专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20150246892A1 N-SUBSTITUTED BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS 有权
标题翻译： N-取代双（氟甲基）-1,4-苯并嗪酮化合物
公开(公告)号：US20150246892A1
公开(公告)日：2015-09-03
申请号：US14429945
申请日：2013-09-20
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Wen-Ching Han , Patrice Gill , Ashvinikumar V. Gavai , Claude A. Quesnelle
IPC分类号： C07D243/16 , A61K45/06 , C07D401/04 , C07D491/056 , A61K31/5513
CPC分类号： C07D243/16 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K45/06 , C07D243/18 , C07D243/26 , C07D401/04 , C07D491/04 , C07D491/056 , A61K2300/00
摘要： Disclosed are compounds of Formula (I): wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is —CH2CF3, —CH2CN, —CH2(cyclopropyl), pyridinyl, chloropyridinyl, or tetrahydropyranyl; Ring A is phenyl or pyridinyl; Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译：公开了式（I）的化合物：其中：R1是-CH2CH2CF3; R2是-CH2CH2CF3或-CH2CH2CH2CF3; R3是-CH2CF3，-CH2CN，-CH2（环丙基），吡啶基，氯吡啶基或四氢吡喃基; 环A是苯基或吡啶基; Ra，Rb，y和z在本文中定义。还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。

2. 发明申请

US20010014738A1 PROCESS FOR THE PREPARATION OF IMIDAZODIAZEPINE INTERMEDIATES 审中-公开
标题翻译：制备咪达唑定中间体的方法
公开(公告)号：US20010014738A1
公开(公告)日：2001-08-16
申请号：US09343317
申请日：1999-06-30
发明人： MADHUP K. DHAON , PARVIZ LABIB , DEBORAH A. DAVIS , GRANT L. ESSER
IPC分类号： C07D225/00 , C07D295/00
CPC分类号： C07D487/04 , C07D243/16
摘要： The present invention relates to a process for the synthesis of a compound having the formula I, 1 which allows the synthesis to be carried out in a single reaction vessel and without column chromatography purification.
摘要翻译：本发明涉及合成具有式I化合物的方法，其允许在单个反应容器中进行合成并且不进行柱层析纯化。

3. 发明授权

US5331006A Amino acid analogs as CCK antagonists 失效
标题翻译：氨基酸类似物作为CCK拮抗剂
公开(公告)号：US5331006A
公开(公告)日：1994-07-19
申请号：US726656
申请日：1991-07-12
申请人： David C. Horwell , Julian Aranda , Corinne Augelli-Szafran , Hans-Jurgen Betche , Ann Holmes , Michael D. Mullican , Martyn C. Pritchard , Reginald S. Richardson , Edward Roberts , Bruce D. Roth , Bradley D. Tait , Bharat K. Trivedi , Uwe Trostmann , Paul C. Unangst
发明人： David C. Horwell , Julian Aranda , Corinne Augelli-Szafran , Hans-Jurgen Betche , Ann Holmes , Michael D. Mullican , Martyn C. Pritchard , Reginald S. Richardson , Edward Roberts , Bruce D. Roth , Bradley D. Tait , Bharat K. Trivedi , Uwe Trostmann , Paul C. Unangst
IPC分类号： C07C271/34 , C07D207/32 , C07D207/327 , C07D213/56 , C07D213/89 , C07D215/12 , C07D231/56 , C07D233/26 , C07D235/16 , C07D243/16 , C07D243/24 , C07D249/18 , C07D261/08 , C07D277/46 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/82 , C07D333/60 , C07D403/12 , C07D471/04 , A61K31/27 , C07C271/10
CPC分类号： C07D403/12 , C07C271/34 , C07D207/327 , C07D213/56 , C07D213/89 , C07D215/12 , C07D231/56 , C07D233/26 , C07D235/16 , C07D243/16 , C07D243/24 , C07D249/18 , C07D261/08 , C07D277/46 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/82 , C07D333/60 , C07D471/04 , C07C2103/74
摘要： Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.
摘要翻译：公开了用作治疗肥胖症，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药物的新型非天然罂粟脂。此外，化合物是抗焦虑剂和抗溃疡剂。这些化合物是可用于预防慢性治疗或使用尼古丁，地西泮，酒精，可卡因，咖啡因和阿片样物质的戒断反应的药剂。这些化合物也可用于治疗和/或预防恐慌发作。还公开了药物组合物和使用二趾甲的治疗方法以及制备它们的方法和可用于其制备的新型中间体。本发明的另一个特征是本发明化合物用于制备诊断组合物的用途。

4. 发明授权

US4820834A Benzodiazepine analogs 失效
标题翻译：苯二氮卓类似物
公开(公告)号：US4820834A
公开(公告)日：1989-04-11
申请号：US26420
申请日：1987-03-16
申请人： Ben E. Evans , Roger M. Freidinger , Mark G. Bock
发明人： Ben E. Evans , Roger M. Freidinger , Mark G. Bock
IPC分类号： C07D243/14 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K38/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61P43/00 , C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07F9/22 , C07F9/38 , C07F9/645 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/097
CPC分类号： C07D403/04 , C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0821 , A61K38/00
摘要： Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
摘要翻译：公开了作为胃泌素和缩胆囊素（CCK）的拮抗剂的下列公式的苯并二氮杂类似物： I。

5. 发明授权

US4505908A 7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharmaceuticals 失效
标题翻译： 7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂药物
公开(公告)号：US4505908A
公开(公告)日：1985-03-19
申请号：US422297
申请日：1982-09-23
申请人： Horst Zeugner , Michael Ruhland , Hans Liepmann , Wolfgang Milkowski , Herbert Muesch
发明人： Horst Zeugner , Michael Ruhland , Hans Liepmann , Wolfgang Milkowski , Herbert Muesch
IPC分类号： A61K31/55 , A61K31/551 , A61P21/02 , A61P25/00 , A61P25/20 , C07D243/16 , C07D245/06 , C07D487/04
CPC分类号： C07D487/04 , C07D243/16 , C07D245/06
摘要： Disclosed are 7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines of the formula I ##STR1## in which R.sub.1 is a hydrogen atom or a lower alkoxy or alkanoyloxy radical and R.sub.2 is a halogen atom. The compounds possess psychopharmacological, and especially anti-aggressive properties. To manufacture compounds of formula I, corresponding 2-halomethyl-7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines are cyclized to corresponding 7-bromo-1,2-methylene-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines and in these the aziridine ring is opened through treatment with a lower alcohol or a lower carboxylic acid in the presence of a Lewis acid.
摘要翻译：公开了式I的7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂其中R 1是氢原子或低级烷氧基或烷酰氧基， R2是卤素原子。这些化合物具有精神药理学，特别是抗侵袭性。为了制备式I化合物，将相应的2-卤代甲基-7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂环化为相应的7-溴-1,2-亚甲基 -5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂并且在路易斯酸存在下，通过用低级醇或低级羧酸处理来打开氮丙啶环。

6. 发明授权

US4401597A Imidazodiazepines and processes therefor 失效
标题翻译：咪唑二氮类及其制备方法
公开(公告)号：US4401597A
公开(公告)日：1983-08-30
申请号：US242852
申请日：1981-03-12
申请人： Armin Walser , Rodney I. Fryer
发明人： Armin Walser , Rodney I. Fryer
IPC分类号： C07D243/16 , C07D243/20 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561 , A61K31/55 , C07D487/22
CPC分类号： C07D487/04 , C07D243/16 , C07D243/20 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561
摘要： Novel immidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included with the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro or halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof; R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety; and R.sub.2 is hydrogen and lower alkyl.
摘要翻译：新型的咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢和低级烷基，优选甲基; R3和R5是氢; R4是氢，硝基或卤素，最优选氯，而在最优选的实施方式中，当位于咪唑并二氮杂的稠合的苯并部分位于其8-位时; R6是苯基或卤素，硝基或低级烷基取代的苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位; 并且R 2是氢和低级烷基。

7. 发明授权

US4349476A Process for producing imidazodiazepines 失效
公开(公告)号：US4349476A
公开(公告)日：1982-09-14
申请号：US242946
申请日：1981-03-12
申请人： Armin Walser , Rodney I. Fryer
发明人： Armin Walser , Rodney I. Fryer
IPC分类号： C07D243/16 , C07D243/20 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561
CPC分类号： C07D487/04 , C07D243/16 , C07D243/20 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561
摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## wherein A is ##STR2## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR3## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR4## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR5## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR6## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.5 is selected from the group consisting of hydrogen, lower alkanoyloxy and hydroxy; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR7## is selected from the group consisting of ##STR8## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.

8. 发明授权

US4259241A Process for the preparation of imidazobenzodiazepines 失效
标题翻译：咪唑并二氮杂的制备方法
公开(公告)号：US4259241A
公开(公告)日：1981-03-31
申请号：US123318
申请日：1980-02-21
申请人： Armin Walser
发明人： Armin Walser
IPC分类号： C07D243/16 , C07D487/04
CPC分类号： C07D487/04 , C07D243/16
摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is a disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
摘要翻译：提出了一种用于制备下式的咪唑并二氮杂的多步骤方法，其中X选自氢，卤素，硝基和三氟甲基; Y选自氢，卤素或三氟甲基; R1是氢或低级烷基，R2是二取代的胺。还提出了在该方法中使用的新型中间体。终产物和中间体可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。最终产品在用于术前麻醉的静脉内组合物中特别有用。

9. 发明授权

US4155904A Process for the preparation of 1,4-benzo-diazepines and 1,4-benzodiazepinones 失效
标题翻译：制备1,4-苯并二氮杂和1,4-苯并二氮杂酮的方法
公开(公告)号：US4155904A
公开(公告)日：1979-05-22
申请号：US707978
申请日：1976-07-23
申请人： Walter Schlesinger
发明人： Walter Schlesinger
IPC分类号： C07D243/16 , C07D243/24 , C07D243/28 , C07D243/30
CPC分类号： C07D243/16 , C07D243/24
摘要： This invention relates to an improved process for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones and 2,3-dihydro-1H-1,4-benzodiazepines by the condensation of a 2-(2-haloacylamido)-benzophenone or a 2-(2-haloethylamino)-benzophenone, respectively, in the presence of hexamethylenetetramine, a water miscible alcohol containing 5 to 50 volume percent water, and an ammonium salt.
摘要翻译：本发明涉及一种改进的1,3-二氢-2H-1,4-苯并二氮杂-2-和2,3-二氢-1H-1,4-苯并二氮杂的制备方法，该方法是将2-（ 2-卤代酰胺基） - 二苯甲酮或2-（2-卤代乙基氨基） - 二苯甲酮，在六亚甲基四胺的存在下，含有5至50体积％水的水混溶性醇和铵盐。

10. 发明授权

US4146722A Imidazo[1,5-a][1,4]benzodiazepines 失效
标题翻译：咪唑（1,5-A）+8,1,4-苯并二恶英
公开(公告)号：US4146722A
公开(公告)日：1979-03-27
申请号：US928479
申请日：1978-07-27
申请人： Armin Walser , Rodney I. Fryer , Louis Benjamin
发明人： Armin Walser , Rodney I. Fryer , Louis Benjamin
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , A61P25/26 , C07D243/16 , C07D487/04
CPC分类号： C07D487/04 , C07D243/16
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.

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