Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/527)
-
Patent number: 6759404Abstract: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: April 3, 2001Date of Patent: July 6, 2004Inventors: Richard E. Olson, Michael G. Yang
-
Publication number: 20040009966Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: 1Type: ApplicationFiled: June 9, 2003Publication date: January 15, 2004Applicant: The Procter & Gamble CompanyInventors: John August Wos, Yili Wang, Kofi Abeka Oppong, Steven Victor O'Neil, Michael Christopher Laufersweiler, David Lindsey Soper, Biswanath De, Thomas Prosser Demuth
-
Publication number: 20030236249Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1 &agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.Type: ApplicationFiled: June 12, 2002Publication date: December 25, 2003Applicant: ChemocentryxInventor: Brian McMaster
-
Publication number: 20030236401Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Inventors: Nicholas A. Magnus, Pasquale N. Confalone, Scott A. Savage, Matthew Yates, Robert E. Waltermire, David J. Meloni, Silvio Campagna
-
Patent number: 6627629Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 29, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
-
Publication number: 20030134841Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: November 1, 2002Publication date: July 17, 2003Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
-
Publication number: 20030119815Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: November 4, 2002Publication date: June 26, 2003Inventor: Richard E. Olson
-
Publication number: 20030114437Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.Type: ApplicationFiled: October 17, 2002Publication date: June 19, 2003Inventors: Maxwell D. Cummings, Robert W. Marquis Jr, Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
-
Patent number: 6559141Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: May 6, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6552041Abstract: The present invention relates to cyclized amide derivatives of formula (I) These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 3, 2002Date of Patent: April 22, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Michael Mullican, Brian Ledford
-
Patent number: 6544981Abstract: Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, R11 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.Type: GrantFiled: June 5, 2001Date of Patent: April 8, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Stephen P. O'Connor, Yan Shi, Chi Li
-
Patent number: 6544978Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 8, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6541466Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 1, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6534495Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.Type: GrantFiled: October 26, 1999Date of Patent: March 18, 2003Assignee: Akzo NebelInventor: Anton Egbert Peter Adang
-
Patent number: 6511973Abstract: Compound of the formula are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.Type: GrantFiled: July 27, 2001Date of Patent: January 28, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Philip D. Stein, Yan Shi, Stephen P. O'Connor, Chi Li
-
Patent number: 6509330Abstract: Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure wherein R*, R and R1 are as defined herein and A is a dipeptide preferably derived from an amino acid, or is a conformationally restricted dipeptide mimic.Type: GrantFiled: February 9, 2001Date of Patent: January 21, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
-
Patent number: 6503897Abstract: Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.Type: GrantFiled: August 22, 2001Date of Patent: January 7, 2003Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Raymond Paul Beckett, Mark Whittaker, Zoe Marie Spavold
-
Publication number: 20020198376Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects.Type: ApplicationFiled: May 15, 2002Publication date: December 26, 2002Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
-
Patent number: 6495540Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: March 27, 2001Date of Patent: December 17, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventor: Lorin A. Thompson
-
Patent number: 6486315Abstract: Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.Type: GrantFiled: November 16, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Rajendra P. Deshpande, James Simpson
-
Publication number: 20020147188Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: February 13, 2002Publication date: October 10, 2002Applicant: SmithKline Beecham CorporationInventors: Robert Wells Marquis, Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
-
Publication number: 20020137737Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: June 1, 2001Publication date: September 26, 2002Inventor: Richard E. Olson
-
Patent number: 6455521Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.Type: GrantFiled: April 19, 2001Date of Patent: September 24, 2002Assignee: Mitsubishi Pharma CorporationInventors: Koji Seio, Hiroshi Tanaka, Toshiyuki Kohara, Kenji Hashimoto, Masatake Fujimura, Hideki Horiuchi, Hiroshi Yasumatsu, Koreichi Kimura
-
Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
Patent number: 6452001Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;Type: GrantFiled: May 14, 2001Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck -
Patent number: 6444810Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphate reducing agents, zinc metal powder, and sodium hydrosulfite.Type: GrantFiled: November 16, 2001Date of Patent: September 3, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Rajendra P. Deshpande
-
Publication number: 20020103184Abstract: This invention relates to novel cyclic malonamides having the formula (I): 1Type: ApplicationFiled: April 3, 2001Publication date: August 1, 2002Inventors: Richard E. Olson, Michael G. Yang
-
Publication number: 20020086994Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.Type: ApplicationFiled: November 16, 2001Publication date: July 4, 2002Inventors: David R. Kronenthal, Rajendra P. Deshpande
-
Patent number: 6413954Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: May 8, 2001Date of Patent: July 2, 2002Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Richard William Versace, Kenneth Walter Bair
-
Patent number: 6344450Abstract: Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4 is R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.Type: GrantFiled: August 7, 2000Date of Patent: February 5, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
-
Publication number: 20020010172Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: March 27, 2001Publication date: January 24, 2002Inventor: Lorin A. Thompson
-
Patent number: 6331640Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 29, 1999Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
-
Patent number: 6326379Abstract: Compounds of the formulas are useful as inhibitors of cGMP PDE, especially type V.Type: GrantFiled: September 10, 1999Date of Patent: December 4, 2001Assignee: Bristol-Myers Squibb Co.Inventors: John E. Macor, Guixue Yu
-
Publication number: 20010044433Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: ApplicationFiled: March 12, 2001Publication date: November 22, 2001Inventors: Frederick Ray Kinder, Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
-
Patent number: 6297233Abstract: Caprolactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and and Y R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.Type: GrantFiled: February 2, 2000Date of Patent: October 2, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Gregory S. Bisacchi, Yan Shi, Stephen P. O'Connor, Chi Li
-
Patent number: 6262047Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 10, 1997Date of Patent: July 17, 2001Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
-
Patent number: 6207644Abstract: The invention concerns pharmaceutically useful peptide derivatives of the formula (I), P—R1—R2—R3—R4, in which P, R1, R2, R3, and R4 have the various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.Type: GrantFiled: April 16, 1999Date of Patent: March 27, 2001Assignee: Zeneca LimitedInventors: Richard William Arthur Luke, Ronald Cotton
-
Patent number: 6096885Abstract: This invention relates to novel oxoazepine derivatives of Formula (I),R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I)to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.Type: GrantFiled: April 14, 1997Date of Patent: August 1, 2000Assignee: Glaxo Wellcome Inc.Inventors: Milana Dezube, Gavin Charles Hirst, Ronald George Sherrill, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk, Timothy Mark Willson
-
Patent number: 6054579Abstract: The invention relates to an efficient and facile method for the preparation of substituted lactams, as described herein. The method comprises reacting a difunctional component containing an activated carbon, an amine capable of forming an imine with the activated carbon of the difunctional component, and an isocyanide in a nucleophilic polar protic solvent and at a concentration of reactants which facilitates the formation of the substituted lactams. The invention also relates to novel substituted lactams, libraries comprising such lactams, and a method of generating libraries substituted lactams, using the method of the invention.Type: GrantFiled: June 19, 1998Date of Patent: April 25, 2000Assignee: LeukoSite, Inc.Inventor: Geraldine C. B. Harriman
-
Patent number: 6034215Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: October 14, 1997Date of Patent: March 7, 2000Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck
-
Patent number: 6034067Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.Type: GrantFiled: August 12, 1998Date of Patent: March 7, 2000Assignee: Akzo Nobel, N.V.Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
-
Patent number: 5994537Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.Type: GrantFiled: February 14, 1998Date of Patent: November 30, 1999Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
-
Patent number: 5932733Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 3, 1999Assignee: Corvas International, Inc.Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
-
Patent number: 5929067Abstract: 1-Aryl-2-acylaminoethane compounds of formula I ##STR1## wherein R.sub.1 -R.sub.4, X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1 antagonists.Type: GrantFiled: August 21, 1997Date of Patent: July 27, 1999Assignee: Novartis AGInventors: Marc Gerspacher, Andreas Von Sprecher, Silvio Roggo, Robert Mah, Silvio Ofner, Siem Jacob Veenstra, Claudia Betschart, Yves Auberson, Walter Schilling
-
Patent number: 5912242Abstract: The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.Type: GrantFiled: January 8, 1998Date of Patent: June 15, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Mario Varasi, Roberto Maj, Patricia Salvati
-
Patent number: 5889182Abstract: This invention relates to novel oxoazepine derivatives of Formula (I),R.sup.1 R.sup.2 NCOCH.sub.2 N(R.sup.3)COR.sup.4 (I)to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. More particularly, it relates to compounds which exhibit agonist activity for CCK-A receptors thereby enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals.Type: GrantFiled: April 14, 1997Date of Patent: March 30, 1999Assignee: Glaxo Wellcome Inc.Inventors: Milana Dezube, Gavin Charles Hirst, Ronald George Sherrill, Elizabeth Ellen Sugg, Jerzy Ryszard Szewczyk, Timothy Mark Willson
-
Patent number: 5856476Abstract: Processes are disclosed for preparing the azepine intermediates of the formula ##STR1## These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.Type: GrantFiled: October 8, 1997Date of Patent: January 5, 1999Assignee: E. R. Squibbs & Sons, Inc.Inventor: Jeffrey A. Robl
-
Patent number: 5856318Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl 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 hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 11, 1997Date of Patent: January 5, 1999Assignee: 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
-
Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
-
Patent number: 5750687Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## wherein: A is ##STR2## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.Type: GrantFiled: August 20, 1996Date of Patent: May 12, 1998Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
-
Patent number: 5703208Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck