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1. 发明申请

WO99045023A1 S-SUBSTITUTED 11 beta -BENZALDOXIME-ESTRA-4,9-DIENE-CARBONIC ACID THIOLESTERS, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： S-11取代β - 他们BENZALDOXIM雌-4,9-二烯KOHLENSÄURETHIOLESTER，制造方法及其所包含药物制剂
公开(公告)号：WO99045023A1
公开(公告)日：1999-09-10
申请号：PCT/DE1999/000408
申请日：1999-02-10
IPC分类号： A61K31/565 , A61P15/00 , A61P15/18 , C07J41/00 , C07J43/00
CPC分类号： C07J41/0083 , C07J43/006
摘要： The invention relates to S-substituted 11 beta -benzaldoxime-estra-4,9-diene-carbonic acid thiolesters of general formula (I) and the pharmaceutically acceptable salts thereof. The invention additionally relates to a method for the production of said compounds and to the pharmaceutical preparations containing these compounds. The compounds are bonded on the progesterone receptor and comprise a distinctly reduced antiglucocorticoidal effect.
摘要翻译： S-取代的β--Benzaldoxim描述11 - 雌-4,9-二烯kohlensäurethiolester通式（I），以及它们的药学上可接受的盐，一种用于其制备方法和含有这些化合物的药物组合物。化合物结合至黄体酮受体，并且具有显著降低的抗糖皮质激素作用。

2. 发明申请

WO9416709A3 THERAPEUTIC USES AND DELIVERY SYSTEMS OF DEHYDROEPIANDROSTERONE 审中-公开
标题翻译：去糖皮质激素的治疗用药和输送系统
公开(公告)号：WO9416709A3
公开(公告)日：1994-11-24
申请号：PCT/CA9400022
申请日：1994-01-19
申请人： ENDORECHERCHE INC
发明人： LABRIE FERNAND
IPC分类号： A61K8/63 , A61K9/00 , A61K9/70 , A61K31/565 , A61K31/57 , A61K31/58 , A61P5/00 , A61P15/00 , A61P15/02 , A61P17/00 , A61P25/00 , A61Q19/00 , C07J1/00 , C07J17/00 , C07J43/00
CPC分类号： C07J43/006 , A61K31/565 , A61K31/566 , A61K31/5685 , A61K31/57 , A61K31/58 , C07J1/0011 , C07J43/003 , A61K2300/00
摘要： Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these presursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.

3. 发明申请

WO2016086218A1 BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF 审中-公开
标题翻译：双酸衍生物作为FXR / TGR5激动剂及其使用方法
公开(公告)号：WO2016086218A1
公开(公告)日：2016-06-02
申请号：PCT/US2015/062826
申请日：2015-11-27
申请人： ENANTA PHARMACEUTICALS, INC.
发明人： WANG, Guoqiang , OR, Yat Sun , SHEN, Ruichao , LONG, Jiang , DAI, Peng , XING, Xuechao , HE, Jing
IPC分类号： A61K31/56
CPC分类号： C07J41/0066 , C07J9/005 , C07J41/0055 , C07J41/0088 , C07J41/0094 , C07J43/003 , C07J43/006 , C07J51/00
摘要： The present invention provides compounds of amino-substituted bile acid derivatives, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions. In one embodiment the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound or combination of compounds of the present invention, or a pharmaceutically acceptable salt form, stereoisomer, solvate, hydrate or combination thereof, in combination with a pharmaceutically acceptable carrier or excipient.
摘要翻译：本发明提供氨基取代的胆汁酸衍生物的化合物，包含这些化合物的药物组合物和使用这些化合物预防或治疗FXR介导的或TGR5介导的疾病或病症的方法。在一个实施方案中，本发明提供药物组合物，其包含治疗有效量的本发明化合物或化合物或其药学上可接受的盐形式，立体异构体，溶剂合物，水合物或其组合与药学上可接受的载体或赋形剂。

