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1. 发明申请

WO2010147947A2 NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：新型[3,2-c]异烟肼作为葡萄糖激素受体激动剂，其组合物及其用途
公开(公告)号：WO2010147947A2
公开(公告)日：2010-12-23
申请号：PCT/US2010/038619
申请日：2010-06-15
申请人： SCHERING CORPORATION , BIJU, Purakkattle, J. , BERLIN, Michael, Y. , LIM, Yeon-Hee , BITAR, Rema, D. , MCCORMICK, Kevin, D. , ASLANIAN, Robert, G. , LEE, Yoon Joo , ZHENG, Junying , HUANG, Ying , WON, Walter
发明人： BIJU, Purakkattle, J. , BERLIN, Michael, Y. , LIM, Yeon-Hee , BITAR, Rema, D. , MCCORMICK, Kevin, D. , ASLANIAN, Robert, G. , LEE, Yoon Joo , ZHENG, Junying , HUANG, Ying , WON, Walter
IPC分类号： C07J71/00
CPC分类号： C07J71/0047 , C07J71/0063
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: Formula (I) wherein L, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas (H-A), (II-A1 ), (II-A2), (II-A2.1 ), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (Vl), as described herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译：本发明提供具有以下通式结构的式（I）化合物及其药学上可接受的盐，溶剂合物，酯，前体药物，互变异构体或异构体：其中L，R1，R2，R3，R4 R 5和R 6彼此独立地选择并如本文所定义。本发明还提供式（IIa），（Ⅱ-A1），（Ⅱ-A2），（Ⅱ-A2.1），（Ⅱ-A2）的化合物（和盐，溶剂合物，酯，前体药物，互变异构体和异构体） A-2.2），（II-A-2.3），（II-A4），（HB），（HC），（III），（IV），（V），（VI）还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。

2. 发明申请

WO03020214A2 BILE-ACID DERIVED COMPOUNDS FOR ENHANCING ORAL ABSORPTION AND SYSTEMIC BIOAVAILABILITY OF DRUGS 审中-公开
标题翻译：用于增强口服吸收和系统生物利用度的胆汁酸衍生化合物
公开(公告)号：WO03020214A2
公开(公告)日：2003-03-13
申请号：PCT/US0227458
申请日：2002-08-29
申请人： XENOPORT INC , BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
发明人： BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
IPC分类号： C07J9/00 , C07J31/00 , C07J41/00 , C07J53/00 , C07J71/00 , A61K
CPC分类号： C07J31/006 , C07J9/005 , C07J41/0055 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0063
摘要： Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
摘要翻译：公开了表现出穿过动物肠壁的高运输的化合物。所述化合物可以任选地与口服给药后吸收不良或穿过肠壁不良转运的药物连接，以提供口服给药药物 - 化合物缀合物后药物的增强的治疗性和任选延长的治疗性全身血药浓度。还公开了含有和使用这些化合物的方法的药物组合物。

3. 发明申请

WO9518821A3 NOVEL ANTIANDROGENIC AGENTS AND RELATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：新型抗肿瘤药物及相关药物组合物及其使用方法
公开(公告)号：WO9518821A3
公开(公告)日：1995-08-31
申请号：PCT/US9500074
申请日：1995-01-05
申请人： STANFORD RES INST INT
发明人： TANABE MASATO , CHAO WAN-RU , CHONG WESLEY K M , CROWE DAVID F
IPC分类号： A61K31/56 , A61K31/58 , C07J1/00 , C07J21/00 , C07J71/00
CPC分类号： C07J1/0085 , C07J21/00 , C07J71/0063
摘要： Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I), wherein R1 through R10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

4. 发明申请

WO2016135749A1 DIOSGENIN ACETATE-ISOXAZOLE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THEIR ANTIFUNGAL ACTIVITY 审中-公开
标题翻译：二氢睾酮乙酸异恶唑衍生物，其制备方法及其抗真菌活性
公开(公告)号：WO2016135749A1
公开(公告)日：2016-09-01
申请号：PCT/IN2016/050062
申请日：2016-02-22
申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
发明人： DAS, Archana Moni , HAZARIKA, Manash Protim , DEKA BHUYAN, Purnajyoti
IPC分类号： C07J71/00 , A61P31/10 , A61K31/58
CPC分类号： C07J71/0005 , C07J71/0047 , C07J71/0063
摘要： This invention also relates to novel class of diosgenin acetate-Isoxazole and the synthesis of diosgenin acetate-Isoxazole starting from Diosgenin and its relatives with five (5) synthetic routes, acetylation (A), F-ring opening of diosgenin acetate (B), Oxidation of the hydroxyl group on C-26 of E-ring manipulation of diosgenin acetate (C), Formation of oxime (D) and Isoxazole formation on C-26 of E-ring manipulation of diosgenin acetate (E) having potent Antifungal activity against Alternaria alternate fungus.
摘要翻译：本发明还涉及新型乙酸异丝氨酸 - 异恶唑和从薯Di皂苷及其亲属开始的五（5）种合成路线，乙酰化（A），醋酸肌发生素（B）的F-开环，氧化乙酰肌氨酸激酶E的E环操作的C-26上的羟基（C），形成肟（D）和异恶唑形成在E-ring操作的E-ring操作中的醋酸司司丹酸（E）具有有效的抗真菌活性链格孢属交替真菌

5. 发明申请

WO2014207309A1 THERAPEUTICALLY ACTIVE ESTRATRIENTHIAZOLE DERIVATIVES AS INHIBITORS OF 17 B-HYDROXYSTEROID DEHYDROGENASE, TYPE 1 审中-公开
标题翻译：作为17型羟基脱氢酶脱氢酶抑制剂的治疗性活性噻唑衍生物，1型
公开(公告)号：WO2014207309A1
公开(公告)日：2014-12-31
申请号：PCT/FI2014/050517
申请日：2014-06-25
申请人： FORENDO PHARMA LTD
发明人： ELORANTA, Maire , HIRVELÄ, Leena , KANGAS, Lauri , KOSKIMIES, Pasi , LAMMINTAUSTA, Risto , UNKILA, Mikko
IPC分类号： C07J43/00 , C07J51/00 , C07J71/00 , A61K31/585 , A61P5/32
CPC分类号： C07J71/0063 , A61K31/58 , A61K31/704 , C07J43/003 , C07J51/00 , C07J71/0057
摘要： The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R6 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD and in treatment or prevention of steroid hormone de- pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1至R 6如权利要求中所定义。本发明进一步涉及它们作为17β-抑制剂-HSD的抑制剂的用途，以及用于治疗或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-HSD1酶和/或需要降低内源性雌二醇浓度。本发明还涉及前述化合物的制备和包含作为活性成分的一种或多种上述化合物或其药学上可接受的盐的药物组合物。

6. 发明申请

WO2015198232A1 FUSED TRITERPENE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：熔融TRITERPENE化合物及其用途
公开(公告)号：WO2015198232A1
公开(公告)日：2015-12-30
申请号：PCT/IB2015/054725
申请日：2015-06-24
申请人： PIRAMAL ENTERPRISES LIMITED
发明人： SHARMA, Rajiv , BORHADE, Namdev, Narayan , CHAKOR, Narayan, Subhash , MISTRY, Hitesh, Devchandbhai
IPC分类号： C07J71/00 , A61K31/58 , A61P37/00 , A61P35/00
CPC分类号： A61K31/58 , A61K45/06 , C07J63/008 , C07J71/0047 , C07J71/0063
摘要： The present invention discloses fused triterpene compounds, represented by the compounds of Formula I (as described herein), processes for their preparation, pharmaceutical compositions comprising the said compounds, their use as retinoid-related orphan receptors gamma (RORγ) modulators and/or interleukin-17 (IL-17) inhibitors and methods for their use in the treatment of a disease or a disorder mediated by RORγ and/or IL-17.
摘要翻译：本发明公开了由式I化合物（如本文所述）代表的稠合三萜化合物，其制备方法，包含所述化合物的药物组合物，其作为类视黄醇相关孤儿受体γ（RORγ）调节剂和/或白细胞介素 -17（IL-17）抑制剂及其用于治疗由RORγ和/或IL-17介导的疾病或病症的方法。

7. 发明申请

WO0226759A3 17 alpha FLUOROALKYL STEROIDS, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译： 17α-氟烷基stareroids，它们的制备方法和含有这些化合物的药物组合物
公开(公告)号：WO0226759A3
公开(公告)日：2002-06-20
申请号：PCT/DE0103732
申请日：2001-09-28
申请人： JENAPHARM GMBH , RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
发明人： RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
IPC分类号： A61K31/569 , A61K31/58 , A61P5/26 , A61P15/00 , A61P15/10 , A61P15/16 , A61P35/00 , C07J1/00 , C07J11/00 , C07J43/00 , C07J71/00 , A61K31/565
CPC分类号： C07J71/0047 , C07J1/0037 , C07J1/0085 , C07J11/00 , C07J71/0063 , C07J71/0084
摘要： The invention relates to 17 alpha fluoroalkyl steroids of the general formula (I), STEROID (I), wherein R3 represents a group of the formula CnFmHo, wherein n = 1, 2, 3, 4, 5 or 6, m > 1 and m+o = 2n+1. The invention further relates to methods for producing the same and to compositions that contain said compounds. The inventive composition of the general formula (I) possess androgenic activity.
摘要翻译：本发明涉及17阿尔法-Fluoraklylsteroide通式（I）其中R 3是下式基团的CnFmHo，其中n = 1，2，3，4，5或6，M> 1，且m + O = 2N + 1 其制备方法和含有这些化合物的药物组合物。根据本发明的通式（I）的化合物具有雄激素活性。

8. 发明申请

WO01083512A1 3-NITROGEN-6,7-DIOXYGEN STEROIDS AND USES RELATED THERETO 审中-公开
标题翻译： 3-硝基-6,7-二氧杂环十二烷及其相关用途
公开(公告)号：WO01083512A1
公开(公告)日：2001-11-08
申请号：PCT/CA2001/000581
申请日：2001-04-30
IPC分类号： A61K31/56 , A61K31/566 , A61K31/57 , A61K31/58 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/08 , A61P43/00 , C07J41/00 , C07J43/00 , C07J71/00
CPC分类号： C07J41/00 , C07J41/0005 , C07J41/0011 , C07J43/00 , C07J71/0047 , C07J71/0063 , Y02P20/55
摘要： A compound of formula (I) and pharmaceutical acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R and R are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R and R may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R may be a 2, or 3 atom chain to numeral 2 so that —N-R - forms part of a fused bicyclic structure to ring A; R and R are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R and/or R is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
摘要翻译：式（I）化合物及其药学上可接受的盐，溶剂合物，立体异构体和前药，分离或混合，其中独立地在每次出现时：R 1和R 2选自氢，氧，以便形成硝基或肟，氨基，硫酸根和磺酸，以及具有1-30个碳原子并且任选地含有1-6个选自氮，氧，磷，硅和硫的杂原子的有机基团，其中R 1和R 2 可以与它们都键合的N一起形成杂环结构，其可以是具有1-30个碳的有机基团的一部分，并且任选地含有1-6个选自氮，氧和硅的杂原子，并且其中R' 1>可以是2或3个到数字2的原子链，使得-NR 1 - 形成环A的稠合双环结构的一部分; R 3和R 4分别选自6和7的直接键，以便形成羰基，氢或保护基，使得R 3和/或R 4是羟基的一部分或羰基保护基; 数字1至17各自表示如上所述具有取代的碳。化合物可以配制成药物组合物，并用于治疗和/或预防各种病症，包括炎症，哮喘，过敏性疾病，慢性阻塞性肺病，特应性皮炎，实体瘤，AIDS，局部缺血和心律失常。

9. 发明申请

WO1988007051A1 19, 11'beta'-BRIDGED STEROIDS, THEIR PRODUCTION AND PHARMACEUTICAL PREPARATIONS CONTAINING SAME 审中-公开
标题翻译： 19,11β-复合型STEROIDS，其生产和含有其的药物制剂
公开(公告)号：WO1988007051A1
公开(公告)日：1988-09-22
申请号：PCT/DE1988000150
申请日：1988-03-11
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , OTTOW, Eckhard , WIECHERT, Rudolf , NEEF, Günter , BEIER, Sybille , ELGER, Walter , HENDERSON, David, Andrew
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J53/00
CPC分类号： C07J71/0063 , C07J21/006 , C07J31/006 , C07J41/0038 , C07J53/002 , C07J71/0005 , C07J71/0047
摘要： New 19, 11 beta -bridged steroids having the general formula (I), in which R' signifies a methyl or ethyl residue; R signifies a hydrogen or chlorine atom or a C1-C4 alkyl residue; B and G, which are identical or different, signify respectively a hydrogen atom or a C1-C4 alkyl residue, or, together, a second bond between carbon atoms 6 and 7; B and R signify a methylene or ethylene group; Z signifies the residue of a pentagonal or hexagonal ring, which may be substituted and may be unsaturated; V signifies a carbocyclic or heterocyclic aryl residue which may be substituted; the ring A signifies (a), in which M and N together signify a second bond, or M signifies a hydrogen atom and N a hydroxy group, in which B, R , G, R , D and E are then hydrogen atoms and X an oxygen atom, two hydrogen atoms or a hydroxyimino group N SIMILAR OH; R and D, which are identical or different, signify respectively a hydrogen atom, a nitrile residue or a C1-C4 alkyl residue, or, together, a methylene or ethylene group; E signifies a hydrogen atom, a C1-C4 alkyl residue; D and E togethe. signify a second bond between the carbon atoms 1 and 2 or, together, a methylene group; or (b) or (c), R signifying a hydrogen atom or a C1-C8 alkyl residue. The invention also concerns possibly the pharmaceutically compatible additional salts of said steroids with acids. The new compounds possess valuable pharmacological properties.
摘要翻译：新的19,11个具有通式（I）的β-桥连类固醇，其中R'表示甲基或乙基残基; R 2表示氢或氯原子或C 1 -C 4烷基残基; B和G相同或不同，分别表示氢原子或C1-C4烷基残基，或共同表示碳原子6和7之间的第二键; B和R 2表示亚甲基或亚乙基; Z表示可以被取代并且可以是不饱和的五边形或六方晶环的残基; V表示可被取代的碳环或杂环芳基残基; 环A表示（a），其中M和N一起表示第二个键，或M表示氢原子和N a羟基，其中B，R 2，G，R 3，D和E 然后是氢原子，X是氧原子，两个氢原子或羟基亚氨基基团; R 3和D相同或不同，分别表示氢原子，腈残基或C1-C4烷基残基，或共同表示亚甲基或亚乙基; E表示氢原子，C1-C4烷基残基; D和E togethe。表示碳原子1和2之间的第二个键或一起是亚甲基; 或（b）或（c）表示氢原子或C 1 -C 8烷基残基的R 11。本发明还可能涉及所述类固醇与酸的药学上相容的附加盐。新化合物具有宝贵的药理性质。

10. 发明申请

WO2010147947A3 NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：新型[3,2-c]异烟肼作为葡萄糖激素受体激动剂，其组合物及其用途
公开(公告)号：WO2010147947A3
公开(公告)日：2011-03-03
申请号：PCT/US2010038619
申请日：2010-06-15
申请人： SCHERING CORP , BIJU PURAKKATTLE J , BERLIN MICHAEL Y , LIM YEON-HEE , BITAR REMA D , MCCORMICK KEVIN D , ASLANIAN ROBERT G , LEE YOON JOO , ZHENG JUNYING , HUANG YING , WON WALTER
发明人： BIJU PURAKKATTLE J , BERLIN MICHAEL Y , LIM YEON-HEE , BITAR REMA D , MCCORMICK KEVIN D , ASLANIAN ROBERT G , LEE YOON JOO , ZHENG JUNYING , HUANG YING , WON WALTER
IPC分类号： C07J71/00 , A61K31/59 , A61P5/44
CPC分类号： C07J71/0047 , C07J71/0063
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: Formula (I) wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas (H-A), (II-A1 ), (II-A2), (II-A2.1 ), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (Vl), as described herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译：本发明提供具有以下通式结构的式（I）化合物及其药学上可接受的盐，溶剂合物，酯，前体药物，互变异构体或异构体：其中L，R1，R2，R3，R4 ，R5和R6彼此独立地选择并如本文所定义。本发明还提供式（IIa），（Ⅱ-A1），（Ⅱ-A2），（Ⅱ-A2.1），（Ⅱ- A-2.2），（II-A-2.3），（II-A4），（HB），（HC），（III），（IV），（V），（VI）还提供了药物组合物，制备方法和使用这些化合物在治疗和预防广泛范围的免疫，自身免疫和炎性疾病和病症中的方法。

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