Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/142)
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Patent number: 6818774Abstract: Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.Type: GrantFiled: April 16, 2003Date of Patent: November 16, 2004Assignee: Hoffman-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
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Publication number: 20040204448Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: ApplicationFiled: December 29, 2003Publication date: October 14, 2004Applicant: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20040127500Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.Type: ApplicationFiled: December 12, 2003Publication date: July 1, 2004Applicant: Bayer Pharmaceuticals CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Publication number: 20040122030Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: ApplicationFiled: October 21, 2003Publication date: June 24, 2004Inventor: Milton L. Brown
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Patent number: 6720427Abstract: The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission are described.Type: GrantFiled: May 13, 2002Date of Patent: April 13, 2004Assignee: Pfizer Inc.Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
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Patent number: 6716853Abstract: The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and treatment of disorders, the progression of which involve an enhanced activity of matrix metalloproteinase 13, by administering to a patient in need thereof, a pharmaceutically effective amount of such compounds.Type: GrantFiled: February 26, 2003Date of Patent: April 6, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Petra Stahl, Reinhard Kirsch, Sven Ruf, Volkmar Wehner, Klaus-Ulrich Weithmann
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Publication number: 20040053948Abstract: Quinazolinedione derivatives useful for treating cellular proliferative disorders and disorders associated with Kif15 kinesin activity are described.Type: ApplicationFiled: May 8, 2003Publication date: March 18, 2004Applicant: Cytokinetics, Inc.Inventors: Andrew McDonald, Gustave Bergnes, David J. Morgans
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Publication number: 20030225122Abstract: Disclosed are isoquinolino derivatives of the formula 1Type: ApplicationFiled: April 16, 2003Publication date: December 4, 2003Inventors: Andrea Cesura, Rosa Maria Rodriquez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
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Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6602864Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
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Patent number: 6602867Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.Type: GrantFiled: July 11, 2001Date of Patent: August 5, 2003Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
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Patent number: 6586447Abstract: The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R1, R2, R3, R4, and R5 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment, and to methods of preparing compounds of formula 1.Type: GrantFiled: March 31, 2000Date of Patent: July 1, 2003Assignee: Pfizer IncInventors: Joseph Peter Lyssikatos, Bingwei Vera Yang
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Patent number: 6479436Abstract: Hetaroyl derivatives of the formula I where: R1 and R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl or C1-C6-alkoxysulfonyl, where the last 6 radicals may be substituted and/or functionalized; phenyl, phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl, where the last 5 radicals may be substituted; Z is an unsubstituted or substituted four-membered unsaturated, partially or fully saturated chain consisting of three carbons and one nitrogen; Q is unsubstituted or substituted cyclohexane-1,3-dione linked at position 2; and their agriculturally useful salts. A process for preparing the hetaroyl derivatives, compositions comprising them, and the use of these derivatives or these compositions comprising them for controlling undesirable plants.Type: GrantFiled: March 17, 1999Date of Patent: November 12, 2002Assignee: BASF AktiengesellschaftInventors: Martina Otten, Norbert Götz, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Peter Plath, Regina Luise Hill, Matthias Witschel, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6472405Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: GrantFiled: April 26, 1999Date of Patent: October 29, 2002Assignee: Eli Lilly and CompanyInventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, John Michael Morin, Jr., Daniel J. Sall, Marshall A. Skelton, Robert Theodore Vasileff
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Patent number: 6452009Abstract: The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1 to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.Type: GrantFiled: August 19, 1999Date of Patent: September 17, 2002Assignee: Lion Bioscience AGInventors: Kianoush Motesharei, Michal Lebl, Viktor Krchnak, Yidong Ni
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Patent number: 6417178Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 6, 1997Date of Patent: July 9, 2002Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6403607Abstract: The present invention discloses a sulfonamide derivative represented by the following formula (1): [wherein A represents a nitrogen atom, —CH═, etc.; Z represents an oxygen atom, etc.; Ar1 represents an aryl group, etc.; Ar2 represents an alkyl group, etc.; Ra represents a hydrogen atom, etc.; Rb represents a hydrogen atom, etc.; and Rc represents an alkyl group, etc.], or a salt thereof; and drugs containing the derivative or a salt thereof as an active ingredient. This compound exhibits radical scavenging action, gastric mucous secretion augmenting action, and anti-HP action, and thus is effective as a peptic ulcer therapeutic agent.Type: GrantFiled: October 2, 2000Date of Patent: June 11, 2002Inventors: Hiroyoshi Hidaka, Tsutomu Inoue, Isao Umezawa, Hiroyuki Nakano, Hiroshi Nakamura, Naofumi Watanabe, Shizumasa Yokota, Tomomitsu Sasaki, Yumi Yajima
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Patent number: 6362193Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.Type: GrantFiled: April 7, 2000Date of Patent: March 26, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ravi Garigipati
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Patent number: 6281227Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: December 2, 1999Date of Patent: August 28, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
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Patent number: 6262068Abstract: Lactam derivatives of the formula where X is —C(═O)NR3′—, —NR3′C(═O)—, —C(═NCN)NR3′—, —NR3′C(═NCN)—, —CH2NR3′—, —CH(alkyl)NR3′—, —CH(COOalkyl)NR3′—, —CH(CH2OH)NR3′—, —C(CH2Oalkyl)—; R1 is halo, alkyl, cycloalkyl, alkyl(cycloalkyl), aryl, (aryl)alkyl, (aryl)alkenyl, (aryl)alkynyl, O-alkyl, O-alkenyl, O-aryl, O-alky(aryl), O-alkyl(heterocyclo), COO-alkyl, C)-alkyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(aryl), NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(aryl), N(alkyl)CO-alkyl(heterocyclo); R2 is hydrogen, alkyl, halo, aryl, (aryl)alkyl, O-alkyl, amino, substituted amino; R3 and R3′ are the same or different and are independently selected from hydrogen, alkyl or alkyl(aryl); R4 whichType: GrantFiled: January 14, 1999Date of Patent: July 17, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Saleem Ahmad, Francis N. Ferrara
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Patent number: 6255479Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.Type: GrantFiled: December 29, 1998Date of Patent: July 3, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao
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Patent number: 6214857Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.Type: GrantFiled: July 30, 1998Date of Patent: April 10, 2001Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6168776Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: April 18, 1997Date of Patent: January 2, 2001Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6166219Abstract: Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: November 2, 1998Date of Patent: December 26, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Patent number: 6140339Abstract: The present invention provides new monomeric derivatives of the C-8'-7 linked naphthylisoquinoline alkaloid dioncophylline D. The invention also provides new C-4 substituted monomeric arylisoquinoline alkaloid derivatives. The present invention furthermore provides novel dimeric arylisoquinoline alkaloids comprised of coupled first and second arylisoquinoline monomers, wherein either or both of said monomer(s) is (are) monomeric compound(s) of the present invention. Monomeric and dimeric compounds of the present invention have medically useful properties, such as antimicrobial properties, more specifically such as antimalarial and antiviral properties. Monomeric compounds of the present invention are also useful as building blocks or intermediates for synthesis of novel dimeric arylisoquinoline alkaloids.Type: GrantFiled: December 31, 1997Date of Patent: October 31, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Gerhard Bringmann, Michael R. Boyd, Matthias Wenzel
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Patent number: 6040442Abstract: The presently claimed process provides a method for preparing compounds of the formula ##STR1## phosphorous (III) compound and a diester of azodicarboxylate.Type: GrantFiled: June 1, 1995Date of Patent: March 21, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6020343Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: June 15, 1998Date of Patent: February 1, 2000Assignee: Merck Frosst Canada, Inc.Inventors: Michel Belley, Jacques Yves Gauthier, Erich Grimm, Yves LeBlanc, Chun-Sing Li, Michel Therien, Cameron Black, Petpiboon Prasit, Cheuk-Kun Lau, Patrick Roy
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Patent number: 6015820Abstract: Compounds of formula (3) in which:R.sub.1 and R.sub.2 independently represent an atom of hydrogen, an aliphatic group or an alkyloxyalkyl group in which the alkyl chains are from C.sub.1 to C.sub.4 or together form an aromatic ring;R.sub.3 represents:an atom of hydrogen, oran NHR.sub.5 group in which R.sub.5 represents an atom of hydrogen or a COR.sub.6 group in which R.sub.6 is an aliphatic or aromatic group, oran NO.sub.2 group ora COOR.sub.7 group in which R.sub.7 is an aliphatic group,R.sub.4 represents a phenyl or heterocyclic group.These compounds can be used in the treatment of illnesses linked to the HIV virus.Type: GrantFiled: April 15, 1998Date of Patent: January 18, 2000Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Michel Legraverend, Anne-Marie Aubertin, Andre Kirn, Marie-Line Andreola, Laura Tarrago-Litvak, Michel Ventura
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Patent number: 5977367Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 2, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5925637Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.Type: GrantFiled: May 15, 1997Date of Patent: July 20, 1999Assignee: Bayer CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Patent number: 5866579Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: April 11, 1997Date of Patent: February 2, 1999Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, T. G. Murali Dhar, Charles Gluchowski
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Patent number: 5861380Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5837703Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.Type: GrantFiled: November 12, 1993Date of Patent: November 17, 1998Assignee: Cell Therapeutics, Inc.Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5741798Abstract: Antiinflammatory compounds of the formula I or IA ##STR1## wherein, R.sub.1 is hydrogen, halogen, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy;R.sub.2 and R.sub.3 are the same or different and each is hydrogen, halogen, trifluoromethyl, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy; and,R.sub.4 is C.sub.3-4 alkyl, C.sub.1-4 -trifluoroethyl, 2-thienyl, 2-naphthyl, phenyl or phenyl mono- or disubstituted with C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, or nitro.Type: GrantFiled: May 13, 1997Date of Patent: April 21, 1998Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Edward S. Lazer, Charles Cywin, Ronald J. Sorcek
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Patent number: 5739134Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: April 14, 1998Assignee: Janssen Pharmacetuica N.V.Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
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Patent number: 5728712Abstract: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.Type: GrantFiled: May 20, 1996Date of Patent: March 17, 1998Assignee: Chiroscience LimitedInventors: John Gary Montana, Hazel Joan Dyke, Robert James Maxey, Christopher Lowe
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Patent number: 5728844Abstract: Novel amides are inhibitors of TNF.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-phthalimido-3-(3-cyclopentyloxy-4-methoxyphenyl)propionamide.Type: GrantFiled: December 26, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5728715Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: October 30, 1996Date of Patent: March 17, 1998Assignee: Rohm and Haas CompanyInventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
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Patent number: 5728845Abstract: Novel nitriles are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimethoxyphenyl)propionitrile.Type: GrantFiled: August 29, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5723473Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.Type: GrantFiled: April 11, 1995Date of Patent: March 3, 1998Assignee: Zeneca LimitedInventor: Brian Leslie Pilkington
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Patent number: 5719151Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.Type: GrantFiled: January 13, 1995Date of Patent: February 17, 1998Inventors: Sydney Shall, Manoochehr Tavassoli
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Patent number: 5705646Abstract: The compounds of the formula ##STR1## wherein A, R.sub.1, R.sub.3, Z and Y are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.Type: GrantFiled: June 14, 1995Date of Patent: January 6, 1998Assignee: Pfizer Inc.Inventors: Gene M. Bright, Willard M. Welch, Jr.
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Patent number: 5698581Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 7, 1995Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5663449Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 2, 1997Assignee: Hoechst Marion Roussel, Inc.Inventor: Joseph T. Strupczewski
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler
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Patent number: RE37478Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: December 9, 1998Date of Patent: December 18, 2001Assignee: Aventis Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau
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Patent number: RE37729Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler