Halogen Bonded Directly To The Aryl Ring Or Ring System Patents (Class 564/345)
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Patent number: 4933370Abstract: The present invention relates, by way of novel industrial products, to 1-(4-aminophenyl)-2-dimethylaminopropanone derivatives which are selected from:(a) the compounds having the general formula ##STR1## in which R is H or CH.sub.3 CO, and (b) addition salts thereof.These products are useful as antidepressants. Furthermore, 1-(4-acetylamino-3,5-dichlorophenyl)-2-dimethylaminopropanone and non-toxic addition salts thereof are useful as immunostimulants.Type: GrantFiled: January 31, 1989Date of Patent: June 12, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4861854Abstract: A photosensitive polyimide precursor composed of the structural units (A) represented by the following general formula (I) and the structural units (B) represented by the following general formula (II), in which the ratio of the molar quantity of the structural units (A) to the sum of the molar quantity of the structural units (A) and that of the structural units (B) is 0.01 or greater, and having a viscosity of 100 cP or above as measured at 25.degree. C. in the state of a 10% by weight solution in N-methylpyrrolidone: ##STR1## wherein R.sub.1 represents a tetravalent aromatic hydrocarbon residue; R.sub.2 represents a divalent aromatic hydrocarbon residue; X, identical or different represents a halogen or an alkyl group; and m represents 0 or an integer from 1 to 4. The photosensitivity of the present photosensitive polyimide precursor is about 20 to 100 times that of conventional products. After heat dehydration cyclization, it shows a heat resistance of 400.degree. C. or above.Type: GrantFiled: June 1, 1988Date of Patent: August 29, 1989Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Akitoshi Sugio, Takao Kawaki, Makoto Kobayashi, Katsushige Hayashi, Masahito Watanabe
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Patent number: 4847256Abstract: Novel compounds having the following structural formula: ##STR1## wherein - - - may represent the presence of a double bond between the C.sub.6 and C.sub.7 position, Ia, or the absence of a double bond between the C.sub.6 and C.sub.7 position, Ib; R.sub.1 is selected from the group consisting essentially of hydrogen, bromo, chloro, carbamoyl, carboxyl, carboxyalkoxyl where alkoxyl is (C.sub.1 -C.sub.3), cyano, --CO--CF.sub.3, COONa, ##STR2## --CO--C(CH.sub.3).sub.3, and ##STR3## where X is hydrogen, cyano, halogen and nitro; R.sub.2, R.sub.4 and R.sub.5 may be hydrogen and lower alkyl (C.sub.1 -C.sub.3); R.sub.3 is hydrogen, alkyl (C.sub.1 -C.sub.3), ##STR4## where R.sub.7 and R.sub.8 may be the same or different and are selected from the group consisting essentially of hydrogen, halogen, alkyl (C.sub.1 -C.sub.3), nitro, alkoxy (C.sub.1 -C.sub.3), trifluoro-methyl, acetylamino or N-alkylacetylamino where alkyl is (C.sub.1 -C.sub.3), and R.sub.Type: GrantFiled: October 16, 1986Date of Patent: July 11, 1989Assignee: American Cyanamid CompanyInventors: Shin S. Tseng, John P. Dusza, Joseph W. Epstein
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Patent number: 4835315Abstract: The present invention relates to new compounds belonging to the family of fluorophenacyl-amine derivates of formula: ##STR1## [wherein A is CO or CHOH and R is CH(CH.sub.3).sub.2 or C(CH.sub.3).sub.3 ] and selected from the group consisting of N-(4-fluorophenacyl)-isopropylamine, N-(2-fluorophenacyl)-tertiarybutylamine, 1-(2-fluorophenyl)-2-tertiarybutylamino-1-ethanol, 1-(4-fluorophenyl)-2-tertiarybutylamino-1-ethanol, and their addition salts, These new derivatives are useful in therapeutics, particularly as anti-aggressive agents, anti-anorexia nervosa agents, sedative agents, and CNS- antidepressants.Type: GrantFiled: July 1, 1987Date of Patent: May 30, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4816489Abstract: The present invention relates to the preparation of new derivatives selected from the group consisting of:(i) 1-(aminophenyl)-2-(alkylamino)ethanones of the formula: ##STR1## in which R is CH(CH.sub.3).sub.2 or C(CH.sub.3).sub.3 ; and (ii) addition salts thereof.These new derivatives are useful in therapy, in particular as antidepressants or stimulants for the CNS. They are prepared from 1-(acetylaminophenyl)-2-(alkylamino)ethanone derivatives by deacetylation.Type: GrantFiled: September 10, 1987Date of Patent: March 28, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4803225Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 2, 1987Date of Patent: February 7, 1989Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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Patent number: 4762829Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.Type: GrantFiled: October 23, 1986Date of Patent: August 9, 1988Assignee: Eisai Co., Ltd.Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
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Patent number: 4749792Abstract: Analgesic activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2 and R.sub.4 are each independently hydrogen, alkyl, carboxyalkyl, halosubstituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl, and R.sub.3 is hydroxymethylene or carbonyl.Type: GrantFiled: September 26, 1984Date of Patent: June 7, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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Patent number: 4742058Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.Type: GrantFiled: July 14, 1986Date of Patent: May 3, 1988Assignee: Eisai Co., Ltd.Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
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Patent number: 4728659Abstract: Disclosed herein are aminomethyl derivatives each of which is of the following general formula (I): ##STR1## wherein A represents a group --C.tbd.C-- or --CH.dbd.CH--, Y represents a group ##STR2## (in which R.sub.3 being a lower alkyl or alkoxy group or a halogen atom) or ##STR3## (in which R.sub.4 being a hydrogen atom or R.sub.3), and R.sub.1 and R.sub.2 represent individually a lower alkyl group, with a proviso that Y is other than the group ##STR4## when A means the group --CH.dbd.CH--, their preparation process and platelet aggregation inhibitors containing same.Type: GrantFiled: June 25, 1985Date of Patent: March 1, 1988Assignee: SS Pharmaceutical Co., Ltd.Inventors: Susumu Sato, Tadayuki Kouda, Tatsuhiko Katori
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Patent number: 4723039Abstract: Phenylacetaldehydes which are substituted by basic groups, of the formula ##STR1## where R.sup.1 to R.sup.8, m and n have the meanings stated in the description, and their preparation are described. The substances are useful for the treatment of disorders.Type: GrantFiled: December 4, 1986Date of Patent: February 2, 1988Assignee: BASF AktiengesellschaftInventors: Werner Seitz, Verena Baldinger, Josef Gries, Dieter Lenke, Manfred Raschack, Klaus Ruebsamen
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Patent number: 4720586Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.Type: GrantFiled: October 18, 1984Date of Patent: January 19, 1988Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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Patent number: 4670535Abstract: The photosensitive polyimide precursor of the invention has a recurring unit represented by the following general formula [I]: ##STR1## (R.sub.1 represents a tetravalent aromatic hydrocarbon residue; R.sub.2 and R.sub.3 each represent a divalent aromatic or aliphatic hydrocarbon residue; and R.sub.4 represents a divalent aromatic hydrocarbon residue represented by ##STR2## wherein R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12, identical or different, each represent hydrogen atom, a halogen group or an alkyl group). The photosensitive polyimide precursor of the invention has a viscosity of 50 centipoises or above as measured at 23.degree. C. in the state of a 10% (by weight) solution in N,N-dimethylacetamide. Its photosensitivity is as high as about 20-100 times that of prior products. After heat cyclization, it exhibits a heat resistance of 400.degree. C. or above.Type: GrantFiled: June 17, 1986Date of Patent: June 2, 1987Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Akitoshi Sugio, Takao Kawaki, Katsushige Hayashi
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Patent number: 4467094Abstract: New derivatives of 1,2-ethylenediamine and salts thereof endowed with vascular antispasmodic and antiallergic activity; processes for preparing them, some new intermediates useful in their preparation and pharmaceutical compositions containing them.Type: GrantFiled: December 3, 1982Date of Patent: August 21, 1984Assignee: Simes S.p.A.Inventors: Cesare Casagrande, Giorgio Ferrari
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Patent number: 4438138Abstract: A method of treatment for reducing cholesterol in humans by the administration of the compound of the formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof in a non-toxic, effective therapeutic amount (calculated as base) to a human in need thereof.Type: GrantFiled: December 6, 1982Date of Patent: March 20, 1984Assignee: Burroughs Wellcome Co.Inventor: Warren C. Stern
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Patent number: 4400380Abstract: Compounds of the formula ##STR1## wherein R is H, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, 3,4-methylenedioxy, CF.sub.3, NO.sub.2, NH.sub.2, N(C.sub.1-4 alkyl).sub.2, CN, OH, --S(C.sub.1-4 alkyl) or --SO.sub.2 (C.sub.1-4 alkyl); R.sub.1 and R.sub.2 are independently each H or C.sub.1-4 alkyl or taken together with the attached N atom are morpholino, piperidino, pyrrolidino, piperazino, or N-- C.sub.1-4 -alkyl piperazino; and, when R is halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, x is 0-3 and, otherwise, is 0 or 1;or a pharmaceutically acceptable salt thereof with an acid or for the compounds wherein R.sub.1 and R.sub.2 are both not H, a quaternary ammonium salt thereof with a C.sub.1-4 alkyl halidehave valuable antiviral activity, e.g., for treatment of infections caused by a herpes virus.Type: GrantFiled: June 22, 1981Date of Patent: August 23, 1983Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Harry W. Ritter, Michael L. Edwards
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Patent number: 4326077Abstract: Novel N-haloacetylphenylamino carbonyl oximes represented by the formula ##STR1## wherein Ar is phenyl or substituted phenyl; R.sup.1 is halomethyl; R.sup.2 and R.sup.3 are each independently hydrogen, alkyl, phenyl, benzyl, substituted phenyl or benzyl, haloalkyl, cyanoalkyl, alkoxyalkyl, alkylthioalkyl or thiocyanoalkyl; R.sup.4 is hydrogen or alkyl; n is 0 or 1; m is 0 or 1; R is hydrogen, alkyl, alkenyl, alkynyl, alkylthioalkyl, haloalkyl, alkoxyalkyl, cyanoalkyl, phenyl, benzyl, substituted phenyl or benzyl, or R is acyl of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, acetonyl, or the group --NR'R" wherein R' and R" are independently hydrogen, alkyl or phenyl; with the proviso that R.sup.2 and R.sup.3 may be joined together to form a carbocyclic ring or a heterocyclic ring; or R and R.sup.2 may be joined together to form a heterocyclic ring; or R and R.sup.3 may be joined together to form a heterocyclic ring.Type: GrantFiled: September 22, 1980Date of Patent: April 20, 1982Assignee: Chevron Research CompanyInventors: William L. Schinski, David C. K. Chan, Irene C. Huang
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Patent number: 4308400Abstract: Aromatic-aliphatic ketones of the formulae I, II, III or IV ##STR1## wherein n is 1 or 2, Ar is an aryl radical, R.sup.1 and R.sup.2 are monvalent aliphatic, cycloaliphatic or araliphatic radicals, R.sup.3 is a direct bond or a divalent organic radical, X is a hydroxyl or amino group or the monovalent etherification or silylation products thereof, and X' is a divalent amino, ether or silyloxy group, Y is a direct bond or CH.sub.2 and Z is O, S, SO.sub.2, CH.sub.2 or C(CH.sub.3).sub.2, are suitable sensitizers for the photopolymerization of unsaturated compounds and for the photochemical crosslinking of polyolefins. Some of these compounds are novel and can be obtained by methods analogous to those for obtaining the known compounds of this type.Type: GrantFiled: December 28, 1979Date of Patent: December 29, 1981Assignee: Ciba-Geigy A.G.Inventors: Louis Felder, Rudolf Kirchmayr, Rinaldo Husler
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Patent number: 4288624Abstract: A process or acylating or sulfenylating 1-amino-2-phenyl-1-butene-3-ones to prepare the corresponding 4-acyl or 4-substituted-thio compounds provides intermediates useful for preparing herbicides.Type: GrantFiled: August 21, 1980Date of Patent: September 8, 1981Assignee: Eli Lilly and CompanyInventors: Riaz F. Abdulla, Lawrence A. Morgan
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Patent number: 4277474Abstract: New propanone derivatives, useful for treating allergic diseases, the pharmacologically allowable salts thereof, their manufacturing process and pharmaceutical composition containing at least one of them as the active ingredient.Type: GrantFiled: September 27, 1979Date of Patent: July 7, 1981Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Akihide Kohda, Teikichi Kurosaki
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Patent number: 4271294Abstract: Compounds of the formula I ##STR1## wherein Ar.sup.1 and Ar.sup.2 represent unsubstituted or substituted phenyl, R.sup.1 represents hydrogen, alkyl, alkoxy, hydroxyalkyl, allyl, benzyl or a group --O--R.sup.2 -NR.sup.3 R.sup.4, R.sup.2 represents alkylene and --NR.sup.3 R.sup.4 is an open chain or cyclic organic amino group, are effective initiators for the photopolymerization of unsaturated compounds or for the photocrosslinking of polyolefins. They can be obtained by different methods which are in themselves known, in particular by reaction of the corresponding haloalkyl ethers or haloalkyl ketals with primary or secondary amines.Type: GrantFiled: March 13, 1980Date of Patent: June 2, 1981Assignee: Ciba-Geigy CorporationInventors: Louis Felder, Rudolf Kirchmayr, Rinaldo Kusler
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Patent number: 4256641Abstract: The preparation of racemic and optically pure tryptophans is described. The D-enantiomers of the 6-substituted compounds possess a potent sweetening capability. Novel intermediates are also disclosed.Type: GrantFiled: July 30, 1979Date of Patent: March 17, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Andrew D. Batcho, Urs O. Hengartner, Willy Leimgruber, John W. Scott, Donald Valentine, Jr.