1,2,3-triazoles (including Hydrogenated) Patents (Class 548/255)
Polycyclo heterocyclic ring system containing ring oxygen (Class 548/256)
Polycyclo ring system having the triazole ring as one of the cyclos (Class 548/257)
  • Antibacterial oxalidinones
    Patent number: 7186738
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: March 6, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
    Patent number: 7179910
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: February 20, 2007
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
  • Tachykinin receptor antagonists
    Patent number: 7179804
    Abstract: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: February 20, 2007
    Assignee: Eli Lilly and Company
    Inventors: Albert Kudzovi Amegadzie, Kevin Matthew Gardinier, Erik James Hembre, Jian Eric Hong, Louis Nickolaus Jungheim, Michael Alan Robertson, Kenneth Allen Savin
  • Use of benzotriazole UV absorbers
    Patent number: 7179924
    Abstract: The use of benzotriazole UV absorbers of formula wherein A is a radical of formula B is a radical of formula R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, C1–C16 alkyl; C5–C7cycloalkyl; halogen; R9 is hydrogen, C1–C12alkyl; or C5–C7cycloalkyl; R7, R8 and R10 are each independently of the others hydrogen, C1C12alkyl, C5–C7cycloalkyl, C1–C12hydroxyalkyl; X is halogen; a radical of formula (1s) ?sulfate, phosphate, lactate, citrate, tartrate; R11 is C1–C12alkyl; or C5–C7cycloalkyl; R12 and R13 are each independently of the other hydrogen; or C1–C5alkyl; x is from 0 to 10; and y is from 1 to 20; in the cosmetic treatment of human hair for protection against UV radiation is described.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: February 20, 2007
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Thomas Ehlis
  • Cytokine inhibitors
    Patent number: 7166628
    Abstract: Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: January 23, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Derek A. Cogan, Ming-Hong Hao, Kevin Chungeng Qian, Alan David Swinamer
  • Antibacterial 1,3-oxazolidin-2-one derivatives
    Patent number: 7157482
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: January 2, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
    Patent number: 7138414
    Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: November 21, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
  • Use of benzotriazole UV absorbers
    Patent number: 7129198
    Abstract: The use of benzotriazole UV absorbers of formula wherein A is a radical of formula B is a radical of formula R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, C1–C16alkyl; C5–C7cycloalkyl; halogen; R9 is hydrogen, C1–C12alkyl; or C5–C7cycloalkyl; R7, R8 and R10 are each independently of the others hydrogen, C1–C12alkyl, C5–C7cycloalkyl, C1–C12hydroxyalkyl; X is halogen; a radical of formula sulfate, phosphate, lactate, citrate, tartrate; R11 is C1–C12alkyl; or C5–C7cycloalkyl; R12 and R13 are each independently of the other hydrogen; or C1–C5alkyl; x is from 0 to 10; and y is from 1 to 20; in the cosmetic treatment of human hair for protection against UV radiation is described.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: October 31, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Thomas Ehlis
  • Thienylazolylalkoxyethanamines, their preparation and their application as medicaments
    Patent number: 7129361
    Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.
    Type: Grant
    Filed: February 13, 2004
    Date of Patent: October 31, 2006
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Inhibitors of cathepsin S
    Patent number: 7109243
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: September 19, 2006
    Assignee: IRM LLC
    Inventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
  • Sulfonamide derivatives
    Patent number: 7109203
    Abstract: Sulfonamide derivitives of the formula I wherein R1-R6 are as defined in the description, processes for their production, their use as pharmaceuticals, particularly for use in the treatment or prevention of diseases in which bradykinin B1 receptor activation plays a role or is implicated, and pharmaceutical compositions comprising them
    Type: Grant
    Filed: May 13, 2002
    Date of Patent: September 19, 2006
    Assignee: Novartis AG
    Inventors: Terance W Hart, Timothy J Ritchie
  • Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
    Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5
    Patent number: 7105548
    Abstract: Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: September 12, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Nicholas D. P. Cosford, Petpiboon Prasit, Jeffrey R. Roppe, Nicholas D. Smith, Lida R. Tehrani
  • Expanded anionic compounds comprising hydroxyl or quiescent reactive functionality and catalyst activators therefrom
    Patent number: 7094901
    Abstract: A cocatalyst or cocatalyst component, including a compound corresponding to the formula: (A*+a)b(Z*J*j)?cd, wherein: A* is a cation of from 1 to 80 atoms, not counting hydrogen atoms, Z* is an anion group of from 1 to 50 atoms, not counting hydrogen atoms, containing two or more Lewis base sites; J* is a Lewis acid of from 1 to 80, not counting hydrogen atoms, coordinated to at least one Lewis base site, and optionally two or more such J* groups may be joined together in a moiety having multiple Lewis acidic functionality, j is from 2 to 12 and a, b, c, and d are integers from 1 to 3, with the proviso that a×b is equal to c×d, and provided further that one or more of A*, Z* or J* comprises a hydroxyl group or a polar group containing quiescent reactive functionality.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: August 22, 2006
    Assignee: Dow Global Michigan Technologies Inc.
