The Additional Hetero Ring Also Contains Nitrogen Patents (Class 548/518)
Ring carbon of each of the two nitrogen containing hetero rings is bonded directly to chalcogen (e.g., both rings may be bonded to the same oxygen atom or to different oxygen atoms, etc.) (Class 548/519)
Ring nitrogens of the two nitrogen containing hetero rings are bonded directly to the same atom or chain, which chain may include a ring (Class 548/523)
  • Preparation and use of bifunctional molecules having DNA sequence binding specificity
    Patent number: 6555692
    Abstract: Novel small molecule polyamides that specifically bind with subnanomolar affinity to a predetermined sequence with potential use in molecular biology and human medicine are described. The designed compounds which target the minor groove of B-form double helical DNA offer a general approach for the control of gene-expression. Simple rules are disclosed which provide for rational control of the DNA-binding sequence specificity of synthetic polyamides containing N-methylpyrrole and N-methylimidazole amino acids. A series of molecular templates for polyamide design are disclosed which provide for small molecules which recognize predetermined DNA sequences with affinities and specificities comparable to sequence-specific DNA-binding proteins. The pyrrole-imidazole polyamides described herein represent a class of designed small molecules that can bind any predetermined sequence of double helical DNA.
    Type: Grant
    Filed: August 1, 2001
    Date of Patent: April 29, 2003
    Assignee: California Institute of Technology
    Inventor: Peter B. Dervan
  • Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions
    Patent number: 6555541
    Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: July 10, 2000
    Date of Patent: April 29, 2003
    Assignee: Astrazeneca UK Limited
    Inventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
  • Mediators of hedgehog signaling pathways, compositions and uses related thereto
    Patent number: 6552016
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: April 22, 2003
    Assignee: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Stephen Price, Lee Rubin
  • Tetrapyrroles
    Publication number: 20030069281
    Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
    Type: Application
    Filed: June 14, 2001
    Publication date: April 10, 2003
    Inventors: Irwin Fridovich, Ines Batinic-Haberle, Ivan Spasojevic, James D. Crapo, Brian J. Day
  • Urotensin-II receptor antagonists
    Patent number: 6544992
    Abstract: The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: April 8, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven David Knight, Jian Jin, Richard McCulloch Keenan
  • 4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors
    Patent number: 6541491
    Abstract: Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S-dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: April 1, 2003
    Assignee: Zeneca Limited
    Inventors: David Huw Davies, Francis Thomas Boyle, James Michael Wardleworth, Peter Wedderburn Kenny, Peter Beverley Scholes, Zbigniew Stanely Matusiak
  • Pyrrolidine derivatives
    Patent number: 6541638
    Abstract: The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: April 1, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Johannes Aebi, Denise Blum, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Bernd Michael Loeffler, Ulrike Obst, Sabine Wallbaum
  • Prodrugs of COX-2 inhibitors
    Publication number: 20030055012
    Abstract: A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, suitable for use in the treatment of a cyclooxygenase-2 mediated disease is provided.
    Type: Application
    Filed: April 16, 2002
    Publication date: March 20, 2003
    Inventor: Jeffery S. Carter
  • GPE analogs and peptidominetics
    Publication number: 20030055004
    Abstract: This invention relates to analogs and peptidomimetics of glycyl-L-prolyl-L-glutamic acid (GPE). In particular, this invention relates to GPE analogs and peptidomimetics that are anti-apoptotic and anti-necrotic, to methods of making them, to pharmaceutical compositions containing them, and to their use.
