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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 Substituted 1,3,4-benzotriazepines, a method of preparing the same and theire use as medicaments EP83108291.2 1983-08-23 EP0102580A1 1984-03-14 Martin, Lawrence Leo; Setescak, Linda Louise

This invention relates to substituted-1,3,4-benzotriazepines of the formula wherein X and Y are each independently hydrogen, lower alkyl, halogen, lower alkoxy, nitro and hydroxyl; R1 and R3 are each independently hydrogen or alkyl; R2 is hydrogen, lower alkyl, cycloalkyl lower alkyl, phenyl, aryl lower alkyl, hydroxyl and sulfhydryl; m and n are each independently integers of 0 or 1 and when m is 0, n is 1 and vice-versa; and p and q are independently integers of 1 or 2. Also included in the invention are the substituted-1,3,4-benzotriazepine derivatives of tautomeric form when the substituent for R, and or R3 in the above formula is hvdrogen.

The invention relates further to a process for the preparation of the mentioned compounds and their use as antihypertensive agents.

142 Light-sensitive silver halide color photographic material EP83301537 1983-03-18 EP0089834A3 1984-02-29 Nakagawa, Satoshi; Kida, Shuzi; Sugita, Horoshi; Uemura, Morito; Kishi, Ken-Ichi

There is disclosed a light-sensitive silver halide photographic material containing a compound represented by the formula (1):

Formula (I): wherein G, R1, R2 and X have the same meanings as defined in the specification.

The 1-naphthol coupler which is contained in the light-sensitive silver halide photographic material is high in reactivity with an oxidized product of a color forming developing agent and can efficiently impart imagewise photographic effects to light-sensitive silver halide photographic materials.

143 N-substituted 2-pyridyl indoles, process for their preparation, pharmaceutical compositions containing them, and their therapeutical use EP82110582 1982-11-16 EP0080154A3 1983-09-28 Renfroe, Harris Burt, Dr.
144 N-Substituierte 2-Pyridylindole, Verfahren zu ihrer Herstellung, pharmazeutische Präparate enthaltend diese Verbindungen, sowie ihre therapeutische Verwendung EP82110582.2 1982-11-16 EP0080154A2 1983-06-01 Renfroe, Harris Burt, Dr.

Die Erfindung betrifft Thromboxan-Synthetase hemmende Verbindungen der Formel worin R1 Wasserstoff oder Niederalkyl bedeutet, Ar für unsubstituisrtes oder durch Niederalkyl, Carboxy, Niederalkoxycarbonyl oder Carbamoyl substituiertes Pyridyl steht, R2 und R3 unabhängig voneinander Wasserstoff, Niederalkyl, Halogen, Trifluormethy!, Hydroxy, Nlederalkoxy, Carboxyniederalkyl, Niederafkoxycarbonyl-niederalkyl, Carboxy, Niederalkoxycarbonyl oder Nlederalkyl-(thio, sulfinyl oder sulfonyl) bedeutet, oder R2 und R3 zusammen, an benachbarten Kohlenstoffatomen, für Nlederalkylendioxy stehen; A für Alkylen mit 1 bis 12 Kohlenstoffatomen, Alkenylen mit 2 bis 12 Kohlenstoffatomen, Alkynylen mit 2 bis 12 Kohlenstoffatomen, Niederalkylen-phenylen-niederafkylen, Nisderatkylen-phenylen, Phenylen-niederalkylen, Phenylen, eine direkte Bindung, Niederalkylen-(thio oder oxy)-niederalkylen, (Thio oder Oxy)-phenylen, Niederalkylen-(thio oder oxy)-phenylen, Phenylen-(thio oder oxy)-niederalkylen oder Phenylen-niederalkenylen steht, B Carboxy, Niederalkoxycarbonyl, Carbamoyl, Mono- oder Di-niederalkyl-carbamoyl, Hydroxymethyl, Hydroxycarbamoyl, 5-Tetrazolyl oder Formyl bedeutet; ihre N-Oxide; und ihre Salze, insbesondere ihre therapeutisch verwendbaren Salze. Sie können z.B. durch Ringschluß von Verbindungen der Formel erhalten werden.

145 Propionsäureamide, Herstellung dieser Verbindungen, Unkrautbekämpfungsmittel, die diese Verbindungen als Wirkstoffe enthalten, sowie Verwendung solcher Verbindungen und Mittel zur Bekämpfung von Unkräutern EP82104524.2 1982-05-24 EP0065780A2 1982-12-01 Fráter, Georg, Dr.; Suchy, Milos, Dr.; Wenger, Jean, Dr.; Winternitz, Paul, Dr.

Die Erfindung betrifft Propionsäureamide der Formel worin R1, R2 und R die in der Beschreibung angegebenen Bedeutungen besitzen, Verfahren zu deren Herstellung, Unkrautbekämpfungsmittel, die diese Verbindungen als Wirkstoffe enthalten, sowie die Verwendung solcher Verbindungen bzw. Mittel zur Bekämpfung von Unkräutern.

146 Optisch aktive alpha-Phenoxypropionsäure Derivate EP78101792.6 1978-12-20 EP0002800B1 1981-12-02 Nestler, Hans Jürgen, Dr.; Hörlein, Gerhard, Dr.; Handte, Reinhard, Dr.; Bieringer, Hermann, Dr.; Schwerdtle, Friedhelm, Dr.; Langelüddeke, Peter, Dr.; Frisch, Peter, Dr.
147 New pyrrolobenzotriazepines, their production and pharmaceutical compositions containing them EP80107903.9 1980-12-15 EP0031115A1 1981-07-01 Fischer, Rudolf, Dr.; Künzle, Franz Martin; Schmutz, Jean, Dr.

Compound of formula l, wherein

  • R, and R. are each hydrogen, halogen, alkyl, alkoxy, alkylthio or trifluoromethyl,
  • R2 is hydrogen, alkyl, hydroxyalkyl or a physiologically acceptable hydrolyzable esterthereof, and
  • R3 is hydrogen, alkyl, alkenyl or benzyl, or an acid addition salt thereof, are useful as neuroleptics, anti-depressants or soporifics.

148 New peptides, processes for their preparation and pharmaceutical compositions containing them EP80106143 1980-10-09 EP0027260A3 1981-06-03 Kitaura, Yoshihiko; Nakaguchi, Osamu; Hemmi, Keiji; Aratani, Matsuhiko; Takeno, Hidekazu; Okada, Satoshi; Tanaka, Hirokazu; Hashimoto, Masashi

A compound of the formula or its pharmaceutically acceptable salt:

  • wherein R1 is hydrogen or acyl;
  • R2 is carboxy or protected carboxy or a group of the formula:
    • -COHN-R2 wherein R2a is carboxy(lower)alkyl or protected carboxy(lower)alkyl;
  • R3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl ora graup oftheformula: R3a-CH-R3b wherein R3a is hydrogen, amino, protected amino or a cylamino, R3b is carboxy or protected carboxy;
  • RPis carboxy, protected carboxy, carbamoyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl; ℓ isaninteger0or2, m is an integer 0 to 3 and n is an integer 0 to 1, with certain provisions, and pharmaceutically acceptable salts thereof and process for their preparation, and also a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.

149 Tetrahydro-fluorene compounds, processes for their preparation and pharmaceutical compositions thereof EP80106232.4 1980-10-14 EP0027948A1 1981-05-06 Cragoe, Edward J., Jr.; Stokker, Gerald E.; Gould, Norman P.

The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkanoic and cycloalkanoic acid esters, analogs, the parent acids and their salts, and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

150 N-(Alpha-Chlorpropionyl)-1,2,3,4-tetrahydro-chinaldin, Verfahren zu dessen Herstellung und dessen Verwendung als Gegenmittel zum Schutz von Kulturpflanzen vor Schädigungen durch Herbizide EP80104059.3 1980-07-14 EP0023306A1 1981-02-04 Riebel, Hans-Jochem, Dr.; Eue, Ludwig, Dr.; Faust, Wilfried, Dr.

N-(a -Chlorpropionyl)-1,2,3,4 -tetrahydro-chinaldin der Formel ein Verfahren zu dessen Herstellung sowie dessen Verwendung als Gegenmittel zum Schutz von Kulturpflanzen vor Herbizidschaden.

Herbizide Wirkstoffkombinationen auf Basis von N-(a-Chloropropionyl) -1,2,3,4-tetrahydro-chinaldin und herbizid wirksamen Thiocarbamaten bzw. Acetaniliden.

151 N-AZOLYLALKYL-HALOGENOACETANILIDES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES EP79100240 1979-01-29 EP0003539A3 1979-09-05 STETTER, JORG, DR.; DRABER, WILFRIED, DR.; THOMAS, RUDOLF, DR.; EUE, LUDWIG, DR.; SCHMIDT, ROBERT RUDOLF, DR.; LUNKENHEIMER, WINFRIED, DR.
152 Methyladamantyl hydrazines, their pharmaceutically acceptable salts and pharmaceutical compositions containing them EP78101411.3 1978-11-20 EP0002065A1 1979-05-30 Weiner, Ben-Zion; Suchi, Raul; Sterling, Jeffrey; Yellin, Haim

The invention provides novel 1- or 2-adamantylmethyl hydrazines of the general formulaA

In this formula Ad is 1- or 2-adamantyl, R1 and R2 are the same or different and are each hydrogen or a lower unsubstituted or substituted alkyl group of 1-4 carbon atoms; R, and R4 are the same or different and are each hydrogen, an unsubstituted or substituted radical being a lower alkyl group of 1-4 carbon atoms, a lower alkanoic acid radical of 2-4 carbon atoms or a lower alkyl ester thereof, adamantyl, aryl, aralkyl in which the alkyl moiety has 1-4 carbon atoms or an unsubstituted or substituted heterocyclic radical of aromatic character; or R3 and R4 together with the nitrogen atom to which they are attached form a cyclic radical of non-aromatic character.

The invention further provides pharmaceutically acceptable acid addition salts of the above compounds.

Several methods of preparation of the new compounds are described.

The novel compounds according to the invention possess valuable antifungal (human and plant), antiviral, antiprotozoal and antimicrobial properties.

153 5,8-dichloro--1,4,9,10- anthracene Tetoron JP16678094 1994-07-19 JPH07110829B2 1995-11-29 HAWAADO DANIERU HORISU SHOOORUTAA; JUUDEISU ERU JONSON; REZURII EMU WAABERU; EDOWAADO EFU ERUSURAAGAA
154 JPH0339482B2 - JP18361284 1984-09-01 JPH0339482B2 1991-06-14 RICHAADO BII ROJAASU; BII KURIFUOODO GAAUITSUKU ZA SAADO
155 New hydrazine derivative JP15561290 1990-06-15 JPH03115255A 1991-05-16 HANSUYURUKU BUETSUTAA; PEETAA BAUMAISUTAA; PAURU RADEIMERUSUKII; PIEERU MARUTEIN
NEW MATERIAL: A hydrazine derivative of formula I or II (where R=H, CHO, COR', COOR', CONH 2; R' = a 1-4C alkyl, benzyl, phenyl) or a salt of a compd. of formula II (where R=H) and an org. or inorg. acid. EXAMPLE: 1-[2-(2,4-Dichlorophenyl)pentylidene]-2-acetylhydrazine. USE: A synthesis intermediate of 1-[2-(2,4-dichlorophenyl) pentyl]-1H-1,2,4-triazole useful as an bactericide. PROCESS: A compd. of formula I is obtd. by reacting 2-(2,4-dichlorophenyl)- valeronitrile with a hydrazine of formula III under the existence of H, an acid and a catalyst for hydrogenation. A compd. of formula II is obtd. by catalytically hydrogenating a compd. of formula I. COPYRIGHT: (C)1991,JPO
156 JPH0331248B2 - JP14609783 1983-08-10 JPH0331248B2 1991-05-02 KOBAYASHI HIDETOSHI; OBAYASHI KEIJI
157 JPH0327560B2 - JP5443588 1988-03-08 JPH0327560B2 1991-04-16 KURODA YOSHIO; IGUCHI HIDEKO; KOSAKA MASANOBU; AOKI HATSUO; IMANAKA HIROSHI; KITAURA YOSHIHIKO; NAKAGUCHI OSAMU; HENMI KEIJI; ARAYA MATSUHIKO; TAKENO SHUICHI; OKADA TATSU; TANAKA HIROKAZU; HASHIMOTO SHINJI
This invention relates to the new peptides of the general formula: More particularly, this invention relates to this new peptide and the pharmaceutically acceptable salt thereof, which have pharmacological activities, to processes for the preparation thereof and to a new intermediate for preparing the active peptide, and to the pharmaceutical composition comprising the same and a method of use thereof.
158 4-pyridone-3-carboxylic acid and its derivative JP18089 1989-01-05 JPH02117664A 1990-05-02 KURAUSU GUROE; HANSUUYOAHIMU TSUAIRAA; KAARU GEORUKU METSUTSUGAA
NEW MATERIAL: A 4-pyridone-3-carboxylic acid and/or its derivative of formula I (wherein R 1a is a t-alkyl, a cycloalkyl or the like; R 2 is H, an alkyl, an aralkyl or an aromatic; R 3a is carboxyl, A, B and D are carbon atoms, A is N, B, D and E are carbon atoms, D is N, A, B and E are carbon atoms, A and B are N atoms, D and E are C atoms, and E is a C atom or the like) and salts thereof. EXAMPLE: Ethyl 1,2,7-trimethyl-4-oxo-1,8-naphthyridine-3-carboxylate. USE: An antifungel agent and a feed additive. PREPARATION: For example, an enamine of formula II (wherein R 1 is an alkylene, a cycloalkyl or the like; R 2 is H, an alkyl, an aralkyl or the like; and R 3 is a derivative of carboxyl) is reacted with a compound of formula III (wherein X 1 and X 2 are each a halogen) to obtain a compound of formula I. COPYRIGHT: (C)1990,JPO
159 JPH0152742B2 - JP4580982 1982-03-20 JPH0152742B2 1989-11-09 NAKAGAWA SATOSHI; SUGITA HIROSHI; KIDA SHUJI; UEMURA MORITO; KUZUMI KENICHI
160 4-pyridone-3-carboxylic acid derivative JP18189 1989-01-05 JPH01246265A 1989-10-02 KURAUSU GUROE; HANSUUYOAHIMU TSUAIRAA; KAARU GEORUKU METSUTSUGAA
NEW MATERIAL: A compd. of formula I (0 to 3 pieces of A to E are N and the rest are (substd.) carbon atoms) and its salt. EXAMPLE: 1-Cycropropyl-7-methyl-4-oxo-1,8-naphthylidine-3-carboxylic acid. USE: An antimicrobial agent, fungicidal agent and growth regulator usable also as a feed additive. PROCESS: A compd. of formula I is obtd. by bringing the compd. of the formula I (R 1 is cyclopropyl; R 2 is H, alkyl, aralkyl or aryl; R 3 is a deriv. of COOH, more preferably COOR 6 or CONR 7R 8; R 6 to R 8 are each 1-4C alkyl, further, R 7 to R 8 are each H, R 8 is (substd.) phenyl) and compd. formula II (X 1 and X 2 are each halogen) into reaction at 0 to 80°C in the presence of a base in an absolute proton solvent in a first reaction step and at 80 to 250°C in the presence of a base in a second reaction step, then changing R 3 to COOH. COPYRIGHT: (C)1989,JPO
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