4. 发明申请

WO2012109752A1 STEROID ALKALOIDS AND USES THEREOF AS ANTIMICROBIAL AGENTS AGAINST ELECTRON TRANSPORT-DEFICIENT MICROBES AND AS POTENTIATORS FOR ANTIMICROBIAL AGENTS AGAINST PATHOGENIC BACTERIA 审中-公开
标题翻译：甾体碱性成分及其作为抗电泳剂的电子运输缺陷型微生物的抗微生物剂及其作为致病菌的抗微生物剂的潜力
公开(公告)号：WO2012109752A1
公开(公告)日：2012-08-23
申请号：PCT/CA2012/050087
申请日：2012-02-15
申请人： SOCPRA SCIENCES ET GÉNIE, S.E.C. , MALOUIN, François , MITCHELL, Gabriel , BOUARAB, Kamal , MARSAULT, Eric , CHAGNON, Félix , BOULANGER, Simon , GUAY, Isabelle
发明人： MALOUIN, François , MITCHELL, Gabriel , BOUARAB, Kamal , MARSAULT, Eric , CHAGNON, Félix , BOULANGER, Simon , GUAY, Isabelle
IPC分类号： C07J71/00 , A61K31/58 , A61L2/16 , A61P31/00 , A61P31/04 , C07J53/00 , C12Q1/18
CPC分类号： A61K31/58 , A01N45/00 , A61K31/395 , A61K31/7036 , A61L2/16 , C07J7/002 , C07J7/006 , C07J7/007 , C07J7/0085 , C07J41/005 , C07J41/0055 , C07J43/003 , C07J43/006 , C07J51/00 , G01N2800/52 , A61K2300/00
摘要： The present invention includes novel compounds based on the tomatidine skeleton as well as composition comprising these compounds alone and in combination with known compounds, which exhibit antimicrobial activity against extracellular or intracellular electron transport-deficient microbes and/or increase the antimicrobial activity of aminoglycoside antibiotics against their targets, and which are useful as antibacterial agents for treatment or prophylaxis of monomicrobiotic or polymicrobic bacterial infections or for the reduction of antibiotic resistance development in animals or in humans, or for use as antiseptics or agents for sterilization or disinfection.
摘要翻译：本发明包括基于西马齿蛋白骨架的新型化合物以及单独包含这些化合物的组合物和与已知化合物组合的组合物，其具有抗细胞外或细胞内电子转运缺陷微生物的抗微生物活性和/或增加氨基糖苷类抗生素对抗它们的靶标，并且其可用作用于治疗或预防单生或多微生物细菌感染的抗菌剂或用于在动物或人体中降低抗生素耐药性发展，或用作消毒剂或用于灭菌或消毒的试剂。

5. 发明申请

WO1994016709A2 THERAPEUTIC USES AND DELIVERY SYSTEMS OF DEHYDROEPIANDROSTERONE 审中-公开
标题翻译：去糖皮质激素的治疗用药和输送系统
公开(公告)号：WO1994016709A2
公开(公告)日：1994-08-04
申请号：PCT/CA1994000022
申请日：1994-01-19
申请人： ENDORECHERCHE INC.
发明人： ENDORECHERCHE INC. , LABRIE, Fernand
IPC分类号： A61K31/57
CPC分类号： C07J43/006 , A61K31/565 , A61K31/566 , A61K31/5685 , A61K31/57 , A61K31/58 , C07J1/0011 , C07J43/003 , A61K2300/00
摘要： Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these presursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.
摘要翻译：性类固醇前体如脱氢表雄酮和脱氢表雄酮硫酸盐，以及体内转化成前述物质的化合物用于治疗和/或预防阴道萎缩，性腺机能减退，性欲降低，骨质疏松症，尿失禁，卵巢癌，子宫癌，皮肤萎缩，避孕，以及与雌激素和/或孕激素组合用于治疗绝经。可以配制前体用于经皮或经粘膜给药。提供用于给予这些哺乳动物的凝胶，溶液，洗剂，霜剂，软膏和透皮贴剂，以及某些药物组合物和试剂盒，其可用于预防和治疗与性类固醇分泌减少相关的各种各样的病症前体由肾上腺。

6. 发明申请

WO2014170221A1 PROCESS FOR PRODUCING A SOLID FORM OF ABIRATERONE ACETATE 审中-公开
标题翻译：生产乙酸阿贝特酮固体形式的方法
公开(公告)号：WO2014170221A1
公开(公告)日：2014-10-23
申请号：PCT/EP2014/057375
申请日：2014-04-11
申请人： ZACH SYSTEM
发明人： POIRIER, Patricia , DERRIEN, Yvon , FORCATO, Massimiliano , COTARCA, Livius , MORICE, Pierrick
IPC分类号： C07J43/00
CPC分类号： C07J43/003 , C07J43/006
摘要： The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of preparing micro size abiraterone or derivatives thereof in high yield and purity by means of a spherical agglomeration process.
摘要翻译：本发明涉及一种制备17-取代的类固醇的方法，更具体地说，涉及通过球形聚集方法以高产率和纯度制备微尺寸阿比特酮或其衍生物的改进方法。

7. 发明申请

WO2012129673A1 INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10 审中-公开
标题翻译： 17β-HSD1,17β-HSD3和17β-HSD10的抑制剂
公开(公告)号：WO2012129673A1
公开(公告)日：2012-10-04
申请号：PCT/CA2012/000316
申请日：2012-03-26
申请人： UNIVERSITE LAVAL , POIRIER, Donald , ROY, Jenny , MALTAIS, Rene
发明人： POIRIER, Donald , ROY, Jenny , MALTAIS, Rene
IPC分类号： C07J1/00 , A61K31/565 , A61K31/566 , A61K31/58 , A61K31/675 , A61K31/69 , A61K51/04 , A61P35/00 , C12N9/04
CPC分类号： C07J41/0005 , A61K31/566 , A61K31/567 , A61K31/5685 , A61K31/58 , A61K31/675 , A61K31/69 , A61K45/06 , A61K51/04 , C07J1/0007 , C07J1/0062 , C07J21/00 , C07J21/008 , C07J31/006 , C07J41/0011 , C07J41/0038 , C07J41/0072 , C07J43/003 , C07J43/006 , C07J51/00 , C12Y101/01051
摘要： The present application discloses 17β hydroxy steroid dehydrogenase (17β HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17β HSDl inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17β HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17β HSDl and 17β HSD3 that have a spiro-morpholine substituent at C20.
摘要翻译：本申请公开了17β羟基类固醇脱氢酶（17βHSD）类型1,3,10抑制剂及其用途（单独和组合）用于治疗癌症和其他疾病。 17βHSD1抑制剂包括在C 16上具有非 - 氨基甲酰基苄基取代基的雌二醇衍生物。17βHSD3/ HSD10抑制剂包括在C3位被磺酰胺哌嗪取代的雄酮衍生物。还公开了作为在C20具有螺吗啉取代基的17βHSD1和17βHSD3的抑制剂的化合物。

8. 发明申请

WO2007025780A2 ALDOSTERONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：阿托品酮受体拮抗剂
公开(公告)号：WO2007025780A2
公开(公告)日：2007-03-08
申请号：PCT/EP2006/008593
申请日：2006-09-01
申请人： RECORDATI IRELAND LIMITED , RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.P.A.
发明人： LEONARDI, Amedeo , RIVA, Carlo , TAVECCHIA, Paolo , SIRONI, Giorgio
IPC分类号： C07J21/00 , C07J31/00 , C07J41/00 , C07J71/00 , A61K31/58
CPC分类号： C07J21/003 , C07J21/00 , C07J31/006 , C07J41/0038 , C07J43/006 , C07J53/001 , C07J71/00 , C07J71/0015
摘要： Compounds of the formula (I), (R 1 is one of a wide range of substituents; R 2 = H, halogen and R 3 = H, hydroxymethyl or CR 2 R 3 = cyclopropyl ring; CR 4 R 5 is one of formula (II), formula (III) and formula (IV) R a and R b are a bond between carbons 9 and 11 or an -O-, -S-, -CH 2 - or -CF 2 - bridge; R 6 is H, alkyl, -CH 2 OR x , -CH 2 SR x , -CH 2 SO-alkyl, -CH 2 SO 2 -alkyl, -CH 2 NHR x , -CH 2 N(alkyl)(R x ), -C(=O)O-alkyl, -C(=O)-alkyl, -C(=O)NHR x or -C(=O)N(alkyl)(R x ); R 7 = R 8 = H or CR 7 R 8 is a cyclopropyl ring; R 9 and R 9’ are H, halogen, alkyl or alkoxycarbonyl or a bond between carbons 22 and 23; R 10 is H or -C(=O)OR x ; R x is H, alkyl or acyl; R y is H, alkyl; R z is H, alkyl) are provided. They are aldosterone receptor antagonists, useful for the treatment of aldosteronism including hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease and insulinopathies.
摘要翻译：式（I），（R 1）的化合物是宽范围的取代基之一; R 2 = H，卤素和R 3， = H，羟甲基或CR 2 R 3 =环丙基环; CR 4 R 5是式（ II），式（III）和式（IV）R aa和R bb是碳9和11之间的键或-O - ， - S - ， - CH 2 - 或-CF 2 - 桥; R 6是H，烷基，-CH 2或 - CH 2 SO 2，CH 2 SO 2 - ， - CH 2， CH 2，NH 2，CH 2，N（烷基）（R -C（= O）O-烷基，-C（= O） - 烷基，-C（= O）NHR x或-C（= O））N（烷基）（R xx）; R 7 = R 8 = H或CR 7 R SUP> 8是环丙基环; R 9和R 9是H，卤素，烷基或烷氧基羰基或碳22和23之间的键; R 10是H或-C（= O）OR x; R x是H，烷基或酰基; H，烷基; R z是H，烷基）。它们是醛固酮受体拮抗剂，可用于治疗醛固酮增多症，包括高血压，心血管疾病，肾功能不全，水肿，脑血管疾病和胰岛素过敏。

