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41. 发明授权

US5935975A Agonist-antagonist combination to reduce the use of nicotine and other drugs 失效
标题翻译：激动剂 - 拮抗剂组合，以减少使用尼古丁和其他药物
公开(公告)号：US5935975A
公开(公告)日：1999-08-10
申请号：US54144
申请日：1993-04-30
申请人： Jed R. Rose , Edward D. Levin
发明人： Jed R. Rose , Edward D. Levin
IPC分类号： A24B15/16 , A24B15/18 , A24F47/00 , A61K31/44 , A61K31/465 , A61K47/48 , A61K9/70
CPC分类号： B82Y5/00 , A24B15/16 , A24B15/165 , A24B15/18 , A24F47/008 , A61K47/48738 , Y10S514/81 , Y10S514/812 , Y10S514/813 , Y10S514/922 , Y10S514/947
摘要： A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or an agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or an agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or an agonist while there is a substantial amount of the drug or an agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or an agonist thereof. In another embodiment, the drug or an agonist is first administered and the antagonist is self-administered by a subject in a manner which mimics the use of the drug thereby counter-conditioning the drug user to the stimuli associated with the normal administration of the drug. The invention further provides a method of therapeutically treating psychophysiologic diseases and disorders involving neuronal dysregulation. The method additionally provides a pharmacologic composition for the treatment and reduction of drug dependence and which relies upon a combination of an agonist and an antagonist.
摘要翻译：提供了治疗和减少药物依赖性的方法，例如尼古丁依赖性。该方法包括向受试者施用一定量的药物，例如尼古丁或该药物的激动剂，其量通常将提供所需的药理作用，并且至少部分地使用者满足药物的需要。该方法还包括以足以至少部分阻断药物或激动剂的药理作用的量向受试者施用药物拮抗剂或激动剂，同时存在大量药物或体内存在的激动剂的用户。在本发明的一个实施方案中，药物和拮抗剂基本上同时施用，以便占据该药物用量的大部分受体，从而阻断或减弱药物或其激动剂的任何进一步摄入的作用。在另一个实施方案中，首先施用药物或激动剂，并且受试者以模拟药物使用的方式自身施用拮抗剂，从而使药物使用者与药物的正常给药相关的刺激反应。本发明还提供治疗性治疗涉及神经元失调的心理生理疾病和病症的方法。该方法另外提供用于治疗和降低药物依赖性并且依赖于激动剂和拮抗剂的组合的药物组合物。

42. 发明授权

US5744463A Treatment of side effects of progestins and progesterone analogues used for birth control 失效
标题翻译：治疗用于避孕的孕激素和孕酮类似物的副作用
公开(公告)号：US5744463A
公开(公告)日：1998-04-28
申请号：US656737
申请日：1996-06-03
申请人： Glenn O. Bair
发明人： Glenn O. Bair
IPC分类号： A61K31/57 , A61K31/56
CPC分类号： A61K31/569 , A61K31/57 , A61K31/575 , Y10S514/922
摘要： The present invention provides methods for treating the deleterious effects of progestins and progesterone analogues used for birth control. The invention also provides pharmaceutical compositions useful in those methods.
摘要翻译：本发明提供了治疗用于避孕的孕激素和孕酮类似物的有害作用的方法。本发明还提供了可用于那些方法的药物组合物。

43. 发明授权

US5574052A Agonist-antagonist combination to reduce the use of nicotine and other drugs 失效
标题翻译：激动剂 - 拮抗剂组合，以减少使用尼古丁和其他药物
公开(公告)号：US5574052A
公开(公告)日：1996-11-12
申请号：US235454
申请日：1994-04-29
申请人： Jed E. Rose , Edward D. Levin
发明人： Jed E. Rose , Edward D. Levin
IPC分类号： A24B15/16 , A24B15/18 , A24F47/00 , A61K31/44 , A61K31/465 , A61K47/48
CPC分类号： B82Y5/00 , A24B15/16 , A24B15/165 , A24B15/18 , A24F47/008 , A61K47/48738 , Y10S514/81 , Y10S514/812 , Y10S514/813 , Y10S514/922 , Y10S514/947
摘要： A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist. In another embodiment, the drug or its other agonist is first administered and the antagonist is self-administered by a subject in a manner which mimics the use of the drug thereby counter-conditioning the drug user to the stimuli associated with the normal administration of the drug. The invention further provides a method of therapeutically treating psychophysiologic diseases and disorders involving neuronal dysregulation. The method additionally provides a pharmacologic composition for the treatment and reduction of drug dependence.
摘要翻译：提供了治疗和减少药物依赖性的方法，例如尼古丁依赖性。该方法包括首先向受试者施用一定量的药物，例如尼古丁或另一种药物激动剂，其量通常将提供所需的药理作用并且至少部分地满足使用者对药物的需要。该方法还包括以足以至少部分阻断药物或其其它激动剂的药理作用的量将药物或其它激动剂的拮抗剂施用给受试者，同时存在大量的药物或其它激动剂用户的系统。在本发明的一个实施方案中，基本上同时施用药物和拮抗剂，以占据该药物的使用者的大部分受体，从而阻断或减弱药物或其它激动剂的任何进一步摄入的影响。在另一个实施方案中，首先施用药物或其它激动剂，并且拮抗剂以模仿药物使用的方式由受试者自身给药，从而使药物使用者对与正常给药相关的刺激进行反调节药物。本发明还提供治疗性治疗涉及神经元失调的心理生理疾病和病症的方法。该方法另外提供用于治疗和减少药物依赖性的药理学组合物。

44. 发明授权

US5496804A Method for treating taxol side-effects with G-CSF 失效
标题翻译：用G-CSF治疗紫杉醇副作用的方法
公开(公告)号：US5496804A
公开(公告)日：1996-03-05
申请号：US342797
申请日：1994-11-21
申请人： Eddie Reed , Elise Kohn , Gisele Sarosy
发明人： Eddie Reed , Elise Kohn , Gisele Sarosy
IPC分类号： A61K38/19 , A61K38/00
CPC分类号： A61K38/193 , Y10S514/922
摘要： A method of treating a host using taxol comprising administering granulocyte colony-stimulating factor to the host being treated with taxol. The present inventive method allows for increased levels of taxol to be administered to the host in the treatment of various conditions, particularly with respect to ovarian tumors.
摘要翻译：一种使用紫杉醇治疗宿主的方法，包括对用紫杉醇进行治疗的宿主施用粒细胞集落刺激因子。本发明的方法允许在治疗各种病症，特别是关于卵巢肿瘤时，向宿主施用提高的紫杉醇水平。

45. 发明授权

US5405837A Method for the treatment of neoplastic disease utilizing tiazofurin and ribavirin 失效
标题翻译：利用噻唑啉和利巴韦林治疗肿瘤性疾病的方法
公开(公告)号：US5405837A
公开(公告)日：1995-04-11
申请号：US65348
申请日：1993-05-18
申请人： George Weber
发明人： George Weber
IPC分类号： A61K31/70 , A61K20060101 , A61K31/00 , A61P35/00
CPC分类号： A61K31/70 , Y10S514/908 , Y10S514/922
摘要： The present invention relates to the treatment of neoplastic disease in warm blooded animals using the sequential administration of tiazofurin and ribavirin. Tiazofurin is administered first in a high dose in order to facilitate a sharp decrease in IMP DH activity. These gains are consolidated by the continual administration of tiazofurin until the hematological levels have stabilized and remission is achieved. Once the patient is in remission, ribavirin is administered in steadily tapering dosages until the minimum dosage that will retain the beneficial effect of the tiazofurin is achieved. The IMP DH activity, GTP concentration, and hematological data is continually monitored throughout the treatment and dosages adjusted.
摘要翻译：本发明涉及使用连续施用噻唑啉和利巴韦林治疗温血动物的肿瘤性疾病。为了促进IMP DH活性急剧下降，首先以高剂量施用噻唑呋喃。这些增益通过连续施用噻唑呋喃来巩固，直到血液水平稳定并达到缓解。一旦患者缓解，利巴韦林以稳定的锥度剂量施用，直到达到保留噻唑呋喃的有益效果的最小剂量。在整个治疗期间持续监测IMP DH活性，GTP浓度和血液学数据，并调整剂量。

46. 发明授权

US5298257A Method for the treatment of withdrawal symptoms associated with smoking cessation and preparations for use in said method 失效
标题翻译：用于治疗与戒烟相关的戒断症状的方法和用于所述方法的制剂
公开(公告)号：US5298257A
公开(公告)日：1994-03-29
申请号：US855457
申请日：1992-03-19
申请人： Yvonne B. Bannon , John Corish , Owen I. Corrigan , Edward J. Geoghegan , Joseph G. Masterson
发明人： Yvonne B. Bannon , John Corish , Owen I. Corrigan , Edward J. Geoghegan , Joseph G. Masterson
IPC分类号： A61K9/06 , A61K9/70 , A61K31/465 , A61K47/34 , A61K47/36 , A61K47/42 , A61P25/30 , A61K9/14 , A61K31/44
CPC分类号： A61K9/7069 , A61K31/465 , A61K47/34 , A61K47/36 , A61K47/42 , A61K9/7023 , A61K9/7084 , Y10S514/813 , Y10S514/922 , Y10S514/936 , Y10S514/944 , Y10S514/946 , Y10S514/964 , Y10S514/965 , Y10S514/974
摘要： A preparation for the once-daily, percutaneous administration of nicotine comprises nicotine uniformly distributed in a solid, semi-solid or mucilaginous medium which can be placed in intimate contact with the skin, the solid, semi-solid or mucilaginous medium is formed by adding a given amount of nicotine to a solution of a solidifying or gel-forming agent or mixture thereof in a suitable solvent or mixture of solvents and mixing or heating the mixture thereby obtained so as to form the solid, semi-solid or mucilaginous medium. The preparation can be used in a method of treating withdrawal symptoms associated with smoking cessation and for combating the psychological dependence that occurs through frequent smoking.
摘要翻译：每日一次的经皮给药尼古丁的制剂包括均匀分布在固体，半固体或粘液培养基中的尼古丁，其可以与皮肤紧密接触，固体，半固体或粘液培养基通过加入给予一定量的尼古丁至固化或凝胶形成剂或其混合物在合适的溶剂或溶剂混合物中的溶液，并混合或加热由此获得的混合物，以形成固体，半固体或粘液培养基。该制剂可用于治疗与戒烟相关的戒断症状并通过频繁吸烟来抵御心理依赖的方法。

47. 发明授权

US5264217A Method of increasing the total fat content of milk 失效
标题翻译：增加牛奶总脂肪含量的方法
公开(公告)号：US5264217A
公开(公告)日：1993-11-23
申请号：US959472
申请日：1992-10-09
申请人： David F. Horrobin
发明人： David F. Horrobin
IPC分类号： A61K31/20
CPC分类号： A61K31/20 , Y10S514/922
摘要： Methods for increasing the total fat and therefore energy content of mammalian and particularly human milk, the essential fatty acid content of that milk and the flow of that milk during lactation, or for preventing or reducing the normal decrease in milk fat content that occurs during prolonged lactation, by administering gamma linolenic acid, dihomo-gamma-linolenic acid or their mixture, alone or a physiologically acceptable diluent or carrier, in a form administrable to the lactating female.
摘要翻译：增加哺乳动物和特别是人乳的总脂肪，因此能量含量的方法，该乳的必需脂肪酸含量和哺乳期间该奶的流动，或用于预防或减少在长时间内发生的乳脂含量的正常降低通过以可施用于哺乳期雌性的形式单独或单独或生理上可接受的稀释剂或载体施用γ-亚麻酸，二亚非 - γ-亚麻酸或其混合物。

48. 发明授权

US5240700A Pharmaceutical composition comprising a medicament and 3-oxygermylpropionic acid 失效
标题翻译：药物组合物，其包含药物和3-氧基甲基丙酸
公开(公告)号：US5240700A
公开(公告)日：1993-08-31
申请号：US881318
申请日：1992-05-07
申请人： Kiichi Sawai , Masayasu Kurono , Kazumasa Nakano , Kyoichi Asano , Takahiko Mitani , Naohisa Ninomiya , Bunkichi Kato
发明人： Kiichi Sawai , Masayasu Kurono , Kazumasa Nakano , Kyoichi Asano , Takahiko Mitani , Naohisa Ninomiya , Bunkichi Kato
IPC分类号： A61K31/28 , A61K31/80 , A61K33/24
CPC分类号： A61K31/80 , A61K31/28 , A61K33/24 , Y10S424/15 , Y10S514/922
摘要： A composition for inhibiting the degeneration of cells including liver cells by drugs and relieving the toxicity of drugs to internal organs including the liver contains as an essential component a 3-oxygermylpropionic acid polymer which is represented by:[(O.sub.1/2).sub.3 GeCH.sub.2 CH.sub.2 COOH].sub.nwherein n is an integer of at least 1, takes the form of a white acicular crystal and has a melting point of about 230.degree. C. at which it decomposes or coagulates. The present composition may be used with a carrier hydroxypropylcellulose in an amount of 0.005 to 50% by weight relative to 0.005 to 5% by weight of the 3-oxygermylpropionic acid polymer.
摘要翻译：用于通过药物抑制包括肝细胞在内的细胞变性的组合物，并且缓解药物对包括肝脏在内的器官的毒性的组合物含有：[（O1 / 2）3GeCH2CH2COOH] n的3-氧基甲基丙酸聚合物作为必要组分其中n为至少为1的整数，呈白色针状晶体的形式，其熔点约为230℃，其分解或凝结。本发明组合物可与载体羟丙基纤维素一起使用，其含量相对于3-氧基甲基丙酸聚合物的0.005-5重量％为0.005至50重量％。

49. 发明授权

US5236899A 6-position cyclosporin a analogs as modifiers of cytotoxic drug resistance 失效
标题翻译： 6位环孢菌素类似物作为细胞毒性药物抗性的修饰剂
公开(公告)号：US5236899A
公开(公告)日：1993-08-17
申请号：US752169
申请日：1991-08-23
申请人： Philippe L. Durette
发明人： Philippe L. Durette
IPC分类号： A61K38/00 , C07K7/64
CPC分类号： C07K7/645 , A61K38/00 , Y10S514/885 , Y10S514/908 , Y10S514/922 , Y10S514/97
摘要： Cyclosporin analogs containing a MeAla or MeAbu residue at the 6-position of the cyclic undecapeptide have been discovered to sensitize multidrug resistant cells to certain chemotherapeutic agents. These cyclosporin analogs have also been shown to increase the sensitivity of cells already susceptible to the chemotherapeutic agents. In addition, these cyclosporin A analogs lack the nephrotoxic and immunosuppressive activity of cyclosporin A.
摘要翻译：已经发现在环十一肽的6位含有MeAla或MeAbu残基的环孢菌素类似物使多药耐药细胞对某些化学治疗剂敏感。这些环孢菌素类似物也已显示增加已经对化学治疗剂敏感的细胞的敏感性。此外，这些环孢菌素A类似物缺乏环孢菌素A的肾毒性和免疫抑制活性。

50. 发明授权

US5219553A Composition of a n-carboxymethylated tetraazacyclododecane chelating agent, a paramagnetic metal and excess calcium ions for MRI 失效
标题翻译： N-羧甲基化四氮杂环十二烷螯合剂，顺磁金属和过量钙离子的组成
公开(公告)号：US5219553A
公开(公告)日：1993-06-15
申请号：US743212
申请日：1991-08-09
申请人： Karl F. Kraft , Steven C. Quay , Scott M. Rocklage , Dilip Worah
发明人： Karl F. Kraft , Steven C. Quay , Scott M. Rocklage , Dilip Worah
IPC分类号： A61K49/06 , C07D259/00 , C07F5/00 , C07F9/38 , C07F13/00 , G01R33/28
CPC分类号： G01R33/5601 , A61K49/06 , C07D259/00 , C07F13/005 , C07F5/003 , C07F9/3817 , Y10S424/90 , Y10S436/806 , Y10S514/836 , Y10S514/922 , Y10T436/24
摘要： Magnetic resonance imaging contrast media used to affect the relaxation times of atoms in body tissues undergoing NMR diagnosis are disclosed. Such media comprise (1) a paramagnetic, physiologically compatible complex of (a) a chelant consisting of a N-carboxy methylated tetraazacyclododecane, and (b) a paramagnetic ion of a lanthanide element of atomic numbers 59-70, or of a transition metal of atomic numbers 21-29, 42 or 44, or a physiologically compatible salt of such a complex, and (2) a toxicity-reducing amount of labile calcium ions. The labile calcium ions can be derived from a source other than a salt of said chelant, e.g. an inorganic or organic calcium salt. NMR image-enhancing compositions comprising NMR image-enhancing effective amounts of said contrast media and pharmaceutically acceptable diluents are also disclosed.
摘要翻译：公开了用于影响经历NMR诊断的身体组织中的原子的弛豫时间的磁共振成像造影剂。这种培养基包括（1）由（a）由N-羧基甲基化四氮杂环十二烷组成的螯合剂和（b）原子序数59-70的镧系元素的顺磁离子或过渡金属的原子序数21-29,42或44，或这种络合物的生理上相容的盐，和（2）不稳定的钙离子的毒性减少量。不稳定的钙离子可以衍生自除所述螯合剂的盐之外的来源，例如，无机或有机钙盐。还公开了包含NMR图像增强有效量的所述造影剂和药学上可接受的稀释剂的NMR图像增强组合物。

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