| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | Production of optically active (s)-(-) and (r)-(+)-deoxyspergulain and its new intermediate | JP25425396 | 1996-09-26 | JPH09110822A | 1997-04-28 | SHIYUEBAO WAN; JIYON KEI SOTSUTASHIRU |
| PROBLEM TO BE SOLVED: To obtain a compound having antitumor activity and other various bioactivities and pharmacological activities. SOLUTION: Deoxyspergualin as the objective compound and expressed by formula I can be existed as (S)-(-) and (R)-(+)-deoxyspergualin and a systematic name is N-[4-(3-aminopropyl)aminobutyl]-2-substituted ethanamide. The compound of the formula I is obtained by reacting a compound of formula II (R and R 1 are each a nitrogen protecting group such as benzyloxycarbonyl or t-butoxycarbonyl(BOC)) with a compound of formula III (R 2 and R 3 are each a nitrogen protecting group such as benzyloxycarbonyl or BOC) in an organic solvent such as methylene chloride in the presence of a condensing agent such as propyl phosphonate anhydride/a dehydrating agent and a base such as triethylamine to obtain a compound of formula IV, then de-protecting and hydrocracking the resultant compound. COPYRIGHT: (C)1997,JPO | ||||||
| 142 | New halo-lower alkyl guanidino substituted amino acid compounds and their preparation | JP25464985 | 1985-11-12 | JP2542362B2 | 1996-10-09 | JON JOSEFU NESUTAA; BURAIAN HENRII BITSUKARII |
| 143 | Perfluoroalkyl-substituted benzolyguanidines, their preparation, their use as medicament or diagnostic agent, and medicament containing the same | JP11418895 | 1995-05-12 | JPH07304729A | 1995-11-21 | HAINTSUUBUERUNAA KUREEMAN; HANSUUYOOHEN RANGU; YANNROOBERUTO SHIYUBUARUKU; ANDOREEASU BUAIHIERUTO; BUORUFUGANGU SHIYORUTSU; UUDOO ARUBUSU |
| PURPOSE: To obtain the subject new compounds extremely suitable as an antiarrhythmic formulation having a cardioprotective component for prevention of infarction, treatment of infarction and treatment of angina pectoris. CONSTITUTION: The compound of formula I [R(1) is R(6)-SO m {R(6) is a 1-6C perfluoroalkyl; (m) is 0-2}; R(2) and R(3) are each H, a halogen, a 1-4C alkyl, a 1-4C alkoxy, a substitutable phenoxy or a substitutable 1-, 2- or 3-pyrolyl; R(4) and R(5) are each H, a 1-3C alkyl, a halogen, CN, OR(7), NR(8)R(9) {R(7) to R(9) are each H or a 1-4C alkyl} or -(CH 2) n-(CF 2) o-CF 3 {(n) is 0 or 1; (o) is 0-2}] or its salt, e.g. 4-(4-fluorophenoxy)-3- trifluoromethylsulfonylbenzoylguanidine. The compound is obtained by reacting a compound of formula II (L is a leaving group) with guanidine and is suitable for preparing a chemical tool for an inhibitor of Na +/H + exchanger in a diagnosis of hypertension and productive disease. COPYRIGHT: (C)1995,JPO | ||||||
| 144 | Phenyl-substituted alkylcarboguanidide having perfluoroalkyl group and preparation thereof | JP871595 | 1995-01-24 | JPH07224022A | 1995-08-22 | YANNROOBERUTO SHIYUBUARUKU; HAINTSUUBUERUNAA KUREEMAN; HANSUUYOOHEN RANGU; ANDOREEASU BUAIHIERUTO; BUORUFUGANGU SHIYORUTSU; UUDOO ARUBUSU |
| PURPOSE: To provide a novel phenyl-substd. alkylcarboguanidide having a perfluoroalkyl group suppressing an Na +/H + exchange mechanism of cells and effective against all of diseases developed by ischemia. CONSTITUTION: This compd. is represented by formula I [wherein R(A) is H, F, Cl, Br, I, CN, OR(6) (wherein R(6) is H, alkyl, alkenyl, cycloalkyl, phenyl or benzyl), alkyl, cycloalkyl, Or(CH 2) aC bF 2b+1 (wherein (r) is 0 or 1; (a) is 0-4; and (b) is 1-8) or the like; R(B) is same to R(A); (x) is 1-3; R(1) is H, alkyl, -O t(CH 2) dC eF 2e+1 (wherein (t) is 0 or 1; (d) is 0-4; (e) is 1-8) or the like; and R(2)-R(5) are same to R(1)] or a salt thereof, for example 3-(3- trifluoromethylphenyl)propionoguanidide. The compd. represented by formula I is obtained by reacting a compd. represented by formula II (wherein L is an easily uncleophilically substituted group to be removed) with a guanidine and useful as a remedy for arrhythmia, myocardial infarction, angina pectoris, ischemic symptoms or the like. COPYRIGHT: (C)1995,JPO | ||||||
| 145 | Sulfonamidocarboxamides | JP6908093 | 1993-03-05 | JPH0625195A | 1994-02-01 | JIYAN ATSUKAAMAN; DEIBITSUDO BANNAA; KURAUSU GUBERUNATOORU; KURUTO HIRUPAATO; JIERAARU SHIYUMITSUTO |
| PURPOSE: To provide the subject compounds comprising sulfonamidocarboxamides containing a nitrogen-containing heterocycle, which have an ability to inhibit thrombin-induced blood platelet aggregation and coagulation of fibrinogen in plasma and are useful for controlling thrombosis, cardiac failure, arteriosclerosis or the like. CONSTITUTION: The objective sulfonamidocarboxamides of formula VII are prepared by reacting sec. amine compounds of formula I (R 3 is H, a lower alkyl, lower alkenyl, aryl or the like; R 4 is H, a lower alkyl, aryl or the like; R 5 is H, a lower alkyl, COOH or the like) with carboxylic acid compounds of formula II (Boc is t-butyloxycarbonyl; t-Bn is t-butyl; Y is H, CH 2COOH or the like) to obtain amide-compounds of formula III, then subjecting the amide- compounds to sulfonation reaction and hydrolysis to obtain carboxylic acid compounds of formula IV (A is an aryl, heteroaryl or alkyl; M is a group of formula V), further reacting the resulting carboxylic acid compounds with the compounds of formula Q-NHX (Q is H, a lower alkyl or the like; X is a group of formula VI (T is CH 2 or O; R 1, R 2 are each H, a COO-lower alkyl) or the like]. COPYRIGHT: (C)1994,JPO | ||||||
| 146 | Production of aluminate of guanidine compound | JP10700692 | 1992-04-24 | JPH05306263A | 1993-11-19 | YOSHIYAMA TETSUO |
| PURPOSE: To produce the subject compound of high purity, useful as a raw material of aluminum nitride with a simple operation in a relatively short time by reacting a guanidine compound with an aluminum alcoholate. CONSTITUTION: The subject compound can be obtained by reacting a compound of the formula (R 1 to R 4 are each H, an alkyl, an aryl, an alkylaryl or a hydroxyalkyl. R 1 may be amino) with an organoaluminum compound in an organic solvent (e.g. isopropyl alcohol) at room temperature to 100°C for several min to several hr. The guanidine compound is used in an amount of ≥ an equivalent weight to aluminum, preferably more than 50% in excess of the equivalent weight. The subject compound is obtained in the form of fine powder and a remarkably high-purity substance can be obtained in comparison with that obtained by the aqueous solvent method. COPYRIGHT: (C)1993,JPO&Japio | ||||||
| 147 | Production of nitroguanidine derivative, its intermediate and its production | JP13080591 | 1991-03-22 | JPH05112521A | 1993-05-07 | AOKI ISAO; MINAMIDA ISAO |
| PURPOSE:To obtain a general production method capable of industrially producing from a new intermediate a nitroguanidine derivative especially having a safe and advantageous property as an agricultural insect pest control agent, useful in the fields of medicines and agricultural chemicals. CONSTITUTION:A new compound of formula I (A is 2-4C alkylene capable of having a substituent; G is O, S; L is electron-attracting group) or its salt us reacted with a compound of formula II [R1, R2 are H, hydrocarbon group capable of having a substituent; further R<2> is (CH2)Y, NR<1a>, cyclic amino group; Y is cyclic hydrocarbon capable of having a substituent, 5 or 6-membered heterocyclic group (capable of having a substituent) containing one to three hetero atoms (N, 0, S); m is 1 or 2] its salt to obtain a compound of formula III or its salt. The compound of formula III or its salt is, if necessary, acylated when R1 is H, and subsequently reacted with a compound of formula IV (R<3> is each group of R<1a>; R<4> is each group of R<2>) or its salt to obtain a compound of formula V (R<1> us R<1a>, acyl) or its salt. | ||||||
| 148 | Production of nitroguanidine derivative | JP30396091 | 1991-10-23 | JPH04330049A | 1992-11-18 | PEETAA MAIENFUITSUSHIYU; OTSUDO KURISUCHIYANSEN; RAURENTSU GUSEERU |
| PURPOSE: To obtain a nitroguanidine deriv. which is an effective component to prevent and exterminate harmful organisms by hydrolysis of 2-nitroimino-1,3,5- triazacyclohexane. CONSTITUTION: A compd. expressed by formula I is hydrolyzed in a water-acid medium at normal pressure at 0 to 120°C, preferably 20 to 80°C to obtain a compd. expressed by formula II such as 1-(2-chloropyridi-5-ylmethyl)-2-nitro-3-n- propylguanidine. In formula I, R 1 is H, a 1 to 4 C alkyl; R 2 is a 1 to 6 C alkyl, a 3 to 6 C cycloalkyl, CH 2B (B is phenyl, 3-pyridyl, 5-thiazolyl which may have substituents); R 3 is a 1 to 10 C alkyl, a 3 to 6 C cycloalkyl, phenyl, benzyl; A is an aromatic or nonaromatic monocyclic or bicyclic heterocyclic functional group which may have substituents. COPYRIGHT: (C)1992,JPO | ||||||
| 149 | Benzoylguanidine, its production and medicament containing it | JP23344490 | 1990-09-05 | JPH03106858A | 1991-05-07 | HAINRITSUHI KURISUTEIAN ENGURE; HANSUUYOHEN RANGU; BUORUFUGANGU RINTSU; BERUNBUARUTO SHIERUKENSU; BUORUFUGANGU SHIYORUTSU |
| NEW MATERIAL: A benzoylguanidine of formula I [R(1) and R(2) are each R(6)-S(O) n, formula II, H, F, Cl, C 1-4 alkyl, etc.; R(6) is C 1-6 alkyl, C 5-7 cycloalkyl, cyclopentylmethyl, etc.; R(7) and R(8) are each H, C 1-6 alkyl, etc., or R(7) and R(8) when taken together may form a straight or branched C 4-C 7 chain, etc.; R(3)-R(5) are each H or C 1-2 alkyl, or R(3) and R(4) when taken together may form a (C 2-C 4) alkylene chain, or R(4) and R(5) when taken together may form a (C 4-C 7) alkylene chain; n is 0-2]. EXAMPLE: 3-Methylsulfonyl-4-(1-piperidinyl)benzoylguanidine. USE: Treatment or prophylaxis of myocardial infarction, angina pectoris, arrhythmia, and cardiac ischemia disease. PROCESS: The compound of formula I is obtained by reacting a compound of formula III with a compound of formula IV. COPYRIGHT: (C)1991,JPO | ||||||
| 150 | Aryl cyanoguanidines being potassium channel activator and production thereof | JP20658289 | 1989-08-09 | JPH0291057A | 1990-03-30 | KAANEIRU ESU ATSUUORU; JIYON AARU MATSUKAROU; GEIRII JIEI GUROOBAA |
| NEW MATERIAL: A compd. represented by formula I (wherein R 1 is alkyl, alkenyl or alkynyl; R 2 is -C≡N, -NO 2 or -CF 3; and R 3 and R 4 are each -R 2, H, alkyl, alkenyl, alkynyl or alkoxy), its tautomer and salt. EXAMPLE: 4-[[(Cyanoimino) [(1,2,2,-trimethylpropyl) amino]methyl]amino]benzonitrile. USE: A potassium channel activator and an anti-artial fibrillation agent. This new material is low in heart action and useful for treating hypertension. PROCESS: An isocyanate represented by formula II and cyanamide represented by the formula, M +NH-C=N (M + is an alkali metal) are reacted to obtain a thiourea compd. represented by formula III. Subsequently, this compd. is reacted with an alkylating agent (e.g. methyl iodide) and further reacted with a compd. represented by the formula, NH 2-R 1 to obtain the compd. represented by formula I. COPYRIGHT: (C)1990,JPO | ||||||
| 151 | JPH027564B2 - | JP3397884 | 1984-02-24 | JPH027564B2 | 1990-02-19 | YOSHIOKA NOBUYUKI; HACHIKURA KOJI; MIURA YASUNAO; MORI YOSHIKAZU; ADACHI EIICHI; KATAOKA YASUKATSU |
| 152 | Production of 4-guanidinomethylcyclohexanecarboxylic acid | JP9202589 | 1989-04-13 | JPH026459A | 1990-01-10 | SHIYUTEFUAN UAITSUSU; HERUMUUTO KUROMUMERU |
| PURPOSE: To obtain a compound useful as a medicine in a high purity and high yields in a nonpolluting advantageous manner by reacting 3aminomethylcyclohexanecarboxylic acid with an O-alkylisourea derivative in a polar protonic solvent. CONSTITUTION: 1 mol. of 4-aminomethylcyclohexanecarboxylic acid is reacted with at least 1 mol. of an O-alkylisourea derivative (e.g. Oalkylisourea salt) at 10-50°C desirably in the presence of a base (e.g. NaOH) in a solvent (e.g. methanol) to obtain the purpose product. This product has antihistaminic action, an antiulcer action, an antiallergic action, an anti-inflammatory action and a proteolytic enzyme inhibiting action. COPYRIGHT: (C)1990,JPO | ||||||
| 153 | Selective amidination of diamines | JP22624187 | 1987-09-09 | JPS6388166A | 1988-04-19 | ARZENO HUMBERTO B; MORGANS DAVID J JR |
| 154 | Nona- and decapeptide as lhrh antagonist | JP25464985 | 1985-11-12 | JPS61122297A | 1986-06-10 | NESTOR JOHN JOSEPH; VICKERY BRIAN HENRY |
| 155 | Adduct of omega-guanidino-fatty acid amide and glyoxylic acid, and its preparation | JP3429884 | 1984-02-27 | JPS60178852A | 1985-09-12 | UMEDA YOSHIHISA; MORIGUCHI MAKOTO; IGAI KATSUSHIGE; NAKAMURA TERUYA; FUJII AKIO; TAKEUCHI TOMIO; UMEZAWA HAMAO |
| NEW MATERIAL:The compound of formula I (n is 6W8; R 1 is H, lower alkyl or benzyl), and its salt. EXAMPLE: (±)-N-(7-Guanidinoheptanoyl)-α-hydroxyglycine. USE: A synthetic intermediate of carcinostatic agent. PREPARATION: The objective compound of e.g. formula IV can be prepared by the dehydrative condensation of the ω-guanidinofatty acid amide of formula IIwith glycoxylic acid of formula III. The compound of formula IV can be converted to the chemically stable compound of formula V by the O-alkylation of the 2-hydroxyl group. When a spergualin-relating compound is synthesized via the compound of formula V, it is not necessary to protect and deprotect the highly reactive aldehyde group of the glyoxylic acid, and the group can be converted rapidly to a functional group having high chemical stability and poor reactivity. An optically active compound which has been difficult to resolve optically, can be synthesized relatively easily by this method. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 156 | JPS5934163B2 - | JP1597077 | 1977-02-15 | JPS5934163B2 | 1984-08-21 | EGUCHI TAMYUKI; MORI SEIICHI; SHIMOKAWA MASAAKI |
| 157 | (-)-15-deoxyspergualin, its preparation and its intermediate | JP8139882 | 1982-05-17 | JPS58198455A | 1983-11-18 | UMEZAWA HAMAO; TAKEUCHI TOMIO; KONDOU SHINICHI |
| NEW MATERIAL:The (-)-15-deoxyspergualin of formula I and its salt. USE: Carcinostatic agent having excellent carcinostatic activity compared with 15-deoxyspergualin. PROCESS: The compound of formula I is prepared by deoxidizing the 15-position OH group of the (-)-spergualin derivative of formula II (R 1 is protected amino; R 2 and R 3 are protecting group), and then removing the protecting groups. The deoxidization at the 15-position can be achieved by conventional process, e.g. by converting the 15-position OH group to sulfonic acid ester by a sulfonylation agent (e.g. methanesulfonyl chloride), treating the product with a halogenating agent (e.g. NaI) in a solvent to obtain a 15-iodized or brominated derivative, and dehalogenating the derivative by the catalytic reduction in the presence of Pd or Pt catalyst. COPYRIGHT: (C)1983,JPO&Japio | ||||||
| 158 | Chlorhexidinedinaploxenate derivative, manufacture and antiinflammatory, bactericide and antibacterial | JP17246782 | 1982-09-29 | JPS5899458A | 1983-06-13 | REONARU DE BINCHIENTEIISU |
| 159 | JPS5745737B2 - | JP3267774 | 1974-03-25 | JPS5745737B2 | 1982-09-29 | |
| 160 | Manufacture of guanidine-hydrochloride | JP2560881 | 1981-02-25 | JPS56133255A | 1981-10-19 | PEETAA SHIYARUKE; MANFUREETO RANGAA; KURAUSU FUUTOMATSUHAA |
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