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    • 2. 发明申请
    • 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES
    • 1H-4(5) - 取代的咪唑衍生物
    • WO1996038142A1
    • 1996-12-05
    • PCT/US1996007873
    • 1996-05-29
    • GLIATECH, INC.PHILLIPS, James, G.TEDFORD, Clark, E.CHATURVEDI, Nishith, C.
    • GLIATECH, INC.
    • A61K31/415
    • C07D233/56A61K31/417A61K31/4174A61K31/4178C07D233/64C07D403/12C07D405/12
    • The present invention provides, in its principal aspect, compounds of general formula (1.0) or a pharmaceutically acceptable salt or hydrate thereof, wherein: where A is -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-, -COCH2-, -CH2CH2-, -CH(OH)CH2-, or -CC-; X is H, CH3, NH2, NH(CH3), N(CH3)2, OH, OCH3, or SH; R2 is hydrogen or a methyl or ethyl group; R3 is hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) phenyl or substituted phenyl; (d) heterocyclic; (e) decahydronaphthalene and (f) octahydroindene; or R1 and X may be taken together to denote a 5,6 or 6,6 saturated bicyclic ring structure when X is NH, O, or S. The individual stereoisomers of compounds of structural formula (1.0) above, as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The compounds of the present invention have H3 histamine receptor antagonist activity. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of formula 1.0. The present invention also provides a method of treating conditions in which antagonism of histamine H3 receptors may be of therapeutic importance.
    • 本发明在其主要方面提供了通式(1.0)的化合物或其药学上可接受的盐或水合物,其中:A是-NHCO - , - N(CH 3)-CO - , - NHCH 2 - , - N (CH 3)-CH 2 - , - CH = CH - , - COCH 2 - , - CH 2 CH 2 - , - CH(OH)CH 2 - 或-CC-; X是H,CH 3,NH 2,NH(CH 3),N(CH 3)2,OH,OCH 3或SH; R2是氢或甲基或乙基; R3是氢或甲基或乙基; n是0,1,2,3,4,5或6; 并且R 1选自(a)C 3至C 8环烷基; (b)苯基或取代的苯基; (d)杂环; (e)十氢萘和(f)八氢茚; 或者当X是NH,O或S时,R 1和X可以一起表示5,6或6,6饱和的双环结构。上述结构式(1.0)化合物的各个立体异构体以及它们的混合物 也被认为落入本发明的范围内。 本发明化合物具有H3组胺受体拮抗剂活性。 本发明还提供药物组合物,其包含药学上可接受的载体与有效量的式1.0化合物的组合。 本发明还提供了治疗组胺H 3受体的拮抗作用具有治疗意义的病症的方法。
    • 3. 发明申请
    • INHIBITION OF BETA AMYLOID BINDING TO GLYCOSAMINOGLYCANS FOR TREATMENT OF ALZHEIMER'S DISEASE
    • 用于治疗阿尔茨海默病的β-淀粉样蛋白结合抑制剂
    • WO1995006477A1
    • 1995-03-09
    • PCT/US1994009853
    • 1994-08-29
    • GLIATECH, INC.
    • GLIATECH, INC.BRUNDEN, Kurt, R.GUPTA-BANSAL, RekhaRICHTER-COOK, Nancy, J.FREDERICKSON, Robert, C., A.
    • A61K38/00
    • A61K38/07A61K38/08C07K5/1005C07K5/1016C07K5/1019C07K5/1021C07K14/4711
    • The present invention relates to compounds that inhibit the binding of glycosaminoglycans and proteoglycans to beta amyloid peptide (A(beta); A beta ), and to compounds that inhibit A beta activation of complement. In one aspect, the compound is a peptide having an amino acid sequence X-X-N-X, in which X is an amino acid with a cationic side chain and N is a neutral amino acid. In another aspect, the compound is a peptide having an amino acid sequence X-X-N-X-Z, in which X is an amino acid with a cationic side chain, N is a neutral amino acid and Z is a neutral amino acid. In yet another aspect, the compound is peptide having an amino acid sequence X1-N-X2-X3, in which at least two of X1, X2, and X3 are independently an amino acid with an anionic side chain and the third X is an amino acid with an anionic side chain or a neutral amino acid and N is independently a neutral amino acid. In yet a further aspect, the compound is an anionic disaccharide. The invention also relates to a method for treating Alzheimer's disease comprising administering a therapeutically effective amount of a compound as described above to a subject suffering from Alzheimer's disease. Pharmaceutical compositions are also provided.
    • 本发明涉及抑制糖胺聚糖和蛋白多糖与β淀粉样肽(A(β);Aβ)的结合的化合物,以及抑制补体的Aβ激活的化合物。 一方面,化合物是具有氨基酸序列X-X-N-X的肽,其中X是具有阳离子侧链的氨基酸,N是中性氨基酸。 另一方面,化合物是具有氨基酸序列X-X-N-X-Z的肽,其中X是具有阳离子侧链的氨基酸,N是中性氨基酸,Z是中性氨基酸。 另一方面,化合物是具有氨基酸序列X1-N-X2-X3的肽,其中X1,X2和X3中的至少两个独立地是具有阴离子侧链的氨基酸,而第三个X是 具有阴离子侧链或中性氨基酸的氨基酸,N独立地为中性氨基酸。 在另一方面,该化合物是阴离子二糖。 本发明还涉及一种治疗阿尔茨海默氏病的方法,包括向患有阿尔茨海默病的受试者施用治疗有效量的如上所述的化合物。 还提供药物组合物。
    • 4. 发明申请
    • 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES
    • 1H-4(5) - 取代的咪唑衍生物
    • WO1996040126A1
    • 1996-12-19
    • PCT/US1996009498
    • 1996-06-06
    • GLIATECH, INC.PHILLIPS, James, G.KHAN, Amin, MohammedTEDFORD, Clark, E.
    • GLIATECH, INC.
    • A61K31/415
    • C07D233/64A61K31/4164A61K31/422C07D413/04
    • The present invention is directed to 1H-4(5)-substituted imidazole derivates of formula (I), wherein A is (a); (b); or (c) where R1 is lower alkyl or lower alkoxy; R2, R3, R4, R5, R7 and R8 are each independently hydrogen or lower alkyl; R6 is hydrogen, lower alkyl or lower alkoxy and R5 and R6 can be joined to form a 4, 5 or 6 membered ring. The compounds of formula (I) have H3 histamine receptor agonist activity. The pharmaceutically acceptable salts, and individual stereoisomers of compounds of formula (I) above, as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The present invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of formula (I). The present invention also provides a method of treating conditions in which activation of histamine H3 receptors may be of therapeutic importance such as allergy, inflammation, cardio or cerebrovascular disease (i.e., hyper or hypotension, ischemia, stroke, migraine), gastrointestinal disorders (acid secretion, motility) and CNS disorders involving psychiatric disorders (i.e., including anxiety, manic/depressive disorder, schizophrenia, obsessive-compulsive disorders, etc.).
    • 本发明涉及式(I)的1H-4(5) - 取代的咪唑衍生物,其中A是(a); (B); 或(c)其中R 1为低级烷基或低级烷氧基; R2,R3,R4,R5,R7和R8各自独立地为氢或低级烷基; R6是氢,低级烷基或低级烷氧基,R5和R6可以连接形成4,5或6元环。 式(I)化合物具有H3组胺受体激动剂活性。 上述式(I)化合物的药学上可接受的盐和单独的立体异构体以及它们的混合物也被认为落入本发明的范围内。 本发明还提供药物组合物,其包含药学上可接受的载体与有效量的式(I)化合物的组合。 本发明还提供了治疗组胺H 3受体活化可能具有治疗重要性的病症的方法,例如过敏,炎症,心脑血管疾病(即高血压或低血压,局部缺血,中风,偏头痛),胃肠道疾病 分泌,运动)和涉及精神障碍的CNS疾病(即包括焦虑,躁狂/抑郁障碍,精神分裂症,强迫症等)。
    • 5. 发明申请
    • 2-(1H-4(5)-IMIDAZOYL) CYCLOPROPYL DERIVATIVES
    • 2-(1H-4(5)-IMIDAZOYL)环丙基衍生物
    • WO1996038141A1
    • 1996-12-05
    • PCT/US1996007833
    • 1996-05-29
    • GLIATECH, INC.PHILLIPS, James, G.TEDFORD, Clark, E.KHAN, Amin, MohammedYATES, Stephen, L.
    • GLIATECH, INC.
    • A61K31/415
    • C07D233/64
    • The present invention provides compounds having H3 histamine receptor antagonist activity of general formula (1.0), wherein R2 is a hydrogen or a methyl or ethyl group; R3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronaphthalene; and (f) octahydroindene; with the provisos that when X is H, A can be -CH2CH2-, -COCH2-, -CONH-, -CON(CH3)-, -CH=CH-, alpha , -CH2-NH-, -CH2-N(CH3)-, -CH(OH)CH2-, -NH-CH2-, -N(CH3)-CH2-, -CH2O-, -CH2S-, and -NHCOO-; when X is NH2, NH(CH3), N(CH3)2, OH, OCH3, CH3, SH and SCH3; A can be -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-, -COCH2-, -CH2CH2-, -CH(OH)CH2-, or beta ; and when R1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O, or S. The pharmaceutically acceptable salts, hydrates, and individual stereoisomers of compounds of structral formula (1.0), as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of said formula and a method of treating conditions in which antagonism of histamine H3 receptors may be of therapeutic importance.
    • 本发明提供具有通式(1.0)的H3组胺受体拮抗剂活性的化合物,其中R2是氢或甲基或乙基; R3是氢或甲基或乙基; n是0,1,2,3,4,5或6; 并且R 1选自(a)C 3至C 8环烷基; (b)苯基或取代的苯基; (c)烷基; (d)杂环; (e)十氢萘; 和(f)八氢茚; 条件是当X是H时,A可以是-CH 2 CH 2 - , - COCH 2 - , - CONH - , - CON(CH 3) - , - CH = CH-,α,-CH 2 -NH-, - CH 2 -N CH 3) - , - CH(OH)CH 2 - , - NH-CH 2 - , - N(CH 3)-CH 2 - , - CH 2 O - , - CH 2 S - 和-NHCOO-; 当X是NH 2时,NH(CH 3),N(CH 3)2,OH,OCH 3,CH 3,SH和SCH 3; A可以是-NHCO - , - N(CH 3)-CO - , - NHCH 2 - , - N(CH 3)-CH 2 - , - CH = CH - , - COCH 2 - , - CH 2 CH 2 - , - CH(OH) ,或beta 并且当R 1和X一起表示5,6或6,6饱和双环结构时,X可以是NH,O或S.结构式(1.0)化合物的药学上可接受的盐,水合物和单独的立体异构体, 以及它们的混合物也被认为落入本发明的范围内。 本发明还提供药物组合物,其包含药学上可接受的载体与有效量的所述式的化合物的组合以及治疗其中组胺H3受体的拮抗作用具有治疗意义的病症的方法。
    • 6. 发明申请
    • METHODS AND COMPOSITIONS BASED ON INHIBITION OF CELL INVASION AND FIBROSIS BY ANIONIC POLYMERS
    • 基于静电聚合物抑制细胞侵入和纤维化的方法和组合物
    • WO1992021354A1
    • 1992-12-10
    • PCT/US1992004474
    • 1992-05-29
    • GLIATECH, INC.ROUFA, DiklaHAREL, AdrianFREDERICKSON, Robert, C., A.
    • GLIATECH, INC.
    • A61K31/725
    • A61K31/734A61K31/727A61K31/728A61K31/737A61K31/738A61K38/1703A61K38/39A61L27/20A61L27/34A61L31/042Y10S530/857Y10S623/915Y10S623/924Y10S977/788Y10S977/793Y10S977/795Y10S977/908Y10S977/91A61K31/715A61K2300/00C08L5/00C08L5/02C08L5/04
    • The present invention relates to the discovery that biocompatible anionic polymers can effectively inhibit fibrosis, scar formation, and surgical adhesions. The invention is predicated on the discovery that anionic polymers effectively inhibit invasion of cells associated with detrimental healing processes, and in particular, that the effectiveness of an anionic polymer at inhibiting cell invasion correlates with the anionic charge density of the polymer. Thus, the present invention provides a large number of materials for use in methods of inhibiting fibrosis and fibroblast invasion. Anionic polymers for use in the invention include but are not limited to natural proteoglycans, and the glycosaminoglycan moieties of proteoglycans. Additionally, anionic carbohydrates and other anionic polymers may be used. The anionic polymers dextran sulfate and pentosan polysulfate are preferred. In a more preferred embodiment, dextran sulfate, in which the sulfur content is greater than about 10 % by weight, may be used. In a more preferred embodiment, the average molecular weight is about 40,000 to 500,000 Daltons. The present invention provides compositions and methods to inhibit fibrosis and scarring associated with surgery. The invention further provides compositions and methods to inhibit glial cell invasion, detrimental bone growth and neurite outgrowth. In a preferred embodiment, the inhibitory compositions further comprise an adhesive protein.
    • 本发明涉及生物相容性阴离子聚合物可有效抑制纤维化,瘢痕形成和手术粘连的发现。 本发明基于以下发现:阴离子聚合物有效地抑制与有害愈合过程相关的细胞的侵袭,特别是阴离子聚合物抑制细胞侵袭的有效性与聚合物的阴离子电荷密度相关。 因此,本发明提供了大量用于抑制纤维化和成纤维细胞侵袭的方法的材料。 用于本发明的阴离子聚合物包括但不限于天然蛋白聚糖和蛋白聚糖的糖胺聚糖部分。 此外,可以使用阴离子碳水化合物和其它阴离子聚合物。 阴离子聚合物硫酸葡聚糖和聚山梨糖多糖是优选的。 在更优选的实施方案中,可以使用其中硫含量大于约10重量%的硫酸葡聚糖。 在更优选的实施方案中,平均分子量为约40,000至500,000道尔顿。 本发明提供抑制与手术相关的纤维化和瘢痕形成的组合物和方法。 本发明还提供抑制胶质细胞侵袭,有害的骨生长和神经突生长的组合物和方法。 在优选的实施方案中,抑制组合物还包含粘合蛋白。
    • 7. 发明申请
    • INHIBITION OF CELL GROWTH BY KERATAN SULFATE, CHONDROITIN SULFATE, DERMATAN SULFATE AND OTHER GLYCANS
    • 通过硫酸钙,硫酸锌,硫酸铝和其他甘油的细胞生长抑制
    • WO1991006303A1
    • 1991-05-16
    • PCT/US1990006189
    • 1990-10-26
    • CASE WESTERN RESERVE UNIVERSITYGLIATECH, INC.
    • CASE WESTERN RESERVE UNIVERSITYGLIATECH, INC.SNOW, Diane, M.SILVER, JerryHAREL, AdrianROUFA, Dikla
    • A61K31/715
    • A61K31/715A61K31/70C07K16/18C12N9/2408Y02A50/472A61K2300/00
    • The present invention is directed to methods of using keratan sulfate, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin, and hyaluronic acid, and molecules and compositions comprising keratan sulfate, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin, and hyaluronic acid, to inhibit or prevent neurite outgrowth, i.e., axonal growth, or nerve regeneration (colectively termed herein ''nerve growth''), or glial cell migration or invasion, or regeneration, and therapeutically, where the foregoing is desired. In another embodiment of the invention, inhibitors and antagonists of keratan sulfate, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin, and hyaluronic acid, and molecules and compositions containing the same, may be used to promote nerve growth or glial cell migration or invasion, and can be administered therapeutically. Such inhibitors and antagonists include but are not limited to antibodies, degradative enzymes, lectins; and disaccharide antagonists of the receptors for keratan sulfate, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin or hyaluronate.
    • 本发明涉及使用硫酸角质素,硫酸软骨素,硫酸皮肤素,硫酸乙酰肝素,肝素和透明质酸的方法,以及包含硫酸角质素,硫酸软骨素,硫酸皮肤素,硫酸乙酰肝素,肝素和透明质酸的分子和组合物, 抑制或预防神经突生长,即轴突生长或神经再生(本文称为“神经生长”)或神经胶质细胞迁移或侵袭或再生,并且在治疗上需要上述内容。 在本发明的另一个实施方案中,可以使用硫酸角质素,硫酸软骨素,硫酸皮肤素,硫酸乙酰肝素,肝素和透明质酸的抑制剂和拮抗剂,以及包含其的分子和组合物来促进神经生长或神经胶质细胞迁移或侵袭 ,并且可以治疗地施用。 这些抑制剂和拮抗剂包括但不限于抗体,降解酶,凝集素; 以及硫酸角质素,硫酸软骨素,硫酸皮肤素,硫酸乙酰肝素,肝素或透明质酸的受体的二糖拮抗剂。