Piperazine Ring Patents (Class 544/121)
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5399693Abstract: Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen;R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms;Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group;R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl;R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group;R.sup.2 R.sup.3 and R.sup.Type: GrantFiled: January 23, 1990Date of Patent: March 21, 1995Assignee: British Technology Group LimitedInventors: Jeffrey C. Watkins, Arwel W. Jones
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Patent number: 5389635Abstract: Heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##Type: GrantFiled: April 12, 1993Date of Patent: February 14, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventor: Richard E. Olson
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Patent number: 5384319Abstract: Aminoalkylphenyl derivatives of formula I ##STR1## wherein alk, R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.Type: GrantFiled: December 20, 1993Date of Patent: January 24, 1995Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 5382661Abstract: Disclosed are amino substituted steroids (XI) which contain a pyrazinylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: December 1, 1992Date of Patent: January 17, 1995Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 5382583Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.Type: GrantFiled: December 29, 1992Date of Patent: January 17, 1995Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5373008Abstract: 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: January 27, 1993Date of Patent: December 13, 1994Assignee: The Boots Compant plc.Inventor: Balasubramanian Gopalan
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Patent number: 5364849Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, into alia, for the treatment of CNS disorders, such as anxiety.Type: GrantFiled: July 10, 1992Date of Patent: November 15, 1994Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5362729Abstract: Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:a) C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy; orb) --(CH.sub.2).sub.m --O--(CH.sub.2).sub.n --NR.sub.a R.sub.b wherein each of m and n, which may be the same or different is an integer of 1 to 3, each of R.sub.a and R.sub.b, which may be the same or different, is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by a morpholino;each of R.sub.1 and R.sub.2 is independently a group --OR' wherein R' is C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 1, 1992Date of Patent: November 8, 1994Assignee: Farmitalia Carlo ERBA S.r.l.Inventors: Paolo Cozzi, Maria Menichincheri, Laura Capolongo, Nicola Mongelli
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Patent number: 5356893Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.Type: GrantFiled: September 17, 1992Date of Patent: October 18, 1994Assignee: Glaxo Group LimitedInventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
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Patent number: 5350747Abstract: Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, Z, X, W and Y are as defined below. The compounds are useful in the treatment of psychosis and anxiety.Type: GrantFiled: February 20, 1992Date of Patent: September 27, 1994Assignee: Pfizer IncInventor: Harry R. Howard
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Patent number: 5348955Abstract: Diacylpiperazines of general structural formula: ##STR1## are: angiotensin II (A-II) antagonists with affinity for both AT.sub.1 and AT.sub.2 receptors useful in the treatment of hypertension, congestive heat failure, cerebrovascular, cognitive, and CNS disorders.Type: GrantFiled: June 22, 1993Date of Patent: September 20, 1994Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Mu T. Wu
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Patent number: 5344830Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: December 10, 1992Date of Patent: September 6, 1994Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
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Patent number: 5340812Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl, and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, inter alia, for the treatment of CNS disorders, such as anxiety.Type: GrantFiled: January 7, 1993Date of Patent: August 23, 1994Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5340822Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.Type: GrantFiled: May 4, 1992Date of Patent: August 23, 1994Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
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Patent number: 5332732Abstract: Compounds of the general formula I ##STR1## wherein A is N; Ar is aryl, substituted aryl or benzofuranyl, wherein the substituents are selected from C.sub.1 -C.sub.8 alkoxy; B is CO or CH.sub.2 and HET is selected from any of piperizine, piperidine, hexahydroazepine, morpholine, thiomorpholine or pyrrolidine, which may be substituted with one of more oxo groups are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.Type: GrantFiled: September 11, 1992Date of Patent: July 26, 1994Assignee: McNeilab, Inc.Inventors: Malcolm K. Scott, Allen B. Reitz, Frank J. Villani, Jr., C. Royce Rasmussen
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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: 5314887Abstract: There are provided novel 1,4-dihydropyridine compounds possessing both calcium agonist and alpha.sub.1 -antagonist activity useful for treating congestive heart failure, pharmaceutical compositions containing them and methods of using these compounds to treat congestive heart failure in a mammal.Type: GrantFiled: October 30, 1992Date of Patent: May 24, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Paul E. Aldrich, Richard A. Earl, Philip Ma
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Patent number: 5306719Abstract: Novel carbostyril derivatives and salts thereof having useful pharmacological activities such as myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity, hypotensive activity, activity for inhibiting vasoconstriction induced by norepinephrine, and anti-inflammatory effect in one hand, while they do not possess activity for increasing heart beat at all substantially as well as show quite low toxicity and low side-effects in central nervous system activities.Type: GrantFiled: September 16, 1991Date of Patent: April 26, 1994Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shigeharu Tamada, Takafumi Fujioka, Hidenori Ogawa, Shuji Teramoto, Kazumi Kondo
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Patent number: 5302613Abstract: This invention relates to compounds of Formula I ##STR1## which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.Type: GrantFiled: April 9, 1993Date of Patent: April 12, 1994Assignee: The Upjohn CompanyInventor: Joel Morris
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Patent number: 5292726Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: May 19, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
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Patent number: 5286728Abstract: Amino-substituted piperazine derivatives of formula I ##STR1## wherein R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, have properties inhibiting the biosynthesis of interleukin-1 (IL-1) as well as analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.Type: GrantFiled: July 14, 1992Date of Patent: February 15, 1994Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 5270319Abstract: The present invention is novel compounds which are 5-hydroxy-2-pyrimidinylmethylene derivatives and pharmaceutically acceptable addition salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, preferably inflammation.Type: GrantFiled: July 7, 1992Date of Patent: December 14, 1993Assignee: Warner-Lambert CompanyInventors: Thomas R. Belliotti, David T. Connor, Catherine R. Kostlan
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Patent number: 5266568Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: October 10, 1991Date of Patent: November 30, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Michel L. Belley, Yves LeBlanc, Marc Labelle
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Patent number: 5252735Abstract: This invention relates to compounds of Formula I ##STR1## which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.Type: GrantFiled: February 25, 1992Date of Patent: October 12, 1993Assignee: The Upjohn CompanyInventor: Joel Morris
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Patent number: 5250528Abstract: This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity and represented by the general formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, aryl, ar(lower)alkoxy or a heterocyclic group, each of which may be substituted with halogen,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is cyclo(lower)alkyl, aryl or ar(lower)-alkyl, each of which may be substituted with halogen,A is ##STR2## or lower alkylene, and Y is ##STR3## and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: October 8, 1992Date of Patent: October 5, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Eishiro Todo, Yoshihiro Yokota, Hiroshi Kayakiri, Masashi Hashimoto
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Patent number: 5250533Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
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Patent number: 5245034Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: March 23, 1992Date of Patent: September 14, 1993Assignee: Kiroyoshi HidakaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5224980Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms, and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.Type: GrantFiled: September 20, 1991Date of Patent: July 6, 1993Assignee: Imperial Chemical Industries PLCInventors: Peter W. Austin, Neville Tyreman
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Patent number: 5219856Abstract: Novel heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##Type: GrantFiled: April 6, 1992Date of Patent: June 15, 1993Assignee: E. I. du Pont de Nemours and CompanyInventor: Richard E. Olson
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Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
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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: 5187276Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.Type: GrantFiled: November 28, 1990Date of Patent: February 16, 1993Assignee: Troponwerke GmbH & Co. KG.Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Thurman
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Patent number: 5177078Abstract: Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is hydrogen or lower alkyl,R.sup.1 is an aryl or heteroaryl radical,R.sup.2 is a mono- or bicyclic heterocyclic radical,R.sup.3 is hydrogen, lower alkyl or hydroxy andR.sup.4 is a aryl or heteroaryl radical,and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS--disorders such as anxiety.Type: GrantFiled: September 30, 1991Date of Patent: January 5, 1993Assignee: John Wyeth & Brother LimitedInventors: Terence J. Ward, Graham J. Warrellow
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Patent number: 5175281Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: August 26, 1991Date of Patent: December 29, 1992Assignee: The Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
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Patent number: 5169845Abstract: Piperazine derivative of formula ##STR1## and the pharmaceutically acceptable acid addition salts, where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, m is 0, 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is aryl or a mono- or bicyclic heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is a heteroaryl radical, R.sup.4 is hydrogen, lower alkyl or aryl, and R.sup.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom are 5--HT.sub.1A -binding agents and may be used, for example, as anxiolytics.Type: GrantFiled: September 30, 1991Date of Patent: December 8, 1992Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Graham J. Warrellow
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Patent number: 5164388Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: April 18, 1991Date of Patent: November 17, 1992Assignee: Abbott LaboratoriesInventors: Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
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Patent number: 5144035Abstract: This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).Type: GrantFiled: April 10, 1990Date of Patent: September 1, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Toshimitsu Yamada
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Patent number: 5130317Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.Type: GrantFiled: September 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5116835Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.Type: GrantFiled: December 7, 1989Date of Patent: May 26, 1992Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5086051Abstract: New derivatives of formula (I) in which R.sub.1 =H, halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH, CH, phenyl or phenoxy, Ar=phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, thienyl, thieno[2,3-b]thienyl or thieno[3,2-b]thienyl (these groups optionally substituted with halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH or CN), p=0, 1 or 2, andA--either Z=valency bond and R.sub.2 =HB--or Z=valency bond and R.sub.2 =pyridyl, quinuclidinyl, 3-pyrrolidinyl, 3- or 4-piperidyl (these groups optionally being substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl)C--or Z=alkylene radical (1 to 4C) and R.sub.2 =2-, 3- or 4-pyridyl, 3-quinuclidinyl, 2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl (optionally substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl) or R.sub.2 =CON(R.sub.3)(R.sub.4) wherea) either R.sub.3 and R.sub.4 form a piperazine optionally substituted with alkyl, hydroxyalkyl, pyridyl, phenyl or phenylalkyl,b) or R.sub.Type: GrantFiled: March 14, 1990Date of Patent: February 4, 1992Assignee: Rhone-Poulenc SanteInventors: Claude James, Daniel Lave, Francoise Soler
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Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5077402Abstract: Compounds of the formula I, II, III and IIIa ##STR1## in which Ar.sup.1 is an unsubstituted or substituted aromatic radical and at least one of the radicals R.sup.1 and R.sup.2 is an alkenyl, cycloalkenyl or arylmethyl group, are effective photoinitiators for photopolymerization of unsaturated compounds. They are particularly suitable for photocuring of pigmented systems.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: Ciba-Geigy CorporationInventors: Vincent Desobry, Kurt Dietliker, Rinaldo Husler, Werner Rutsch, Manfred Rembold, Franciszek Sitek
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Patent number: 5073544Abstract: This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, ##STR2## wherein R" is H orType: GrantFiled: March 23, 1989Date of Patent: December 17, 1991Assignee: Whitby, Inc.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 5073558Abstract: Disclosed are an aminopyrimidine compound or an acid addition salt thereof represented by the formula: ##STR1## wherein R1, R2, R3, R4, R5 and Y have the same meanings defined in the specification;a process for preparing the compound and insecticide or bactericide containing the compound.Type: GrantFiled: October 26, 1989Date of Patent: December 17, 1991Assignee: Ube Industries, Ltd.Inventors: Tokio Obata, Katsutoshi Fujii, Isamu Narita, Shoji Shikita
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Patent number: 5071856Abstract: Novel carbostyril derivatives and salts thereof having useful pharmacological activities such as myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity, hypotensive activity, activity for inhibiting vasoconstriction induced by norepinephrine, and anti-inflammatory effect in one hand, while they do not possess activity for increasing heart beat at all substantially as well as show quite low toxicity and low side-effects in central nervous system activities.Type: GrantFiled: September 11, 1989Date of Patent: December 10, 1991Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shigeharu Tamada, Takafumi Fujioka, Hidenori Ogawa, Shuji Teramoto, Kazumi Kondo
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Patent number: 5051504Abstract: Triphenylmethane dyes of the formula ##STR1## where each R.sup.1 is independently of the others hydrogen or substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, or two R.sup.1 radicals together with the nitrogen atom joining them form a heterocyclic radical,R.sup.2 and R.sup.5 is independently of the others hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.3 and R.sup.4 is independently of the others hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or halogen,An.sup..crclbar. is one equivalent of an anion, andn is 1 or 2,preparable from piperazine derivatives as intermediates, are useful for coloring paper.Type: GrantFiled: May 10, 1990Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Erwin Hahn, Walter Breitschaft, Udo Mayer, Gunter-Rudolf Schroeder
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Patent number: 5047406Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: May 2, 1990Date of Patent: September 10, 1991Assignee: Warner-Lambert Co.Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise