Polycyclo Ring System Having A 1,3,5-triazine As One Of The Cyclos Patents (Class 514/246)
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Patent number: 5789407Abstract: The present invention relates to an antidepressant containing as an active ingredient a triazine derivative or a pharmaceutically acceptable salt thereof, the derivative being represented by the following Formula (I): ##STR1## in which, R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower alkanoyl; R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a substituted or unsubstituted heterocyclic group; X represents a single bond, O, S, S(O), S(O).sub.2, or NR.sup.4 (in which R.sup.4 represents hydrogen, or substituted or unsubstituted lower alkyl; or R.sup.2 and NR.sup.4 are combined to form a substituted or unsubstituted 4 to 6-membered saturated heterocyclic group); and A represents N or CR.sup.5 (in which R.Type: GrantFiled: April 25, 1995Date of Patent: August 4, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Fumio Suzuki, Nobuaki Koike, Junichi Shimada, Shigeto Kitamura, Shunji Ichikawa, Joji Nakamura, Shizuo Shiozaki
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Patent number: 5773445Abstract: The application describes new 3-methoxy-2-phenyl-acrylic esters of the formula (I) ##STR1## in which R and Y have the meanings given in the description,a process for their preparation, and their use as pesticides.Type: GrantFiled: May 20, 1996Date of Patent: June 30, 1998Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Otto Schallner, Stefan Dutzmann, Heinz-Wilhelm Dehne, Gerd Hanssler
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Patent number: 5696127Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
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Patent number: 5696133Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiting steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi, Lawrence G. Hamann, Luc J. Farmer, Robert L. Davis
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Patent number: 5696130Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
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Patent number: 5693647Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
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Patent number: 5693646Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
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Patent number: 5688808Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
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Patent number: 5688810Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5610157Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: March 11, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5604224Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: May 30, 1995Date of Patent: February 18, 1997Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5420128Abstract: The invention discloses a pyrimidien derivative expressed in Formula [I]: ##STR1## where R.sup.1 denotes a hydrogen atom or hydroxyl group, R.sup.2 denotes a hydrogen atom, lower alkoxycarbonyl group, lower alkoxy group, halogen atom, lower alkyl group, cycloalkyl group with 3 to 8 carbon atoms, lower alkoxycarbonyl lower alkyl group, carboxyl group, carboxy lower alkyl group, group: --CONHR.sup.6 (R.sup.Type: GrantFiled: June 9, 1992Date of Patent: May 30, 1995Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Kiyokawa, Satoshi Yamada, Keisuke Miyajima, Kinji Hashimoto, Masatoshi Inai, Makoto Inoue, Kunihiko Tatsumi, Takeshi Yamauchi, Kazunobu Kurisu, Yoshifumi Chone
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Patent number: 5409928Abstract: This invention provides a condensed pyrazole derivative of the Formula (1): ##STR1## (where A denotes CH or N, R.sup.0 and R.sup.3 denote same or different, a hydrogen atom or a lower alkyl group, R.sup.1 and R.sup.2 denote same or different, a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a nitro group or a halogen atom, m denotes 1 or 2, and n denotes 1, 2 or 3, provided that, when n is 2, two R.sup.2 may be connected to each other to form a lower alkylenedioxy group), or its pharmaceutically acceptable salt. This derivative or its salt is excellent in the effect of inhibiting the expression of action of androgen, thereby being excellent in therapeutical effect of benign prostatic hypertrophy, prostatic carcinoma, etc., and has a long lasting of efficacy and high oral absorption.Type: GrantFiled: October 20, 1993Date of Patent: April 25, 1995Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Kiyokawa, Satoshi Yamada, Keisuke Miyajima, Koji Edamatsu, Kunihiko Tatsumi, Takeshi Yamauchi, Kazumasa Kishi, Kunihiko Kiyono
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Patent number: 5380714Abstract: Compounds of the formula I: ##STR1## wherein: X is O, S or NH;n is O or an integer of from 1 to 3;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is CH.sub.2 R.sup.3, NHR.sup.4, SO.sub.2 NR.sup.5 YNR.sup.6 R.sup.7 or R.sup.8, in which R.sup.3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R.sup.4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1-dimethylethyl)amino-1-hydroxyethyl)phenyl; R.sup.5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R.sup.6 and R.sup.7 are independently (1-4C)alkyl, or R.sup.6 is hydrogen and R.sup.7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylaminocarbonyl or (5-6C)cycloalkylaminocarbonyl; and R.sup.8 is a sugar residue of formula II in which R.sup.Type: GrantFiled: November 20, 1992Date of Patent: January 10, 1995Assignee: Imperial Chemical Industries PLCInventors: Geraint Jones, Roger James, Rodney B. Hargreaves
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Patent number: 5358947Abstract: The invention provides novel 2,3-substituted pyrazolo[1,5-a]-1,3,5-triazin-4(3H)-ones having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are described in the specification which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: September 13, 1993Date of Patent: October 25, 1994Assignee: American Cyanamid CompanyInventor: Aranapakam M. Venkatesan
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Patent number: 5356894Abstract: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is (1-6C)alkyl substituted by a group of formula R.sup.10 Xb(CO).sub.m in which m is 0 or 1, provided that when m is 0, X and Xb are separated by at least two carbon atoms, Xb is an imino group of formula --NRb in which Rb together with R.sup.10 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring;and X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.Type: GrantFiled: July 21, 1993Date of Patent: October 18, 1994Inventors: Peter W. Rodney, Geraint Jones, Michael G. Collis, Simon M. Poucher
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Patent number: 5302596Abstract: Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 23, 1992Date of Patent: April 12, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5290776Abstract: A compound of the formula I ##STR1## wherein: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is phenyl, a C-linked aromatic 5- or 6-membered heterocyclic ring containing one of oxygen and sulphur and/or one or two nitrogen, or (1-8C)alkyl, alkenyl or alkynyl unsubstituted or substituted by a phenyl or a C-linked aromatic 5- or 6-membered heterocylic ring containing one of oxygen and sulphur and/or one or two nitrogen, any phenyl being unsubstituted or substituted by one, two or three of (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, hydroxy, benzyloxy and (1-5C)alkanoyloxy;A is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof, processes for the manufacture of the compounds, and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.Type: GrantFiled: May 21, 1992Date of Patent: March 1, 1994Assignee: Imperial Chemical Industries, PLCInventors: Peter W. R. Caulkett, Geraint Jones, Michael G. Collis, Simon M. Poucher
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Patent number: 5270311Abstract: The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is hydrogen, (3-12C)cycloalkyl, (3-6C)alkenyl, phenyl(3-6C)alkenyl, tetrafluorophenyl, pentafluorophenyl, 5- or 6-membered heteroaryl, optionally substituted (1-6C)alkyl or optionally substituted phenyl;X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a 4 to 6-membered saturated heterocyclic ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.Type: GrantFiled: May 28, 1991Date of Patent: December 14, 1993Assignee: Imperial Chemical Industries PLCInventors: Peter W. R. Caulkett, Geraint Jones, Michael G. Collis, Simon M. Poucher
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Patent number: 5238950Abstract: A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed.Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.Type: GrantFiled: December 17, 1991Date of Patent: August 24, 1993Assignee: Schering CorporationInventors: John W. Clader, Harry R. Davis, Deborra Mullins, Stuart Rosenblum, Jay Weinstein
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Patent number: 5232924Abstract: A heterocyclic compound represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, an aryl group which may be substituted with one or more substituents selected from the group consisting of a halogen atom, an alkoxy group, an alkyl group and a trihalogenomethyl group; .lambda. represents 0 or 1; ring A represents a 6 membered heterocyclic ring containing the nitrogen atom shared with the triazine ring and which may contain one or more double bonds; Y represents a substituted or unsubstituted alkylene group having 1 to 15 carbon atoms; and Q represents a group represented by formula (II): ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are represented by substituents disclosed herein; or salt thereof, and intermediates therefor are described.The compound of formula (I) or salt thereof exhibit selective serotonin 2-receptor antagonistic activity and are useful for the prevention or treatment of circulatory diseases, e.g.Type: GrantFiled: June 5, 1990Date of Patent: August 3, 1993Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Yoshifumi Watanabe, Hiroyuki Usui, Toshiro Shibano, Tsuyoshi Tanaka, Yoshiyuki Morishima, Megumi Yasuoka
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Patent number: 5137887Abstract: The invention relates to a salt selected from group consisting of alkali metal salts and alkaline earth metal salts of an optically active form of a 4-hydroxy-8-(3-lower alkoxy-4-phenylsulfinylphenyl)pyrazolo[1,5-a]-1,3,5-triazine, a process for producing said optically active compound or salt thereof, and a pharmaceutical composition, such as an antipodagric agent, comprising an effective amount of the salt together with a pharmaceutically acceptable nontoxic carrier.Type: GrantFiled: August 15, 1990Date of Patent: August 11, 1992Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kinji Hashimoto, Masatoshi Inai
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Patent number: 5135929Abstract: By using .sub..alpha. -mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilization of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.Type: GrantFiled: September 5, 1990Date of Patent: August 4, 1992Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4970208Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilization of fodder and the ratio of muscle to fat in favour of the proportion of muscle and protein.Type: GrantFiled: October 25, 1988Date of Patent: November 13, 1990Assignee: Boehringer Ingelheim GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4931438Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants.Type: GrantFiled: June 22, 1989Date of Patent: June 5, 1990Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey
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Patent number: 4853402Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.Type: GrantFiled: February 26, 1987Date of Patent: August 1, 1989Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4824834Abstract: Pyrazolotriazine compounds of the formula: ##STR1## wherein R.sup.1 is OH or alkanoyloxy; R.sup.2 is H, OH, or SH; R.sup.3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) ##STR2## R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) ##STR3## or (xx) ##STR4## (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.Type: GrantFiled: October 8, 1987Date of Patent: April 25, 1989Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Setsuro Fujii, Hiroyuki Kawamura, Hiroshi Kiyokawa, Satoshi Yamada
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Patent number: 4734413Abstract: Substituted 1,2,4-triazolo[1,5-a]triazines as bronchodilators are disclosed. Pharmaceutical formulations comprising such compounds and pharmacological methods of using such compounds are also described.Type: GrantFiled: March 2, 1987Date of Patent: March 29, 1988Assignee: Riker Laboratories, Inc.Inventor: James J. Wade
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Patent number: 4734414Abstract: The invention features compounds having anti-arthritic activity and having the formula ##STR1## wherein X is an alkyl group having between 1 and 8, inclusive, carbon atoms and Y is a hydroxyalkylamino group having between 2 and 8, inclusive, carbon atoms; a dialkylamino group having between 2 and 12, inclusive, carbon atoms; a carboxyalkylamino group having between 2 and 9, inclusive, carbon atoms; a heterocycloalkyl group having between 2 and 5, inclusive, carbon atoms and having nitrogen as a hetero atom; an alkylthioalkylamino group having between 3 and 10, inclusive, carbon atoms; or a heteroarylalkylthioalkylamino group having between 5 and 14, inclusive, carbon atoms and having ntrogen as a hetero atom.Type: GrantFiled: September 12, 1986Date of Patent: March 29, 1988Assignee: Biomeasure, Inc.Inventor: Sun H. Kim
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Patent number: 4716169Abstract: The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.Type: GrantFiled: December 17, 1985Date of Patent: December 29, 1987Assignee: Dr. Karl Thomae GmbHInventors: Joachim Heider, Norbert Hauel, Volkhard Austel, Klaus Noll, Andreas Bomhard, Jacques van Meel, Willi Diederen
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Patent number: 4636502Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.Type: GrantFiled: May 17, 1985Date of Patent: January 13, 1987Assignee: Eli Lilly and CompanyInventor: Wayne A. Spitzer
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Patent number: 4565815Abstract: A compound having anti-ulcer activity and having the formula ##STR1## wherein D is H, SH, NH.sub.2, OH, R.sup.4 S where R.sup.4 is a lower alkyl group; E is OH or NH.sub.2 ; J is H or aryl; X is CH or N; Y is CH, N, or CT, wherein T is a halogen; Z is CH or N; A is ##STR2## and replaces a hydrogen of D, X, or E; R.sup.1 is H or CH.sub.3 ; L is CH.sub.2 S; Q is O or CH.sub.2 S; n is 0 or 1; 2 m 4; each R.sup.2 and R.sup.3, independently, is H, lower alkyl, cycloalkyl, or arylalkyl; or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4, 5, or 6 membered heterocyclic ring containing 0, 1, or 2 oxygen atoms and 1, 2, or 3 nitrogen atoms and being unsubstituted or lower alkyl substituted; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 25, 1984Date of Patent: January 21, 1986Assignee: Biomeasure, Inc.Inventors: Sun H. Kim, Jacques-Pierre Moreau
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Patent number: 4537889Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.Type: GrantFiled: May 3, 1984Date of Patent: August 27, 1985Assignee: Eli Lilly and CompanyInventor: Wayne A. Spitzer