专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明申请

WO1995000532A1 17-HALOGENO-4-AZAANDROSTENE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： 17-卤代-4-氮杂环丁烷衍生物及其制备方法
公开(公告)号：WO1995000532A1
公开(公告)日：1995-01-05
申请号：PCT/HU1993000040
申请日：1993-06-24
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , TUBA, Zoltán , HORVATH, Judit , SZÉLES, János , LOVASNÉ MARSAI, Mária , BALOGH, Gábor
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The invention relates to novel 4-azaandrostene derivatives of general formula (I), wherein R represents hydrogen or a C1-3alkyl group; X represents chlorine, bromine or iodine; and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line represents a single or double bond.
摘要翻译：本发明涉及通式（I）的新型4-氮杂雄甾烯衍生物，其中R代表氢或C1-3烷基; X表示氯，溴或碘; 而 - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_ bond line代表单一或双重债券。

42. 发明申请

WO1995000531A1 NOVEL PROCESS FOR PREPARING 17beta-SUBSTITUTED 4-AZAANDROSTANE DERIVATIVES 审中-公开
标题翻译：制备17β-衍生的4-氮杂双环衍生物的新方法
公开(公告)号：WO1995000531A1
公开(公告)日：1995-01-05
申请号：PCT/HU1993000039
申请日：1993-06-24
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , TUBA, Zoltán , HORVATH, Judit , SZÉLES, János , KOLLAR, László , BALOGH, Gábor
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The invention relates to a novel process for preparing 17 beta -substituted 4-azaandrostane derivatives of general formula (I) wherein R represents hydrogen or a C1-3alkyl group; R represents a carboxamido group mono- or disubstituted by C1-8alkyl group(s); or a free carboxyl group; or a carboxyl group esterified with a C1-5 alcohol; and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line represents a single or double bond; as well as their salts. The process comprises reacting a 17-halogeno-4-azaandrostene derivative of general formula (II) wherein R and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line are as defined above, and X is chlorine, bromine or iodine, with a primary or secondary alkylamine or a C1-5 alcohol, in dimethylformamide or dimethylsulfoxide medium in the presence of a palladium(II) salt and phosphines or a palladium(II) complex and a tertiary amine base in carbon monoxide atmosphere at a temperature between 35 DEG C and 80 DEG C, then, if desired, transforming an obtained compound of general formula (I) to another compound of general formula (I) by hydrogenation, hydrolysis or salt forming reaction.
摘要翻译：本发明涉及一种制备通式（I）的17β-取代的4-氮杂雄甾烷衍生物的新方法，其中R表示氢或C1-3烷基; R 1表示被C 1-8烷基单取代或二取代的甲酰胺基; 或游离羧基; 或用C 1-5醇酯化的羧基; - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_ bond line代表单一或双重债券; 以及它们的盐。该方法包括使通式（II）的17-卤代-4-氮杂雄甾烯衍生物（其中R和 - ）与上述定义同上，X是氯，溴或碘在二氯甲烷或二甲基亚砜介质中，在一氧化碳气氛中，在钯（II）盐和膦或钯（II）配合物和叔胺碱的存在下，在一个一氧化碳气氛中，在35℃至80℃之间，如果需要，通过氢化，水解或成盐反应将得到的通式（I）化合物转化为通式（I）的另一化合物。

43. 发明申请

WO1994011387A2 A PROCESS FOR THE PRODUCTION OF FINASTERIDE 审中-公开
标题翻译：一种生产杀虫剂的方法
公开(公告)号：WO1994011387A2
公开(公告)日：1994-05-26
申请号：PCT/US1993010659
申请日：1993-11-05
申请人： MERCK & CO., INC. , DOLLING, Ulf, H. , McCAULEY, James, A. , VARSOLONA, Richard, J.
发明人： MERCK & CO., INC.
IPC分类号： C07J73/00
CPC分类号： C07F3/003 , C07J73/005 , H04N5/7458
摘要： Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17 beta -carboalkoxy-4-aza-5 alpha -androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride. Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.
摘要翻译：公开了一种生产非那雄胺的新方法，其包括使17β-烷氧基-4-氮杂-5α-雄甾-1-烯-3-酮的卤化镁盐与叔丁基氨基卤化镁反应，其存在于至少2 ：在惰性气氛下，在环境温度下，在惰性有机溶剂中，由叔丁胺和脂族/芳基卤化镁形成1摩尔比，然后加热和回收非那雄胺产物。还公开了非那雄胺的两种多晶型晶型I和II及其生产方法。

44. 发明申请

WO1994007909A1 NOVEL 17'beta'-SUBSTITUTED 4-AZAANDROSTANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型17β-衍生的4-AZAANDROSTANE衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994007909A1
公开(公告)日：1994-04-14
申请号：PCT/HU1993000058
申请日：1993-10-01
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , TUBA, Zoltán , HORVATH, Judit , KOLLAR, László , LOVASNÉ, Marsai, Mária , BALOGH, Gábor , CSEHI, Attila , JAVOR, András , HAJOS, György , SZPORNY, László
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The invention relates to novel 17 beta -substituted 4-azaandrostane derivatives of general Formula (I), wherein R means hydrogen or a C1-3alkyl group; R and R are the same or different and stand for hydrogen or a C1-4alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; or R and R together mean an alpha , omega -alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and - &cir& _- &cir& _- &cir& _ bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general Formula (I). The compounds of general Formula (I) exert a 5 alpha -reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseases, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.
摘要翻译：本发明涉及通式（I）的新型17β-取代的4-氮杂雄甾烷衍生物，其中R表示氢或C 1-3烷基; R 1和R 2相同或不同，代表氢或C 1-4烷基，条件是只有在n高于5的情况下，两者均可表示氢; 或R 1和R 2一起表示含有5至7个碳原子的α，ω-亚烷基，所述亚烷基的末端碳原子与相同的环碳原子结合; n为4,5,6或7; 和 - ＆cir＆_-＆cir＆_-＆cir＆_ bond line代表单一或双重债券。此外，本发明涉及含有这些化合物的药物组合物以及制备通式（I）化合物的方法。通式（I）的化合物发挥5α-还原酶抑制作用，因此它们可用于治疗所有疾病，其目的是减少组织二氢睾酮水平，例如良性前列腺增生，痤疮，皮脂溢，女性多毛症或雄激素性脱发。

45. 发明申请

WO1994003475A1 FLUORINATED 17'beta'-SUBSTITUTED 4-AZA-5'alpha'-ANDROSTAN-3-ONE DERIVATIVES 审中-公开
标题翻译：氟化17β-取代的4-AZA-5α-二脱氧-3-α衍生物
公开(公告)号：WO1994003475A1
公开(公告)日：1994-02-17
申请号：PCT/EP1993002037
申请日：1993-07-29
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , PANZERI, Achille , NESI, Marcella , DI SALLE, Enrico
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： Compounds of formula (I), wherein: the symbol . &cir& _. &cir& _. &cir& _. &cir& _ represents a single or a double bond; B is a bond or a straight or branched C1-C6 alkylene chain; R is hydrogen or C1-C4 alkyl; R1 is hydrogen, C1-C6 alkyl or benzyl; R2 is a) hydrogen, fluorine, C1-C6 alkyl, C5-C7 cycloalkyl or C6-C9 cycloalkylalkyl; or b) aryl or C7-C10 arylalkyl; R3 is a) hydrogen, fluorine or C1-C4 alkyl; or b) aryl or C7-C10 arylalkyl; R4 is hydrogen, fluorine, or is absent when Y is a double bond; R5 is hydrogen, fluorine or C1-C6 alkyl; and when Y is a single bond, A is hydrogen, fluorine or (i) wherein each of R6, R7 and R8 independently is hydrogen, fluorine or C1-C6 alkyl; and when Y is a double bond, A is a (ii) wherein each of R6 and R7 is independently hydrogen, fluorine or C1-C6 alkyl; with the proviso that at least one of the groups R, R1, R2, R3, R4, R5 or A contains at least one fluorine atom.
摘要翻译：式（I）化合物，其中：符号。＆cir＆_。＆cir＆_。＆cir＆_。＆cir＆_代表单一或双重债券; B是键或直链或支链C1-C6亚烷基链; R是氢或C 1 -C 4烷基; R1是氢，C1-C6烷基或苄基; R2是a）氢，氟，C1-C6烷基，C5-C7环烷基或C6-C9环烷基烷基; 或b）芳基或C7-C10芳基烷基; R3是a）氢，氟或C1-C4烷基; 或b）芳基或C7-C10芳基烷基; R4是氢，氟，或当Y是双键时不存在; R5是氢，氟或C1-C6烷基; 当Y为单键时，A为氢，氟或（i）其中R6，R7和R8各自独立地为氢，氟或C1-C6烷基; 当Y是双键时，A是（ⅱ）其中R6和R7各自独立地是氢，氟或C1-C6烷基; 条件是基团R，R 1，R 2，R 3，R 4，R 5或A中的至少一个含有至少一个氟原子。

46. 发明申请

WO1992017489A1 NOVEL OXA- OR AZASTEROID DERIVATIVE 审中-公开
标题翻译：新的氧化亚砷酸酯衍生物
公开(公告)号：WO1992017489A1
公开(公告)日：1992-10-15
申请号：PCT/JP1992000364
申请日：1992-03-26
申请人： TEIKOKU HORMONE MFG. CO., LTD. , KOIZUMI, Naoyuki , TAKEGAWA, Shigehiro , IWASHITA, Shigeki , KAWACHI, Tomoko , MATSUI, Teruaki , HONMA, Seijiro , TAKAHASHI, Hiroo , MIEDA, Mamoru , MINATO, Koichi , SHIBATA, Kenyu , NUMAZAWA, Mitsuteru
发明人： TEIKOKU HORMONE MFG. CO., LTD.
IPC分类号： C07J73/00
CPC分类号： C07J73/005 , C07J73/003
摘要： A compound represented by general formula (I), which has an aromatase inhibitory activity and is useful for preventing and treating diseases caused by hyperestrogenosis, such as mastocarcinoma, metrocarcinoma and prostatomegaly. In formula (I) A represents C=O, CH2, C=CH2 or C=CH-lower alkyl; B represents O, NH or N-lower alkyl; X is nil, or represents C=O or CH2; n is 2 or 3 when X is nil, or 1 or 2 when X represents C=O or CH2; and the broken line between the 1-position and the 2-position in the steroidal skeleton means an optional presence of a double bond therebetween.

47. 发明申请

WO2020056174A1 TRIPTOLIDE AND PRODRUGS THEREOF FOR USE IN METHODS TO TREAT FIBROSIS, NASH, AND NAFLD 审中-公开
公开(公告)号：WO2020056174A1
公开(公告)日：2020-03-19
申请号：PCT/US2019/050866
申请日：2019-09-12
申请人： MINNEAMRITA THERAPEUTICS, LLC
发明人： SALUJA, Ashok K. , DUDEJA, Vikas , LAVANIA, Shweta , NIKAM, Aniket , BANERJEE, Sulagna
IPC分类号： C07J73/00 , A61K31/585 , A61P1/16
摘要： The invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of fibrosis, nonalcoholic fatty liver disease (NAFLD) or nonalcoholic steatohepatitis (NASH).

48. 发明申请

WO2017205964A8 AMINOSTEROID DERIVATIVES AND PROCESS FOR PRODUCING SAME 审中-公开
公开(公告)号：WO2017205964A8
公开(公告)日：2017-12-07
申请号：PCT/CA2017/000140
申请日：2017-06-02
申请人： UNIVERSITÉ LAVAL
发明人： POIRIER, Donald , MALTAIS, René , PERREAULT, Martin
IPC分类号： C07J43/00 , A61K31/567 , A61P35/00 , C07J73/00
摘要： Estrane-based and androstane-based aminosteroid derivatives are described herein. More specifically, the following piperazinyl-steroid compounds of Formula I, Formula II, Formula III, and Formula IV are described. The compounds display cytotoxicity on a variety of cancer cell lines. A process for producing the compounds and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.

49. 发明申请

WO2017205964A1 AMINOSTEROID DERIVATIVES AND PROCESS FOR PRODUCING SAME 审中-公开
标题翻译：氨基类衍生物及其生产方法
公开(公告)号：WO2017205964A1
公开(公告)日：2017-12-07
申请号：PCT/CA2017/000140
申请日：2017-06-02
申请人： UNIVERSITÉ LAVAL
发明人： POIRIER, Donald , MALTAIS, René , PERREAULT, Martin
IPC分类号： C07J43/00 , A61K31/567 , A61P35/00 , C07J73/00
CPC分类号： C07J73/005 , A61K31/58 , A61K45/06 , A61P35/00 , C07J43/003 , C07J51/00 , A61K2300/00
摘要： Estrane-based and androstane-based aminosteroid derivatives are described herein. More specifically, the following piperazinyl-steroid compounds of Formula I, Formula II, Formula III, and Formula IV are described. The compounds display cytotoxicity on a variety of cancer cell lines. A process for producing the compounds and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.
摘要翻译：本文描述了基于Estrane的和基于雄甾烷的氨基甾体衍生物。更具体地，描述了式I，式II，式III和式IV的以下哌嗪基 - 甾族化合物。这些化合物对多种癌细胞系显示出细胞毒性。还公开了生产这些化合物的方法及其在制备药物制剂和/或组合物中的用途。

50. 发明申请

WO2015085447A1 新的雷公藤甲素衍生物及其制备方法和用途审中-公开
公开(公告)号：WO2015085447A1
公开(公告)日：2015-06-18
申请号：PCT/CN2013/001551
申请日：2013-12-11
申请人：香港浸会大学
发明人：张戈 , 吕爱平 , 王成 , 吕诚 , 鲁军 , 刘彪
IPC分类号： C07J73/00 , C12N15/115 , A61P35/00
CPC分类号： C12N15/115 , A61K31/585 , A61K31/7088 , A61K47/549 , C07J73/003 , C12N2310/16 , C12N2310/351 , C12N2320/30
摘要：本发明公开了雷公藤甲素和核酸适配子的衍生物、制备方法及其用途。雷公藤甲素和核酸适配子的衍生物的结构如式Ｉ，其中R 1 -R 7 ，G，A，B，M，Z，X的定义如说明书所述。本发明以核酸适配子与雷公藤甲素或其修饰物为起始原料，在雷公藤甲素中的C-14羟基、环氧基团和五元环内酯处引入连接基团A，再连接核酸适配子B，得到雷公藤甲素和核酸适配子的衍生物。本发明所述的雷公藤甲素和核酸适配子的衍生物具有靶向性好、抗癌活性强、毒副作用低、水溶性好、生物利用度高的特点，且本发明的制备方法科学合理，质量可控，重现性好，适于生产。

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