9. 发明申请

WO1998007740A1 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES, PROCESS FOR PREPARING THE SAME, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES AND THEIR USE FOR PREPARING MEDICAMENTS 审中-公开
标题翻译： 7ALPHA-（XI-氨基烷基） - 雌三烯，制造方法药物制剂THAT THIS 7ALPHA-（XI-氨基烷基） - 雌三烯容纳和它们在药物的生产
公开(公告)号：WO1998007740A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004517
申请日：1997-08-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , BOHLMANN, Rolf , BITTLER, Dieter , HEINDI, Josef , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KÜNZER, Hermann , SAUER, Gerhard , HEGELE-HARTUNG, Christa , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
IPC分类号： C07J53/00
CPC分类号： C07J53/008 , C07J41/0072 , C07J43/006 , C07J53/002
摘要： The present invention describes new substituted 7α-(κ-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 or 2; A is a hydrogen atom or a C1-5-alkyl group; B and D represent each a hydrogen atom, or A and B represent together an alkylene group -(CH2)p- where p = 2, 3, 4 or 5 and D is a hydrogen atom, or A and D form together an alkylene group -(CH2)q- where q = 2, 3 or 4 and B is a hydrogen atom; and E is a non-substituted ethyl radical or an ethyl radical fluorinated one to five times; or the terminal substituent -(CH2)3-E in the side chain is substituted by an optionally substituted aryl or heteroaryl radical bonded to the sulphur atom directly or by a mono-, di- or trimethylene group; R3 is a hydrogen atom, a hydrocarbon radical with up to 8 carbon atoms or a radical of partial formula R3'-C(O)-, where R3' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms or a phenyl radical; R11 is a hydrogen atom, a halogen atom or a nitrooxy group -O-NO¿2?, R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom or R?14 and R15α¿ are an additional bond or a methylene bridge, or R15β is a methyl group and R15α is a hydrogen atom, R?15α and R15β¿ represent each a methyl group, or R?15β and R16β¿ form together a methylene bridge, or R?16α or R16β¿ are a halogen atom or R?16α and R16β¿ form together a methylidene group, and the remaining substitutents R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom, R17' at the α- or β-position is a hydrogen atom, a C¿1-5? alkyl, C2-5 alkenyl or C2-5 alkinyl group or a trifluoromethyl group; and R?17'¿ is a hydrogen atom or a radical of partial formula R17'''-C(O)-, where R17''' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms, or when R17' is at the α-position, R17' forms together with R14 an ethano bridge, provided that when A and B do not stand together for -(CH¿2?)p- or A and D stand together for -(CH2)q-, at least one of the substituents R?11, R14, R15α, R15β, R16α and R16b¿ be not a hydrogen atom. Also disclosed are the physiologically tolerable addition salts of these compounds with organic and inorganic acids. These new compounds have a very strong anti-estrogenic activity. Some of them are pure anti-estrogenes, others are anti-estrogenes with a partial estrogenic effect. Because of their spectrum of activity, these new compounds are most suitable for preparing medicaments for tumor therapy and hormone substitution therapy.

10. 发明申请

WO2014071984A1 PROCESS FOR MAKING ABIRATERONE-3-ACETATE 审中-公开
标题翻译：制备ABIRATERONE-3-ACETATE的方法
公开(公告)号：WO2014071984A1
公开(公告)日：2014-05-15
申请号：PCT/EP2012/072208
申请日：2012-11-09
申请人： SYNTHON BV
发明人： CASTULIK, Jakub , GIELING, Rene , VYKLICKY, Libor
IPC分类号： C07J31/00 , C07J43/00
CPC分类号： C07J31/006 , C07J43/006
摘要： The present invention relates to an improved process for making abiraterone-3-acetate of formula (1) starting from dehydroepiandrosterone-3-acetate (DHEA) of formula (2). In particular, it relates to an improved process of converting the 17- triflate compound of formula (5) into abiraterone-3-acetate (1) in 2- methyl-THF as the solvent and producing a product of high purity via its acid addition salt abiraterone-3-acetate esylate (1A).
摘要翻译：本发明涉及从式（2）的脱氢表雄酮-3-乙酸酯（DHEA）开始制备式（1）的阿比特龙-3-乙酸酯的改进方法。特别涉及将式（5）的17-三氟甲磺酸酯化合物转化为在二甲基THF中的阿比特龙-3-乙酸酯（1）作为溶剂的改进方法，并通过其酸加成产生高纯度的产物盐酸阿比特龙-3-醋酸盐（1A）。

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