    Type: Application
    Filed: May 24, 2002
    Publication date: March 20, 2003
    Inventors: Norman A. Abood, Margaret Anne Brimble
  • Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
    Patent number: 6534491
    Abstract: This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stroinelysins and collagenases) and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr;converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: March 18, 2003
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
  • Nitrile derivatives that inhibit cathepsin K
    Patent number: 6531612
    Abstract: Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: March 11, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Tobias Gabriel, Michael Pech, Sabine Wallbaum
  • N-protected synthesis method for use in making porphyrins
    Patent number: 6528659
    Abstract: One aspect of the present invention relates to a method of forming chemical compounds and, in particular, chemical intermediates having one or more pyrrole sub-units and at least one protecting group bonded to an atom within a pyrrole sub-unit. The method further involves removal of the protecting group so as to provide a desired chemical compound having one or more pyrrole sub-units. The method can be employed in making porphyrin compounds.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: March 4, 2003
    Assignee: Emory University
    Inventors: Eric G. Nickel, Lanny S. Liebeskind
  • Sodium channel modulators
    Publication number: 20030027822
    Abstract: The invention provides sodium channel modulating compounds of formula I: 1
    Type: Application
    Filed: August 30, 2001
    Publication date: February 6, 2003
    Inventors: Jason P. Chinn, Seok-Ki Choi, Paul R. Fatheree, Daniel Marquess, S. Derek Turner
  • Chalcone and its analogs as agents for the inhibition of angiogenesis and related disease states
    Publication number: 20030027830
    Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
    Type: Application
    Filed: July 18, 2002
    Publication date: February 6, 2003
    Applicant: University of Georgia Research Foundation, Inc.
    Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
  • Thrombin inhibitors
    Patent number: 6515011
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
  • Urotensin-II receptor antagonists
    Patent number: 6514970
    Abstract: The present invention relates to pyrrolidiones, pharmaceutical compostions containing them and their use as antagonist of urotensin II.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven David Knight, Gregory Lee Warren, Jian Jin, Katherine L. Widdowson, Richard McCulloch Keenan
  • Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    Publication number: 20030023031
    Abstract: According to the invention, there is provided a method of manufacturing a medicament for use in the treatment of cancer or viral infections which comprises obtaining a cancer treating effective amount of a compound of formula (I), 1
    Type: Application
    Filed: July 17, 2002
    Publication date: January 30, 2003
    Applicant: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Cozzi, Italo Beria, Giovanni Biasoli, Marina Caldarelli, Laura Capolongo, Cristina Franzetti
  • Hetarylbenzene compounds
    Patent number: 6512122
    Abstract: A method of preparing a compound of formula I is described. In this compound, each of R1-R6 is, independently, in which Y is O, S, NH, or C(R7)═C(R8). Each of R7-R11 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C6-20 aryl, or substituted or unsubstituted C4-20 heteroaryl. Alternatively, each of R7-R11 is OH, C1-6 alkoxy, or N(R12)(R13), in which each of R12 and R13 is, independently, H, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, or substituted or unsubstituted C6-20 aryl. Each of R7-R11 can also be NO2, CN, or CO2R14, in which R14 is H or C1-6 alkyl.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: January 28, 2003
    Assignee: Academia Sinica
    Inventors: Jiann T'suen Lin, Iuan-Yuan Wu, Yu-Tai Tao, E. Balasubramaniam
  • Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
    Publication number: 20030018057
    Abstract: Novel thiol derivatives of formula I 1
    Type: Application
    Filed: June 13, 2002
    Publication date: January 23, 2003
    Inventors: Cynthia Anne Fink, Faribroz Firooznia
  • Process for preparing N-benzyl indoles
    Patent number: 6509476
    Abstract: This invention relates to a method of making N-benzyl indoles, and to intermediates for use in the method, and to certain substantially optically pure N-benzyl indoles obtained by the method.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: January 21, 2003
    Assignees: The University of East Anglia, Eli Lilly and Company
    Inventors: Nicholas James Bach, Stephen Richard Baker, Jeremy Gilmore, Russell Andrew Lewthwaite, Alexander McKillop, Jason Scott Sawyer, George Richard Stephenson, Michael William John Urquhart
  • 3,4-diaryl thiophenes and analogs thereof having use as anti-inflammatory agents
    Publication number: 20030013744
    Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.
    Type: Application
    Filed: July 1, 2002
    Publication date: January 16, 2003
    Applicant: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
  • Inhibitors of bacterial NAD synthetase
    Patent number: 6500852
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: December 31, 2002
    Assignee: University of Alabama Research Foundation
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanandan E. Velu
  • Polyamide analogs
    Publication number: 20020198254
    Abstract: This invention is directed to novel antibacterial/antifungal/antiparasitic agents of Formula (I): 1
    Type: Application
    Filed: December 27, 2001
    Publication date: December 26, 2002
    Inventors: Mark D. Velligan, Alexander Khorlin, Natalia B. Dyatkina, Dong-Fang Shi, Janos Botyanszki, Sebastian Liehr
  • Sulfonamide hydroxamates
    Patent number: 6492394
    Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 10, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
  • Amino-substituted compounds useful as inhibitors of impdh enzyme
    Publication number: 20020183315
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 5, 2002
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Publication number: 20020169196
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Application
    Filed: February 15, 2002
    Publication date: November 14, 2002
    Applicant: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
  • Compounds and methods for regulating cell differentiation
    Publication number: 20020169201
    Abstract: The present invention makes available methods and reagents for inhibiting cell growth or promoting cell differentiation comprising contacting the cell with a differeguline in a sufficient amount to inhibit cell proliferation or promote cell differentiation.
    Type: Application
    Filed: November 13, 2001
    Publication date: November 14, 2002
    Applicant: President & Fellows of Harvard College
    Inventor: Kenneth H. Falchuk
  • Azetidine derivatives, their preparation and pharmaceutical compositions containing them
    Patent number: 6479479
    Abstract: Compounds of formula: in which R represents a CR1R2, C═C(R5)SO2R6 or C═C(R7)SO2alk radical, their preparation and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: November 12, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Method of preparing intermediates useful in synthesis of retroviral protease inhibitors
    Publication number: 20020161234
    Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
    Type: Application
    Filed: April 3, 2002
    Publication date: October 31, 2002
    Applicant: G.D. Searle & Co.
    Inventors: John S. Ng, Claire A. Przybyla, Richard A. Mueller, Michael L. Vazquez, Daniel P. Getman
  • Isophthalic acid derivatives as matrix metalloproteinase inhibitors
    Publication number: 20020156061
    Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula 1
    Type: Application
    Filed: February 13, 2002
    Publication date: October 24, 2002
    Inventors: Nicole Chantel Barvian, David Thomas Connor, Richard Dennis Dyer, Adam Richard Johnson, William Chester Patt
  • Non-oxidizable bilirubin substitutes and uses therefor
    Publication number: 20020146630
    Abstract: Compositions and methods are disclosed for use in the analysis and quantitation of conjugated and unconjugated bilirubin in patient or other samples.
    Type: Application
    Filed: February 13, 2001
    Publication date: October 10, 2002
    Inventors: Alex Michael Seizew, Sean Michael Teel
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6458787
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: May 2, 2001
    Date of Patent: October 1, 2002
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
  • Processes for large scale production of tetrapyrroles
    Publication number: 20020137924
    Abstract: Processes for the large scale production of tetrapyrrolic compounds useful as photosensitizers in photodynamic therapy, such as meso-formyl porphyrins, meso-acrylate porphyrins, purpurins and benzochlorins. In particular, tin ethyl etiopurpurin (SnET2) and the intermediates necessary for its production without chromatography are disclosed.
    Type: Application
    Filed: January 23, 2001
    Publication date: September 26, 2002
    Applicant: Miravant Pharmaceuticals, Inc.
    Inventors: Byron C. Robinson, Barbara A. Garcia
  • Inhibitors of neuraminidases
    Patent number: 6455571
    Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: September 24, 2002
    Assignee: Abbott Laboratories
    Inventors: Clarence J. Maring, Yu Gui Gu, Hui-Ju Chen, Yuanwei Chen, David A. Degoey, William J. Flosi, Vincent L. Giranda, David J. Grampovnik, Warren M. Kati, Dale J. Kempf, April Kennedy, Larry L. Klein, Allan C. Krueger, Zhen Lin, Darold L. Madigan, Keith F. McDaniel, Steven W. Muchmore, Hing L. Sham, Kent D. Stewart, Vincent S. Stoll, Minghua Sun, Noah P. Tu, Frank L. Wagenaar, Gary T. Wang, Sheldon Wang, Paul E. Wiedeman, Yibo Xu, Ming C. Yeung, Chen Zhao, Stephen Hanessian, Malken Bayrakdarian, Xuehong Luo
  • Substituted piperidine amides and methods of their use
    Publication number: 20020119960
    Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.
    Type: Application
    Filed: December 19, 2000
    Publication date: August 29, 2002
    Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
  • Heterarylbenzene compounds
    Publication number: 20020115870
    Abstract: A method of preparing a compound of formula I is described.
    Type: Application
    Filed: November 21, 2001
    Publication date: August 22, 2002
    Inventors: Jiann T?apos;suen Lin, Iuan-Yuan Wu, Yu-Tai Tao, E. Balasubramaniam
  • Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
    Publication number: 20020111340
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: November 16, 2001
    Publication date: August 15, 2002
    Inventors: Youssef Bennani, Ramin Faghih
  • Aryl sulfonic acids and derivatives as FSH antagonists
    Publication number: 20020111369
    Abstract: This invention provides compounds of formula I having the structure 1
    Type: Application
    Filed: January 10, 2002
    Publication date: August 15, 2002
    Applicant: American Home Products Corporation
    Inventors: Jay E. Wrobel, John F. Rogers, Daniel M. Green, Wenling Kao, James W. Jetter
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6423710
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: July 23, 2002
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
  • Aralkyl and aralkylidene heterocyclic lactams and imides
    Patent number: 6403592
    Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: June 11, 2002
    Assignee: Pfizer INC
    Inventor: Harry Ralph Howard
  • Lactam metalloprotease inhibitors
    Patent number: 6403632
    Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: June 11, 2002
    Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
  • Novel 2-nitromethylidene/2-cyanimino/2-nitro-imino-pyrrolidines and piperidines, intermediates, and their use as pesticides
    Publication number: 20020068733
    Abstract: Compounds of formula 1
    Type: Application
    Filed: December 11, 2001
    Publication date: June 6, 2002
    Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
  • Efflux pump inhibitors
    Patent number: 6399629
    Abstract: Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: June 4, 2002
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Suzanne Chamberland, Yohei Ishida, Ving J Lee, Roger Leger, Kiyoshi Nakayama, Toshiharu Ohta, Masami Ohtsuka, Thomas E. Renau, William J. Watkins, Zhijia J. Zhang
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Publication number: 20020065302
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Application
    Filed: December 14, 2001
    Publication date: May 30, 2002
    Applicant: ICOS Corporation
    Inventors: Kerry W. Fowler, Amy Oliver, Joshua Odingo
  • Anticoccidial compounds
    Patent number: 6384052
    Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: May 7, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Bitfu, Danqing D. Feng
  • Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6380188
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagaraian, Joseph J. McDonald
  • Treatment of diseases using endothelin antagonists
    Patent number: 6380241
    Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 30, 2002
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
  • Aralkyl and aralkylidene heterocyclic lactams and imides
    Publication number: 20020049214
    Abstract: The present invention relates to compounds of the formula I 1
    Type: Application
    Filed: December 8, 2000
    Publication date: April 25, 2002
    Inventors: Megan Ann Gibbs, Harry Ralph Howard, Jeffrey Scott Sprouse, Joel Barry Schachter, Phillip Branch Chappell
  • BENZYLOXY PRODIGIOSINE COMPOUNDS
    Publication number: 20020049248
    Abstract: A compound which is a 2-(1H-pyrrol-2-yl)-5[(2H-pyrrol-2-ylidene)methyl]-1H-pyrrole of formula (I), wherein R1 is hydrogen or C1-C5 alkyl; R2 is a C1-C5 alkyl; or a pharmaceutically acceptable salt thereof, is useful as an immunomodulating agent and for treating adult-T-cell leukemia-lymphoma.
    Type: Application
    Filed: October 7, 1999
    Publication date: April 25, 2002
    Inventors: ROBERTO D'ALESSIO, ERMES VANOTTI, ALBERTO BARGIOTTI, MARCELLINO TIBOLLA, MARIO FERRARI, ANNA MARIA ISETTA, FRANCESCO COLOTTA
  • Process for the preparation of 3-amino-2-oxo-pyrrolidines, novel intermediates and their use
    Publication number: 20020045763
    Abstract: The present invention relates to a process for the preparation of &ggr;-lactams of the general formula I 1
    Type: Application
    Filed: December 7, 2001
    Publication date: April 18, 2002
    Applicant: Degussa-Huls Aktiengensellschaft
    Inventors: Karlheinz Drauz, Gunter Knaup, Michael Schwarm