The -c(=x)- Is Part Of A -c(=x)x- Group Wherein The X's Are The Same Or Diverse Chalcogens (e.g., 3-pyrrolidinemethanol Propionates, Etc.) Patents (Class 548/572)
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Publication number: 20010041709Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: January 26, 2001Publication date: November 15, 2001Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Publication number: 20010031788Abstract: The present invention relates to compounds of the general formula (1) 1Type: ApplicationFiled: May 30, 2001Publication date: October 18, 2001Inventors: Andreas Schoop, Gerhard Mueller, Ulf Brueggemeier, Delf Schmidt, Beatrix Stelte-Ludwig, Joerg Keldenich
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Patent number: 6245801Abstract: Branched alkyl pyrrolidines of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropatnological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: October 13, 2000Date of Patent: June 12, 2001Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, Ihoezo Victor Ekhato, David Christopher Horwell, Rong Ling, Jean-Marie Receveur, David Juergen Wustrow
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Patent number: 6211226Abstract: 11-aza analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: October 29, 1999Date of Patent: April 3, 2001Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Peter G. Klimko
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Patent number: 6201130Abstract: Compounds of the formula I: stereoisomeric forms, and physiologically tolerable salts thereof are suitable for the production of pharmaceuticals for the therapy and prophylaxis of disorders involving matrix-degrading metalloproteinases.Type: GrantFiled: November 5, 1999Date of Patent: March 13, 2001Assignee: Aventis Pharma Duetschland GmbHInventors: Wilfried Schwab, Werner Thorwart, Manfred Schudok, Burkhard Haase
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Patent number: 6177427Abstract: Compositions of non-steroidal glucocorticoid antagonists for treating glaucoma or ocular hypertension and methods for their use are disclosed.Type: GrantFiled: July 1, 1999Date of Patent: January 23, 2001Assignee: Alcon Laboratories, Inc.Inventors: Abbot F. Clark, Raymond E. Conrow
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Patent number: 6174879Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: March 17, 1999Date of Patent: January 16, 2001Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6100428Abstract: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.Type: GrantFiled: October 6, 1999Date of Patent: August 8, 2000Assignee: The University of KansasInventors: Laxminarayan Bhat, Gunda I. Georg
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Patent number: 6084120Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.Type: GrantFiled: June 22, 1998Date of Patent: July 4, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jawad Alzeer, Jacques Chollet, Christian Hubschwerlen, Hugues Matile, Robert George Ridley
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 5998401Abstract: A class of substituted phenoxy naphthalene compounds of the structure: ##STR1## where n is 2 or 3; R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl; R.sup.2 is is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl, or halo; and R.sup.3 is 1-piperidinyl, 1-pyrollidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; are useful in the treatment of pathological conditions associated with post-menopause including osteoporosis, endometriosis, uterine fibroid disease, cardiovascular disease (particularly hyperlipidemia), and hormonally-dependent cancers (particularly breast and uterine cancer).Type: GrantFiled: February 28, 1995Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5965119Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: B is a leaving group or a residue of an amine-containing target moiety;G is ##STR2## or CH.sub.2 ; Y.sub.1-2 are independently O or S;M is X or Q; where X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2);R.sub.1, R.sub.4, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.13 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls, substituted C.sub.1-6 heteroalkyls;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.Type: GrantFiled: December 30, 1997Date of Patent: October 12, 1999Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 5962507Abstract: Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl having up to 17 carbon atoms.Type: GrantFiled: December 5, 1997Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5955608Abstract: Novel processes for producing benzothiophenes employing ethylene carbonate or propylene carbonate are provided.Type: GrantFiled: January 30, 1998Date of Patent: September 21, 1999Assignee: Eli Lilly and CompanyInventor: Douglas P. Kjell -
Patent number: 5935585Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: February 23, 1996Date of Patent: August 10, 1999Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Laurence Vigne
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5919786Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.Type: GrantFiled: March 25, 1998Date of Patent: July 6, 1999Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5917086Abstract: A method for the purification of a keto acid having the general formula ##STR1## wherein R1 and R2 independently represent a straight or branched chain alkyl of 1-18 carbon atoms, a cycloalkyl of 4-8 carbon atoms or a phenyl both of which may be substituted by at least one substituent selected from the group consisting of halogen atoms and alkyls having 1-4 carbon atoms, an aralkyl of 7-10 carbon atoms, alkoxyalkyl having 2-20 carbon atoms, tetrahydrofuryl alkyl, alkylcarboxy alkyl, alkyl carboxy benzyl, or R1 and R2 together with the adjacent nitrogen atom may form a heterocyclic ring, or one of R.sub.1 and R.sub.2 is hydrogen, which comprises slurrying the keto acid with an alcohol solvent, maintaining the slurry at elevated temperature in a sealed vessel until the Rhodamine impurity has dissolved, cooling and isolating the pure keto acid by filtration.Type: GrantFiled: January 9, 1998Date of Patent: June 29, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: James Philip Taylor, John Barry Henshall, John Whitworth
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5741799Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: November 8, 1995Date of Patent: April 21, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau, Steven E. Hall, Wen-Ching Han
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5731436Abstract: Processes for producing benzothiophenes employing ethylene carbonate or propylene carbonate are provided.Type: GrantFiled: August 31, 1994Date of Patent: March 24, 1998Assignee: Eli Lilly and CompanyInventor: Douglas P. Kjell -
Patent number: 5731434Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: March 24, 1998Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5691356Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.Type: GrantFiled: September 4, 1996Date of Patent: November 25, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Spencer D. Kimball, Wan Fang Lau
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Patent number: 5661161Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid antoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 14, 1995Date of Patent: August 26, 1997Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Terrence M. Ciccarone, S. Jane deSolms, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
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Patent number: 5656656Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: May 23, 1995Date of Patent: August 12, 1997Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5620971Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.Type: GrantFiled: March 25, 1994Date of Patent: April 15, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
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Patent number: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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Patent number: 5559248Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH.dbd.CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.c is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl and these compounds are useful in preventing and treating skin disorders.Type: GrantFiled: April 5, 1995Date of Patent: September 24, 1996Assignee: Bristol-Myers Squibb Co.Inventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
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Patent number: 5494921Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##Type: GrantFiled: September 16, 1994Date of Patent: February 27, 1996Assignee: Merck & Co., Inc.Inventors: Melissa S. Egbertson, George D. Hartman, Laura A. Birchenough
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Patent number: 5489562Abstract: A herbicidal composition having acivicin, its derivatives or salts or combinations thereof as its active component.A process for controlling unwanted plants comprising applying a herbicidally effective amount of acivicin, its derivatives or salts or combinations thereof to the unwanted plant.Type: GrantFiled: July 13, 1994Date of Patent: February 6, 1996Assignee: Rohm and Haas CompanyInventors: Ernest L. Burdge, Lori A. Spangler
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Patent number: 5470921Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.Type: GrantFiled: May 20, 1994Date of Patent: November 28, 1995Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5401869Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.Type: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
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Patent number: 5302751Abstract: A process is disclosed that is useful for separating the enantiomers of a racemic mixture of an aliphatic carboxylic acid having the formula ##STR1## where R.sub.1 is hydrogen or alkyl, R.sub.2, R.sub.3 and R.sub.4 are independently different and are hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, haloalkyl, alkoxyalkyl, alkylthioalkyl, phenylalkyl, substituted phenylalkyl, heteroalkylalkyl, substituted heteroalkylalkyl or cycloalkylalkyl.Type: GrantFiled: January 21, 1992Date of Patent: April 12, 1994Assignee: Ethyl CorporationInventors: Thanikavelu Manimaran, Alicia A. Potter
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Patent number: 5296494Abstract: Compounds of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, m, n, and R are as defined in the Specification.Medicinal products containing the same are useful in the treatment or prevention of thrombotic afflictions due to their thromboxane A.sub.2 receptor antagonistic activity and their thromboxane A.sub.2 synthase inhibitory activity.Type: GrantFiled: December 18, 1992Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Michel Laubie, Tony Verbeuren
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Patent number: 5278338Abstract: A method for racemizing an optically active carboxylic acid, or ester thereof, of the formula: ##STR1## where R.sub.1 is hydrogen, hydroxy, halo, cyano, C.sub.1 to C.sub.6 linear or branched alkoxy, amino or substituted amino or the group ##STR2## is nitrile; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched haloalkyl, aralkyl, cycloalkyl, alkyl substituted cycloalkyl, C.sub.6 to C.sub.10 aryl, C.sub.1 to C.sub.6 linear or branched alkoxy, C.sub.6 to C.sub.10 aryloxy, C.sub.1 to C.sub.6 alkylthio, C.sub.3 to C.sub.8 cycloalkylthio, C.sub.6 to C.sub.10 arylthio, C.sub.6 to C.sub.10 arylcarbonyl, C.sub.4 to C.sub.8 cycloalkenyl, trifluoromethyl, halo, C.sub.4 to C.sub.5 heteroaryl, C.sub.10 to C.sub.14 aryl, or biphenyl unsubstituted or substituted with methyl or halo, comprising heating said optically active carboxylic acid or ester thereof in the presence of water at a temperature of from about 40.degree. C.Type: GrantFiled: November 4, 1992Date of Patent: January 11, 1994Assignee: Ethyl CorporationInventor: Rhonda L. Trace
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Patent number: 5240956Abstract: 2-Heteroaromatic alkanoate esters which are useful as inhibitors of human leukocyate or neutrophil elastase.Type: GrantFiled: April 13, 1992Date of Patent: August 31, 1993Assignee: Cortech, Inc.Inventors: Gary P. Kirschenheuter, Raymond T. Cunningham, John C. Cheronis
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Patent number: 5221765Abstract: A method for racemizing an optically active carboxylic acid, or ester thereof, of the formula: ##STR1## where R.sub.1 is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched haloalkyl, aralkyl, cycloalkyl, alkyl substituted cycloalkyl, C.sub.6 to C.sub.10 aryl, C.sub.1 to C.sub.6 linear or branched alkoxy, C.sub.6 to C.sub.10 aryloxy, C.sub.1 to C.sub.6 alkylthio, C.sub.2 to C.sub.8 cycloalkylthio, C.sub.6 to C.sub.10 arylthio, C.sub.6 to C.sub.10 arylcarbonyl, C.sub.4 to C.sub.8 cycloalkenyl, trifluoromethyl, halo, C.sub.4 to C.sub.5 heteroaryl, C.sub.10 to C.sub.14 aryl, or biphenyl unsubstituted or substituted with methyl or halo, comprising heating said optically active carboxylic acid or ester thereof in the presence of water at a temperature of from about 75.degree. C. to about 200.degree. C.Type: GrantFiled: January 24, 1992Date of Patent: June 22, 1993Assignee: Ethyl CorporationInventors: Deepak R. Patil, Azfar A. Choudhury, Abbas Kadkhodayan
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Patent number: 5220053Abstract: An improved process for the separation of enantiomers of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process involves adding a mixture of the aliphatic carboxylic acid to the material formed by: (i) forming a solution comprising said racemic mixture of a C.sub.1 to C.sub.6 linear or branched aliphatic carboxylic acid and an organic or inorganic solvent; (ii) treating said solution with a chiral organic nitrogenous base; (iii) precipitating from the reaction solution formed in step (ii) a crystalline material comprised of the less soluble diastereomeric salt. The solution is admixed with the crystalline material for a time sufficient to cause an increase in the amount of the less soluble diastereomeric salt in the crystalline material.Type: GrantFiled: January 24, 1992Date of Patent: June 15, 1993Assignee: Ethyl CorporationInventors: Azfar A. Choudhury, Abbas Kadkhodayan, Deepak R. Patil
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Patent number: 5192763Abstract: [(1-Arylpyrrolidin-2-yl)methyl]piperazine compounds corresponding to the formula ##STR1## in which Z denotes a group of formula N-R.sub.1 in which R.sub.1 is either a hydrogen atom or a C.sub.1-3 alkyl group or a group of formula Ar--C.sub.n H.sub.2n in which n denotes 0, 1 or 2 and Ar denotes a phenyl group optionally substituted by one or more halogen atoms and/or C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals, or a group of formula COR.sub.2 in which R.sub.2 denotes the CH.sub.3, C.sub.6 H.sub.5, CH.sub.2 C.sub.6 H.sub.5 or OC.sub.2 H.sub.5 group and their salts of addition to pharmaceutically acceptable acids. The compounds are useful for the treatment of neurological disorders.Type: GrantFiled: June 6, 1991Date of Patent: March 9, 1993Assignee: SynthelaboInventors: Pascal George, Jacques Menin, Jean-Pierre Merly, Dennis Bigg, Daniel Obitz, Michel Peynot, Corinne Veronique
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Patent number: 5177069Abstract: The present invention provides a novel class of naphthylsulfonylalkanoic acid compounds such as a structure corrresponding to the formula: ##STR1## or a pharmaceutically acceptable salt thereof. A present invention naphthylsulfonylalkanoic acid compound is useful for prevention or treatment of irritable bowel syndrome, biliary dyskinesia and acute pancreatitis.Type: GrantFiled: December 6, 1990Date of Patent: January 5, 1993Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Masuo Akahane, Yasushi Nakano, Atsushi Tsubaki, Kazuaki Sato, Masaaki Ban, Michihiro Kobayashi
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Patent number: 5164503Abstract: A process is described for the preparation of compounds of the formula ##STR1## in which W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH-- or --CH.sub.2 Ch.sub.2 --Y is a saturated heterocyclic amino group, andR.sup.2 is substituted or unsubstituted phenyl-, thienyl- or naphthyl-alkyl, or cinnamyl,and their salts and solvates.The process comprises hydrolysing a corresponding ester, amide, nitrile or ortho-ester. The starting materials are preferably prepared by reducing the corresponding cyclopentanone and hydrolysis can take place simultaneously with reduction.Type: GrantFiled: May 13, 1991Date of Patent: November 17, 1992Assignee: Glaxo Group LimitedInventors: Ian Waterhouse, David R. Marshall, Eric W. Collington, Christopher J. Wallis, Peter Hallett
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Patent number: 5145958Abstract: 2,4- or 2,6-dihalogeno-aniline can be prepared by reacting an amino-benzoic acid ester of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated in the description, with 2-2.5 moles of a chlorinating or brominating agent in an inert reaction medium at a temperature of 40.degree.-160.degree. C. and subsequently hydrolyzing and decarboxylating the dihalogenated amino-benzoic acid ester.Type: GrantFiled: November 26, 1991Date of Patent: September 8, 1992Assignee: Bayer AktiengesellschaftInventors: Wolfram Kissener, Helmut Fiege
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Patent number: 5134147Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.Type: GrantFiled: October 21, 1991Date of Patent: July 28, 1992Assignee: Adir et CompagnieInventors: Jean L. Peglion, Francis Colpaert
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5097064Abstract: This invention relates to a process for preparing an optically active 2-arylpropionic acid of general formula (I), by the hydrogenation, in a heterogeneous aqueous-organic medium, of a 2-arylacrylic acid of general formula (II) in the presence of a catalyst consisting of a rhodium derivative and a water-soluble chiral ligand.Type: GrantFiled: August 30, 1990Date of Patent: March 17, 1992Assignee: Rhone-Poulenc SanteInventor: Jean-Michel Grosselin
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Patent number: 5095133Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of alkoxides of the formulaM.sup.1 OR.sup.10 (IV)where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.10, X.sup.- and M.sup.1 have the meaning mentioned in the description.Type: GrantFiled: July 16, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz U. Blank, Helmut Kraus
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Patent number: RE33907Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: =n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;=R.sub.2 is hydrogen or hydroxyl; andR.sub.Type: GrantFiled: August 15, 1989Date of Patent: April 28, 1992Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis