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1. 发明授权

US06821960B2 Glucagon antagonists/inverse agonists 失效
公开(公告)号：US06821960B2
公开(公告)日：2004-11-23
申请号：US09995987
申请日：2001-11-16
申请人： Anker Steen Jørgensen , Peter Madsen
发明人： Anker Steen Jørgensen , Peter Madsen
IPC分类号： A61K3166
CPC分类号： C07D209/48 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/42 , C07C311/47 , C07C317/42 , C07C323/44 , C07C2601/14 , C07C2601/16 , C07D257/04 , C07D271/06 , C07D319/08 , C07D319/20 , C07D333/36
摘要： A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

2. 发明授权

US06720313B1 Biocidal composition containing phosphite ions 有权
标题翻译：含有亚磷酸根离子的杀生物组合物
公开(公告)号：US06720313B1
公开(公告)日：2004-04-13
申请号：US09688693
申请日：2000-10-17
申请人： Nigel Paul Maynard
发明人： Nigel Paul Maynard
IPC分类号： A61K3166
CPC分类号： A01N59/26 , A01N43/42 , B27K3/32 , B27K3/50 , A01N59/20 , A01N59/16 , A01N47/18 , A01N43/84 , A01N43/78 , A01N43/653 , A01N43/52 , A01N33/12 , A01N25/02 , A01N2300/00
摘要： A biocidal composition useful for providing antifungal or antibacterial protection to a substrate such as wood, the composition comprises in its use form a use solution of pH of 4 or below containing at least one biocide and a source of free phosphite ions. A preferred source of phosphite ions is phosphorous acid. The composition allows deep penetration of a biocide such as copper oxine into where it can be fixed by pH change and confer a degree of protection beyond that hitherto obtained with such a biocide simply applied to the surface of the substrate.
摘要翻译：用于向底物例如木材提供抗真菌或抗菌保护的杀生物组合物，该组合物的使用形式包括含有至少一种杀生物剂和游离亚磷酸盐离子源的pH为4或更低的pH值的溶液。亚磷酸盐离子是亚磷酸。组合物允许将杀生物剂如铜氧化物的深度渗透到可以通过pH变化固定的地方，并赋予一定程度的保护，超过迄今为止通过简单施加到基底表面的杀生物剂获得的保护。

3. 发明授权

US06680307B1 Use of ibandronate for promoting osseointegration of endoprostheses 有权
标题翻译：使用伊班膦酸钠促进内固定的骨整合
公开(公告)号：US06680307B1
公开(公告)日：2004-01-20
申请号：US09857035
申请日：2001-05-31
申请人： Frieder Bauss , Andreas A. Kurth
发明人： Frieder Bauss , Andreas A. Kurth
IPC分类号： A61K3166
CPC分类号： A61K31/663
摘要： The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.
摘要翻译：本发明涉及伊班膦酸（1-羟基-3-（N-甲基-N-戊基）氨基丙基-1,1-二膦酸）或其生理相容性盐或酯用于改善无水泥锚固内假体的骨整合。伊班膦酸盐或其盐在插入内置假体后立即施用短时间，令人惊奇的结果是在手术后5周或更短时间内获得植入物的二次稳定性。

4. 发明授权

US06677320B2 Parenteral bisphosphonate composition with improved local tolerance 有权
标题翻译：肠胃外二膦酸盐组合物具有改善的局部耐受性
公开(公告)号：US06677320B2
公开(公告)日：2004-01-13
申请号：US09758605
申请日：2001-01-11
申请人： Anke Diederich , Pierre Goldbach , Thomas Pfister
发明人： Anke Diederich , Pierre Goldbach , Thomas Pfister
IPC分类号： A61K3166
CPC分类号： A61K47/18 , A61K9/0019 , A61K31/66 , A61K31/663 , A61K47/183
摘要： The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.
摘要翻译：本发明涉及包含双膦酸或其药学上可接受的盐（二膦酸盐）作为活性成分和药学上可接受的螯合剂的肠胃外组合物，该组合物的制备方法及其用于治疗和预防涉及骨吸收的疾病，特别是骨质疏松症，佩吉特氏病，恶性高钙血症和代谢性骨病。当肠胃外给药时，组合物特别可用于改善活性成分的局部耐受性。

5. 发明授权

US06670341B1 Compositions and methods for double-targeting virus infections and targeting cancer cells 有权
标题翻译：用于双向靶向病毒感染和靶向癌细胞的组合物和方法
公开(公告)号：US06670341B1
公开(公告)日：2003-12-30
申请号：US09693658
申请日：2000-10-19
申请人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
发明人： Louis S. Kucera , Ronald A. Fleming , Khalid S. Ishaq , Gregory L. Kucera , Susan L. Morris-Natschke
IPC分类号： A61K3166
CPC分类号： C07H19/06 , A61K31/66 , A61K31/675 , C07F9/10 , C07H19/10 , C07H19/16 , Y02A50/463
摘要： The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
摘要翻译：本发明包括通过双重靶向病毒（即在病毒生命周期的多于一个阶段靶向病毒）并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。本发明的组合物包括包含与一种或多种抗病毒剂（例如核苷类似物，蛋白酶抑制剂等）共价结合到脂质主链的磷酸胆碱部分的化合物。本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。本发明的方法包括将治疗感染的本发明化合物，其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。另外，本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。本发明的组合物包括包含与抗癌剂（例如核苷类似物）共价缀合的烷基脂质或磷脂部分的化合物。本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。本发明的方法包括给予本发明的化合物，其药学上可接受的盐或本发明的药物组合物，其量可以有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。

6. 发明授权

US06596711B1 (Aminopropyl)methylphosphinic acids 失效
标题翻译：（氨基丙基）甲基次膦酸
公开(公告)号：US06596711B1
公开(公告)日：2003-07-22
申请号：US09786220
申请日：2001-03-01
申请人： Kosrat Amin , Thomas Elebring , Peter Guzzo , Thomas Olsson , Marianne Swanson , Sverker Von Unge
发明人： Kosrat Amin , Thomas Elebring , Peter Guzzo , Thomas Olsson , Marianne Swanson , Sverker Von Unge
IPC分类号： A61K3166
CPC分类号： C07C271/16 , C07C215/08 , C07F9/301
摘要： Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.
摘要翻译：（3-氨基-2-羟丙基）甲基次膦酸的外消旋物; ii）（S） - （3-氨基-2-羟丙基）甲基次膦酸; iii）（R） - （3-氨基-2-羟丙基）甲基次膦酸; iv）（3-氨基-2-羟丙基）二氟甲基次膦酸; 对于一种或多种GABA B受体具有亲和性，它们的药学上可接受的盐，溶剂合物和立体异构体，以及它们的制备方法，含有所述治疗活性化合物的药物组合物和所述活性化合物在治疗中的用途。

7. 发明授权

US06562804B2 Hair-growing agent 失效
标题翻译：发丝剂
公开(公告)号：US06562804B2
公开(公告)日：2003-05-13
申请号：US10073113
申请日：2002-02-12
申请人： Ayako Kamimura , Tomoya Takahashi , Takashi Mimura , Shinkichi Honda
发明人： Ayako Kamimura , Tomoya Takahashi , Takashi Mimura , Shinkichi Honda
IPC分类号： A61K3166
CPC分类号： A61Q7/00 , A61K8/55 , A61K8/553 , A61K8/556
摘要： The present invention provides a hair-growing agent comprising, as an active ingredient, a phosphatidic acid represented by formula (I): (wherein R1 represents alkyl, alkenyl, alkanoyl or alkenoyl; and when R1 represents alkyl or alkenyl, R2 represents alkyl, alkenyl, alkanoyl or alkenoyl, and when R1 represents alkanoyl or alkenoyl, R2 represents alkyl or alkenyl).
摘要翻译：本发明提供一种毛发生长剂，其包含作为活性成分的由式（I）表示的磷脂酸:(其中R 1表示烷基，烯基，烷酰基或烯酰基;当R 1表示烷基或烯基时，R 2表示烷基，烯基，烷酰基或烯酰基，当R 1表示烷酰基或烯酰基时，R 2表示烷基或链烯基）。

8. 发明授权

US06548488B2 Composition comprising camptothecin or a camptothecin derivative and an alkylating agent for the treatment of cancer 失效
标题翻译：组合物，其包含喜树碱或喜树碱衍生物和用于治疗癌症的烷化剂
公开(公告)号：US06548488B2
公开(公告)日：2003-04-15
申请号：US09799615
申请日：2001-03-07
申请人： Marie-Christine Bissery
发明人： Marie-Christine Bissery
IPC分类号： A61K3166
CPC分类号： A61K31/4745 , A61K31/47 , A61K31/655 , A61K31/66 , A61K31/675 , A61K31/195 , A61K31/415 , A61K2300/00
摘要： The present invention relates to therapeutic associations for the treatment of cancer, comprising an effective amount of a camptothecin, or a camptothecin derivative, with an effective amount of an alkylating agent, such as melphalan, dacarbazine, or cyclophosphamide, and methods of using such therapeutic associations.
摘要翻译：本发明涉及用于治疗癌症的治疗协会，其包含有效量的喜树碱或喜树碱衍生物与有效量的烷化剂如美法仑，达卡巴嗪或环磷酰胺，以及使用这种治疗剂协会

9. 发明授权

US06498152B1 Use of a farnesyl transferase inhibitor in the manufacture of a medicament for local administration to the vascular wall in the prevention of restenosis 失效
标题翻译：法呢基转移酶抑制剂在制备用于局部给予血管壁以预防再狭窄的药物中的用途
公开(公告)号：US06498152B1
公开(公告)日：2002-12-24
申请号：US09674584
申请日：2000-12-21
申请人： Cherry Lindsey Wainwright , Roger Martin Wadsworth , Nigel John Pyne , Susan Pyne , Lorraine Margaret Work
发明人： Cherry Lindsey Wainwright , Roger Martin Wadsworth , Nigel John Pyne , Susan Pyne , Lorraine Margaret Work
IPC分类号： A61K3166
CPC分类号： A61K31/662 , A61K9/0019 , A61K9/0024 , A61K31/00 , A61K31/045 , A61K31/365 , A61K31/70 , A61K47/10
摘要： The present invention relates to the prevention of restenosis of vascular passages following surgical removal of obstructions, by means of local administration of farnesyl transferase inhibitors to the vascular wall. This allows effective use of particularly low dosages with minimal side effects.
摘要翻译：本发明涉及通过将法呢基转移酶抑制剂局部施用于血管壁来预防手术切除障碍物后的血管通路再狭窄。这允许有效地使用具有最小副作用的特别低的剂量。

10. 发明授权

US06458775B1 NAALADase inhibitors useful as pharmaceutical compounds and compositions 失效
标题翻译：用作药物化合物和组合物的NAALADase抑制剂
公开(公告)号：US06458775B1
公开(公告)日：2002-10-01
申请号：US09346711
申请日：1999-07-02
申请人： Paul F. Jackson , Keith M. Maclin , Eric Wang , Barbara S. Slusher , Rena S. Lapidus , Pavel Majer
发明人： Paul F. Jackson , Keith M. Maclin , Eric Wang , Barbara S. Slusher , Rena S. Lapidus , Pavel Majer
IPC分类号： A61K3166
CPC分类号： C07C309/17 , C07C309/24 , C07C317/44 , C07C323/12 , C07C323/52 , C07C323/56 , C07C327/18 , C07C327/36 , C07C329/12 , C07C333/14 , C07C333/20 , C07D213/55
摘要： The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.
摘要翻译：本发明涉及N-乙酰化的α-连接酸性二肽酶（NAALADase）抑制剂酶活性，包含这些抑制剂的药物组合物及其用于抑制NAALADase酶活性的方法，从而影响神经元活性，抑制血管发生和治疗谷氨酸异常，强迫症，前列腺疾病，疼痛和糖尿病性神经病变。

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