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1. 发明专利

JPS63165338A BIPHENYL DERIVATIVE AND ANTIALLERGIC AGENT CONTAINING SAID DERIVATIVE AS ACTIVE INGREDIENT 失效
公开(公告)号：JPS63165338A
公开(公告)日：1988-07-08
申请号：JP31026086
申请日：1986-12-27
申请人： TSUMURA & CO
发明人： EDA SHOEI , NISHIOKA ITSUO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： C07C69/16 , A61K31/11 , A61K31/22 , A61P37/08 , C07C45/00 , C07C47/27 , C07C47/565 , C07C67/00
摘要： NEW MATERIAL:A compound expressed by the formula (R1 and R4 are OH or acetoxy; R2 and R5 are H, allyl or lower alkyl; R3 and R6 are formyl or formylvinyl). EXAMPLE:2,2'-Dihydroxy-5,5'-bis[(E)-2-formylvinyl)]biphenyl. USE:An antiallergic agent. PREPARATION:For example, p-hydroxybenzaldehyde is used as a raw material and halogenated at the 3-position. The hydroxyl group at the 4-position is then protected and coupled to provide a biphenyl derivative. The formyl group of the resultant biphenyl derivative is subsequently converted into an acetal and the number of carbon atoms is increased. The protecting group is eliminated and then converted into an alpha,beta-unsaturated aldehyde to afford the aimed compound expressed by the formula.

2. 发明专利

JPH0551346A NOVEL COMPOUND AND LIPOPEROXIDE PRODUCTION INHIBITOR WITH THE SAME AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH0551346A
公开(公告)日：1993-03-02
申请号：JP23375291
申请日：1991-08-22
申请人： TSUMURA & CO
发明人： NAITO TAKASHI , IKETANI YUKINOBU , YANAGISAWA TOSHIHIKO , MIHASHI HIROSHI
IPC分类号： A61K31/12 , A61K31/34 , A61K36/18 , A61P3/06 , A61P9/00 , A61P9/10 , C07C50/06 , C07D493/04
摘要： PURPOSE:To provide novel phthalide and quinoline found in rhizome of Cnidium officinale as a crude drug, having lipoperoxide production-inhibitory activity effective for the therapy of circulatory diseases. CONSTITUTION:The objective compounds of formula I, formula II, and formula III, respectively. These compounds can be obtained by the following processes: Cnidium officinale or an analogous plant is extracted with at least one solvent selected from hexane, diethyl ether, petroleum ether, ethyl acetate, chloroform, acetone, methanol, ethanol and water, and the solvent is removed from the resultant extract; the resulting residue is then put to a chromatography using a carrier such as a porous polymer or silica gel with, as eluting solvent, at least one solvent selected from hexane, diethyl ether, petroleum ether, ethyl acetate and chloroform to effect fractionation. The present compounds are extremely low toxic and highly safe.

3. 发明专利

JPH02193916A VASODILATOR 失效
公开(公告)号：JPH02193916A
公开(公告)日：1990-07-31
申请号：JP869589
申请日：1989-01-19
申请人： TSUMURA & CO
发明人： MORIKAWA MASAKO , INOUE MICHIKO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： A61K31/045 , A61P9/08 , C07C33/26
摘要： PURPOSE:To obtain a vasodilator containing a specific lignan as an active ingredient. CONSTITUTION:2,3-Dibenzyl-1,4-butanediol expressed by the formula is contained as an active ingredient in the aimed vasodilator. The above-mentioned compound is preferably administered at an amount of 50mg-5g divided several times daily when used as an oral medicament and preferably administered at a dose of 0.1mg-1g daily by intravenous injection, drop intravenous injection, hypodermic injection or intramuscular injection when used as a parenteral medicament. The above-mentioned compound is obtained by coupling hydrocinnamic acid to afford 2,3-dibenzylsuccinic acid which is a mixture of (+ or -)body and meso body, further recrystallizing 2,3-dibenzylsuccinic acid with a mixed solvent such as methanol-water to give (+ or -)body thereof, then methylating the (+ or -)body thereof and reducing the resultant dl-dimethyl 2,3-dibenzylsuccinate.

4. 发明专利

JPH0240323A IMMUNOSUPPRESSIVE AGENT 失效
公开(公告)号：JPH0240323A
公开(公告)日：1990-02-09
申请号：JP18685388
申请日：1988-07-28
申请人： TSUMURA & CO
发明人： OKA KITAROU , HIRANO TOSHIHIKO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： A61K31/05 , A61K31/047 , A61K31/075 , A61K31/22 , A61K31/34 , A61K31/341 , A61P37/06 , C07C33/24 , C07C39/15 , C07C43/20 , C07C69/21 , C07D307/10 , C07D307/33
摘要： PURPOSE:To provide an immunosuppressive agent containing a specific lignan as an active ingredient. CONSTITUTION:An immunosuppressive agent contains as an active ingredient a lignan of formula I (A0, A1, A2 are OH, H or methoxy; A3 is H, methyl or acetyl), formula II (B1 is OH, H or methoxy), formula III (C1 is H or methoxy) or formula IV (D1 is H or methoxy; D2 is H, OH or methoxy) as an active ingredient. The compound are obtained by reacting hydrocinnamic acid, 3- methoxyhydrocinamic acid prepared by the hydrogenation of 3-methoxycinnamic acid or 3,4-dimethoxyhydrocinnamic acid prepared by the hyudrogenation of 3,4-dimethoxycinnamic acid with diisopropyl amine, n-butyl lithium and iodine in THF to form a compound of formula V (R1 and R2 are H or methoxy), methyl-esterifying the compound of formula V, reducing the esterified product with lithium aluminum hydride into an alcohol derivative thereof and, if necessary, further demethylating the alcohol derivative, etc.

5. 发明专利

JPH07233060A VASODILATOR 失效
公开(公告)号：JPH07233060A
公开(公告)日：1995-09-05
申请号：JP4326894
申请日：1994-02-18
申请人： TSUMURA & CO
发明人： NAITO TAKASHI , IKETANI YUKINOBU , KUBOTA KIYOSHI , SHIMODA YUMI
IPC分类号： C07D493/04 , A61K31/22 , A61K31/365 , A61K36/23 , A61P9/08 , C07C69/618 , C07D493/10
摘要： PURPOSE:To obtain a vasodilator containing coniferyl ferulate, etc. and effective in treating cardiovascular diseases. CONSTITUTION:This vasodilator contains Cnidii Rhizoma which is a galenical medicine or a compound of the formula (coniferyl ferulate) isolated from Cnidii Rhizoma, Cnidium officinale Makino which is an orginal plant for Cnidii Rhizoma or a plant belonging to the same genus as the plant as an active ingredient. The Cnidii Rhizoma of the galenical medicine is an umbelliferous plant and it has central inhibitory action and muscle relaxing action. The compound of the formula is directly used or blended with a conventional preparation carrier and can be prepared in a form for oral administration, e.g. tablet, capsule, granule, fine granule or powdery preparation or in a form for parenteral administration, e.g. injection or suppository and in the case of oral administration, the agent is administered in several portions at a dose of 100mg to 2g/day expressed in terms of the weight of the compound of the formula. Further, this vasodilator can contain a phthalide derivative consisting of a phthalide dimer (Tokinolide B, Levistolide A, Riligustilide or Senkyunolide P) contained in Cnidii Rhizoma as an active ingredient.

6. 发明专利

JPH07173188A NEW ALISOL, AND CEREBRAL FUNCTION-IMPROVING AGENT CONTAINING ALISOL COMPOUND AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH07173188A
公开(公告)日：1995-07-11
申请号：JP34330093
申请日：1993-12-17
申请人： TSUMURA & CO
发明人： YAMADA SUMIE , YAMAGUCHI TAKUJI , NAITO TAKASHI , HASHIMOTO KAZUNORI
IPC分类号： A61K31/575 , A61K36/18 , A61P25/28 , C07J17/00 , C07J71/00
摘要： PURPOSE:To provide a new alisol having a specific molecular structure, activating the activity of choline acetyltransferase, and useful for cerebral function-improving agents used for the therapy of Alzhemmer's disease, etc., severe amyosthenma-treating medicines, gastrointestinal function improving agents, etc. CONSTITUTION:A new alisol of formula I. A cerebral function-improving agent contains an alisol compound of formula II (R1 to R4 are H, OH, acetyl ; R1 and R3 together form 0) as an active ingredient. The cerebral function-improving agent is compounded with an excipient, a binder, a disintegrator, a surfactant, a lubricant, a flowability- accelerating agent, a flavor, a coloring agent, a perfume, etc., and subsequently prepared into the form of an oral agent such as tablets, capsules, granules, pills or powder, an injection, a suppository, etc. The prepared medicine activates the activity of choline acetyltransferase and is used as a medicine such as a cerebral function-improving agent for treating Alzheimer's disease and Alzheimer type dementia, a therapeutic medicine for severe amyosthenia, a gastrointestin function-improving agent, etc. These compounds are obtained extracting a galenical: Alismatis Rhizoma and, if necessary, subsequently chemically modifying the extract.

7. 发明专利

JPH0532580A NEW LIGNAN AND IMMUNOSUPPRESSIVE AGENT CONTAINING THE SAME LIGNAN AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH0532580A
公开(公告)日：1993-02-09
申请号：JP21141791
申请日：1991-07-30
申请人： TSUMURA & CO
发明人： OKA KITAROU , HAGITANI SACHIKO , WATANABE TOSHIHIKO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： A61K31/12 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/495 , A61P37/06 , C07C49/395 , C07C49/493 , C07C49/753 , C07D295/10 , C07D307/12 , C07D307/30 , C07D307/33 , C07D333/16 , C07D333/18 , C07D333/32 , C07D333/48 , C07D339/08
摘要： PURPOSE:To obtain a new compound, having suppressing action on human lymphocytic proliferation and high safety and useful for treating collagen diseases such as systemic lupus erythematosus or chronic rheumarthritis and autoimmune diseases such as glomerulonephritis, polymyopathy or autoimmune hemolytic anemia. CONSTITUTION:A compound, e.g. trans-3,4-bis(3,4-dimethoxybenzyl) tetrahydrothiophen-2-one expressed by formula I [R1 is H, methyl, acetyl, etc.; R2 is O, S, carbonyl, etc.; R3 and R4 are H, OH, B (B is formula II), etc., except that R1 is H; R2 is O and both R3 and R4 are H, etc.]. The compound expressed by formula I is obtained by subjecting arctigenin contained in Forsythia viridissima Lindl., etc., to reducing, ring opening, brominating, cyclizing, oxidizing, methylating, acetylating, thiololactonizing, dithiolactonizing and esterifying reactions.

8. 发明专利

JPH01228928A LIGNANS AND ANTITUMOR AGENT CONTAINING LIGNANS AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH01228928A
公开(公告)日：1989-09-12
申请号：JP5355088
申请日：1988-03-09
申请人： TSUMURA & CO
发明人： OKA KITAROU , HIRANO TOSHIHIKO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： A61K31/075 , A61K31/045 , A61K31/085 , A61K31/22 , A61K31/34 , A61K31/341 , A61K31/365 , A61P35/00 , C07C41/00 , C07C43/164 , C07C67/00 , C07C69/157 , C07D307/10 , C07D307/32 , C07D307/33
摘要： NEW MATERIAL:Compounds expressed by formulas I-III. EXAMPLE:dl-2,3-Dibenzyl-1,4-dimethoxybutane. USE:An antitumor agent. PREPARATION:Hydrocinnamic acid, 3-methoxyhydrocinnamic acid or 3,4- dimethoxyhydrocinnamic acid is reacted with diisopropylamine, n-butyl-lithium and iodine in tetrahydrofuran to provide a compound expressed by formula IV (R1 and R2 are H or OCH3). The resultant compound expressed by formula IV as a raw material is (i) converted into methyl ester, reduced with hydrogen to form an alcohol derivative or further demethylated or (ii) the above-mentioned alcohol derivative is then converted into the methyl ether, acetylated or intramolecularly etherified. Alternatively, (iii) the afore-mentioned raw material is converted into acid anhydride and then reacted with methanol to provide a monoester derivative, which is subsequently reduced with diborane and then heated to form a lactone derivative or further demethylated to afford the aimed compounds expressed by formulas I-III.

9. 发明专利

JPH05247022A 失效
公开(公告)号：JPH05247022A
公开(公告)日：1993-09-24
申请号：JP19364591
申请日：1991-07-09
申请人： TSUMURA & CO
发明人： NAITO TAKASHI , IKETANI YUKINOBU , YAMAGUCHI TAKUJI , MIHASHI HIROSHI
IPC分类号： A61K31/365 , A61P25/28 , C07D307/88
摘要： PURPOSE:To obtain a new phthalide having choline acetyltransferase activating action and useful as a medicine for brain function improver, etc. CONSTITUTION:A phthalide of formula I (either one of R1 and R2 is formula II and the other is formula III), a phthalide of formula IV, a phthalide of formula IV or a phthalide of formula V. The phthalide is obtained by extracting Cnidii Rhizoma of a crude drug, Cnidium officinale Makino which is its raw plant or other plant belonging to the same genus with a solvent, removing a solvent from the extract and fractionating the residue with chromatography. A phthalide of formula VI (R3 is H or OH; R4 is formula VII or formula VIII or R3 and R4 together form formula VI, formula X, etc.; R5 and R10 are all H or at least a pair of combination of R5 and R10, R6 and R7 and R8 and R9 is bound and others are H or at least a pair of combination of R5 and R6, R7 and R8 and R9 and R10 is bound and others are H), formula XI (R11 is H and R12 is formula VII or R11 and R12 together form formula IX or formula X; R13 is OH or butylyl; R14 is OH or Cl) or formula VII (When R15 is H, R16 are formula VII or R15 and R16 together form formula IX or formula X; R17 is OH or methoxy) is used as a brain function improver.

10. 发明专利

JPH02101011A CARDIOTONIC AGENT 失效
公开(公告)号：JPH02101011A
公开(公告)日：1990-04-12
申请号：JP25000288
申请日：1988-10-05
申请人： TSUMURA & CO
发明人： OKAKI TAROU , HIRANO TOSHIHIKO , NAITO TAKASHI , HOSAKA KUNIO
IPC分类号： A61K31/045 , A61K31/047 , A61K31/075 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/365 , A61P9/04 , C07C39/12 , C07C43/178 , C07C43/23 , C07D307/06 , C07D307/12 , C07D307/33
摘要： PURPOSE:To provide a cardiotonic agent containing lignans as active component. CONSTITUTION:The objective agent contains a compound of formula I (A0, A1 and A2 are OH, H or methoxy; A3 is H, methyl or acetyl (e.g., dl-2,3- dibenzyl-1,4-butanediol), a compound of formula II (B1 is OH, H or methoxy; B2 is H or methyl), a compound of formula III (C1 is H or methoxy) (e.g., trans- dibenzyltetrahydrofuran) or a compound of formula IV (D1 is H or methoxy; D2 is H, OH or methoxy) (e.g., trans-2,3-dibenzyl-lactone) as an active component. The above compounds can be produced from a compound of formula V (R1 and R2 are H or methoxy) produced by reacting hydrocinnamic acid, 3-methoxyhydrocinnamic acid (produced by reducing 3-methoxycinnamic acid) or 3,4-dimethoxyhydrocinnamic acid (produced by reducing 3, 3- dimethoxycinnamic acid) with diisopropylamine, n-butyllithium and iodine in THF.

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