Hydrogen Or Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., 2 Pyrrolidine Acrylamide, Etc.) Patents (Class 548/568)
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Patent number: 6413987Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.Type: GrantFiled: June 6, 2000Date of Patent: July 2, 2002Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6399824Abstract: Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by reaction of a compound II with guanidine.Type: GrantFiled: September 18, 2001Date of Patent: June 4, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Armin Hofmeister, Max Hropot, Uwe Heinelt, Markus Bleich, Hans-Jochen Lang
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Patent number: 6365621Abstract: A therapeutic or preventive agent for intractable epilepsy comprising as an active ingredient a compound represented by R2—CH2CONH—R1 (I), wherein R1 is a phenyl group or a pyridyl group, which may have a substituent and R2 is a 2-oxo-1-pyrrolidinyl group which may have a substituent.Type: GrantFiled: February 6, 2001Date of Patent: April 2, 2002Assignee: Pharmaceutical Co., Ltd.Inventors: Tatsuya Tanaka, Akira Takazawa, Mitsunobu Yoshii, Yoshiya Murashima
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6337398Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 13, 1995Date of Patent: January 8, 2002Assignee: G.D. Searle & Co.Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6335350Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: November 22, 1999Date of Patent: January 1, 2002Assignee: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Publication number: 20010006619Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.Type: ApplicationFiled: January 5, 2001Publication date: July 5, 2001Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Patent number: 6255336Abstract: Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: July 9, 1999Date of Patent: July 3, 2001Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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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: 6172064Abstract: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof. Also described are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine.Type: GrantFiled: August 25, 1999Date of Patent: January 9, 2001Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Marc Werner Andersen, David John Cowan, David Norman Deaton, Scott Howard Dickerson, David Harold Drewry, Michael David Gaul, Michael Joseph Luzzio, Brian Edward Marron, Michael Howard Rabinowitz
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Patent number: 6166015Abstract: This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 18, 1999Date of Patent: December 26, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Daniel Harry Rogers, John Saunders, John Patrick Williams
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Patent number: 6140505Abstract: A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO.sub.3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0.degree. C. to about 75.degree. C., cooling, if necessary, to a temperature of from about -25.degree. C. to about 65.degree. C. and then adding oxalyl halide.Type: GrantFiled: May 19, 1998Date of Patent: October 31, 2000Assignee: G. D. Searle & Co.Inventors: Sastry A. Kunda, Leo J. Letendre, Gary A. De Crescenzo
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Patent number: 6060504Abstract: The invention relates to a novel heat-stable form of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diph enylacetamide and to a process for the preparation and isolation of this compound in this novel form and to use for the production of medicaments which contain this compound and/or one of its physiologically acceptable salts.Type: GrantFiled: August 26, 1996Date of Patent: May 9, 2000Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Inge Stein, Holger Beeres, Klaus Beschmann, Steffen Neuenfeld, Andrew Barber
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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: 6030995Abstract: Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: October 29, 1998Date of Patent: February 29, 2000Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6015543Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.Type: GrantFiled: June 6, 1995Date of Patent: January 18, 2000Assignee: Research Corporation Technologies, Inc.Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Patent number: 6004964Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: November 2, 1998Date of Patent: December 21, 1999Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5965601Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 3, 1998Date of Patent: October 12, 1999Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 5922770Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.Type: GrantFiled: July 17, 1997Date of Patent: July 13, 1999Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Th.o slashed.gersen
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Patent number: 5917044Abstract: Phenolic amides, useful as stabilizers for organic materials such as polyols and polyurethanes, possess the general formula ##STR1## wherein n is 0 to 3, R.sub.1, is alkyl of from 1 to about 6 carbon atoms, R.sub.2 is hydrogen or alkyl of from 1 to about 6 carbon atoms, R.sub.3 is hydrogen or hydrocarbyl of up to about 20 carbon atoms, optionally containing one or more heterocyclic groups, R.sub.4 is hydrocarbyl of up to about 20 carbon atoms, optionally containing one or more heterocyclic groups, or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms.Type: GrantFiled: April 15, 1997Date of Patent: June 29, 1999Assignee: Uniroyal Chemical Company, Inc.Inventors: Robert G. Rowland, John R. Baranski
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Patent number: 5907043Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).Type: GrantFiled: January 27, 1998Date of Patent: May 25, 1999Assignee: Zeneca LimitedInventors: Stephen John Pegg, George Joseph Sependa, Elwyn Peter Davies, Chris Allan Veale
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Patent number: 5837720Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.Type: GrantFiled: April 17, 1997Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventor: Fumitaka Ito
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Patent number: 5830897Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: November 3, 1998Assignees: G. D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5780494Abstract: Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: April 23, 1997Date of Patent: July 14, 1998Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson
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Patent number: 5776972Abstract: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.Type: GrantFiled: June 27, 1996Date of Patent: July 7, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Andrew Barber, Christoph Seyfried, Gerd Bartoszyk, Rudolf Gottschlich
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Patent number: 5763460Abstract: Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each represents 0, 1, 2 or 3 such that the sum of a+b is 0, 1, 2 or 3, the dotted line represents an optional double bond which may be present in the ring, provided that a is at least 1, A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is a mono or bicyclic aryl or heteroaryl radical with the proviso that R is not an unsubstituted phenyl group, R.sup.1 is a mono or bicyclic heteroaryl radical, and R.sup.2 is cycloalkyl or cycloalkenyl.Type: GrantFiled: January 16, 1996Date of Patent: June 9, 1998Assignees: John Wyeth & Brother Limited, American Home Products CorporationInventors: Ian Anthony Cliffe, Terence James Ward, Chapman White Alan, Antony Ashwell Mark, Bernhard Baudy Reinhardt
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Patent number: 5756765Abstract: The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds.Type: GrantFiled: March 14, 1997Date of Patent: May 26, 1998Assignee: Chong Kun Dang Corp.Inventors: Hyo Sung Kwak, Chong Ryul Lee, Sang Choon Lee, Hong Woo Lee, Hoi Choo Son, Eung Nam Kim, Kyeong Bok Min
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Patent number: 5716993Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.Type: GrantFiled: September 14, 1995Date of Patent: February 10, 1998Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
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Patent number: 5688955Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.The compounds of formulae I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ;R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; andY, Z and n are as described in the specification.Type: GrantFiled: February 5, 1997Date of Patent: November 18, 1997Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 5679679Abstract: Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl;each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.Type: GrantFiled: December 2, 1994Date of Patent: October 21, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5674864Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.Type: GrantFiled: May 24, 1995Date of Patent: October 7, 1997Assignee: Roussel UclafInventors: Fran.cedilla.ois Clemence, Odile Le Martret, Francis Petit
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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: 5646121Abstract: The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation, and to their use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: September 7, 1994Date of Patent: July 8, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas-J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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Patent number: 5641778Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.Type: GrantFiled: December 6, 1995Date of Patent: June 24, 1997Assignee: Ciba-Geigy CorporationInventors: Jurgen Klaus Maibaum, Pascal Rigollier, Peter Herold, Nissim Claude Cohen, Richard Goschke, Stefan Stutz
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Patent number: 5633231Abstract: The present invention relates to valine-containing, substituted pseudopeptides of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation, and to their use as anti-viral agents, in particular against cytomegaloviruses.Type: GrantFiled: September 7, 1994Date of Patent: May 27, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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Patent number: 5633277Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed.Type: GrantFiled: September 26, 1995Date of Patent: May 27, 1997Assignee: Miles Inc.Inventors: Richard D. Connell, David G. Osterman, Michael E. Katz, Robert D. Dally
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Patent number: 5622949Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 22, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5607950Abstract: The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Alexander R. Mackenzie
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Patent number: 5605926Abstract: The present invention relates to new trifluoromethyl-containing pseudopeptides of the general formula (I) ##STR1## in which W, A, B, D, E, R.sub.1, R.sub.2 and R.sub.3 have the meaning as outlined of their making and use as pharmaceuticals.Type: GrantFiled: April 10, 1995Date of Patent: February 25, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter H abich, Wolfgang R oben, Jutta Hansen, Arnold Paessens
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Patent number: 5585374Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.Type: GrantFiled: February 1, 1995Date of Patent: December 17, 1996Assignee: John Wyeth Brother, LimitedInventors: Ian A. Cliffe, Alan C. White
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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: 5559130Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## or, if appropriate, its tautomer ##STR4## and ##STR5## or E is --COOR.sub.3 and G is ##STR6## wherein A, Y, R, Ra, R.sub.1 and R.sub.2 are as defined in the specification.Type: GrantFiled: November 29, 1994Date of Patent: September 24, 1996Assignee: Roussel UclafInventors: Fran.cedilla.ois Clemence, Michel Fortin, Odile Le Martret
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Patent number: 5532266Abstract: Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.Type: GrantFiled: May 30, 1995Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk, Frank Mauler, Manfred Stohrer, Andrew Barber
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Patent number: 5521212Abstract: Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: August 26, 1994Date of Patent: May 28, 1996Assignee: Pfizer Inc.Inventors: Takafumi Ikeda, Akiyoshi Kawai, Takashi Mano, Yoshiyuki Okumura, Rodney W. Stevens
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Patent number: 5506356Abstract: An N-acylamino acid derivative of the formula: ##STR1##Type: GrantFiled: January 20, 1995Date of Patent: April 9, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5481036Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.Type: GrantFiled: January 10, 1994Date of Patent: January 2, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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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: 5430151Abstract: The present invention relates to new trifluoromethyl-containing pseudopeptides of the general formula (I) ##STR1## in which W, A, B, D, E, R.sub.1, R.sub.2 and R.sub.3 have the meaning as outlined of their making and use as pharmaceuticals.Type: GrantFiled: July 24, 1992Date of Patent: July 4, 1995Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Wolfgang Roben, Jutta Hansen, Arnold Paessens
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Patent number: 5401775Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.Type: GrantFiled: December 22, 1993Date of Patent: March 28, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht