-
1.发明申请DIOSGENIN ACETATE-ISOXAZOLE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THEIR ANTIFUNGAL ACTIVITY 审中-公开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
Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Inventor： DAS, Archana Moni , HAZARIKA, Manash Protim , DEKA BHUYAN, Purnajyoti
CPC classification number: C07J71/0005 , C07J71/0047 , C07J71/0063
Abstract: 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.
Abstract translation: 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
-
2.发明申请OCTAHYDRO-2-H-NAPHTHO[1,2-F] INDOLE-4-CARBOXAMIDE DERIVATIVES AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开OCTAHYDRO-2-H-NAPHTHO [1,2-F]吲哚-4-羧酰胺衍生物作为选择性葡糖苷酸受体调节剂
公开(公告)号：WO2004026248A3
公开(公告)日：2004-07-15
申请号：PCT/US0329494
申请日：2003-09-17
Applicant: MERCK & CO INC , ALI AMJAD , ASTER SUSAN D , BALKOVEC JAMES M , GRAHAM DONALD W , HUNT JULIANNE A , KALLASHI FLORIDA , SINCLAIR PETER J , TATA JAMES R , TAYLOR GAYLE E , GOULET JOUNG L
Inventor： ALI AMJAD , ASTER SUSAN D , BALKOVEC JAMES M , GRAHAM DONALD W , HUNT JULIANNE A , KALLASHI FLORIDA , SINCLAIR PETER J , TATA JAMES R , TAYLOR GAYLE E , GOULET JOUNG L
IPC: A61K20060101 , A61K31/4162 , C07D231/44 , C07D231/54 , C07D417/00
CPC classification number: C07J71/0047 , C07D231/54 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/113
Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
Abstract translation: 本发明包括式I化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 还包括药物组合物和使用方法。
-
公开(公告)号：WO2016173524A1
公开(公告)日：2016-11-03
申请号：PCT/CN2016/080635
申请日：2016-04-29
Applicant: 正大天晴药业集团股份有限公司 , 南京明德新药研发股份有限公司
IPC: C07J9/00 , C07J53/00 , C07J71/00 , C07J43/00 , C07J31/00 , C07J33/00 , C07J41/00 , A61K31/58 , A61K31/575 , A61P43/00
CPC classification number: C07J9/00 , C07J9/005 , C07J31/006 , C07J41/0055 , C07J41/0061 , C07J41/0088 , C07J43/003 , C07J51/00 , C07J53/004 , C07J71/0047 , C07J71/0094
Abstract: 本申请公开了式Ⅰ、式Ⅱ、式Ⅲ、式Ⅳ或式Ⅴ所示化合物、其互变异构体、其立体异构体或其药学上可接受的盐，并公开了其在制备治疗FXR相关疾病药物中的应用。
-
4.发明申请NOVEL DERIVATIVES OF STEROIDAL[3,2-C]PYRAZOLE COMPOUNDS WITH GLUCOCORTICOID ACTIVITY 审中-公开具有葡萄糖激活活性的甾体[3,2-C]吡唑化合物的新衍生物
公开(公告)号：WO2010114476A1
公开(公告)日：2010-10-07
申请号：PCT/SE2010/050367
申请日：2010-04-01
Applicant: ASTRAZENECA AB , BLADH, Håkan , BURKAMP, Frank , GABOS, Balint , HANSEN, Peter
Inventor： BLADH, Håkan , BURKAMP, Frank , GABOS, Balint , HANSEN, Peter
CPC classification number: A61K31/58 , C07J71/0047
Abstract: The present invention provides named compounds of formula (I), and pharmaceutical compositions containing them and their use in therapy.
Abstract translation: 本发明提供命名的式（I）化合物和含有它们的药物组合物及其在治疗中的用途。
-
5.发明申请NOVEL STEROIDAL[3,2-C]PYRAZOL DERIVATIVES WITH GLUCOCORTICOID ACTIVITY 审中-公开具有葡萄糖激活作用的新型Steroidal [3,2-C]吡唑衍生物
公开(公告)号：WO2010114473A1
公开(公告)日：2010-10-07
申请号：PCT/SE2010/050357
申请日：2010-03-31
Applicant: ASTRAZENECA AB , BURKAMP, Frank , HANSEN, Peter
Inventor： BURKAMP, Frank , HANSEN, Peter
CPC classification number: A61K31/58 , C07J71/0047
Abstract: The present invention provides compounds of formula (I) wherein n, p, R 1 , R 2 , X 1 , X 2 , X 3 , X 4 , X 5 , R 3a , R 3b , R 4 , R 5 , R 6 , are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Abstract translation: 本发明提供式（I）化合物，其中n，p，R1，R2，X1，X2，X3，X4，X5，R3a，R3b，R4，R5，R6如说明书中所定义， 制剂，含有它们的药物组合物及其在治疗中的用途。
-
Patent Agency Ranking6.发明申请METHOD OF PREPARATION OF A SOLUBLE FORMULATION OF WATER-INSOLUBLE PENTACYCLIC AND TETRACYCLIC TERPENOIDS, A SOLUBLE FORMULATION OF A PENTACYCLIC OR TETRACYCLIC TERPENOID AND A PHARMACEUTICAL COMPOSITION CONTAINING THIS SOLUBLE FORMULATION 审中-公开可溶性配方水不溶性戊二酸和四环戊二烯的制备方法，可溶性配方的PENTACYCLIC或TETRACYCLIC TERPENOID和含有该溶解配方的药物组合物
公开(公告)号：WO2008037226A2
公开(公告)日：2008-04-03
申请号：PCT/CZ2007/000088
申请日：2007-09-25
Applicant: UNIVERZITA KARLOVA V PRAZE, PRÍRODOVEDECKÁ FAKULTA , UNIVERZITA PALACKÉHO V OLOMOUCI , I.Q.A., A.S. , SAREK, Jan , HAJDUCH, Marian , SVOBODA, Michal , NOVAKOVA, Katerina , SPACILOVA, Pavla , KUBELKA, Tomas , BIEDERMANN, David
Inventor： SAREK, Jan , HAJDUCH, Marian , SVOBODA, Michal , NOVAKOVA, Katerina , SPACILOVA, Pavla , KUBELKA, Tomas , BIEDERMANN, David
CPC classification number: C07J71/0047 , A61K31/56 , A61K47/6951 , B82Y5/00 , C07J63/008
Abstract: The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids, wherein the water-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized on this functional group with a substituent selected from the group comprising substituents of general formula Xa bound to the hydroxy group of the terpenoid, wherein Xa is -OC-R-COOH, substituents of general formula Xa bound to the amino group of the terpenoid, wherein Xa is -OC-R-COOH, quarternary ammonium substituents of general formula Xb bound to the carboxy group of the terpenoid, wherein Xb is -(CH2)nN+R3Y-, quarternary ammonium substituents of general formula Xc bound to the carboxy group of the terpenoid, wherein Xc je -(CH2)nR+Y-, substituents of general formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents -R-COOH, glycosylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy group of the terpenoid, wherein Xe is selected from the group comprising glucosyl, galactosyl, arabinosyl, rhamnosyl, lactosyl, cellobiosyl, maltosyl and the 2-deoxyanalogues thereof, and subsequently, the prepared derivative is dissolved in the solution containing water, a cyclodextrin and optionally pharmaceutically acceptable auxiliary substances, forming an inclusion derivative with the cyclodextrin. Object of the invention is further a soluble formulation of a pentacyclic or tetracyclic triterpenoid, containing an inclusion complex of the derivatized pentacyclic or tetracyclic terpenoid with a cyclodextrin, and optionally water and pharmaceutically acceptable auxiliary substances and further a pharmaceutical composition containing the soluble formulation.
Abstract translation: 本发明涉及一种制备水不溶性五环和四环萜类化合物的可溶性制剂的方法，其中具有游离羧酸，羟基或氨基官能团的水不溶性萜类化合物在该官能团上衍生自选自下组的取代基 包括与萜类化合物的羟基结合的通式Xa的取代基，其中Xa是-OC-R-COOH，与萜类化合物的氨基结合的通式Xa的取代基，其中Xa是-OC-R-COOH， 通式Xb的铵取代基与萜类化合物的羧基结合，其中Xb是 - （CH2）nN + R3Y-，通式Xc的季铵取代基与萜类化合物的羧基结合，其中Xc je-（CH2） nR + Y-，与萜类化合物的羧基结合的通式Xd的取代基，其中Xd表示-R-COOH，由α或β糖苷键与羟基结合的糖基取代基Xe或 萜类化合物的羧基，其中Xe选自包括葡糖基，半乳糖基，阿拉伯糖基，鼠李糖基，乳糖基，纤维二糖基，麦芽糖基及其2-脱氧醛糖基的组，随后将制备的衍生物溶解于含有水，环糊精 和任选的药学上可接受的辅助物质，与环糊精形成包合物衍生物。 本发明的另一目的是五环或四环三萜类化合物的可溶性制剂，其含有衍生的五环或四环萜类化合物与环糊精的包合物，以及任选的水和药学上可接受的辅助物质，以及含有可溶性制剂的药物组合物。
-
7.发明申请BILE-ACID DERIVED COMPOUNDS FOR ENHANCING ORAL ABSORPTION AND SYSTEMIC BIOAVAILABILITY OF DRUGS 审中-公开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
Applicant: XENOPORT INC , BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
Inventor： BHAT LAXMINARAYAN , GALLOP MARK A , JANDELEIT BERND
CPC classification number: C07J31/006 , C07J9/005 , C07J41/0055 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0063
Abstract: 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.
Abstract translation: 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。
-
8.发明申请POLYMERIC BILE ACID DERIVATIVES INHIBIT HEPATITIS B AND D VIRUS AND NTCP TRANSPORT 审中-公开聚合胆酸衍生物抑制乙型肝炎病毒和D型病毒和NTCP运输
公开(公告)号：WO2016045642A1
公开(公告)日：2016-03-31
申请号：PCT/CN2015/091000
申请日：2015-09-28
Inventor： LI, Wenhui , QI, Xiangbing , YAN, Huan , LIU, Yang , WANG, Zhiqiang , PENG, Bo , ZHANG, Lei
IPC: A61K31/575 , C07J9/00 , A61P31/20
CPC classification number: A61K31/585 , A61K31/575 , A61K31/58 , A61K45/06 , C07J9/00 , C07J9/005 , C07J41/005 , C07J41/0055 , C07J41/0061 , C07J43/003 , C07J71/0047
Abstract: The invention provides for treating HBV or HDV infection or inhibiting human sodium taurocholate co-transporting polypeptide (hNTCP) with a polymeric bile acid or salt thereof, and pharmaceutical compositions comprising a polymeric bile acid or salt thereof, and a second HBV or HDV medicament.
Abstract translation: 本发明提供用聚合胆汁酸或其盐治疗HBV或HDV感染或抑制人牛磺胆酸共转运多肽（hNTCP），以及包含聚合胆汁酸或其盐和第二种HBV或HDV药物的药物组合物。
-
9.发明申请NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS, COMPOSITIONS AND USES THEREOF 审中-公开新型[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
Applicant: 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
Inventor： 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: C07J71/00
CPC classification number: C07J71/0047 , C07J71/0063
Abstract: 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.
Abstract translation: 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。
-
10.发明申请NOVEL AMIDE DERIVATIVES OF STEROIDAL[3,2-C]PYRAZOLE COMPOUNDS WITH GLUCOCORTICOID ACTIVITY 审中-公开具有葡萄糖激活活性的甾体[3,2-C]吡唑化合物的新型衍生物
公开(公告)号：WO2010114471A1
公开(公告)日：2010-10-07
申请号：PCT/SE2010/050354
申请日：2010-03-31
Applicant: ASTRAZENECA AB , BURKAMP, Frank , GABOS, Balint , IVANOVA, Svetlana , LISIUS, Alice Ingrid Annéa
Inventor： BURKAMP, Frank , GABOS, Balint , IVANOVA, Svetlana , LISIUS, Alice Ingrid Annéa
CPC classification number: C07J71/0047 , A61K31/58
Abstract: The present invention provides compounds of formula (I) wherein n, R 1 , R 2 , X 1 , X 2 , X 3 , X 4, X 5 , R 3a , R 3b , R 4 , R 5 and R 6 are defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Abstract translation: 本发明提供式（I）化合物，其中n，R1，R2，X1，X2，X3，X4，X5，R3a，R3b，R4，R5和R6在本说明书中定义，其制备方法，药物组合物 包含它们及其在治疗中的用途。
-
-
-
-
-
-
-
-
-
Search Results
28
records
(took 0.017 seconds)
