Oxadiazole Ring (including Hydrogenated) Patents (Class 544/138)
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Publication number: 20090029986Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 29, 2007Publication date: January 29, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Patent number: 7482448Abstract: Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: April 24, 2006Date of Patent: January 27, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Sukanthini Thurairatnam, David John Aldous, Vincent Leroy, Andreas Paul Timm
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Publication number: 20090012057Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: February 28, 2006Publication date: January 8, 2009Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Publication number: 20090012073Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 26, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Publication number: 20080318955Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: ApplicationFiled: March 20, 2006Publication date: December 25, 2008Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jorg Velker, Thomas Weller
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Publication number: 20080312220Abstract: Compounds of formula are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R1 is hydrogen or methyl and R2 is optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having to 6 ring atoms; or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having 4 to 6 ring atoms: or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl ring having 4 to 6 ring atoms; R is hydrogen or an optional substitutent by 1, 2 or 3 optional substituents; A is hydrogen or C1-C3 alkyl; and ring Ar is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring.Type: ApplicationFiled: November 22, 2006Publication date: December 18, 2008Inventors: Jean-Marie Receveur, Ann Christensen, Marie Grimstrup, Thomas Hoegberg
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080293702Abstract: The invention provides novel compositions and kits comprising at least one nitric oxide enhancing pyruvate compound, or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (n) treating reperfusion injury following ischemia; and/or (m) preserving tissues, organs, organ parts and/or limbs. The nitric oxide enhancing pyruvate compounds comprise at least one nitroxide group.Type: ApplicationFiled: December 19, 2006Publication date: November 27, 2008Applicant: NITROMED, INC.Inventor: David S. Garvey
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Publication number: 20080293678Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 17, 2006Publication date: November 27, 2008Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Patent number: 7452992Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: December 12, 2003Date of Patent: November 18, 2008Assignee: SmithKline Beecham CorporationInventors: Christopher Joseph Aquino, Pek Yeng Chong, Maosheng Duan, Wieslaw Mieczyslaw Kazmierski
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Publication number: 20080280876Abstract: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.Type: ApplicationFiled: December 14, 2007Publication date: November 13, 2008Inventors: Adrian D. Hobson, Shannon R. Fix-Stenzel, Kevin P. Cusack, Eric C. Breinlinger, Graham K. Ansell, Robert H. Stoffel
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Publication number: 20080261979Abstract: The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.Type: ApplicationFiled: March 26, 2008Publication date: October 23, 2008Applicant: SANOFI-AVENTISInventors: Stefanie Keil, Matthias Urmann, Patrick Bernardelli, Maike Glien, Wolfgang Wendler, Karen Chandross, Lan Lee
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Publication number: 20080255109Abstract: Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ?CR13— or ?N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY? and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ?O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl, Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ?CH— and ?N—; X is selected from CH2, O, S, SO2, NH and N-lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)cCOY3,Type: ApplicationFiled: April 28, 2008Publication date: October 16, 2008Inventors: Michael Bryan Roe, Andrzej Roman Batt, David Michael Evans, Gary Robert William Pitt, David Philip Rooker
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Patent number: 7390804Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: December 22, 2004Date of Patent: June 24, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Publication number: 20080139538Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: January 13, 2006Publication date: June 12, 2008Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
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Publication number: 20080103143Abstract: The invention is concerned with novel heteroaryl carboxamides of formula (I) wherein A, R1, R2, X, Y, Z and m are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used for the treatment or prevention of thrombotic disorders.Type: ApplicationFiled: October 19, 2007Publication date: May 1, 2008Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Bernd Kuhn, Narendra Panday, Fabienne Ricklin
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Patent number: 7348427Abstract: Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein.Type: GrantFiled: December 2, 2004Date of Patent: March 25, 2008Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Roland W. Bürli, Jacob Kaizerman, Peter Jones
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Patent number: 7226921Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: June 24, 2005Date of Patent: June 5, 2007Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.Inventors: Jiayo Li, David J. Aldous, Sukanthini Thurairatnam
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Patent number: 7220745Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: GrantFiled: May 15, 2003Date of Patent: May 22, 2007Assignee: Rigel PharmaceuticalsInventors: Rajinder Singh, Dane Goff, John Partridge
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Patent number: 7214694Abstract: Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.Type: GrantFiled: December 9, 2003Date of Patent: May 8, 2007Assignee: Pfizer IncInventors: Usa Datta, Paul Vincent Fish, Kim James, Gavin Alistair Whitlock
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Patent number: 7151175Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: GrantFiled: March 21, 2005Date of Patent: December 19, 2006Assignee: N-Gene Research Laboratories Inc.Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7064123Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: December 24, 2001Date of Patent: June 20, 2006Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.Inventors: Michael Graupe, John W. Patterson, Stephen D. Pickett, John O. Link, Jiayao Li, David Aldous, Sukanthini Thurairatnam, Andreas P. Timm, Frank Halley, Justine Lai Yeun Quai
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Patent number: 7041685Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: June 10, 2002Date of Patent: May 9, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
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Patent number: 7030116Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: June 26, 2002Date of Patent: April 18, 2006Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.Inventors: Michael Graupe, James T. Palmer, John W. Patterson, David J. Aldous, Sukanthini Thurairatnam, Andreas P. Timm, John Link, Jiayao Li
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Patent number: 6992083Abstract: The invention relates to compounds of formula wherein R is phenyl, unsubstituted or substituted by halogen or —CH2N(CH3)(CH2)nOCH3, or is benzyl, lower alkyl, lower alkoxy, —(CH2)nOCH3, or is pyridin 3 -or 4-yl, unsubstituted or substituted by lower alkyl, halogen, morpholinyl, —(CH2)n-halogen, —(CH2)nOCH3, —(CH2)n-morpholin-4-yl, or —(CH2)n-pyrrolidin-1-yl; R1 is phenyl, unsubstituted or substituted by halogen, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl or morpholin-4-yl; n is independently from each other 1 or 2; and to pharmaceutically acceptable salts thereof for the treatment of diseases related to the adenosine A2A-receptor.Type: GrantFiled: January 9, 2004Date of Patent: January 31, 2006Assignee: Hoffman-La Roche Inc.Inventor: Roger David Norcross
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Patent number: 6977256Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: November 14, 2002Date of Patent: December 20, 2005Assignees: Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.Inventors: Jiayo Li, David J. Aldous, Sukanthini Thurairatnam
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Patent number: 6897306Abstract: Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.Type: GrantFiled: July 16, 2002Date of Patent: May 24, 2005Assignee: Pfizer Products, Inc.Inventors: Simon Bailey, Stephane Billotte, Paul Vincent Fish, Kim James, Nicholas Murray Thomson, Andrew Michael Derrick
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Patent number: 6852719Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below.Type: GrantFiled: October 26, 2001Date of Patent: February 8, 2005Assignees: Pfizer Inc., Pfizer Products, Inc.Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
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Publication number: 20040142986Abstract: Compounds of formula (I): 1Type: ApplicationFiled: December 9, 2003Publication date: July 22, 2004Inventors: Usa Datta, Paul Vincent Fish, Kim James, Gavin Alistair Whitlock
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Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Publication number: 20040097564Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I: 1Type: ApplicationFiled: September 25, 2003Publication date: May 20, 2004Inventor: Martin Gall
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Publication number: 20040092517Abstract: Compounds of the formula (I) in which R1 is CN, or C(═NH)—NH2, CON(R3)2 or [C(R4)2]nN(R3)2, each of which is unsubstituted or monosubstituted by C(═O)R3, COOR3, or3 or by a conventional amino-protecting group, or W is —NR3CO—, —NR3COC(R4)2, NR3C(R4)2) or —C(R4)2NR3C(4)2—, X is —C(R3)2—, —[C(R3)2]2—, —C(R—3)2O— or —C(R3)2NR3, Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl, T is OR3, N(R3)2, N(R3)2CON(R3)2, a monocyclic or bicyclic, saturated, unsaturated or aromatic heterocyclic radical having from 1 to 4 N, O and/sor S atoms which is unsubstituted or monosubstituted, disubstituted or trisubstituted, or a phenyl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.Type: ApplicationFiled: September 3, 2003Publication date: May 13, 2004Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes, Bertram Cezanne
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Publication number: 20040087582Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.Type: ApplicationFiled: December 18, 2003Publication date: May 6, 2004Inventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
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Patent number: 6730671Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.Type: GrantFiled: February 13, 2003Date of Patent: May 4, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20040082563Abstract: Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R2, R2′, and R2″ are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.Type: ApplicationFiled: September 16, 2003Publication date: April 29, 2004Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20040063940Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: June 26, 2003Publication date: April 1, 2004Applicant: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
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Publication number: 20040014741Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.Type: ApplicationFiled: October 26, 2001Publication date: January 22, 2004Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
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Publication number: 20030220315Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.Type: ApplicationFiled: May 27, 2003Publication date: November 27, 2003Inventors: Mark S. Cushman, Agustin Casimiro-Garcia, William G. Rice
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Publication number: 20030216386Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, 1Type: ApplicationFiled: April 10, 2003Publication date: November 20, 2003Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Publication number: 20030199506Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: ApplicationFiled: November 14, 2002Publication date: October 23, 2003Inventors: Jiayo Li, David J. Aldous, Sukanthini Thurairatnam
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Publication number: 20030186975Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: October 2, 2003Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Patent number: 6617323Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), wherein X is —C(O)—, —C(S)—, or —S(O)2—; A is an optionally-substituted saturated or unsaturated monocyclic or bicyclic ring; B is a saturated or unsaturated monocyclic or bicyclic ring system having at least one substituent Q which is selected from R7 and R8; R7 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R7 is substituted with R8 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R8 is substituted with and Z1 through Z5 are as defined in the specification.Type: GrantFiled: May 23, 2002Date of Patent: September 9, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
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Patent number: 6608057Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.Type: GrantFiled: October 24, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6576630Abstract: The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.Type: GrantFiled: March 15, 2000Date of Patent: June 10, 2003Assignee: AXYS Pharmaceuticals, Inc.Inventors: John O. Link, Arnold J. Martelli, Valeri Martichonok, John W. Patterson, Oliver L. Saunders, Sheila Zipfel
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Patent number: 6566509Abstract: Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds at which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.Type: GrantFiled: June 8, 1999Date of Patent: May 20, 2003Assignee: Theravance, Inc.Inventors: John H. Griffin, John L. Pace
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Publication number: 20030069291Abstract: Compounds of formula (I): 1Type: ApplicationFiled: March 29, 2002Publication date: April 10, 2003Inventors: Simon Bailey, Paul Vincent Fish, Kim James, Gavin Alistar Whitlock
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Publication number: 20020187982Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: ApplicationFiled: November 16, 2001Publication date: December 12, 2002Inventors: Carsten Behrens, Jesper Lau, Peter Madsen
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Publication number: 20020187979Abstract: Compounds of formula (I) 1Type: ApplicationFiled: March 29, 2002Publication date: December 12, 2002Inventors: Paul Vincent Fish, Jackie Diane Kendall, Gavin Alistair Whitlock
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Publication number: 20020132849Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: ApplicationFiled: September 15, 2001Publication date: September 19, 2002Inventors: Donald W. Hansen, Ronald Keith Webber, Barnett S. Pitzele, James Sikorski, Mark A. Massa, Timothy J. Hagen, Margaret Grapperhaus, Lijuan Jane Wang, Arija A. Bergmanis, Steven W. Kramer, E. Ann Hallinan