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1. 发明申请

WO2015170341A1 PROCESS FOR PREPARATION OF 7-DEHYDROCHOLESTEROL 审中-公开
标题翻译：制备7-脱氢胆甾醇的方法
公开(公告)号：WO2015170341A1
公开(公告)日：2015-11-12
申请号：PCT/IN2015/000198
申请日：2015-05-06
申请人： FERMENTA BIOTECH LIMITED
发明人： DATLA, Anupama , TAMORE, Jagdish , TRIVIKRAM, Sreenath
IPC分类号： C07J9/00 , C07J31/00
CPC分类号： C07J9/00 , C07J31/003
摘要： The invention discloses an improved cost-effective process for preparation of 7-Dehydrocholesterol of formula I with good yield and purity, comprising:a) epimerizing 7(alpha+beta) bromo protected cholesterol in presence of tetrabutyl ammonium bromide in toluene or a ketonic solvent or combinations thereof to obtain predominantly 7.alpha-bromo 3-protected cholesterol; b) Reacting 7.apha-bromo 3- protected cholesterol with substituted or unsubstituted thiophenol or its salts in presence of a liquor ammonia to obtain predominantly 7.beta.-thiophenyl)-3-protected cholesterol; c) Oxidizing 7. beta. - thiophenyl 3-protected cholesterol in presence of Cumene hydrogen peroxide and Titanium tetraisopropoxide to obtain 7. beta. -phenyl sulfoxide 3-protected cholesterol; d) Converting 7. beta. -phenyl sulfoxide 3-protected cholesterol into 7-Dehydro 3-protected cholesterol in presence of base; e) purifying 7-Dehydro 3-protected cholesterol by suspending in a suitable organic solvent; and f) Deprotecting the 7-Dehydro 3-protected cholesterol by treating with alkali in presence of methanol to obtain 7-Dehydrocholesterol followed by purification of 7-Dehydrocholesterol from an organic solvent.
摘要翻译：本发明公开了一种用于制备具有良好产率和纯度的式I的7-脱氢胆固醇的改进的成本有效的方法，其包括：a）在甲苯或酮溶剂中存在四丁基溴化铵的7（α+β）溴保护的胆固醇差向异构化或其组合以主要获得7.α-溴3-保护的胆固醇; b）在液氨的存在下，将7-溴-3-保护的胆固醇与取代或未取代的苯硫酚或其盐反应，主要得到7.β-噻吩基）-3-保护的胆固醇; c）氧化7.β。在苯甲酸过氧化氢和四异丙氧基钛的存在下，将噻吩-3-保护的胆固醇得到7.β。苯基亚砜3-保护胆固醇; d）转换7. beta。苯基亚砜将3-保护的胆固醇转化为7-脱氢3-保护的胆固醇，在碱的存在下; e）通过悬浮在合适的有机溶剂中纯化7-脱氢3-保护的胆固醇; 和f）通过在甲醇存在下用碱处理来脱保护7-脱氢3-保护的胆固醇，得到7-脱氢胆固醇，然后从有机溶剂中纯化7-脱氢胆固醇。

2. 发明申请

WO2013154752A1 A NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3β-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVER DISEASES AND ATHEROSCLEROSIS 审中-公开
标题翻译：一种新型胆固醇代谢物，5-烯醇，3β-25-二醇，二异丙酚（25HCDS），用于治疗代谢性疾病，高脂血症，糖尿病，脂肪肝疾病和甲状腺功能亢进
公开(公告)号：WO2013154752A1
公开(公告)日：2013-10-17
申请号：PCT/US2013/031861
申请日：2013-03-15
申请人： VIRGINA COMMONWEALTH UNIVERSITY
发明人： REN, Shunlin
IPC分类号： C07J31/00 , C07C401/00
CPC分类号： C07J31/006 , A61J1/14 , C07J9/00 , C07J31/003
摘要： 5-cholesten, 3β, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR ϒ agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.
摘要翻译：已经发现5-胆甾醇，3β，25-二醇，二硫酸盐（25HCDS）是可信的PPARγ激动剂和LXR拮抗剂，并且用于治疗脂质疾病和炎性疾病，包括但不限于脂肪肝，炎性肠和动脉粥样硬化性疾病。

3. 发明申请

WO2013053691A1 PROCESS FOR PREPARING 17-SUBSTITUTED STEROIDS 审中-公开
标题翻译：制备17种取代的甾体的方法
公开(公告)号：WO2013053691A1
公开(公告)日：2013-04-18
申请号：PCT/EP2012/069937
申请日：2012-10-09
申请人： ZACH SYSTEM
发明人： DERRIEN, Yvon , POIRIER, Patricia , FORCATO, Massimiliano , PINTUS, Tony , COTARCA, Livius , MEUNIER, Sébastien , GRAINDORGE, Laurence
IPC分类号： C07J13/00 , C07J43/00 , C07J75/00
CPC分类号： C07J43/003 , C07J1/0059 , C07J31/003 , C07J31/006
摘要： The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.
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，涉及通过关键的3-甲酸中间体以高产率和纯度合成阿比酮酮或其衍生物的改进方法。

4. 发明申请

WO2013036835A1 NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF 审中-公开
标题翻译：神经性甾体，组合物及其用途
公开(公告)号：WO2013036835A1
公开(公告)日：2013-03-14
申请号：PCT/US2012/054261
申请日：2012-09-07
申请人： SAGE THERAPEUTICS, INC. , UPASANI, Ravindra, B. , HARRISON, Boyd, L. , ASKEW, Benny, C. Jr. , DODART, Jean-Cosme , SALITURO, Francesco, G. , ROBICHAUD, Albert, J.
发明人： UPASANI, Ravindra, B. , HARRISON, Boyd, L. , ASKEW, Benny, C. Jr. , DODART, Jean-Cosme , SALITURO, Francesco, G. , ROBICHAUD, Albert, J.
IPC分类号： C07J41/00 , C07J31/00 , C07J9/00 , A61K31/57 , A61K31/575 , A61P25/18 , A61P25/28
CPC分类号： C07J41/00 , C07J1/00 , C07J1/0029 , C07J3/00 , C07J7/007 , C07J9/00 , C07J9/005 , C07J31/003 , C07J31/006 , C07J41/0005 , C07J41/0011 , C07J41/0055 , C07J43/003
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L 1 , L 2 , L 3 , X 1 , X 2 , Y, R z4 , R z5 , R z6 , n, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b , R 6a , R 6b , R 7a , R 7b , R 11a , R 11b , R 14 , R 17 , R 19 , R 20 , R 23a , R 23b , and R 24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
摘要翻译：根据式（I）和其药学上可接受的盐提供化合物，其中Z是式（i），（ii），（iii），（iv）或（v）的基团，其中L 1， L3，X1，X2，Y，Rz4，Rz5，Rz6，n，R1，R2，R3a，R3b，R4a，R4b，R6a，R6b，R7a，R7b，R11a，R11b，R14，R17，R19，R20， R23b和R24如本文所定义，及其药物组合物。本发明的化合物可用于预防和治疗哺乳动物中各种CNS相关病症。

5. 发明申请

WO2008157460A1 ANDROSTANE AND PREGNANE STEROIDS WITH POTENT ALLOSTERIC GABA RECEPTOR CHLORIDE IONOPHORE MODULATING PROPERTIES 审中-公开
标题翻译：安非他酮和前列腺素与耐药性GABA受体氯离子离子调节特性
公开(公告)号：WO2008157460A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/067059
申请日：2008-06-16
申请人： COOK, Kevin, M. , RUNYON, Scott, P. , ROGAWSKI, Michael , KEPLER, John , NAVARRO, Hernan , KAMINSKI, Rafal , ORR, Matthew
发明人： RUNYON, Scott, P. , ROGAWSKI, Michael , KEPLER, John , NAVARRO, Hernan , KAMINSKI, Rafal , ORR, Matthew
IPC分类号： A61K31/56 , A61P25/02
CPC分类号： C07J41/0005 , C07J7/00 , C07J31/003
摘要： This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
摘要翻译：本发明描述了结构1,2和3的化合物及其作为GABA受体氯离子载体复合物的变构调节剂的用途，以缓解压力，焦虑，情绪障碍，癫痫发作，抑郁症，药物和酒精滥用的治疗，记忆，经前期障碍，和神经系统损伤。

6. 发明申请

WO1990004398A1 A NEW PHARMACEUTICAL USE OF FUSIDIC ACID AND DERIVATIVES THEREOF 审中-公开
标题翻译：一种新的药物使用方法及其衍生物
公开(公告)号：WO1990004398A1
公开(公告)日：1990-05-03
申请号：PCT/DK1989000254
申请日：1989-10-30
申请人： BENDTZEN, Klaus
IPC分类号： A61K31/575
CPC分类号： C07J13/007 , A61K31/565 , C07J31/003 , C07J31/006 , C07J41/0027 , C07J41/0061
摘要： The use of fusidic acid or a derivative thereof for the manufacture of a composition for interfering with cytokines in a biological system, in particular for interfering with a cytokine such as a lymphokine, interleukine, monokine, interferon or colony-stimulating factor. Fusidic acid and derivatives thereof are useful for preventing effects of cytokines known to be pathogenetically involved in pathological conditions. Said conditions may e.g. be: insulin-dependent diabetes mellitus (Type 1), hyper- or hypo-functioning of the thyroid gland (e.g. thyroiditis), Addison's disease, endogenous uveitis, eye surgery such as cornea transplantation, cataract operation and laser surgery, transplant rejection, graft-versus-host disease, Crohn's disease or ulcerative colitis, pernicious anemia, celiac disease, contact dermatitis, allergic/atopic dermatitis, pemphigus vulgaris or pemphigoid, multiple sclerosis, systemic lupus erythematosus, polymyalgia rheumatica, conditions related to vasculitis phenomena, neoplastic diseases such as multiple myeloma, septic shock caused by gram-negative bacteria, DIC, arteriosclerosis, periodontal diseases, arthritis, osteoarthrosis or arthritis urica.
摘要翻译：使用夫西地酸或其衍生物用于制造用于干扰生物系统中的细胞因子的组合物，特别是用于干扰细胞因子如淋巴因子，白细胞介素，单核因子，干扰素或集落刺激因子。夫西地酸及其衍生物可用于预防已知病理学参与病理状况的细胞因子的作用。所述条件可以例如。是：胰岛素依赖性糖尿病（1型），甲状腺（例如甲状腺炎），艾迪生病，内源性葡萄膜炎，角膜移植等眼外科手术，白内障手术和激光手术，移植排斥反应，移植物 - 抗宿主病，克罗恩病或溃疡性结肠炎，恶性贫血，腹腔疾病，接触性皮炎，过敏性/特应性皮炎，寻常型天疱疮或类天疱疮，多发性硬化症，系统性红斑狼疮，风湿性多肌痛，与血管炎现象相关的病症，肿瘤性疾病作为多发性骨髓瘤，革兰氏阴性菌引起的败血性休克，DIC，动脉硬化，牙周病，关节炎，骨关节炎或关节炎尿。

7. 发明申请

WO2011127465A3 SHIP INHIBITORS AND USES THEREOF 审中-公开
标题翻译：船舶抑制剂及其用途
公开(公告)号：WO2011127465A3
公开(公告)日：2012-03-15
申请号：PCT/US2011031930
申请日：2011-04-11
申请人： UNIV NEW YORK STATE RES FOUND , SYRACUSE UNIVERSITY TECHNOLOGY TRANSFER AND IND DEV OFFICE , KERR WILLIAM G , CHISHOLM JOHN D
发明人： KERR WILLIAM G , CHISHOLM JOHN D
IPC分类号： C07C401/00 , A61K31/56 , A61K31/565 , A61K31/575 , A61P35/00
CPC分类号： C07J41/0005 , A61K31/56 , A61K31/565 , A61K31/575 , C07J1/0007 , C07J1/0011 , C07J9/00 , C07J31/003 , C07J31/006 , C07J41/0011 , C07J41/0027 , C07J41/005 , C07J41/0055
摘要： The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
摘要翻译：本发明涉及SHIP抑制剂化合物和使用这些化合物的方法。特别地，本发明公开了以下方法：（i）在受试者中治疗移植物抗宿主病的方法; （ii）抑制细胞中SHIP1蛋白的方法; （iii）选择性抑制细胞中SHIP1蛋白的方法; （iv）在器官或组织移植受者中治疗或预防移植物抗宿主病（GVHD）的方法; （v）调节表达SHIP1或SHIP2的细胞中SHIP活性的方法; （vi）移植物的离体或体外治疗方法; （vii）抑制受试者的肿瘤生长和转移的方法; （viii）治疗受试者血液恶性肿瘤的方法; （ix）诱导多发性骨髓瘤细胞凋亡的方法; （x）治疗受试者中多发性骨髓瘤的方法; （i）抑制人乳腺癌细胞增殖的方法; 和（xii）治疗受试者乳腺癌的方法。

8. 发明申请

WO2009059765A3 PROCESS FOR THE PREPARATION OF DROSPIRENONE 审中-公开
标题翻译：制备灭活雄激素的方法
公开(公告)号：WO2009059765A3
公开(公告)日：2009-10-15
申请号：PCT/EP2008009372
申请日：2008-11-06
申请人： CHORISIS S R L , GALLIANI GUIDO , RADAELLI VINCENZO , TERRANEO ALBERTO
发明人： GALLIANI GUIDO , RADAELLI VINCENZO , TERRANEO ALBERTO
IPC分类号： C07J1/00 , A61K31/585 , A61P15/18 , C07J31/00 , C07J53/00
CPC分类号： C07J1/0011 , C07J31/003 , C07J53/008
摘要： The present invention describes a process for the preparation of drospirenone (I) using androstendione as a starting material. In particular, androstendione protected on carbonyl group in position 3 as an enol-ether is functionalized in position 16 with a sulfoxide group and the derivative thus obtained undergoes thermal elimination in alkaline to give androsta-4,15- diene-3, 17-dione (V) which is further transformed into Drospirenone (I).
摘要翻译：本发明描述了使用雄甾烯二酮作为原料制备屈螺酮（I）的方法。特别是，在3位的羰基上保护的雄甾烯二酮为烯醇醚，在16位上用亚砜基官能化，并且由此得到的衍生物在碱性下经受热消除，得到雄甾-4,15-二烯-3,17-二酮（V），其进一步转化为屈螺酮（I）。

9. 发明申请

WO2009059765A2 PROCESS FOR THE PREPARATION OF DROSPIRENONE 审中-公开
标题翻译：制备吡罗昔酮的方法
公开(公告)号：WO2009059765A2
公开(公告)日：2009-05-14
申请号：PCT/EP2008/009372
申请日：2008-11-06
申请人： CHORISIS S.R.L. , GALLIANI, Guido , RADAELLI, Vincenzo , TERRANEO, Alberto
发明人： GALLIANI, Guido , RADAELLI, Vincenzo , TERRANEO, Alberto
IPC分类号： C07J1/00 , C07J31/00 , C07J53/00 , A61K31/585 , A61P15/18
CPC分类号： C07J1/0011 , C07J31/003 , C07J53/008
摘要： The present invention describes a process for the preparation of drospirenone (I) using androstendione as a starting material. In particular, androstendione protected on carbonyl group in position 3 as an enol-ether is functionalized in position 16 with a sulfoxide group and the derivative thus obtained undergoes thermal elimination in alkaline to give androsta-4,15- diene-3, 17-dione (V) which is further transformed into Drospirenone (I).
摘要翻译：本发明描述了使用雄烯二酮作为原料制备屈螺酮（I）的方法。特别地，作为烯醇 - 醚在3位上被羰基保护的雄烯二酮在第16位用亚砜官能化，所得衍生物在碱性条件下进行热消除，得到雄甾-4,15-二烯-3,17-二酮（V），其进一步转化为屈螺酮（I）。

10. 发明申请

WO2006003013B1 NOVEL 2-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-ONES USED IN THE FORM OF INHIBITORS OF 17ß-HYDROXYSTEROIDDEHYDROGENASE OF TYPE 1 审中-公开
标题翻译： NEW 2-取代的雌-1,3,5（10） - 三烯-17-酮作为17-β-羟类固醇脱氢酶类型1抑制剂
公开(公告)号：WO2006003013B1
公开(公告)日：2006-08-31
申请号：PCT/EP2005007315
申请日：2005-07-04
申请人： SCHERING AG , HILLISCH ALEXANDER , REGENHARDT WILKO , GEGE CHRISTIAN , PETERS OLAF , BOTHE ULRICH , ADAMSKI JERZY , MOELLER GABRIELE , ROSINUS ANDREA , ELGER WALTER , SCHNEIDER BIRGITT
发明人： HILLISCH ALEXANDER , REGENHARDT WILKO , GEGE CHRISTIAN , PETERS OLAF , BOTHE ULRICH , ADAMSKI JERZY , MOELLER GABRIELE , ROSINUS ANDREA , ELGER WALTER , SCHNEIDER BIRGITT
IPC分类号： C07J1/00 , A61K31/566 , A61P5/32 , C07J31/00 , C07J41/00 , C07J53/00
CPC分类号： C07J53/004 , A61K31/565 , A61K45/06 , C07J1/0059 , C07J31/003 , C07J41/0094 , A61K2300/00
摘要： The invention relates to novel 2-substituted estra-1,3,5(10)-trien-17-ones of formula (I), wherein R 2 is an C 1 -C 8 alkyl saturated or unsaturated group, an C 1 -C 5 -alkyloxy group, an aralkyl- or alkylaryl rest, an -O-C n F m H o rest, wherein n=1,2,3,4,5 or 6, m=1 and m = 2n+1, or a CH 2 XY group in which X is an oxygen atom and Y is an alkyl rest containing 1 to 4 carbon atoms, a halogen atom and a nitrile group, R 13 is a hydrogen atom or a methyl group, R 16 is a hydrogen or fluorine atom, Z is an oxygen or sulfur atom, each R 4 and R 6 independently of each other represents a or ß hydrogen atom, an C 1 -C 5 alkyl, C 1 -C 5 -alkyloxy, C 1 -C 5 -acyl or hydroxy group or an aralkyl- or alkylaryl rest, R 3 and R 4 represent together an oxygen atom, R 5 and R 6 represent together an oxygen atom, each R 7 and R 8 represents a hydrogen atom or together an oxygen atom, each R 7 and R 8 represents a hydrogen atom or together a CH 2 group. Pharmaceutically acceptable salts of said compounds, the production and use thereof in the form of drags which are usable for preventing and treating estrogen-dependent diseases and are influenced by inhibiting 17ß-hydroxysteroiddehydrogenase of type 1 are also disclosed.
摘要翻译：本发明涉及新的2-取代的雌-1,3,5（10） - 三烯-17-酮的通式（I），其中R ^{2 是饱和或不饱和的C _{1 < / SUB> -C _{8 烷基，一个C _{1 -C _{5 烷氧基，芳烷基或烷芳基，基团-O-C < 其中n = 1,2,3,4,5或6，m = 1，m = 2n + 1 ，或基团CH _{2 XY，其中X表示氧原子，Y是碳原子数为1〜4的烷基，卤素原子或腈基，R ^{13 氢原子或甲基，R ^{16 代表氢原子或氟原子，Z是氧或硫原子，R ^{3 和R ^{5 各自独立地为表示α-或β-位置氢原子，R ^{4 和R ^{6 各自独立地为α-或β-位置氢原子，C _{1 1 -C _{5 酰基，或羟基或芳烷基或烷芳基，R _{3 和R _{4 一起为氧原子，R _{5 和R _{6 一起为氧原子，R ^{7 和R ^{8 各自为氢原子或一起CH _{2 是一个基团，及其药学上可接受的盐，它们的制备和作为药物的雌激素依赖性疾病的预防和治疗为特征的抑制17-Hydroxysteroiddehydro-的使用 genase 1型影响。}}}}}}}}}}}}}}}}}}}}}

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