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1. 发明授权

US09993563B2 Compounds and methods for trans-membrane delivery of molecules 有权
公开(公告)号：US09993563B2
公开(公告)日：2018-06-12
申请号：US15222559
申请日：2016-07-28
申请人： Aposense LTD.
发明人： Ilan Ziv
IPC分类号： A61K47/48 , A61K48/00 , A61K31/713 , A61K47/28 , C12N15/113 , A61K38/00 , C07J41/00 , C07J43/00 , A61K38/46
CPC分类号： A61K47/554 , A61K31/713 , A61K38/465 , A61K47/54 , B82Y5/00 , C07J1/0077 , C07J41/00 , C07J41/0011 , C07J41/005 , C07J41/0072 , C07J43/00 , C07J43/003 , C12N15/113 , C12N2310/14 , C12N2310/3145 , C12N2310/3231 , C12N2310/351
摘要： A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA. The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.

2. 发明申请

US20140011793A1 NEW STEROIDS HAVING INCREASED WATER SOLUBILITY AND RESISTANCE AGAINST METABOLISM, AND METHODS FOR THEIR PRODUCTION 审中-公开
标题翻译：具有提高水分溶解性和抗性的新型甾体化合物及其生产方法
公开(公告)号：US20140011793A1
公开(公告)日：2014-01-09
申请号：US13788074
申请日：2013-03-07
申请人： Umecrine AB
发明人： Torbjörn Bäckström , Gianna Ragagnin
IPC分类号： C07J41/00 , C07J7/00
CPC分类号： C07J7/009 , C07J1/00 , C07J1/0011 , C07J5/0015 , C07J7/00 , C07J7/002 , C07J7/0065 , C07J7/007 , C07J41/00 , C07J41/0016 , C07J41/005
摘要： Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.
摘要翻译：公开了具有增加的耐代谢性和增加的水溶性的类固醇化合物及其生产方法。这些物质适用于制备用于治疗类固醇相关或类固醇诱导的中枢神经系统疾病的药物，并且用于预防，减轻或治疗这些疾病的方法。

3. 发明申请

US20110098260A1 Steroid Compounds and Formulations 失效
标题翻译：类固醇化合物和制剂
公开(公告)号：US20110098260A1
公开(公告)日：2011-04-28
申请号：US12957661
申请日：2010-12-01
申请人： James M. Frincke
发明人： James M. Frincke
IPC分类号： A61K31/57 , C07J5/00 , C07J31/00 , C07J1/00 , C07J9/00 , A61K31/575 , A61K31/568 , A61P35/00 , A61P5/24
CPC分类号： A61K31/568 , A61K31/565 , A61K31/567 , A61K31/5685 , A61K45/06 , C07J1/00 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0048 , C07J31/00 , C07J41/00
摘要： The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
摘要翻译：本发明提供了治疗诸如前列腺癌或改善与前列腺癌相关的一种或多种症状的病症或调节雄激素受体生物学活性的药物的方法。本发明还提供适用于治疗应用的方法和组合物。

4. 发明授权

US07863261B2 Breast and prostate cancer treatment method 失效
标题翻译：乳腺癌和前列腺癌治疗方法
公开(公告)号：US07863261B2
公开(公告)日：2011-01-04
申请号：US11835397
申请日：2007-08-07
申请人： James M. Frincke
发明人： James M. Frincke
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： A61K31/568 , A61K31/565 , A61K31/567 , A61K31/5685 , A61K45/06 , C07J1/00 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0048 , C07J31/00 , C07J41/00
摘要： The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
摘要翻译：本发明提供了治疗诸如前列腺癌或改善与前列腺癌相关的一种或多种症状的病症或调节雄激素受体生物学活性的药物的方法。本发明还提供适用于治疗应用的方法和组合物。

5. 发明申请

US20100113408A1 21-SUBSTITUTED PROGESTERONE DERIVATIVES AS NEW ANTIPROGESTATIONAL AGENTS 有权
标题翻译： 21替代的孕酮衍生物作为新的抗菌药物
公开(公告)号：US20100113408A1
公开(公告)日：2010-05-06
申请号：US12641172
申请日：2009-12-17
申请人： Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta
发明人： Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta
IPC分类号： A61K31/56 , A61P15/00
CPC分类号： C07J5/00 , C07J5/0053 , C07J7/00 , C07J7/0085 , C07J9/00 , C07J21/006 , C07J41/00 , C07J41/0016 , C07J41/0083 , C07J41/0094 , C07J51/00 , C07J71/001 , Y10S514/841
摘要： A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
摘要翻译：具有以下通式的化合物：其中：R 1是选自-OCH 3，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是选自氢和烷基的成员。除了提供式I化合物之外，本发明提供了其中式I化合物有利地用于拮抗内源性孕酮的方法; 诱发月经; 治疗子宫内膜异位症; 治疗痛经; 治疗内分泌激素依赖性肿瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导劳动; 和避孕。

6. 发明申请

US20100093687A1 Method Of Treating Disorder Related To High Cholesterol Concentration 审中-公开
标题翻译：治疗高胆固醇浓度相关疾病的方法
公开(公告)号：US20100093687A1
公开(公告)日：2010-04-15
申请号：US12637165
申请日：2009-12-14
申请人： Ching Song , Shutsung Liao , Qing Dai
发明人： Ching Song , Shutsung Liao , Qing Dai
IPC分类号： A61K31/575 , A61P7/00 , A61P25/00 , A61P9/10 , A61P25/28 , C07J9/00
CPC分类号： C07J41/0061 , A61K31/56 , A61K31/575 , C07J9/00 , C07J41/00
摘要： A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and compositions for treating a disorder in a subject where an activator of liver X alpha is indicated, such as in, for example, treating a high cholesterol disease.
摘要翻译：一种治疗与高胆固醇浓度相关的病症的方法，包括向有需要的受试者施用式（I）化合物：还公开了用于治疗受试者中的病症的方法，试剂盒，组合和组合物，其中活化剂指示肝Xα，例如在例如治疗高胆固醇疾病中。

7. 发明申请

US20100063308A1 LIPID NANOPARTICLE BASED COMPOSITIONS AND METHODS FOR THE DELIVERY OF BIOLOGICALLY ACTIVE MOLECULES 有权
标题翻译：基于脂质纳米颗粒的组合物和用于递送生物活性分子的方法
公开(公告)号：US20100063308A1
公开(公告)日：2010-03-11
申请号：US12617079
申请日：2009-11-12
申请人： Tongqian Chen , Chandra Vargeese , Kurt Vagle , Weimin Wang , Ye Zhang
发明人： Tongqian Chen , Chandra Vargeese , Kurt Vagle , Weimin Wang , Ye Zhang
IPC分类号： C07C229/00
CPC分类号： C07C217/28 , A61K9/0073 , A61K9/1271 , A61K9/1272 , A61K47/543 , A61K47/6911 , C07C217/42 , C07C217/58 , C07C239/20 , C07J41/00 , C12N15/88
摘要： The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).
摘要翻译：本发明涉及新型阳离子脂质，转染剂，微粒，纳米颗粒和短干扰核酸（siNA）分子。本发明还涉及用于研究，诊断和治疗对受试者或生物体中基因表达和/或活性的调节作用的性状，疾病和病状的组合物和方法。具体地说，本发明涉及有效转染或递送生物活性分子的新型阳离子脂质，微粒，纳米颗粒和转染剂，例如抗体（例如单克隆抗体，嵌合型，人源化等），胆固醇，激素，抗病毒剂，肽，蛋白质，化学治疗剂，小分子，维生素，辅因子，核苷，核苷酸，寡核苷酸，酶核酸，反义核酸，形成三链体的寡核苷酸，2,5-A嵌合体，dsRNA，同源酶，适体，诱饵及其类似物和小核酸酸分子，如短干扰核酸（siNA），短干扰RNA（siRNA），双链RNA（dsRNA），微RNA（miRNA）和短发夹RNA（shRNA）分子）相关细胞和/或组织，例如受试者或生物体。这样的新型阳离子脂质，微粒，纳米颗粒和转染剂可用于例如提供预防，抑制或治疗细胞，受试者或生物体中的疾病，病症或性状的组合物。本文所述的组合物通常被称为配制的分子组合物（FMC）或脂质纳米颗粒（LNP）。

8. 发明申请

US20100063018A1 BILE ACID DERIVATIVES AS FXR LIGANDS FOR THE PREVENTION OR TREATMENT OF FXR-MEDIATED DISEASES OR CONDITIONS 有权
标题翻译：双酸衍生物作为预防或治疗FXR介导的疾病或病症的FXR配偶
公开(公告)号：US20100063018A1
公开(公告)日：2010-03-11
申请号：US12435063
申请日：2009-05-04
申请人： Roberto Pellicciari , Stefano Fiorucci , Mark Pruzanski
发明人： Roberto Pellicciari , Stefano Fiorucci , Mark Pruzanski
IPC分类号： A61K31/575 , C07J9/00 , A61P1/16 , A61P1/00 , A61P9/00 , A61P9/10 , A61P3/00 , A61P3/04 , A61P3/10
CPC分类号： C07J41/00 , C07J9/00
摘要： The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.
摘要翻译：本发明涉及式（I）化合物，其中：R1是氢或烷基; R2是氢或卤素，硝基，烷氧基，氨基或羧基; Y是CH 2，氧或硫; n是1至4的整数，以及其药学上可接受的盐，溶剂合物或氨基酸缀合物，用于治疗FXR介导的疾病或病症。

9. 发明申请

US20100003711A1 Methods to identify therapeutic agents 审中-公开
标题翻译：确定治疗剂的方法
公开(公告)号：US20100003711A1
公开(公告)日：2010-01-07
申请号：US11990547
申请日：2006-08-14
申请人： Paul Wentworth
发明人： Paul Wentworth
IPC分类号： C12Q1/02
CPC分类号： G01N33/5055 , C07D313/04 , C07J9/00 , C07J41/00 , G01N33/5064 , G01N33/566 , G01N33/92
摘要： As illustrated herein, cholesterol is oxidized when it is present in atherosclerotic plaques. This reaction generates cholesterol oxidation or ozonation products that can act as chemotactic attractants of macrophages, can promote differentiation of monocytes into macrophages and can increase expression of E-selectin and Class A scavenger receptor (SR-A). The present application is directed to methods of using such cholesterol ozonoation products to identify agents that can be used to treat atherosclerosis and other inflammatory artery diseases.
摘要翻译：如本文所示，当胆固醇存在于动脉粥样硬化斑块中时，胆固醇被氧化。该反应产生胆固醇氧化或臭氧化产物，其可以作为巨噬细胞的趋化性引诱剂，可促进单核细胞向巨噬细胞分化，并可增加E-选择蛋白和A类清道夫受体（SR-A）的表达。本申请涉及使用这种胆固醇异种产物来鉴定可用于治疗动脉粥样硬化和其它炎性动脉疾病的药剂的方法。

10. 发明授权

US07641915B2 Lipid nanoparticle based compositions and methods for the delivery of biologically active molecules 失效
标题翻译：基于脂质纳米颗粒的组合物和递送生物活性分子的方法
公开(公告)号：US07641915B2
公开(公告)日：2010-01-05
申请号：US12048023
申请日：2008-03-13
申请人： TongQian Chen , Chandra Vargeese , Kurt Vagle , WeiMin Wang , Ye Zhang
发明人： TongQian Chen , Chandra Vargeese , Kurt Vagle , WeiMin Wang , Ye Zhang
IPC分类号： A61K9/127 , A61K31/56
CPC分类号： C07C217/28 , A61K9/0073 , A61K9/1271 , A61K9/1272 , A61K47/543 , A61K47/6911 , C07C217/42 , C07C217/58 , C07C239/20 , C07J41/00 , C12N15/88
摘要： The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).
摘要翻译：本发明涉及新型阳离子脂质，转染剂，微粒，纳米颗粒和短干扰核酸（siNA）分子。本发明还涉及用于研究，诊断和治疗对受试者或生物体中基因表达和/或活性的调节作用的性状，疾病和病状的组合物和方法。具体地说，本发明涉及有效转染或递送生物活性分子的新型阳离子脂质，微粒，纳米颗粒和转染剂，例如抗体（例如单克隆抗体，嵌合型，人源化等），胆固醇，激素，抗病毒剂，肽，蛋白质，化学治疗剂，小分子，维生素，辅因子，核苷，核苷酸，寡核苷酸，酶核酸，反义核酸，形成三链体的寡核苷酸，2,5-A嵌合体，dsRNA，同源酶，适体，诱饵及其类似物和小核酸酸分子，如短干扰核酸（siNA），短干扰RNA（siRNA），双链RNA（dsRNA），微RNA（miRNA）和短发夹RNA（shRNA）分子）相关细胞和/或组织，例如受试者或生物体。这样的新型阳离子脂质，微粒，纳米颗粒和转染剂可用于例如提供预防，抑制或治疗细胞，受试者或生物体中的疾病，病症或性状的组合物。本文所述的组合物通常被称为配制的分子组合物（FMC）或脂质纳米颗粒（LNP）。

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