The Additional Hetero Ring And The Bicyclo Ring System Are Attached Directly To The Same Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/468)
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Patent number: 5760059Abstract: This invention relates to compounds of formula ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group .dbd.O;R.sub.Type: GrantFiled: March 29, 1996Date of Patent: June 2, 1998Assignee: Glaxo Wellcome SpAInventors: Alfredo Cugola, Romano DiFabio, Giorgio Pentassuglia
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Patent number: 5712300Abstract: The present invention provides novel hydroxamic acid derivatives represented by the compound of formula I ##STR1## or pharmaceutical acceptable salts thereof, wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, including collagenase, stromelysin, and gelatinase, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthrits, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.Type: GrantFiled: March 4, 1997Date of Patent: January 27, 1998Assignee: Pharmacia & Upjohn CompanyInventor: E. Jon Jacobsen
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Patent number: 5708178Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compounds for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.Type: GrantFiled: September 20, 1996Date of Patent: January 13, 1998Assignee: Lockheed Martin CorporationInventors: Susan P. Ermer, Doris S. Y. Leung, Steven M. Lovejoy
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Patent number: 5703070Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen, halogen, alkyl, alkoxy, trihalomethyl or hydroxyl,R.sub.2 represents hydrogen, alkyl or phenyl which is optionally substituted, ##STR2## or alternatively ##STR3## represents --O--N.dbd., 1.ltoreq.n.ltoreq.6, ##STR4## represents any one of the groups defined in the description, its isomers and its addition salts with a pharmaceutically acceptable acid or base, a medicinal products containing the same are useful in the treatment of schizophrenia.Type: GrantFiled: June 6, 1996Date of Patent: December 30, 1997Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Valerie Audinot
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Patent number: 5691334Abstract: New and known 5-?(2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole derivatives, having immunomodulating activity and, represented by the general formula (I) and the pharmaceutically acceptable salts thereof, are disclosed.Type: GrantFiled: August 21, 1995Date of Patent: November 25, 1997Assignee: Pharmacia & Upjohn S.p.A.Inventors: Gianfederico Doria, AnnaMaria Isetta, Marcellino Tibolla, MariaChiara Fornasiero, Mario Ferrari, Domenico Trizio
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Patent number: 5679694Abstract: The invention relates to compounds of formula (I) which have been found to possess anti-tumor activity. Pharmaceutical compositions and methods of treating tumors are also disclosed.Type: GrantFiled: November 4, 1996Date of Patent: October 21, 1997Assignees: The Wellcome Foundation Ltd., University College Cardiff Consultants LimitedInventors: Karl Witold Franzmann, Jeremy Nigel Stables, Patrick Vivian Richard Shannon, Nagaraja Kodanda Ranganatha Rao, Laddawan Chunchatprasert
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Patent number: 5654400Abstract: A method of making a peptide compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is lower alkyl or halogen,R.sup.3 is hydrogen, lower alkyl or halogen,R.sup.4 is lower alkyl,R.sup.5 is ar(lower)alkyl,R.sup.6 is amino or optionally protected hydroxy, andX is O, S or N--R.sup.7, in which R.sup.7 is N,N-di(lower)alkylamino(lower)alkyl,which is useful as tachykinin antagonist.Type: GrantFiled: August 9, 1996Date of Patent: August 5, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
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Patent number: 5654431Abstract: Novel 5-alkoxy tryptamine derivatives are provided, corresponding to the general formula: ##STR1## in which R may be alkaline, X may be amino, and Y is various N-heterocyclic or N-branched chain moieties. The compounds show selective binding to 5-HT.sub.1D receptor subtypes, and have potential pharmaceutical utility in manufacture of migraine-treating drugs.Type: GrantFiled: May 30, 1996Date of Patent: August 5, 1997Inventors: Qingchang Meng, Abdelmalik Slassi, Sumanas Rakhit
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Patent number: 5648502Abstract: 4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R.sup.3 is (C.sub.1 -C.sub.6) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein, and removing the silyl group R.sub.3 Si--. The product is useful as an intermediate in making pharmaceutical products.Type: GrantFiled: July 7, 1995Date of Patent: July 15, 1997Assignee: Pfizer Inc.Inventors: Laurence E. Burgess, Gary R. Schulte
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Patent number: 5639779Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R.sup.1 is a substituted alkylene; C.sub.3 -C.sub.7 cycloalkyl optionally substituted with HO; C.sub.3 -C.sub.6 alkenyl optionally substituted with aryl; C.sub.5 -C.sub.7 cycloalkenyl; or C.sub.3 -C.sub.6 alkynyl; R.sup.2 is H; halo; F.sub.3 C; NC; R.sup.8 R.sup.9 NOC; a substituted alkylene; R.sup.8 R.sup.9 NO.sub.2 S; R.sup.10 S(O).sub.m ; R.sup.12 CON(R.sup.11); R.sup.10 SO.sub.2 N(R.sup.11); R.sup.8 R.sup.9 NOCN(R.sup.11); R.sup.10 O.sub.2 CN(R.sup.11); R.sup.13 (CH.sub.2).sub.n CH.dbd.CH; or R.sup.7 O are selective 5-HT.sub.1 -like receptor agonists useful in the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Type: GrantFiled: October 6, 1994Date of Patent: June 17, 1997Assignee: Pfizer Inc.Inventors: Martin James Wythes, John Eugene Macor
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Patent number: 5639752Abstract: Compounds of the formula ##STR1## wherein Z is ##STR2## R.sub.1 is ##STR3## X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.Type: GrantFiled: May 20, 1994Date of Patent: June 17, 1997Assignee: Pfizer IncInventor: John Eugene Macor
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Patent number: 5621116Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienyhmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.Type: GrantFiled: April 27, 1995Date of Patent: April 15, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Richard C. Effland, David G. Wettlaufer
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Patent number: 5610177Abstract: Novel acylated amino acids which are antagonists of endothelin are described. Methods for their preparation and pharmaceutical compositions containing them are also included. The compounds are expected to be useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, diabetes, head injury, and stroke.Type: GrantFiled: August 8, 1994Date of Patent: March 11, 1997Assignee: Warner-Lambert CompanyInventors: Annette M. Doherty, Harriet W. Hamilton, James S. Kaltenbronn, John Quin, III
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Patent number: 5607959Abstract: Compounds of formula (I) where R.sup.1 is thienyl, phenyl or furyl, X and Y are halogen or hydrogen and Q is alkoxy or amino are useful as analgesic and antiinflamatory agents.Type: GrantFiled: July 21, 1995Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventor: Ralph P. Robinson
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Patent number: 5607951Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined in the description and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate.Type: GrantFiled: June 6, 1995Date of Patent: March 4, 1997Assignee: Pfizer IncInventors: John E. Macor, Martin J. Wythes
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Patent number: 5596000Abstract: The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR2## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: September 2, 1993Date of Patent: January 21, 1997Assignee: Boehringer Ingelheim KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Birgit Jung, Erich Burger
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Patent number: 5578612Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Pfizer Inc.Inventors: John E. Macor, Martin J. Wythes
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Patent number: 5578574Abstract: This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Robert T. Shuman, Robert B. Rothenberger, Kenneth D. Kurz, Daniel J. Sall, Gerald F. Smith, Michael R. Wiley
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Patent number: 5571835Abstract: The present invention comprises analogs of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sub.1 A.sub.2 X analogs inhibit the farnesylation of Ras. Furthermore, these CA.sub.1 A.sub.2 X analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they have a prolyl like moiety in the A.sub.1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: November 5, 1996Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Samuel L. Graham
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Patent number: 5571833Abstract: The present invention relates to known and novel tryptamine analogues, processes and intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy, in particular for the treatment and/or prophylaxis of disorders characterized by excessive vasodilatation, such as migraine and portal hypertension.Type: GrantFiled: May 26, 1994Date of Patent: November 5, 1996Assignee: SmithKline Beecham plcInventors: Lawrence I. Kruse, Rodney C. Young, Alberto J. Kaumann
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Patent number: 5567726Abstract: Imidazole, triazole and tetrazole derivatives of formula (I) are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated, wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; R.sup.1 represents a group of formula (i), (ii) or (iii).Type: GrantFiled: January 24, 1995Date of Patent: October 22, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Jose L. Castro Pineiro, Alexander R. Guiblin, Austin J. Reeve, Francine Sternfeld, Victor G. Matassa, Leslie J. Street
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Patent number: 5563115Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## a group ##STR3## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen, R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.Type: GrantFiled: May 30, 1995Date of Patent: October 8, 1996Assignee: Zeneca LimitedInventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
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Patent number: 5559246Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Pfizer Inc.Inventor: John E. Macor
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Patent number: 5559129Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Pfizer IncInventors: John E. Macor, Martin J. Wythes
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Patent number: 5556874Abstract: 2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.Type: GrantFiled: May 10, 1995Date of Patent: September 17, 1996Assignee: Warner Lambert CompanyInventors: Ellen M. Dobrusin, Howard D. H. Showalter, William A. Denny, Brian D. Palmer, Gordon W. Rewcastle, Moana Tercel, Andrew M. Thompson
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Preparation of pyrrol and oxazole compounds: formation of C-acyl-.alpha.-amino acid esters therefrom
Patent number: 5554764Abstract: A process for preparation of new or previously known pyrrol derivatives is provided. The process involves reacting a nitroalkane or a nitroalkene with an isocyanoacetate in the presence of a proprophosphatrane "super base" to prepare the pyrrol compounds. Through production of new pyrrol compounds, new pyrrol derivatives such as dipyrromethane and porphyrin may be synthesized. In addition, the high yields of pyrrol compounds produced according to the method of the invention provide for more efficient production of previously known dipyrromethane and porphyrin compounds. The invention further provides a mild, high yield process for de-esterification of esterified pyrrol and dipyrromethane compounds. The invention also provides a synthetic method for the production of high yields of oxazoles through reaction of an aryl halide or acid anhydride with an isocyanoacetate in the presence of a prophosphatrane "super base".Type: GrantFiled: May 16, 1995Date of Patent: September 10, 1996Assignee: Iowa State University Research Foundation, Inc.Inventors: John Verkade, Jiansheng Tang -
Patent number: 5547978Abstract: The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.Type: GrantFiled: November 23, 1994Date of Patent: August 20, 1996Assignee: Meiji Seika Kaisha, Ltd.Inventors: Burton G. Christensen, Takashi Egawa, Yasuyuki Ichimaru, Shokichi Ohuchi, Tsuneo Okonogi, Arthur A. Patchett, Seiji Shibahara, Seiji Tsutsumni
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Patent number: 5545644Abstract: Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: August 13, 1996Assignee: Pfizer Inc.Inventors: John E. Macor, Martin J. Wythes
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Patent number: 5545636Abstract: The present invention discloses compounds of the general formula: ##STR1## The compounds are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: October 18, 1994Date of Patent: August 13, 1996Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Gerd R uhter, Theo Schotten, Wolfgang Stenzel
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Patent number: 5532237Abstract: Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid receptor.Type: GrantFiled: February 15, 1995Date of Patent: July 2, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Michel Gallant, Yves Gareau, Daniel Guay, Marc Labelle, Petpiboon Prasit
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Patent number: 5506237Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the carbon and nitrogen atoms to which it is attached, a heterocycle,B represents, with the nitrogen atom to which it is attached, a heterocycle,n is equal to 1, 2, 3 or 4,R represents phenyl substituted by at least one halogen or alkyl, hydroxyl, alkoxy, trifluoromethyl, nitro, amino, cyano, carboxyl or alkoxycarbonyl, benzyl, thienyl or pyridyl. The compounds may be used as medicaments.Type: GrantFiled: March 23, 1994Date of Patent: April 9, 1996Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Bernard Protevin, Georges Remond, Jean Lepagnol, Veronique Heidet
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5498626Type: GrantFiled: September 14, 1994Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventor: John E. Macor
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Patent number: 5494919Abstract: The present invention is directed to certain piperidine, pyrrolidine, and hexahydro-1H-azepine compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, A, W, X, Y, and n axe as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which s are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 27, 1996Assignee: Merck & Co., Inc.Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
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Patent number: 5492920Abstract: The present invention is directed to certain novel compounds identified as substituted piperidines, pyrrolidines and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A, X, Y and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Ravi Nargund, Arthur A. Patchett, Lihu Yang
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Patent number: 5492916Abstract: The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
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Patent number: 5449788Abstract: The present invention provides a process for preparing 2-oxindole-1-carboxamides, comprising reacting N-acyl 2-oxindole-1-carboxamides with alcohols in the presence of aprotic weak Lewis acid catalysts. In certain processes of the present invention a 2-oxindole-1-carboxamide is prepared from a 2-oxindole by reacting the 2-oxindole with an acyl isocyanate to produce the N-acyl 2-oxindole-1-carboxamide as an intermediate, which is then reacted with alcohol in the presence of aprotic weak Lewis acid catalysts. The N-acyl 2-oxindole-1-carboxamide intermediate may be converted to the 2-oxindole-1-carboxamide without isolation.Type: GrantFiled: January 28, 1994Date of Patent: September 12, 1995Assignee: Catalytica, Inc.Inventor: John M. Gruber
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Patent number: 5449787Abstract: N,N'-disubstituted amide derivatives having potent and selective antagonistic action to 5-HT.sub.3 receptor have been developed by the present invention, which provides antagonistic drugs to 5-HT.sub.3 receptor containing novel N,N'-disubstituted amide derivatives represented by a general formula [I] ##STR1## (wherein R.sub.1 denotes a hydrogen atom or lower alkyl group, R.sub.2 and R.sub.3, which may be identical or different, denote respectively a hydrogen atom, lower alkyl group, lower alkenyl group, nonsubstituted or substituted aryl-lower alkyl group, acyl group or lower alkoxycarbonyl group, R.sub.4 denotes a hydrogen atom, lower alkyl group or lower alkoxy group, A denotes CH or N, and n denotes 1), their hydrates or acid addition salts.Type: GrantFiled: September 6, 1994Date of Patent: September 12, 1995Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsutomo Miyashita, Toshio Maeda, Fumio Kawahara, Fukutaro Taga
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Patent number: 5446162Abstract: A process for the production of 7-acylindoles of the general formula: ##STR1## starting from indoline of the formula: ##STR2## Indoline is cyanized in a first stage to 7-cyanoindoline of the formula: ##STR3## The latter is catalytically dehydrogenated in a second stage to 7-cyanindole of the formula: ##STR4## The latter is then acylated in a third stage with an organometallic compound of the formula:R--Q Vinto the end product according to formula I.Type: GrantFiled: July 26, 1994Date of Patent: August 29, 1995Assignee: Lonaz Ltd.Inventors: Jean-Paul Roduit, Alain Wellig
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Patent number: 5436229Abstract: This invention relates to bisulfite adducts of L-Arginine aldehyde derivatives, pharmaceutical formulations containing those adducts and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: March 4, 1994Date of Patent: July 25, 1995Assignee: Eli Lilly and CompanyInventors: Kenneth J. Ruterbories, Robert T. Shuman
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Patent number: 5397801Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: May 10, 1994Date of Patent: March 14, 1995Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5391705Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.Type: GrantFiled: February 18, 1994Date of Patent: February 21, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
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Patent number: 5384315Abstract: A class of compounds having the structural formula ##STR1## in which R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl or substituted phenyl; N, R.sup.1 and R.sup.2 form a monocyclic or bicyclic nitrogen heterocycle which is at least partially saturated and which may contain oxygen or sulfur or be substituted with lower alkyl; and physiologically acceptable salts thereof is disclosed.A process for forming the thiophene substituted cycloamines of the subject invention is described. A composition comprising the compound of the subject invention and a suitable carrier therefor is taught.A method of controlling phytopathogenetic fungi is disclosed. In this method a fungicidally effective amount of the compound of the present invention is applied to the locus to be protected.Type: GrantFiled: February 14, 1994Date of Patent: January 24, 1995Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Kiong H. Lai, Wan S. Yu, Robert A. Davis
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Patent number: 5384322Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the nitrogen and carbon atoms to which it is bound, a heterocycle,B represents, with the nitrogen atom to which it is bound, a heterocycle,R.sub.1 represents alkoxy, benzyloxy, phenoxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted cycloalkyl,their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid, medicinal products containing the same.Type: GrantFiled: September 30, 1993Date of Patent: January 24, 1995Assignee: Adir et CompagnieInventors: Michel Vincent, Georges Remond, Bernard Portevin, Yolande Herve, Jean Lepagnol, Guillaume de Nanteuil
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Patent number: 5382593Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and X are as defined in the description, its Z and E isomers, its optical isomers, in pure form or in the form of a mixture, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful in treating a disorder resulting from or associated with peroxidation phenomena, disturbances in eicosanoid synthesis, or with platelet aggregation disorders.Type: GrantFiled: July 20, 1993Date of Patent: January 17, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Marie-Renee Nourrisson, Jean-Francois Renaud de la Faverie, Jean-Guy Bizot Espiard, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5371076Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: April 2, 1993Date of Patent: December 6, 1994Assignee: American Cyanamid CompanyInventors: Ving J. Lee, Brian L. Buckwalter, Timothy C. Barden
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Patent number: 5359085Abstract: A fulgimide derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are independently alkyl cycloalkyl aryl etc.; R.sup.4 is thienyl, indolyl, furyl, etc.; X is a divalent organic residue; and R is amino, OH, etc., or a vinyl group, has a photochromic action and can be used for producing photochromic polymers and copolymers.Type: GrantFiled: July 27, 1990Date of Patent: October 25, 1994Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Osamu Iwamoto, Taizo Hara, Haruhiko Sugiyama
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Patent number: 5354772Abstract: Compounds of the formula ##STR1## wherein one of R and R.sub.o is ##STR2## and the other is primary or secondary C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-6 cycloalkyl or phenyl-(CH.sub.2).sub.m --,whereinR.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5a is hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, andm is 1, 2 or 3, with the provisos that both R.sub.5 and R.sub.5a must be hydrogen when R.sub.4 is hydrogen, R.sub.5a must be hydrogen when R.sub.5 is hydrogen, not more than one of R.sub.4 and R.sub.5 is trifluoromethyl, not more than one of R.sub.4 and R.sub.5 is phenoxy, and not more than one of R.sub.4 and R.sub.5 is benzyloxy,R.sub.2 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.3-6 cycloalkyl, C.sub.Type: GrantFiled: November 24, 1993Date of Patent: October 11, 1994Assignee: Sandoz Pharm. Corp.Inventor: Faizulla G. Kathawala
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Patent number: 5348968Abstract: The invention relates to a compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or halogen, alkyl, alkoxy, cyano or aminocarbonyl or any one of the following: ##STR2## in which: m is equal to 1, 2 or 3,n is equal to 0, 1 or 2,T represents a CO or SO.sub.2,R.sub.4 or R.sub.5, which are identical or different, represent hydrogen or alkyl or phenyl,R.sub.2 represents hydrogen or alkyl, phenyl or acyl,R.sub.3 represents hydrogen, alkyl (optionally substituted by hydroxyl or phenyl) or alkoxycarbonyl,--X--Y.dbd. represents --N--C.dbd., --N--N.dbd.or else ##STR3## represents --O--N.dbd.; to its enantiomers, diastereoisomers and epimers and to its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: February 1, 1994Date of Patent: September 20, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Philippe Maillos, Olivier Muller, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
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Patent number: 5330542Abstract: A dye-incorporated composition which comprises a cyanine type dye and an azo metal chelate compound comprising an azo type compound of the following formula (I): ##STR1## (wherein A is a residue forming a hetero ring together with the carbon atom and the nitrogen atom to which it is bonded, B is a residue forming an aromatic ring or a hetero ring together with the two carbon atoms to which it is bonded, and X is a group having an active hydrogen), and a metal, and an optical recording medium comprising a recording layer which contains the dye-incorporated composition.Type: GrantFiled: January 24, 1992Date of Patent: July 19, 1994Assignee: Mitsubishi Kasei CorporationInventors: Shuichi Maeda, Satoru Imamura, Kazuo Mitsuhashi, Takako Tsukahara