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1. 发明申请

WO2019243970A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY SKIN DISEASES AND CANCER 审中-公开
公开(公告)号：WO2019243970A1
公开(公告)日：2019-12-26
申请号：PCT/IB2019/054976
申请日：2019-06-14
申请人： CELLIX BIO PRIVATE LIMITED
发明人： KANDULA, Mahesh
IPC分类号： A61K9/00 , A61P17/00 , C07C229/00
摘要： The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II formula III, formula IV, formula V, formula VI, formula VII, and formula VIII and the methods for the treatment of inflammatory skin diseases and cancer may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of facial hirsutism, GI Polyps, rosacea, acne, melanoma, psoriasis, dermatitis and cancer including gliomas, gastrointestinal polyps, anaplastic astrocytoma and metastatic cancers.

2. 发明申请

WO2019219000A1 CRYSTALLINE FORMS OF 1-(ACYLOXY)-ALKYL CARBAMATE DRUG CONJUGATES OF NAPROXEN AND PREGABALIN 审中-公开
公开(公告)号：WO2019219000A1
公开(公告)日：2019-11-21
申请号：PCT/CN2019/086809
申请日：2019-05-14
申请人： XGENE PHARMACEUTICAL INC. , AI, Xinmiao
发明人： AI, Xinmiao , XU, Feng , LI, Weidong , CHEN, Li
IPC分类号： C07C229/00 , A61K31/19 , A61P25/00
摘要： Crystalline forms of the drug conjugate ( S )-3-(((( R )-1-(( S )-2-(6-methoxynaphthalen-2-yl)propanoyloxy)ethoxy)carbonyl-amino)methyl)-5-methylhexanoic acid and their pharmaceutical compositions are described herein. Also described are methods of using the crystalline forms for treatment of diseases and conditions.

3. 发明申请

WO2017132912A1 苯并脂肪环取代烷基胺类化合物及其用途审中-公开
公开(公告)号：WO2017132912A1
公开(公告)日：2017-08-10
申请号：PCT/CN2016/073384
申请日：2016-02-03
申请人：华东理工大学 , 中国科学院上海药物研究所
发明人：李剑 , 蓝乐夫 , 王友鑫 , 陈菲菲 , 魏汉文 , 蒋华良
IPC分类号： C07C209/00 , C07C211/30 , C07C217/00 , C07C229/00 , A61K31/137 , A61P31/04
CPC分类号： A61K31/137 , C07C209/00 , C07C211/30 , C07C217/00 , C07C229/00
摘要：本发明提供一种苯并脂肪环取代烷基胺类化合物及其用途，具体地，涉及一种式I所示的化合物、或其药学上可接受的盐及其制备方法，以及其在制备金黄色葡萄球菌金黄色色素合成抑制剂类抗菌药物中的应用 (I).

4. 发明申请

WO2017049470A1 PRODRUGS OF GAMMA-HYDROXYBUTYRIC ACID, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译： γ-羟基丁酸的组合物及其用途
公开(公告)号：WO2017049470A1
公开(公告)日：2017-03-30
申请号：PCT/CN2015/090326
申请日：2015-09-23
申请人： XW LABORATORIES INC.
发明人： XIANG, Jia-Ning , XU, Xuesong , ZHANG, Xuan
IPC分类号： C07C53/124 , C07C229/00 , A61K31/19 , A61P25/00
CPC分类号： C07C229/36 , A61K45/06 , C07B59/001 , C07B2200/05 , C07B2200/07 , C07C69/24 , C07C69/612 , C07C69/618 , C07C69/67 , C07C69/74 , C07C69/75 , C07C69/76 , C07C69/78 , C07C69/80 , C07C69/82 , C07C69/92 , C07C69/96 , C07C229/08 , C07C255/57 , C07C271/22 , C07C317/44 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D213/79 , C07D213/80 , C07D277/56 , C07D307/68 , C07D333/38
摘要： The present application discloses prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof.
摘要翻译：本申请公开了γ-羟基丁酸的前药以及其组合物和用途。

5. 发明申请

WO2016161269A1 INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：印度尼西亚2,3-DIOXYGENASE治疗癌症的抑制剂
公开(公告)号：WO2016161269A1
公开(公告)日：2016-10-06
申请号：PCT/US2016/025531
申请日：2016-04-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BALOG, James Aaron , CHERNEY, Emily Charlotte , GUO, Weiwei , HUANG, Audris , MARKWALDER, Jay A. , SEITZ, Steven P. , SHAN, Weifang , WILLIAMS, David K. , MURUGESAN, Natesan , NARA, Susheel Jethanand , ROY, Saumya , THANGAVEL, Soodamani , SISTLA, Ramesh Kumar , CHERUKU, Srinivas , THANGATHIRUPATHY, Srinivasan , KANYABOINA, Yadagiri , PULICHARLA, Nagalakshmi
IPC分类号： C07D309/14 , C07D317/66 , C07D401/12 , C07D405/12 , C07D239/42 , C07D261/14 , C07D487/04 , A61K31/17 , A61P35/00 , C07D335/02 , C07C229/00 , A61K31/136 , C07D409/12
CPC分类号： C07C275/40 , A61K31/17 , A61K31/196 , A61K31/277 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/428 , A61K31/437 , A61K31/445 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K39/3955 , A61K39/39558 , A61K45/06 , C07C229/42 , C07C233/81 , C07C235/38 , C07C235/56 , C07C255/57 , C07C255/58 , C07C275/30 , C07C275/42 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/08 , C07D211/14 , C07D239/34 , C07D239/47 , C07D265/30 , C07D265/36 , C07D277/64 , C07D295/155 , C07D307/22 , C07D309/04 , C07D309/14 , C07D317/46 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
摘要翻译：公开了调节或抑制吲哚胺2,3-双加氧酶（IDO）的酶活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病例如癌症，病毒感染和/或炎症性疾病的方法，其利用发明。

6. 发明申请

WO2015048728A1 METHODS FOR POST-FABRICATION FUNCTIONALIZATION OF POLY(ESTER UREAS) 审中-公开
标题翻译：聚酯（ESTER UREAS）后制备功能化方法
公开(公告)号：WO2015048728A1
公开(公告)日：2015-04-02
申请号：PCT/US2014/058264
申请日：2014-09-30
申请人： BECKER, Matthew , LIN, Fei , THE UNIVERSITY OF AKRON
发明人： BECKER, Matthew , LIN, Fei
IPC分类号： C07C229/00 , C08G63/91 , C08G75/02 , C08G77/04
CPC分类号： C08G71/02 , C07C227/18 , C07C229/34 , C07C247/04 , C07C275/16 , C08G2230/00 , C09D175/02
摘要： Amino acid-based poly(ester urea)s (PEU) are emerging as a class of polymers that have shown promise in regenerative medicine applications. Embodiments of the invention relate to the synthesis of PEUs carrying pendent "clickable" groups on modified tyrosine amino acids. The pendent species include alkyne, azide, alkene, tyrosine-phenol, and ketone groups. PEUs with Mw exceeding 100k Da were obtained via interfacial polycondensation methods and the concentration of pendent groups was varied by copolymerization. The incorporation of derivatizable functionalities is demonstrated using 1H NMR and UV-Vis spectroscopy methods. Electrospinning was used to fabricate PEU nanofibers with a diameters ranging from 350 nm to 500 nm. The nanofiber matricies possess mechanical strengths suitable for tissue engineering (Young's modulus: 30045 MPa; tensile stress: 8.51.2 MPa). A series of bioactive peptides and fluorescent molecules were conjugated to the surface of the nanofibers following electrospinning using bio-orthogonal reactions in aqueous media.
摘要翻译：氨基酸类聚（酯尿素）（PEU）正在出现，这些聚合物在再生医学应用中已显示出希望。本发明的实施方案涉及在修饰的酪氨酸氨基酸上携带侧面的“可点击”基团的PEU的合成。悬挂物种包括炔烃，叠氮化物，烯烃，酪氨酸 - 苯酚和酮基团。通过界面缩聚方法得到Mw超过100kDa的PEU，通过共聚改变侧基的浓度。使用1 H NMR和UV-Vis光谱法证明可衍生化官能度的结合。使用静电纺丝制造直径范围为350nm至500nm的PEU纳米纤维。纳米纤维母材具有适用于组织工程的机械强度（杨氏模量：30045MPa;拉伸应力：8.51.2MPa）。在水性介质中使用生物正交反应进行静电纺丝后，将一系列生物活性肽和荧光分子缀合到纳米纤维的表面。

7. 发明申请

WO2014201111A1 TREATMENT OF MTOR HYPERACTIVE RELATED DISEASES AND DISORDERS 审中-公开
标题翻译： MTV治疗相关疾病和疾病的治疗
公开(公告)号：WO2014201111A1
公开(公告)日：2014-12-18
申请号：PCT/US2014/041902
申请日：2014-06-11
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
发明人： HENSKE, Elizabeth P. , MEDVETZ, Douglas A.
IPC分类号： C07C229/00
CPC分类号： A61K31/7034 , A61K31/133 , A61K31/135 , A61K31/167 , A61K31/192 , A61K31/198 , A61K31/357 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4178 , A61K31/433 , A61K31/465 , A61K31/472 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K45/06 , A61N5/10 , G01N33/573 , G01N2333/912 , G01N2800/52 , G01N2800/7028
摘要： Embodiments disclosed herein provide compositions and methods for treating cancer having deregulated mTOR signaling or mTOR hyperactivity, e.g., lymphangioleiomyomatosis (LAM), LAM/TSC or treating and/or management of tuberous sclerosis complex (TSC). Such methods and compositions comprise at least one compound selected from the group consisting of nateglinide, Z-L-Phe chloromethyl ketone, clemastine fumarate, supercinnamaldehyde, practolol, fluvastatin Na, sulindac, BIO, amorolfine, spectinomucin, sibutramine HCl, nelfinavir mesylate, moroxydine HCl, nicotine ditartrate, trequinsin, meglumine, tizanidine HCl, CGP-74514A hydrochloride, tioconazole, TOVOK™ (afatinib), or kasugamycin.
摘要翻译：本文公开的实施方案提供用于治疗具有失调的mTOR信号传导或mTOR多动症例如淋巴管平滑肌瘤病（LAM），LAM / TSC或治疗和/或治疗结节性硬化综合征（TSC）的癌症的组合物和方法。这些方法和组合物包含至少一种选自那格列奈，ZL-Phe氯甲基酮，富马酸氯马斯汀，超级肉桂醛，促氟洛伐他汀，氟伐他汀钠，舒林酸，BIO，高碘蛋白，壮观蛋白，西布曲明HCl，奈非那韦甲磺酸盐，烟碱酒石酸盐，特灵素，葡甲胺，盐酸替扎尼定，盐酸CGP-74514A，替康唑，TOVOK™（阿伐他汀）或春日霉素。

8. 发明申请

WO2013130968A1 ROS-ACTIVATED COMPOUNDS AS SELECTIVE ANTI-CANCER THERAPEUTICS 审中-公开
标题翻译： ROS活化化合物作为选择性抗癌治疗剂
公开(公告)号：WO2013130968A1
公开(公告)日：2013-09-06
申请号：PCT/US2013/028614
申请日：2013-03-01
申请人： UNIVERSITY OF CINCINNATI , CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER
发明人： MERINO, Edward, J. , MULLOY, James, C. , LI, Guorui , BELL-HORWATH, Tiffany
IPC分类号： C07C229/00 , A01N43/40 , C07C273/00
CPC分类号： C07C217/20 , A61K31/138 , A61K31/145 , A61K31/167 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/451 , A61K45/06 , C07C217/84 , C07C229/42 , C07C233/25 , C07C237/04 , C07C237/08 , C07C321/28 , C07C323/25 , C07D295/096 , A61K2300/00
摘要： Provided are compounds according to the following Formula (I). The Formula (I) compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.
摘要翻译：提供根据下式（I）的化合物。式（I）化合物在活性氧（ROS）的存在下被活化，因此是与升高的ROS相关的癌症的选择性抗癌治疗剂。还提供了用于治疗与增加的ROS相关的癌症的方法和药物组合物。

9. 发明申请

WO2012109256A3 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A3
公开(公告)日：2013-01-24
申请号：PCT/US2012024160
申请日：2012-02-07
申请人： MANNKIND CORP , FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
发明人： FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
IPC分类号： C07D241/08 , B01J31/02 , C07C229/00
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
摘要翻译：所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-（氨基烷基）-2,5-二酮哌嗪的改进方法。公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法，包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。催化剂选自硫酸，磷酸，对甲苯磺酸，1-丙基膦酸环状酸酐，磷酸三丁酯，苯基膦酸和五氧化二磷等。溶剂选自二甲基乙酰胺，N-甲基-2-吡咯烷酮，二甘醇二甲醚，甘醇二甲醚，丙二醇，乙基二甘醇二甲醚，间甲酚，对甲酚，邻甲酚，二甲苯，乙二醇和苯酚等。

10. 发明申请

WO2012109256A2 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A2
公开(公告)日：2012-08-16
申请号：PCT/US2012/024160
申请日：2012-02-07
申请人： MANNKIND, CORP , FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
发明人： FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
IPC分类号： C07D241/08 , C07C229/00 , B01J31/02
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
摘要翻译：所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-（氨基烷基）-2,5-二酮哌嗪的改进方法。公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法，包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。催化剂选自硫酸，磷酸，对甲苯磺酸，1-丙基膦酸环状酸酐，磷酸三丁酯，苯基膦酸和五氧化二磷等。溶剂选自二甲基乙酰胺，N-甲基-2-吡咯烷酮，二甘醇二甲醚，甘醇二甲醚，丙二醇，乙基二甘醇二甲醚，间甲酚，对甲酚，邻甲酚，二甲苯，乙二醇和苯酚等。

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