    Inventors: David A. Babb, David R. Neithamer, Richard E. Campbell, Jr., Grant B. Jacobsen, Edmund M. Carnahan
  • N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres
    Patent number: 7078424
    Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.
    Type: Grant
    Filed: June 24, 2003
    Date of Patent: July 18, 2006
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
  • Use of compounds for decreasing activity of hormone-sensitive lipase
    Patent number: 7067517
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 27, 2006
    Assignee: Nero Nordisk A/S
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Use of benzotriazole UV absorbers
    Patent number: 7066184
    Abstract: The use of benzotriazole UV absorbers of formula (1), wherein A is a radical of formula (1a); (1b); or (1c); B is a radical of formula (1d); (1e); (1f), (1g); (1h); (1i); (1k); (1l); (1m); or (1n); R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, C1–C16alkyl; C5–C7cycloalkyl; halogen; R9 is hydrogen, C1–C12alkyl; or C5–C7cycloalkyl; R7, R8 and R10 are each independently of the others hydrogen, C1–C12alkyl C5–C7cycloalky, C1–C12hydroxyalkyl; X is halogen; a radical of formula (1s); (1t); or (1u); sulfate, phosphate, lactate, citrate, tartrate; R11 is C1–C12alkyl; or C5–C7cycloalkyl; R12 and R13 are each independently of the other hydrogen; or C1–C5alkyl; x is from 0 to 10; and y is from 1 to 20; in the cosmetic treatment of human hair for protection against UV radiation is described.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: June 27, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Thomas Ehlis
  • ACE-2 modulating compounds and methods of use thereof
    Patent number: 7045532
    Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: May 16, 2006
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
  • Compounds useful for inhibiting paramyxovirus neuraminidase
    Patent number: 7045535
    Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: May 16, 2006
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
  • Ethylene derivatives and pesticides containing said derivatives
    Patent number: 7037880
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: May 2, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents
    Patent number: 7022860
    Abstract: A process for preparing a compound represented by formula (IIa?) wherein Q represents group (i) as defined in the specification and R2 to R5, R31, R32, and R52 are as defined in the specification, by (1) reacting a compound represented by formula (V) wherein R2 to R5 and R52 are as defined in the specification. with a compound represented by R31R32C?O wherein R31 and R32 are as defined in the specification; (2) reacting the compound prepared in (1) with a compound represented by R71—C(?O)—R72 wherein R71 and R72 each independently represent a chlorine atom, 4-nitrophenyl, or 1-imidazolyl; and (3) reacting the compound prepared in (2) with a compound represented by R33OH wherein R33 is as defined in the specification.
    Type: Grant
    Filed: February 13, 2002
    Date of Patent: April 4, 2006
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Mami Kawaguchi, Hideo Kitagawa, Hiromi Takata, Takashi Shishikura, Toyoaki Ishikura, Kenichi Fushihara, Yumiko Okada, Sachiko Miyamoto, Maki Shiobara
  • Thioether derivatives
    Patent number: 7005526
    Abstract: Objects of the present invention are the compounds of formula (I) formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: February 28, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Thomas Friess, Lothar Kling, Ulrike Reiff, Edgar Voss
  • 7-pyrrolyl tetracycline compounds and methods of use thereof
    Patent number: 7001918
    Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in the
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: February 21, 2006
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • 2-(1H-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity
    Patent number: 6987122
    Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: January 17, 2006
    Assignee: Novuspharma S.p.A.
