Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
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Patent number: 5354904Abstract: The sulfonamides have the formula ##STR1## where R.sup.1 is C.sub.1 -C.sub.13 -lkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.8 -alkanoyl or substituted or unsubstituted benzoyl, andR.sup.2 and R.sup.3 are each independently of one another substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted piperidinyt, or R.sup.2 may also be hydrogen.Type: GrantFiled: October 8, 1992Date of Patent: October 11, 1994Assignee: BASF AktiengesellschaftInventors: Udo Mayer, Ulrike Schloesser
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5302720Abstract: Compounds of formula I ##STR1## and their salts in which R.sub.1 is optionally substituted phenyl, R.sub.2 is alkyl, cycloalkyl or optionally substituted amino, or R.sub.2 and R.sub.3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R.sub.5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O).sub.m R.sub.8 in which m is 0, 1 or 2 and R.sub.8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.Type: GrantFiled: June 17, 1992Date of Patent: April 12, 1994Assignee: The Boots CompanyInventor: Balasubramanian Gopalan
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Patent number: 5283362Abstract: Process for the preparation of very pure ureas of the formula phenyl--(NH--CO--NR.sub.1 R.sub.2).sub.n in which phenyl represents an unsubstituted or substituted phenyl or phenylene group and R.sub.1 and R.sub.2 are either identical and each represent an alkyl group, or are different, in which case R.sub.1 represents a hydrogen atom and R.sub.2 represents an alkyl or phenyl group, or R.sub.1 and R.sub.2, together with the nitrogen atom, represent an aliphatic heterocyclic ring and n is the number 1 or 2, by reacting a phenylurea of the formula phenyl--(NH--CO--NH.sub.2).sub.n with an amine of the formula NR.sub.1 R.sub.2 H at temperatures from 100 to 200.degree. C. in a diluent which is inert under the reaction conditions, the reaction being interrupted before by-products are formed, and the urea which is formed being removed from the starting compounds, and the unreacted starting compounds being returned to the process if appropriate.Type: GrantFiled: July 31, 1992Date of Patent: February 1, 1994Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Heinz Falk
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Patent number: 5268373Abstract: This invention relates to new heterocyclic derivatives of guanidine and more particularly to such derivatives which have hypoglycemic activity, their methods of use for treating hyperglycemia and novel intermediate compounds for their preparation.Type: GrantFiled: July 28, 1992Date of Patent: December 7, 1993Assignee: McNeilab, Inc.Inventors: Henry J. Breslin, Michael J. Kukla, Chris R. Rasmussen, Robert W. Tuman
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Patent number: 5242919Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halgoen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: June 13, 1991Date of Patent: September 7, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 5234934Abstract: The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.Type: GrantFiled: April 30, 1992Date of Patent: August 10, 1993Assignee: Egis GyogyszergyarInventors: Zoltan Budai, Klara Reiter nee Esses, Eniko Sziri nee Kiszelly, Gizella Zsila, Gabor Gigler, Lujza Petocz, Maria Szecsey nee Hegedus, Marton Fekete, Valeria Hoffmann, Laszlo Kapolnai
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Patent number: 5223498Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.Type: GrantFiled: December 28, 1989Date of Patent: June 29, 1993Assignee: The Boots Company plcInventor: Balasubramanian Gopalan
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Patent number: 5220023Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: April 10, 1992Date of Patent: June 15, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5216153Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, halogen or OR.sup.5 ; R.sup.2 is hydrogen, lower-alkyl lower-alkoxy or halogen; R.sup.3 and R.sup.4 each independently are lower-alkyl or taken together are alkylene with 3-5 C atoms in a straight-chain; R.sup.5 is hydrogen, acyl, lower-alkoxycarbonyl, lower-alkyl, amino-lower-alkyl, mono-alkylamino-lower-alkyl di-alkylamino-lower-alkyl or a N-containing 5-8-membered saturated or unsaturated monocyclic heterocyclic ring which is attached via a N atom to lower alkyl; and M signifies --CONH-- or --NHCO--, which can be used as medicaments, e.g., for the treatment of neoplasms and dermatological indications of an inflammatory and allergic nature.Type: GrantFiled: March 17, 1992Date of Patent: June 1, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5194608Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.Type: GrantFiled: June 24, 1991Date of Patent: March 16, 1993Assignee: Shionogi & Co., Ltd.Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
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Patent number: 5188950Abstract: Novel dipeptide isosteres are the biotransformed products after incubation with rat liver slices. They inhibit HIV protease, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: February 27, 1992Date of Patent: February 23, 1993Assignee: Merck & Co., Inc.Inventors: Suresh K. Balani, Harri G. Ramjit, Steven M. Pitzenberger, Michael S. Schwartz, Anthony Y. H. Lu
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Patent number: 5185334Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.Type: GrantFiled: September 6, 1991Date of Patent: February 9, 1993Assignee: Schering CorporationInventors: Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
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Patent number: 5169952Abstract: An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.Type: GrantFiled: July 2, 1991Date of Patent: December 8, 1992Assignee: Merck & Co., Inc.Inventors: David Askin, Ralph Volante, Michael Wallace, Ichiro Shinkai
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Patent number: 5153226Abstract: The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.Type: GrantFiled: July 30, 1990Date of Patent: October 6, 1992Assignee: Warner-Lambert CompanyInventors: Alexander W. Chucholowski, Mark W. Creswell, William H. Roark, Ila Sircar
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Patent number: 5141937Abstract: Pharmaceutical products containing a 7-diphenylmethylenebicycloheptane or 7-diphenylmethylenebicycloheptene derivative of the formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, or a physiologically tolerated acid addition salt of these compounds, and the use thereof as hypolipidemics are described. In addition, new 7-diphenylmethylenebicycloheptane and -heptene derivatives of the formula Ia ##STR2## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, and the physiologically tolerated acid addition salts thereof, as well as processes for the preparation thereof, are described.Type: GrantFiled: September 21, 1988Date of Patent: August 25, 1992Assignee: Hoechst AktiengesellschaftInventors: Herbert Siegel, Ernold Granzer
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Patent number: 5140026Abstract: Compounds of this invention are represented by the formula: ##STR1## wherein Z is a C.sub.1 -C.sub.6 alkylene group and R is an alkyl or substituted alkyl group. Class III antiarrhythmic activity is determined in vitro using an electrophysiological test where prolongation of the action potential duration is an indication of activity.Type: GrantFiled: May 9, 1991Date of Patent: August 18, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Mark R. Hellberg, James R. Shanklin, Jr.
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Patent number: 5128470Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, halogen or OR.sup.5 ; R.sup.2 is hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.3 and R.sup.4 each independently are lower-alkyl or taken together are alkylene with 3-5 C atoms in a straight-chain; R.sup.5 is hydrogen, acyl, lower-alkoxycarbonyl, lower-alkyl, amino-lower-alkyl, mono-alkylamino-lower-alkyl, di-alkylamino-lower-alkyl or a N-containing 5-8-membered saturated or unsaturated monocyclic heterocyclic ring which is attached via a N atom to lower alkyl; and M signifies --CONH-- or --NHCO--, which can be used as medicaments, e.g., for the treatment of neoplasms and dermatological indications of an inflammatory and allergic nature.Type: GrantFiled: July 12, 1990Date of Patent: July 7, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5126374Abstract: Guanidines I ##STR1## (A=C.sub.5 -C.sub.12 -cycloalkyl which may bear up to three further substituents; benzyl substituted in the para-position; R.sup.1, R.sup.2, R.sup.3 =H, C.sub.1 -C.sub.4 -alkyl; R.sup.4 -C.sub.5 -C.sub.18 -alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.18 -alkenyl, C.sub.4 -C.sub.18 -alkynyl or phenyl-C.sub.1 -C.sub.6 -alkyl, and these groups may bear up to three further substituents and the phenyl moiety of the phenylalkyl may additionally bear a phenoxy group or up to three C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkyl or haloalkyl groups, C.sub.5 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl, where the ring may bear up to three further substituents; A=benzyl and R.sup.4 =C.sub.3 -C.sub.4 -alkyl which may be interrupted by oxygen, or C.sub.4 -alkenyl, both of which may bear up to three further substituents; R.sup.3 +R.sup.4 =C.sub.5 -C.sub.Type: GrantFiled: July 3, 1990Date of Patent: June 30, 1992Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5114937Abstract: The invention concerns novel renin-inhibitory compounds which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by retroviruses including HTLV-I, -II, and -III. Processes for preparing the compounds, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.Type: GrantFiled: November 28, 1989Date of Patent: May 19, 1992Assignee: Warner-Lambert CompanyInventors: James M. Hamby, James S. Kaltenbronn, Joseph T. Repine
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Patent number: 5077428Abstract: Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH-- SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.Type: GrantFiled: June 26, 1990Date of Patent: December 31, 1991Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Hiroyuki Ohno
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Patent number: 5068371Abstract: Titanocenes of the formula I ##STR1## in which R.sup.1 are cyclopentadienyl.sup..crclbar. groups and R.sup.2 and R.sup.3 are aromatic radicals which are substituted in both ortho-positions by fluorine and, in addition, are substituted by a pyrrylalkyl group, amidoalkyl group or imidoalkyl group, are suitable as photoinitiators for the photopolymerization of ethylenically unsaturated compounds.Type: GrantFiled: May 23, 1990Date of Patent: November 26, 1991Assignee: Ciba-Geigy CorporationInventors: Eginhard Steiner, Harry Beyeler, Rinaldo Husler
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5047417Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydrogen or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: May 19, 1989Date of Patent: September 10, 1991Assignee: Eisai Co. Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5030654Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 19, 1989Date of Patent: July 9, 1991Assignee: Pfizer Inc.Inventors: Ian T. Barnish, John C. Danilewicz, Keith James, Gillian M. R. Samuels, Nicholas K. Terrett, Michael T. Williams, Martin J. Wythes
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Patent number: 5015762Abstract: Aralkylphenylureas of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen, alkoxy or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together are unsubstituted or substituted alkylene which may or may not be interrupted by oxygen or sulfur, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 chain which is fused to the benzene ring to give a substituted or unsubstituted naphthyl ring, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl and n is 1, 2, 3 or 4, and herbicides containing these ureas.Type: GrantFiled: May 28, 1981Date of Patent: May 14, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
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Patent number: 5001124Abstract: This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, -SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W where W is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 2, 1990Date of Patent: March 19, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, Bruce H. Devens
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Patent number: 4985595Abstract: Aminobenzamide derivatives of the formula (I) ##STR1## wherein: R.sub.1 and R.sub.2 each represents a lower alkoxy group,R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower acyl group, a lower alkoxycarbonyl group or --R.sub.5 --SO.sub.3 Z, wherein R.sub.5 represents a lower alkylene group and Z represents an alkali metal or an alkaline earth metal,R.sub.4 represents an amino group, a morpholino group or a lower alkylamino group which may be substituted with a hydroxyl group at the alkyl moiety thereof, with the proviso that, when R.sub.3 represents a hydrogen atom, R.sub.4 cannot be an amino group,Y represents a hydrogen atom, a halogen atom or a lower alkoxy group,n represents an integer of from 1 to 6,and salts thereof; are disclosed. These compounds have excellent anti-peptic ulcer activities, and chemical and physical stabilities.Type: GrantFiled: December 1, 1988Date of Patent: January 15, 1991Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Tosaku Miki, Masahide Asano, Toru Hosokami
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Patent number: 4980377Abstract: The present invention relates to the preparation of new 1-(aminophenyl)-2-aminopropanone derivatives of the general formula: ##STR1## in which X is NH.sub.2, Y is H or a halogen atom, Z is H or a halogen atom, R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.2 is H or C.sub.1 -C.sub.4 alkyl, or R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, a heterocyclic group selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methyl-piperazino, 4-(.beta.-hydroxyethyl)piperzaino, 4-phenylpiperazino and 4-(p-chlorophenyl)piperazino groups, and addition salts thereof.These new derivatives are useful as pharmaceuticals. They are obtained by deacetylation of the corresponding acetylated products.Type: GrantFiled: November 14, 1988Date of Patent: December 25, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4959366Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.Type: GrantFiled: April 29, 1987Date of Patent: September 25, 1990Assignee: Pfizer Inc.Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
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Patent number: 4948812Abstract: Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.Type: GrantFiled: November 25, 1987Date of Patent: August 14, 1990Assignee: Boehringer Ingelheim KGInventors: Herbert Koppe, Franz Esser, Walter Kobinge, Christian Lillie
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4939142Abstract: The new compounds of the general Formula I ##STR1## (wherein A stands for a C.sub.2-4 straight or branched chain alkylene group;R.sup.1 and R.sup.2 may be same or different and each stands for hydrogen, halogen, lower alkyl or lower alkoxy; orR.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 and R.sup.4 may be the same or different and each stands for C.sub.1.ident. alkyl or C.sub.3.notident. cycloalkyl orR.sup.3 and R.sup.4 together with the nitrogen atom, they are attached to, form a 4-7 membered ring which may contain as additional ring member an oxygen or sulfur atom or a further nitrogen atom and the latter nitrogen atom may optionally bear a C.sub.Type: GrantFiled: January 26, 1989Date of Patent: July 3, 1990Assignee: EGIS GyogyszergyarInventors: Zoltan Budai, Lujza Petocz, Tibor Mezei, Eniko Szirt nee Kiszelly, Maria Szecsey nee Hegedus, Gabor Gigler, Klara Reiter nee Esses, Aranka Lay nee Konya, Eva Furdyga, Istvan Gertyan, Istvan Gacsalyi
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Patent number: 4935421Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: March 1, 1989Date of Patent: June 19, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier
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Patent number: 4933442Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: July 6, 1989Date of Patent: June 12, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4933367Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.Type: GrantFiled: March 12, 1987Date of Patent: June 12, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
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Patent number: 4931581Abstract: A method and composition for the immunization of healthy useful plants against plant diseases containing as active ingredients compounds of formula ##STR1## in which: X is hydrogen, halogen, hydroxy, methyl, methoxy, HOOC or MOOC;Y is hydrogen, halogen, SO.sub.3 H, SO.sub.3 M, nitro, hydroxy or amino, M being the molar equivalent of an alkali metal or alkaline earth metal ion that is formed from a corresponding base or basic compound; andZ is cyano or --CO--A;A represents either --OH or --SH, the hydrogen atom of which may also be replaced by the molar equivalent of an inorganic or organic cationic residue,or wherein A represents any other organic residue which has a molecular weight of less than 900 and which may also contain one, or more than one, hetero atom, including the salts of the phytophysiologically tolerable 7-carboxylic acid or 7-thiocarboxylic acid with primary, secondary or tertiary amines or with inorganic bases.Type: GrantFiled: August 18, 1988Date of Patent: June 5, 1990Assignee: Ciba-Geigy CorporationInventors: Rolf Schurter, Walter Kunz, Robert Nyfeler
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Patent number: 4921956Abstract: Hydrophilic modifier monomers of the formula [X-T].sub.z' G are disclosed wherein X is a reactive group, G is a hydrophilic group and T is a divalent linking group, z' being a number up to the available valence of G, excess G valences being taken up by hydrogen. The monomers of the invention can be used to boost the hydrophilic nature of a wide variety of polymeric materials or be polymerized themselves with varying degrees of copolymerizable monomers. They are particularly suited for making hydrophilic contact lens materials.Type: GrantFiled: June 21, 1989Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventors: Frank Molock, J. Richard Robertson, Jr., Kai C. Su
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Patent number: 4920222Abstract: 3,3-Diarylacrylic acid amides are prepared by the reaction of a benzophenone with an acetamide in the presence of a base characterized in that a sodium alcoholate is used as the base.Type: GrantFiled: January 30, 1989Date of Patent: April 24, 1990Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Jurgen Curtze, Ludwig Schroder, Paul H. Briner
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Patent number: 4914227Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 3, 1990Assignee: Banyu Pharmaceutical Company, Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Ryosuke Ushijima, Susumu Nakagawa
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Patent number: 4912217Abstract: 3,3-diphenylacrylic acid amides are prepared by the reaction of a benzophenone with an acetamide in the presence of an alkali metal tertiary alcoholate characterized in that an alkali metal mono-alkyl carbonate is additionally present.Type: GrantFiled: May 4, 1989Date of Patent: March 27, 1990Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Jurgen Curtze, Gunter Krummel
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Patent number: 4910200Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## B is ##STR3## R.sup.1 is hydrogen; halogen, cyano or optionally substituted C.sub.1-4 alkyl; andQ is NR.sup.8 R.sup.9 or ##STR4## where R.sup.2 to R.sup.11 are substituents of various types. The compounds are useful as fungicides.Type: GrantFiled: October 9, 1986Date of Patent: March 20, 1990Assignee: Celamerck GmbH & Co. KGInventors: Jurgen Curtze, Helmut Pieper, Josef Nickl, Heinz-Manfred Becher, Guido Albert, Christo Drandarevski, Sigmund Lust, Ludwig Schroder
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Patent number: 4910121Abstract: Titanocenes containing .pi.-cyclopentadienyl ligands, in which one or two carbocyclic or heterocyclic aromatic rings are attached to the metal atom, said aromatic rings being substituted by fluorine in at least one of the two ortho-positions relative to the metal-carbon bonds, are suitable photoinitiators for the photopolymerization of ethylenically unsaturated substrates. They are distinguished by high sensitivity, stability to air and heat, and are very effective in the range from UV light to visible light.Type: GrantFiled: July 28, 1987Date of Patent: March 20, 1990Assignee: Ciba-Geigy CorporationInventors: Martin Riediker, Martin Roth, Niklaus Buhler, Joseph Berger
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4906634Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.Type: GrantFiled: March 8, 1988Date of Patent: March 6, 1990Assignee: Schering A.G.Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
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Patent number: 4898941Abstract: A process for preparing a diphenylalkene derivative of the formula [II] ##STR1## which comprises oxidizing a diphenylalkanoic acid derivative of the formula [I] ##STR2## wherein R.sub.1 and R.sub.2 are each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or substituted or unsubstituted aryl, R.sub.1 and R.sub.2 may form a heteroring together theirwith or with an adjacent benzene ring, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are each hydrogen atom, halogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl or substituted or unsubstituted amino, R.sub.12 and R.sub.13 are each hydrogen atom or substituted or unsubstituted alkyl, X is carboxyl, amide, ester or halide thereof.Type: GrantFiled: August 11, 1987Date of Patent: February 6, 1990Assignee: Kanzaki Paper Manufacturing Co., Ltd.Inventors: Nobuo Kanda, Haruo Omura, Yukihiro Abe, Mitsuru Kondo
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Patent number: 4895847Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: September 21, 1988Date of Patent: January 23, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4879291Abstract: Novel N-alkyl-2,6-dimethyl-morpholinocarboxamide salts of the general formula I, ##STR1## processes for their preparation, and their use as fungicides for controlling pathogenic fungi. The agents according to the invention additionally posses plant growth-regulating properties. The meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X.sup.- are given in the description. (Formula I).Type: GrantFiled: December 30, 1987Date of Patent: November 7, 1989Assignee: Institut fuer Pflanzenschutzforschung Kleinmachnow der Akademie der Landwirtschaftswissenshafen der DDRInventors: Lothar Banasiak, Wilfried Edlich, Horst Lyr, Eva Nega, Marianne Sunkel
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Patent number: 4877812Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: April 16, 1987Date of Patent: October 31, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon