）活性介导的病症和疾病的方法; 本发明的化合物可用于治疗，预防或抑制可能易受腺苷受体拮抗作用改善的疾病和病症，例如哮喘，慢性阻塞性肺病，血管发生，肺纤维化，肺气肿，过敏性疾病，炎症，再灌注损伤，心肌缺血，动脉粥样硬化，高血压，充血性心力衰竭，视网膜病变，糖尿病，肥胖，炎性胃肠道疾病和/或自身免疫性疾病。

3. 发明申请

US20130324562A1 FUSED BICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS 有权
标题翻译：作为DIPEPTIDYL PEPTIDASE-IV抑制剂的FUSED BICYCLIC HETEROCYCLES有用
公开(公告)号：US20130324562A1
公开(公告)日：2013-12-05
申请号：US14000641
申请日：2012-03-01
申请人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
发明人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
IPC分类号： C07D487/04 , A61K45/06 , A61K31/522 , A61K31/519 , C07D473/28
CPC分类号： C07D487/04 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/522 , A61K31/64 , A61K45/06 , C07D473/18 , C07D473/28 , A61K2300/00
摘要： The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式（I）的新型双环杂环，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

4. 发明授权

US08372852B2 Purines as reverse transcriptase inhibitors 失效
标题翻译：嘌呤作为逆转录酶抑制剂
公开(公告)号：US08372852B2
公开(公告)日：2013-02-12
申请号：US13470122
申请日：2012-05-11
申请人： Alex Shaginian , Samedy Ouk , Jean-Michel Vernier , Anthony B. Pinkerton
发明人： Alex Shaginian , Samedy Ouk , Jean-Michel Vernier , Anthony B. Pinkerton
IPC分类号： C07D473/28 , C07D473/34 , A61K31/52 , A61P31/18 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , C07D473/18
摘要： Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders. In some embodiments, the enzyme inhibitors are compounds of formula (I) or a pharmaceutically acceptable salt or tautomer thereof:
摘要翻译：本文描述的是新的酶抑制剂。在一些实施方案中，酶抑制剂是逆转录酶抑制剂，特别是HIV逆转录酶抑制剂。本文还描述了含有它们的组合物和使用它们的方法。因此，本文所述的化合物和组合物可用于体外和体内抑制HIV逆转录酶，作为治疗或预防HIV，AIDS或相关病症的方法。在一些实施方案中，酶抑制剂是式（I）的化合物或其药学上可接受的盐或互变异构体：

5. 发明申请

US20110201629A1 CYCLOHEXYL AMIDE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CRF受体拮抗剂的CYCLOHEXYL AMIDE DERIVATIVES
公开(公告)号：US20110201629A1
公开(公告)日：2011-08-18
申请号：US13017399
申请日：2011-01-31
申请人： Benjamin Atkinson , David Beattie , Andrew James Culshaw , James Dale , Nicholas James Devereux , Jeffrey McKenna
发明人： Benjamin Atkinson , David Beattie , Andrew James Culshaw , James Dale , Nicholas James Devereux , Jeffrey McKenna
IPC分类号： A61K31/522 , C07D209/34 , A61K31/404 , A61P25/18 , A61P25/28 , A61P29/00 , A61P25/30 , A61P1/08 , A61P25/24 , C07D401/12 , A61K31/4439 , C07D471/04 , A61K31/437 , C07D471/10 , C07D217/24 , A61K31/472 , C07D498/04 , C07D473/28
CPC分类号： C07D209/34 , C07D217/24 , C07D401/12 , C07D413/12 , C07D471/04 , C07D471/20 , C07D487/04 , C07D498/04
摘要： There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.
摘要翻译：描述了式I的环己基酰胺衍生物，其可用作促肾上腺皮质激素释放因子（CRF）受体拮抗剂和药物。

6. 发明申请

US20100228015A1 PRODRUG DERIVATIVES OF ACIDS USING ALCOHOLS WITH HOMOTOPIC HYDROXY GROUPS AND METHODS FOR THEIR PREPARATION AND USE 审中-公开
标题翻译：使用醇与单体羟基组合的酸的原料衍生物及其制备和使用方法
公开(公告)号：US20100228015A1
公开(公告)日：2010-09-09
申请号：US12766226
申请日：2010-04-23
申请人： Mitchell A. deLong , Jill M. McFadden , Susan M. Royalty , Eric J. Toone , Jeffrey D. Yingling
发明人： Mitchell A. deLong , Jill M. McFadden , Susan M. Royalty , Eric J. Toone , Jeffrey D. Yingling
IPC分类号： C07H15/18 , C07F7/18 , C07C69/732 , C07D333/54 , C07D307/79 , C07C69/736 , C07C69/73 , C07D309/06 , C07D207/46 , C07D307/20 , C07D333/32 , C07D493/04 , C07D211/42 , C07D241/04 , C07D265/30 , C07D501/18 , C07D401/10 , C07D215/56 , C07D487/04 , C07D277/06 , C07D473/34 , C07D473/28
CPC分类号： C07C219/10 , C07C69/608 , C07C69/738 , C07C69/76 , C07C233/65 , C07C251/48 , C07C317/44 , C07C405/00 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D205/095 , C07D215/56 , C07D233/78 , C07D277/06 , C07D295/116 , C07D333/56 , C07D333/64 , C07D473/30 , C07D473/34 , C07D491/056 , C07D501/34
摘要： This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.
摘要翻译：本发明涉及新的同位素前药和药物及其制备，测试和使用的方法。在一个实施方案中，同位物前药具有以下通式：其中是包含羧酸官能团的生物活性部分，Rb是通过羧酸官能团与生物活性部分键合形成酯的同位素对称醇连接，以及光学异构体，对映异构体，药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺以及它们的组合。

7. 发明授权

US07569573B2 Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase 失效
标题翻译：具有核碱基支架的二酮酸：靶向HIV整合酶的抗HIV复制抑制剂
公开(公告)号：US07569573B2
公开(公告)日：2009-08-04
申请号：US11820444
申请日：2007-06-19
申请人： Vasu Nair , Guochen Chi , Vinod R. Uchil
发明人： Vasu Nair , Guochen Chi , Vinod R. Uchil
IPC分类号： C07D473/28 , C07D473/36 , C07D473/40 , C07D473/00 , A61K31/52 , A61P31/18 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D419/04
CPC分类号： C07D473/30 , C07D239/54 , C07D473/00 , C07F9/6512 , C07F9/65616
摘要： A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
摘要翻译：描述了通过抑制HIV整合酶设计为抑制HIV复制的核碱基支架上构建的一类新的二酮酸。这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用，疫苗和其他治疗剂。还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

8. 发明申请

US20090181989A1 Purine Compunds as HSP90 Protein Inhibitors for the Treatment of Cancer 审中-公开
标题翻译：嘌呤组合作为HSP90蛋白抑制剂治疗癌症
公开(公告)号：US20090181989A1
公开(公告)日：2009-07-16
申请号：US12394891
申请日：2009-02-27
申请人： Paul Andrew BROUGH , Martin DRYSDALE , Xavier BARRIL-ALONSO
发明人： Paul Andrew BROUGH , Martin DRYSDALE , Xavier BARRIL-ALONSO
IPC分类号： A61K31/52 , C07D473/40 , C07D473/36 , C07D473/28 , A61K31/522 , A61P31/12 , A61P29/00 , A61P31/10 , A61P3/10 , A61P35/00
CPC分类号： C07D473/40 , C07D473/30 , C07D473/36
摘要： Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (IA): —X-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, —O—, —S— —S(O)—, —SO2—, or —NH—, Z is —O—, —S—, —(C═O)—, —(C═S)—, —S(O)—, —SO2—, —NRA, or, in either orientation —C(═O)O—, —C(═O)NRA, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH2OH, —C(═O)NH2, —C(═O)H, —C(═O)CH3, or —NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (—CN), C1-C3alkyl optionally substituted with one or more fluorine substituents, C1-C3alkoxy optionally substituted with one or more fluorine substituents, —CH═CH2, —C≡CH, cyclopropyl and —NH2, or R3 and R4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (—OCH2O—) or ethylenedioxy (—OCH2CH2O—) in either of which one or more hydrogens are optionally replaced by fluorine; S1 is hydrogen, or a substituent as defined in the specification.
摘要翻译：式（I）化合物是HSP90的抑制剂，可用于治疗例如癌症：其中环A是芳基或杂芳基环或环系; R 1是氢，氟，氯，溴或式（IA）的基团：-X-Alk1-（Z）m-（Alk2）nQ（IA）其中X是键，-O - ， - S- S（O） - ， - SO 2 - 或-NH-，Z是-O-，-S - ， - （CO） - ， - （CS） - ， - S（O） - ， - SO 2 - ，或者以取代-C（ - O）O - ， - C（-O）NRA，-C（-S）NRA，-SO 2 NR - ， - NRAC（-O） - 或-NRASO 2 - 是氢或其中一个或多个氢任选被氟取代的C 1 -C 6烷基; Alk1和Alk2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基，m和n独立地为0或1，Q为氢或任选取代的碳环或杂环基; R 2是氰基（-CN），氟，氯，溴，甲基，乙基，-OH，-CH 2 OH，-C（-O）NH 2，-C（-O）H，-C（-O） NH2; R 3和R 4独立地选自氢，氟，氯，溴，氰基（-CN），任选被一个或多个氟取代基取代的C 1 -C 3烷基，任选被一个或多个氟取代基取代的C 1 -C 3烷氧基，-CH-CH 2， -C≡CH，环丙基和-NH 2，或者R 3和R 4一起表示稠合于环A或亚甲二氧基（-OCH 2 O-）或亚乙二氧基（-OCH 2 CH 2 O-）的碳环或杂环，其中任一个或多个氢任选地被氟取代; S1是氢或说明书中定义的取代基。

9. 发明申请

US20080293684A1 Heterocyclic Acetophenone Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的杂环苯乙酮电位
公开(公告)号：US20080293684A1
公开(公告)日：2008-11-27
申请号：US11658546
申请日：2005-07-26
申请人： Anthony B Pinkerton , Jean-Michel Vernier , Rowena V. Cube , John H. Hutchinson , Dehua Huang , Celine Bonnefous , Steven P. Govak , Theodore Kamenecka
发明人： Anthony B Pinkerton , Jean-Michel Vernier , Rowena V. Cube , John H. Hutchinson , Dehua Huang , Celine Bonnefous , Steven P. Govak , Theodore Kamenecka
IPC分类号： A61K31/397 , C07D311/02 , A61K31/353 , A61K31/12 , C07C49/213 , C07D211/72 , A61K31/44 , A61K31/505 , C07D239/02 , C07D217/22 , A61K31/472 , A61K31/497 , C07D401/02 , C07D213/24 , A61K31/4427 , C07D471/04 , A61K31/437 , A61K31/4245 , A61P25/08 , A61P25/24 , A61P25/18 , C07D213/62 , A61K31/444 , A61K31/343 , C07D307/77 , C07D473/28 , A61K31/522 , A61K31/41 , C07D257/04 , C07D263/58 , A61K31/423 , A61K31/428 , C07D277/20 , C07D205/02 , C07D271/10 , C07D215/58 , A61K31/47 , C07D403/02 , C07D417/02 , A61K31/427
CPC分类号： C07D311/16 , C07C45/71 , C07C49/84 , C07C69/734 , C07C69/92 , C07C217/76 , C07C217/92 , C07C235/42 , C07C255/54 , C07C323/12 , C07D205/04 , C07D209/08 , C07D213/30 , C07D213/53 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/84 , C07D213/89 , C07D215/20 , C07D217/02 , C07D231/56 , C07D233/20 , C07D233/60 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/18 , C07D239/34 , C07D257/04 , C07D263/58 , C07D271/10 , C07D277/74 , C07D307/80 , C07D311/22 , C07D311/24 , C07D311/58 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/38
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

10. 发明申请

US20080146590A1 P38 map kinase inhibitors and methods for using the same 失效
标题翻译： P38图激酶抑制剂及其使用方法
公开(公告)号：US20080146590A1
公开(公告)日：2008-06-19
申请号：US12002708
申请日：2007-12-18
申请人： Tobias Gabriel , Yan Lou
发明人： Tobias Gabriel , Yan Lou
IPC分类号： A61K31/522 , C07D473/28 , A61P19/02 , A61P1/00 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula Ia or Ib: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
摘要翻译：式Ia或Ib化合物：其中R 1，R 2，R 3和R 4定义如上所定义这里。还公开了制备化合物的方法和使用该化合物治疗p38MAP激酶介导的疾病的方法。

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