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1. 发明申请

US20020161035A1 Medicaments for chemotherapeutic treatment of disease 失效
标题翻译：化疗药物治疗疾病
公开(公告)号：US20020161035A1
公开(公告)日：2002-10-31
申请号：US09900355
申请日：2001-07-06
申请人： Photogen, Inc.
发明人： H. Craig Dees , Timothy C. Scott
IPC分类号： A61K039/395 , A61K031/352
CPC分类号： A61K41/0057 , A61B2017/22062 , A61B2017/22087 , A61F7/00 , A61K9/0014 , A61K9/0019 , A61K31/352 , A61K41/0071 , A61K47/10 , A61K47/12 , A61K47/20 , A61N5/0601 , A61N5/062 , C07D311/82 , Y02A50/473 , Y10T436/193333
摘要： New chemotherapeutic medicaments and certain medical uses and methods for use of such chemotherapeutic medicaments for treatment of disease in human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. Preferably, the halogenated xanthene is Rose Bengal or a functional derivative of Rose Bengal. The halogenated xanthenes constitute a family of useful chemotherapeutic agents that afford selective, persistent accumulation in certain tissues. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs, the mouth and digestive tract and related organs, the urinary and reproductive tracts and related organs, the respiratory tract and related organs, the circulatory system and related organs, the head and neck, the endocrine and lymphoreticular systems and related organs, various other tissues, such as connective tissues and various tissue surfaces exposed during surgery, as well as various tissues exhibiting microbial or parasitic infection. In another preferred embodiment, such medicaments are produced in various formulations useful for intracorporeal or topical administration, including in liquid, semisolid, solid or aerosol delivery vehicles.
摘要翻译：描述了新的化学治疗药物和用于治疗人或动物组织中的这种化学治疗药物的某些医疗用途和方法，其中这种药物的主要活性成分是卤化呫吨或卤代呫吨衍生物。优选地，卤代呫吨是玫瑰红或玫瑰红的功能衍生物。卤代呫吨构成一系列有用的化学治疗剂，其在某些组织中提供选择性的，持续的积累。在优选的实施方案中，这些药物用于治疗影响皮肤和相关器官，口腔和消化道及相关器官，泌尿生殖道和相关器官，呼吸道及相关器官，循环系统内脏和淋巴系统及相关器官，各种其他组织，如结缔组织和手术期间暴露的各种组织表面，以及表现出微生物或寄生虫感染的各种组织。在另一个优选的实施方案中，这些药物可用于体内或局部给药的各种制剂，包括在液体，半固体，固体或气溶胶输送载体中。

2. 发明申请

US20020111377A1 Transdermal delivery of cannabinoids 审中-公开
标题翻译：经皮给予大麻素
公开(公告)号：US20020111377A1
公开(公告)日：2002-08-15
申请号：US10032163
申请日：2001-12-21
申请人： Albany College of Pharmacy
发明人： Audra L. Stinchcomb
IPC分类号： A61K031/352
CPC分类号： A61K31/352 , A61K9/7084 , A61K31/353 , A61K31/473 , A61K31/485 , A61K2300/00
摘要： Disclosed is a method for relieving symptoms associated with illness or discomfort associated with the treatment of illness in a subject. The method includes providing a cannabinoid composition and delivering the cannabinoid transdermally to the subject. The cannabinoid composition used in this method includes at least one cannabinoid selected from the group consisting of null9-THC, cannabinol, cannabidiol, nabilone, levonantradol, (null)-HU-210, (null)-HU-210, 11-hydroxy-null9-THC, null8-THC-11-oic acid, CP 55,940, and R(null)-WIN 55,212-2. Also disclosed is an occlusive body which includes an impermeable backing and a rate-controlling microporous membrane which together define a cavity in which a cannabinoid is disposed. Methods for increasing the concentration of cannabinoids or cannabinoid metabolites in a subject and for assessing the permeability of skin to cannabinoids are also described.
摘要翻译：公开了一种用于缓解与受试者的疾病治疗相关的疾病或不适症状的症状的方法。该方法包括提供大麻素组合物并将大麻素经皮递送至受试者。在该方法中使用的大麻素组合物包括至少一种选自以下的大麻素：DELTA9-THC，大麻酚，大麻二醇，奈匹酮，左旋他丹（ - ） - HU-210，（+） - HU-210,11-羟基 - DELTA9-THC，DELTA8-THC-11-酸，CP 55,940和R（+） - WIN 55,212-2。还公开了一种封闭体，其包括不可渗透背衬和速率控制微多孔膜，它们共同限定其中设置大麻素的空腔。还描述了增加受试者中大麻素或大麻素代谢物浓度以及评估皮肤对大麻素的通透性的方法。

