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1. 发明申请

WO1997024339A1 TETRAZOLE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：四唑衍生物和含有其作为活性成分的药物
公开(公告)号：WO1997024339A1
公开(公告)日：1997-07-10
申请号：PCT/JP1996003801
申请日：1996-12-26
申请人： ONO PHARMACEUTICAL CO., LTD. , OHMOTO, Kazuyuki , TANAKA, Makoto , MIYAZAKI, Tohru , OHNO, Hiroyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D257/04
CPC分类号： C07D257/04 , A61K38/00 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07K5/0205 , C07K5/06052 , C07K5/06139
摘要： Tetrazole derivatives represented by general formula (I), nontoxic salts thereof, and drugs containing the same as the active ingredient. Because of having an inhibitory effect on the interleukin-1 beta converter enzyme, the compounds of general formula (I) are useful in the prevention and/or treatment of various inflammatory diseases, wherein R represents H, alkyl, alkoxy, a carbocycle, a heterocycle, alkyl or alkoxy substituted by a carbocycle or a heterocycle, etc.; AA represents a single bond or (i); AA represents a single bond or (ii); or AA and AA may together form a group of formula (a); Y represents a group of formula (b) wherein the Tet ring represents a tetrazole ring; Z represents alkylene, alkenylene, O, S, SO, SO2, NR or alkylene wherein methylene is substituted by O, S, SO, SO2 or NR ; and E represents H, alkyl, COOR or (iii), wherein the Cyc ring represents a carbocycle or a heterocycle.
摘要翻译：由通式（I）表示的四唑衍生物，其无毒盐和含有与活性成分相同的药物。由于对白细胞介素-1β转化酶具有抑制作用，通式（I）的化合物可用于预防和/或治疗各种炎性疾病，其中R 1表示H，烷基，烷氧基，碳环，杂环，被碳环或杂环取代的烷基或烷氧基等; AA 1表示单键或（i）; AA 2表示单键或（ii）; 或AA 1和AA 2可以一起形成式（a）的基团; Y表示式（b）的基团，其中Tet环表示四唑环; Z表示亚烷基，亚烯基，O，S，SO，SO 2，NR 26或亚烷基，其中亚甲基被O，S，SO，SO 2或NR 26取代; 和E表示H，烷基，COOR 27或（iii），其中环环表示碳环或杂环。

2. 发明申请

WO1996003148A1 METHOD AND DRUG FOR TREATING DIABETES 审中-公开
标题翻译：用于治疗糖尿病的方法和药物
公开(公告)号：WO1996003148A1
公开(公告)日：1996-02-08
申请号：PCT/JP1995001484
申请日：1995-07-26
申请人： ONO PHARMACEUTICAL CO., LTD. , KITAGAWA, Koichiro , HIRANO, Atsushi , OHNO, Hiroyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K45/00
CPC分类号： C07K14/47 , A61K38/00
摘要： A novel protein p82; a method and drug for treating diabetes by tyrosinephosphorylating the protein; a drug for treating diabetes containing a derivative capable of tyrosine-phosphorylating the protein, such as a thiazoline derivative, a benzoquinone derivative, a naphthoquinone derivative or vanadic acid, as the active ingredient; and a method of screening a drug for treating diabetes by using the protein. The tyrosinephosphorylation of protein p82 is an indispensable step for glycogen synthesis and the above treatment method and drug and screening method are useful for the amelioration of hyperglycemia and the prevention, treatement, diagnosis and/or measurement of diabetes, particularly non-insulin-dependent diabetes mellitus.
摘要翻译：一种新型蛋白质p82; 通过酪氨酸磷酸化蛋白质治疗糖尿病的方法和药物; 用于治疗含有能够使酪氨酸磷酸化蛋白质的衍生物（例如噻唑啉衍生物，苯醌衍生物，萘醌衍生物或钒酸）作为活性成分的糖尿病药物; 以及通过使用该蛋白质来筛选用于治疗糖尿病的药物的方法。蛋白质p82的酪氨酸磷酸化是糖原合成不可或缺的一步，上述治疗方法和药物和筛选方法可用于改善高血糖症，预防，治疗，诊断和/或测量糖尿病，特别是非胰岛素依赖性糖尿病糖尿病。

3. 发明申请

WO1996001843A1 POLYPEPTIDE PRODUCED BY STROMAL CELL 审中-公开
标题翻译：由细胞产生的多肽
公开(公告)号：WO1996001843A1
公开(公告)日：1996-01-25
申请号：PCT/JP1995001342
申请日：1995-07-05
申请人： ONO PHARMACEUTICAL CO., LTD. , HONJO, Tasuku , NAKANO, Tohru , HIRANO, Atsushi , SIBAYAMA, Shiro , OHNO, Hiroyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07K14/435
CPC分类号： C07K14/47 , A61K38/00
摘要： A polypeptide produced by mouse marrow stromal cells and composed of 211 amino acid residues, and a human homolog thereof; a process for producing the polypeptide; a DNA coding for the polypeptide; a fragment hybridizing selectively with the DNA sequence; a replication or expression vector comprising the DNA; a host cell transformed by the vector; an antibody against the polypeptide; and a pharmaceutical composition containing the polypeptide or the antibody. The polypeptide is usable for the prevention or treatment of the hypoplasia or abnormal growth of hematopoietic cells, the hyperergasia or hypergasia of the nervous system, diseases related to the hyperergasia or hypergasia of the immune system, such as inflammatory diseases, the decrease of hematopoietic cells after bone marrow transplantation, the decrease of leucocytes, platelets, B cells or T cells after radiation therapy, anemia and infectious diseases; the prevention or treatment of cancer, leukemia and AIDS; the prevention or treatment of various degenerative diseases and nerve injury; the prevention of treatment of metabolic disorder of the bone; and tissue repair.
摘要翻译：由小鼠骨髓基质细胞产生并由211个氨基酸残基组成的多肽及其人类同源物; 一种生产该多肽的方法; 编码该多肽的DNA; 与DNA序列选择性杂交的片段; 包含DNA的复制或表达载体; 由载体转化的宿主细胞; 抗多肽的抗体; 和含有多肽或抗体的药物组合物。该多肽可用于预防或治疗造血细胞发育不全或异常生长，神经系统的高血压或高血压，与免疫系统的高血压或高血压有关的疾病，如炎性疾病，造血细胞减少骨髓移植后，放射治疗后，白细胞，血小板，B细胞或T细胞减少，贫血和感染性疾病; 预防或治疗癌症，白血病和艾滋病; 预防或治疗各种退行性疾病和神经损伤; 预防骨代谢紊乱的治疗; 和组织修复。

4. 发明申请

WO1996000086A1 THERAPEUTIC METHOD AND REMEDY FOR DIABETES 审中-公开
标题翻译：糖尿病的治疗方法和补救措施
公开(公告)号：WO1996000086A1
公开(公告)日：1996-01-04
申请号：PCT/JP1995001267
申请日：1995-06-23
申请人： ONO PHARMACEUTICAL CO., LTD. , KITAGAWA, Koichiro , HIRANO, Atsushi , OHNO, Hiroyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K45/00
CPC分类号： C07K14/47 , A61K38/00
摘要： A novel protein p72; a therapeutic method and a remedy for diabetes, each characterized by tyrosinephosphorylating the protein p72; a remedy for diabetes containing a derivative which tyrosinephosphorylates the protein p72 or a nontoxic salt thereof as the active ingredient; and a method of screening a remedy for diabetes by using the protein p72. The protein p72 tyrosinephosphorylation is an essential step for lowering the blood sugar level by glucose incorporation, and the therapeutic method and remedy for diabetes and the screening method of the invention are useful for ameliorating the hyperglycemic condition, and preventing, treating, diagnosing and/or assaying diabetes, especially noninsulin-dependent diabetes mellitus.
摘要翻译：一种新型蛋白质p72; 糖尿病的治疗方法和治疗方法，其特征在于蛋白质p72的酪氨酸磷酸化; 含有将蛋白质p72酪氨酸磷酸化的衍生物或其无毒性盐作为活性成分的糖尿病补救剂; 以及通过使用蛋白质p72筛选糖尿病治疗方法。蛋白质p72酪氨酸磷酸化是通过葡萄糖掺入降低血糖水平的必要步骤，糖尿病的治疗方法和治疗方法以及本发明的筛选方法可用于改善高血糖状况，以及预防，治疗，诊断和/或测定糖尿病，特别是非胰岛素依赖性糖尿病。

5. 发明申请

WO1990009399A1 NEW NEUROTROPHIC FACTOR 审中-公开
标题翻译：新神经营养因子
公开(公告)号：WO1990009399A1
公开(公告)日：1990-08-23
申请号：PCT/JP1990000154
申请日：1990-02-08
申请人： ONO PHARMACEUTICAL CO., LTD. , KATO, Taiji , TANAKA, Ryo
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07K15/06
CPC分类号： C07K14/475
摘要： This invention relates to a new neurotrophic factor (NTF) isolated and purified from the block of neurofibromata obtained from the patients suffering from the von Recklinghausen disease. The NTF has a polypeptide portion of a molecular weight of 3.000 +/- 500 and is a substance which is thermally stable and sensitive to trypsin and proteinase K. This substance promotes the extension of axons of the neurons of a cerebral cortex in a culture medium of a concentration of 1 to 50 ng/ml.
摘要翻译：本发明涉及从患有冯·雷克灵豪森病的患者获得的神经纤维瘤块中分离和纯化的新的神经营养因子（NTF）。 NTF具有分子量为3.000 +/- 500的多肽部分，并且是对胰蛋白酶和蛋白酶K热稳定和敏感的物质。该物质促进培养基中大脑皮质神经元的轴突的延伸浓度为1至50ng / ml。

6. 发明申请

WO1998027053A1 SULFONAMIDE AND CARBOXAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：磺酰胺和羧酰胺衍生物及其含有作为活性成分的药物
公开(公告)号：WO1998027053A1
公开(公告)日：1998-06-25
申请号：PCT/JP1997004593
申请日：1997-12-12
申请人： ONO PHARMACEUTICAL CO., LTD. , OHUCHIDA, Shuichi , NAGAO, Yuuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C233/25
CPC分类号： C07D213/80 , C07C233/18 , C07C233/75 , C07C311/08 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/17 , C07C311/21 , C07C311/29 , C07C313/06 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D307/64 , C07D307/68 , C07D333/34 , C07D333/38
摘要： Sulfonamide and carboxamide derivatives represented by general formula (I) wherein the rings A and B represent each a carbocycle or a heterocycle; Z represents -COR , -CH=CH-COR , etc.; Z represents H, alkyl, etc.; Z represents a single bond or alkylene; Z represents SO2 or CO; Z represents alkyl, phenyl, a heterocycle, etc., R represents CONR , O, S, NZ , Z -alkylene, alkylene, etc.; R represents H, alkyl, halogeno, CF3, etc.; R represents H, optionally substituted alkyl, etc., and n and t are each from 1 to 4. The compounds of general formula (I) bind to PGE2 receptors and exert an antagonism or agonism thereto. Thus, they are applicable to drugs having the effects of inhibiting uterine muscle contraction, analgesia, inhibiting digestive tract movement, hypnosis, enlarging vesical capacity, contracting the uterine, promoting the digestive tract movement, suppressing the secretion of gastric hydrochloric acid, lowering blood pressure, or diuresis.
摘要翻译：由通式（I）表示的磺酰胺和甲酰胺衍生物，其中环A和B各自表示碳环或杂环; Z 1表示-COR 1，-CH = CH-COR 1等; Z 2表示H，烷基等; Z 3表示单键或亚烷基; Z 4表示SO 2或CO; Z 5表示烷基，苯基，杂环等，R 2表示CONR 8，O，S，NZ 6，Z 7 - 亚烷基，亚烷基等; R 3表示H，烷基，卤代，CF 3等; R 4表示H，任选取代的烷基等，n和t各自为1〜4。通式（I）的化合物与PGE 2受体结合，对其起作用或拮抗作用。因此，它们适用于具有抑制子宫肌肉收缩，镇痛，抑制消化道运动，催眠，扩大膀胱容量，收缩子宫，促进消化道运动，抑制胃酸分泌，降低血压的作用的药物，或利尿。

7. 发明申请

WO1997005091A1 NAPHTHYLOXYACETIC ACID DERIVATIVES AND DRUGS COMPRISING THE SAME AS ACTIVE INGREDIENTS 审中-公开
标题翻译：萘酚酸衍生物和包含它们作为活性成分的药物
公开(公告)号：WO1997005091A1
公开(公告)日：1997-02-13
申请号：PCT/JP1996001833
申请日：1996-07-02
申请人： ONO PHARMACEUTICAL CO., LTD. , NAGAO, Yuuki , TORISU, Kazuhiko , HAMANAKA, Nobuyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C43/178
CPC分类号： C07D257/04 , C07C59/68 , C07C69/712 , C07C217/60 , C07C233/18 , C07C255/16 , C07C317/18 , C07C323/16
摘要： Naphthyloxyacetic acid derivatives represented by general formula (I), wherein A represents H, -(alkylene)COOR , -(alkylene)CONR R , -(alkylene)OH, -(alkylene)tetrazolyl or -(alkylene)-CN; E represents a single bond or alkylene; G represents -S-, -SO-, -SO2-, -O- or -NR -; L represents alkylene, -(CH2)m-CH=CH-(CH2)n- or -(CH2)x-CH(OH)-(CH2)y-; M represents phenyl, phenyl-(thio, oxy, amino), diphenylmethyl or diphenylmethyl(thio, oxy, amino). The compound (I) binds to PGE2 receptors and exhibit an antagonistic or agonistic effect thereon. Thus, it is useful as a hyperlipemia inhibitor, a medecine for preventing abortion, an analgetic agent, an antidiarrheal, a drug for sleep induction, a diuretic agent, an antidiabetic agent, an interrupting agent, a purgative, an antiulcer agent, a drug for gastritis, a hypotensive drug, etc.
摘要翻译：由通式（I）表示的萘并氧基乙酸衍生物，其中A表示H， - （亚烷基）COOR 1， - （亚烷基）CONR 2 R 3 - - （亚烷基）OH， - （亚烷基）四唑基或 - （亚烷基）-CN; E表示单键或亚烷基; G表示-S - ， - SO - ， - SO 2 - ， - O-或-NR 4 - 。 L表示亚烷基， - （CH 2）m -CH = CH-（CH 2）n - 或 - （CH 2）x -CH（OH） - （CH 2）y - M代表苯基，苯基 - （硫基，氧基，氨基），二苯基甲基或二苯基甲基（硫代，氧基，氨基）。化合物（I）与PGE 2受体结合并在其上表现出拮抗作用或激动作用。因此，作为高脂血症抑制剂，防止流产的药物，止痛药，止泻药，睡眠诱导药，利尿剂，抗糖尿病药，中断剂，泻药，抗溃疡剂，药物胃炎，降血压药等

8. 发明申请

WO1997045402A1 PHENYLSULFONAMIDE DERIVATIVES 审中-公开
标题翻译：苯磺酰胺衍生物
公开(公告)号：WO1997045402A1
公开(公告)日：1997-12-04
申请号：PCT/JP1997001735
申请日：1997-05-23
申请人： ONO PHARMACEUTICAL CO., LTD. , TAKAHASHI, Kanji , SUGIURA, Tsuneyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C311/00
CPC分类号： C07D213/42 , C07C311/19 , C07C311/29 , C07C311/53 , C07D207/16 , C07D209/20 , C07D213/52 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Phenylsulfonylamide derivatives represented by general formula (I) and salts thereof, (wherein R is hydrogen or alkyl; R is COOR or CONHOR ; E is vinylene or ethylene; A is hydrogen, alkyl, carbocycle or heterocycle; J is single bond or alkylene; R and R are each hydrogen, (substituted) alkyl, COR , carbocycle, heterocycle, etc.; and R is hydrogen, (substituted) alkyl, etc.); processes for producing the same; a matrix metalloproteinase inhibitor containing the same; and medicines containing the same and serving as preventives and/or remedies for rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontosis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatocirrhosis, corneal injury, diseases due to cancer cell metastasis, infiltration and proliferation, autoimmune diseases (such as Crohn's disease and Sjögren's disease), diseases due to leukocyte emigration or infiltration, and neovascularization.
摘要翻译：由通式（I）表示的苯磺酰胺衍生物及其盐（其中R 1是氢或烷基; R 2是COOR 3或CONHOR 4）; E是亚乙烯基或亚乙基; A是氢，烷基，碳环或杂环; J是单键或亚烷基; R 9和R 10各自是氢，（取代的）烷基，COR 11，碳环，杂环等; R 20是氢，（取代的）烷基等）; 制造方法; 含有它的基质金属蛋白酶抑制剂; 以及用于预防和/或治疗风湿病，骨关节炎，病理性骨吸收，骨质疏松症，牙周病，间质性肾炎，动脉硬化，肺气肿，肝硬化，角膜损伤，癌细胞转移，浸润和增殖的疾病的药物，自身免疫性疾病（如克罗恩病和Siegren病），白细胞迁移或浸润引起的疾病以及新生血管形成。

9. 发明申请

WO1996010013A1 FIVE MEMBERED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：五种成分的杂环化合物
公开(公告)号：WO1996010013A1
公开(公告)日：1996-04-04
申请号：PCT/US1995011962
申请日：1995-09-27
申请人： ONO PHARMACEUTICAL CO., LTD. , LEE, Sung, Jai , SEKO, Takuya , FRIERSON, Manton, Rodgers , SIRCAR, Jagadish, Chandra , CAO, Charles, Xian
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/333
CPC分类号： C07D207/337 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4164 , A61K31/4172 , A61K31/4174 , A61K31/4178 , A61K31/443 , A61K31/4436 , A61K31/4439 , C07D233/64 , C07D307/54 , C07D333/24 , C07D403/10 , C07D405/06 , C07D409/06 , C07D409/10
摘要： This invention is related to: (1) an inhibitory agent on 5 alpha -reductase which comprises a five membered heterocyclic compound of formula (Ia), and non-toxic salts thereof as active ingredient; (2) a five membered heterocyclic compound of formula (Ib), and non-toxic salts thereof; (3) process for the preparation of a five membered heterocyclic ring compound of formula (Ib) and non-toxic salts thereof. The compounds of formula (Ia) are useful for the prevention and treatment of diseases induced by the excess generation of dihydrotestosterone in mammals, for example, alopecia (androgenic alopecia), acnes, hypertrophy of prostate and prostatic cancer.
摘要翻译：本发明涉及：（1）5α-还原酶的抑制剂，其包含式（Ia）的五元杂环化合物及其无毒性盐作为活性成分; （2）式（Ib）的五元杂环化合物及其无毒盐; （3）制备式（Ib）的五元杂环化合物及其无毒盐的方法。式（Ia）化合物可用于预防和治疗由哺乳动物中过量产生二氢睾酮引起的疾病，例如脱发（雄激素性脱发），痤疮，前列腺肥大和前列腺癌。

10. 发明申请

WO1995009008A1 PERCUTANEOUSLY ABSORBABLE PREPARATION 审中-公开
标题翻译： PERCUTANEOUSYOUSLY可吸收制剂
公开(公告)号：WO1995009008A1
公开(公告)日：1995-04-06
申请号：PCT/JP1994001584
申请日：1994-09-27
申请人： TAKIRON CO., LTD. , ONO PHARMACEUTICAL CO., LTD. , SHIKINAMI, Yasuo , HATA, Kunihiro , SASATANI, Seiei , SUDOH, Masao
发明人： TAKIRON CO., LTD. , ONO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K47/30
CPC分类号： A61K9/7084
摘要： A percutaneously absorbable preparation which can long stably preserve a water-soluble drug capable of exhibiting the effect in a small dose and being readily decomposable, solid at ordinary temperature and difficultly absorbable percutaneously and which can sustainedly release the drug percutaneously at a high rate when applied to the skin. The preparation comprises a drug store layer wherein a drug is incorporated and a drug release control membrane for coating the drug release surface of the drug store layer. This layer is made from a heat-sensitive segmented polyurethane which is represented by the following general formula: R-A-(U)-F-(U)-B-R', (wherein A and B represent each a homopolymer or a random or block copolymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide; R and R' represent each H, CH3, C2H5, C3H7 or C4H9 as the terminal of each of A nad B; A=B or A NOTEQUAL B; R=R' or R NOTEQUAL R'; F represents the residue of a diisocyanate compound; and (U) represents a urethane bond) and wherein at least one of A and B is hydrophilic and at least one of them will melt near the human skin temperature. The drug release control membrane comprises a phase-separation membrane wherein a cross-linked gelatin phase and a non-cross-linked segmented polyurethane phase are intermingled.
摘要翻译：一种经皮吸收制剂，其可以长期稳定地保持能够以小剂量显示效果并且易于分解的常温下的固体，并且经皮难以吸收的水溶性药物，并且其可以在施用时以高速率经皮持续释放药物到皮肤。该制剂包括其中掺入药物的药物储存层和用于涂覆药物储存层的药物释放表面的药物释放控制膜。该层由热敏分段聚氨酯制成，其由以下通式表示：RA-（U）-F-（U）-B-R'，（其中A和B各自表示均聚物或随机或环氧乙烷，环氧丙烷，四氢呋喃或1,2-环氧丁烷的嵌段共聚物; R和R'表示作为A nad B各自的H，CH 3，C 2 H 5，C 3 H 7或C 4 H 9; A = B或A B; R = R'或R“等式R”; F表示二异氰酸酯化合物的残基;（U）表示氨基甲酸酯键），并且其中A和B中的至少一个是亲水性的，并且其中至少一个将在近人体皮肤温度。药物释放控制膜包括其中交联的凝胶相和非交联的分段的聚氨酯相混合的相分离膜。

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