3. 发明申请

US20020091100A1 Cromolyn for eye and ear infections 失效
标题翻译： Cromolyn用于眼睛和耳朵感染
公开(公告)号：US20020091100A1
公开(公告)日：2002-07-11
申请号：US09756618
申请日：2001-01-05
发明人： John Lezdey , K. Anne Kronis , Darren Lezdey
IPC分类号： A61K031/352 , A61K031/56 , A61K031/728
CPC分类号： A61K31/728 , A61K9/0048 , A61K31/352 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： The present invention provides a method and composition for treating eye and ear inflammation and eye and ear infections. The compositions contain a cromolyn compound alone or in combination with a corticosteroid. A steroidal antiphlogistic compound, a non-steroidal antiphlogistic compound and optionally hyaluronic acid may be added.
摘要翻译：本发明提供了用于治疗眼睛和耳朵炎症以及眼睛和耳朵感染的方法和组合物。组合物单独或与皮质类固醇组合含有色甘酸化合物。可以加入类固醇消炎化合物，非类固醇消炎药和任选的透明质酸。

4. 发明申请

US20020049245A1 Tumor necrosis factor alpha (TNF-alpha) inhibiting pharmaceuticals 失效
标题翻译：肿瘤坏死因子α（TNF-α）抑制药物
公开(公告)号：US20020049245A1
公开(公告)日：2002-04-25
申请号：US09971821
申请日：2001-10-04
申请人： YISSUM RESEARCH DEVELOPMENT CO.
发明人： Esther Shohami , Ruth Gallily , Raphael Mechoulam
IPC分类号： A61K031/41 , A61K031/352
CPC分类号： A61K31/352 , Y02A50/411
摘要： Pharmaceutical compositions are described for preventing TNF toxicity, comprising as active ingredient the stereospecific (null) enantiomer, having (3S,4S) configuration of null6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to elevated levels of TNF, including septic shock, cachexia and trauma. They are also effective in the treatment of certain chronic degenerative diseases characterized by TNF production, including autoimmune diseases such as AIDS.
摘要翻译：描述了用于预防TNF毒性的药物组合物，其包含具有（3S，4S）构型的DELTA6四氢大麻酚型化合物的立体特异性（+）对映异构体作为活性成分。组合物特别有效地减轻甚至预防由于升高的TNF水平引起的神经毒性，包括败血性休克，恶病质和创伤。它们也有效治疗某些以TNF产生为特征的慢性退行性疾病，包括自身免疫疾病如艾滋病。

5. 发明申请

US20010018530A1 Use of substituted amino-methyl-chromans for the prevention of neuronal degeneration and for the promotion of neuronal regeneration 失效
标题翻译：使用取代的氨基 - 甲基 - 苯并二氢吡喃酮来预防神经元变性和促进神经元再生
公开(公告)号：US20010018530A1
公开(公告)日：2001-08-30
申请号：US09803621
申请日：2001-03-09
发明人： Thomas Fahrig , Irene Gerlach , Ervin Horvath , Reinhard Jork
IPC分类号： C07D311/04 , C07D311/78 , A61K031/352
CPC分类号： A61K31/353
摘要： The invention relates to the use of substituted aminomethyl-chromans for the treatment of neuronal degeneration and for the promotion of neuronal regeneration in cerebral injuries and chronic disorders of the nervous system.
摘要翻译：本发明涉及取代的氨基甲基 - 苯并二氢吡喃酮用于治疗神经元变性和促进脑损伤和神经系统慢性疾病的神经元再生。

6. 发明申请

US20020040053A1 Antioxidant containing vitamin E metabolite 有权
标题翻译：含维生素E代谢物的抗氧化剂
公开(公告)号：US20020040053A1
公开(公告)日：2002-04-04
申请号：US09963365
申请日：2001-09-27
发明人： Kazuo Kondo , Osamu Igarashi , Chikako Kiyose , Hiroyuki Yoshimura , Shigehiro Yoshitake
IPC分类号： A61K031/355 , A61K031/352
CPC分类号： A61K31/355 , A61K31/353 , Y10S514/824
摘要： The present invention provides a method of preventing or treating a disease caused by oxidation in vivo by administering a pharmacologically effective amount of at least one compound selected from the group consisting of: (1) 2,5,7.8-tetramethyl-2-(null-carboxyethyl)-6-hydroxychromane; and (2) 2,7.8-trimethyl-2-(null-carboxyethyl)-6-hydroxychromane. Further, it provides use of a compound selected from the group consisting of (3) a-tocopherol, (4) a-tocotrienol, (5) null-tocopherol and (6) null-tocotrienol for generation in vivo of any of the above compounds (1) and (2) to treat a disease caused by oxidated low density lipoprotein (LDL). As the above-mentioned disease, arteriosclerosis is particularly preferred.
摘要翻译：本发明提供一种通过施用药理学有效量的至少一种选自下组的化合物来预防或治疗由体内氧化引起的疾病的方法：（1）2,5,7,8-四甲基-2-（β - 羧基乙基）-6-羟基苯并二氢吡喃; 和（2）2,7,8-三甲基-2-（β-羧乙基）-6-羟基苯并二氢吡喃。此外，它提供了使用选自（3）α-生育酚，（4）α-生育三烯酚，（5）γ-生育酚和（6）γ-生育三烯酚的化合物，用于在上述任一种中产生化合物（1）和（2）治疗由氧化低密度脂蛋白（LDL）引起的疾病。作为上述疾病，特别优选动脉硬化。

7. 发明申请

US20020032205A1 Benzofuran derivatives, their preparation and use 失效
标题翻译：苯并呋喃衍生物，其制备和用途
公开(公告)号：US20020032205A1
公开(公告)日：2002-03-14
申请号：US09874392
申请日：2001-06-04
申请人： H. Lundbeck A/S
发明人： Kim Andersen , Mario Rottlander , Klaus Peter Bogeso , Henrik Pedersen , Thomas Ruhland , Robert Dancer
IPC分类号： A61K031/496 , C07D49/02 , A61K031/4525 , A61K031/352
CPC分类号： C07D307/87 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04
摘要： The present invention relates to benzofuran derivatives having general Formula (I) 1 wherein A is selected from (1), (2), (3), (4) 2 wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.
摘要翻译：本发明涉及通式（I）的苯并呋喃衍生物，其中A选自（1），（2），（3），（4）其中Z为O或S; s为0或1; q为0或1; R 4是氢，C 1-6 - 烷基，C 2-6烯基，C 2-6炔基，C 1-6 - 烷基 - 芳基或C 1-6 - 烷基-O-芳基; D是选自支链或直链C 1-6 - 亚烷基，C 2-6亚烯基和C 2-6亚炔基的间隔基; 其对映体及其药学上可接受的酸加成盐。这些化合物与5-HT1A受体有很强的结合。

8. 发明申请

US20020013370A1 Methods for identifying and treating resistant tumors 审中-公开
标题翻译：识别和治疗耐药性肿瘤的方法
公开(公告)号：US20020013370A1
公开(公告)日：2002-01-31
申请号：US09836567
申请日：2001-04-17
发明人： Jason Scott Sawyer , Stephen M. Spaethe , James Jacob Starling , Gabriele Jedlitschky , Inka Leier , Dietrich Keppler
IPC分类号： A61K031/41 , A61K031/352 , A61K031/192
CPC分类号： A61K31/00 , A61K31/192 , A61K31/353 , A61K31/47
摘要： This invention provides a method of identifying and reversing multidrug resistance in a multidrug resistant tumor comprising administering a multidrug resistance reversing amount of any of the compounds as defined herein.
摘要翻译：本发明提供了鉴定和逆转多药耐药性肿瘤中的多药耐药性的方法，其包括施用多药耐药反转量的本文定义的任何化合物。

9. 发明申请

US20020010195A1 Mitochondria protecting agents for treating mitochondria associated diseases 失效
公开(公告)号：US20020010195A1
公开(公告)日：2002-01-24
申请号：US09733271
申请日：2000-12-07
发明人： Soumitra S. Ghosh , Scott W. Miller , Robert E. Davis , Walter H. Moos
IPC分类号： A61K031/47 , A61K031/352 , A61K031/216
CPC分类号： A61K31/155 , A61K31/00 , A61K31/05 , A61K31/06 , A61K31/136 , C07C39/08 , C07C39/11 , C07C39/19 , C07C69/017 , C07C215/78 , C07C215/80 , C07C217/84 , C07C279/18 , C07D215/20 , C07D311/72
摘要： The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.

10. 发明申请

US20010027210A1 Combination therapy for cancer 失效
标题翻译：癌症联合治疗
公开(公告)号：US20010027210A1
公开(公告)日：2001-10-04
申请号：US09774002
申请日：2001-01-31
发明人： William R. Wilson
IPC分类号： A61K031/337 , A61K031/352
CPC分类号： A61K45/06 , A61K31/337 , A61K31/352 , A61K2300/00
摘要： This invention relates to a method of treating cancer, and particularly a method including the steps of administering to a mammal in need of such treatment, either simultaneously or sequentially, (i) a compound selected from a paclitaxel and docetaxel, and (ii) a compound of the formula 1 or a pharmaceutically acceptable salt or ester thereof; wherein R1, R2 and R3 are each independently selected from the group consisting of H, C1nullC6 alkyl, halogen, CF3, CN, NO2, NH2, OH, OR, NHCOR, NHSO2R, SR, SO2R or NHR, wherein each R is independently C1nullC6 alkyl optionally substituted with one or more substituents selected from hydroxy, amino and methoxy, and wherein each of R1, R2 and R3 may be present at any of the available positions 1 to 8; and wherein in each of the carbocyclic aromatic rings in formula (I), up to two of the methine (nullCHnull) groups may be replaced by an aza (nullNnull) group; and wherein any two of R1, R2 and R3 may additionally together represent the group nullCH nullCHnullCH nullCHnull, such that this group, together with the carbon or nitrogen atoms to which it is attached, forms a fused 6 membered aromatic ring.
摘要翻译：本发明涉及治疗癌症的方法，特别涉及一种方法，包括以下步骤：同时或依次给予需要这种治疗的哺乳动物，（i）选自紫杉醇和多西紫杉醇的化合物，和（ii）式的化合物或其药学上可接受的盐或酯; 其中R 1，R 2和R 3各自独立地选自H，C 1 -C 6烷基，卤素，CF 3，CN，NO 2，NH 2，OH，OR，NHCOR，NHSO 2 R，SR，SO 2 R或NHR，其中每个R 任选被一个或多个选自羟基，氨基和甲氧基的取代基取代的C 1 -C 6烷基，并且其中R 1，R 2和R 3中的每一个可以存在于任何可用位置1至8; 并且其中在式（I）中的每个碳环芳环中，至多两个次甲基（-CH =）基团可以被氮杂（-N =）基团取代; 并且其中R 1，R 2和R 3中的任何两个可以另外地一起表示基团-CH = CH.CH = CH-，使得该基团与连接的碳原子或氮原子一起形成稠合的6元芳族环。

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