    Inventors: Ernesto Menta, Nicoletta Pescalli
  • Substituted alcohols useful in treatment of Alzheimer's disease
    Patent number: 6982264
    Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: January 3, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Roy Hom, John Tucker
  • Sulfonamide compounds and uses thereof
    Patent number: 6967196
    Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: November 22, 2005
    Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.
    Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
  • HIV protease inhibitors
    Patent number: 6927217
    Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: August 9, 2005
    Assignee: Warner-Lambert Company
    Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
  • Aryl substituted pyrazoles, triazoles and tetrazoles, and the use thereof
    Patent number: 6919363
    Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R8 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: July 19, 2005
    Assignee: Euro-Celtique S.A.
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
  • Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
    Patent number: 6916924
    Abstract: This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): which are useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. X, Ar, L, Q and are described herein.
    Type: Grant
    Filed: February 12, 2002
    Date of Patent: July 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Zhulin Tan, Jinhua J. Song
  • Benzimidazole and pyridylimidazole derivatives
    Patent number: 6916819
    Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: July 12, 2005
    Assignee: Neurogen Corporation
    Inventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
  • Facile synthesis of symmetric esters of alkylenebisphosphonic acids
    Patent number: 6909010
    Abstract: A facile synthesis of symmetric esters of C1-C10 alkylenebisphopsphonic acids is disclosed in which a C1-C10 alkylenebis(phosphonic dichloride) is reacted with an alcohol in the presence of a catalytic amount of 1H-tetrazole and a base in an aprotic solvent to form a first reaction mixture. The first reaction mixture is maintained for a time period sufficient to form a C1-C10 alkylenebis(chloro ester phosphonate) that is reacted under basic conditions with an excess of a hydroxylated compound to form a second reaction mixture that is itself maintained for a time period sufficient to form a C1-C10 alkylenebis(ester phosphonate) partial ester, homoleptic tetraester or mixed tetraester. The material so formed can be recovered or used as is.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: June 21, 2005
    Assignee: Loyola University of Chicago
    Inventors: Albert W. Herlinger, Dominique C. Stepinski
  • Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same
    Patent number: 6894173
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: May 17, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 6875782
    Abstract: Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; and A, R1, R2, R2a, R2b, R2c, R3 and Y are as defined herein.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: April 5, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
  • Phenylene alkyne matrix metalloproteinase inhibitors
    Patent number: 6849648
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: February 1, 2005
    Assignee: Warner-Lambert Company
    Inventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
  • Methods of producing oxazolidinone compounds
    Patent number: 6833453
    Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
    Type: Grant
    Filed: October 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William R. Perrault, Robert C. Gadwood
  • Nonnucleoside reverse transcriptase inhibitors
    Publication number: 20040192666
    Abstract: This invention relates to novel pyrazole derivatives of formula I wherein R1 to R4 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I and pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient.
    Type: Application
    Filed: February 18, 2004
    Publication date: September 30, 2004
    Applicant: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Joan Heather Hogg, Taraneh Mirzadegan, Steven Swallow
  • Pyrazole compositions useful as inhibitors of ERK
    Patent number: 6784195
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: August 31, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
  • Protein-tyrosine phosphatase inhibitors and uses thereof
    Publication number: 20040167188
    Abstract: The present invention is directed to compounds of formula (I), 1
    Type: Application
    Filed: February 14, 2003
    Publication date: August 26, 2004
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Heterocyclic compounds
    Publication number: 20040162325
    Abstract: The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: February 17, 2004
    Publication date: August 19, 2004
    Inventors: Kenji Kuwabara, Tomiyoshi Aoki
  • Retinoid compounds (I)
    Patent number: 6777418
    Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: August 17, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
  • Insecticidal anthranilamides
    Patent number: 6747047
    Abstract: This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula (1) and compositions containing the compounds of Formula (1).
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: June 8, 2004
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George P. Lahm, Brian J. Myers, Thomas P. Selby, Thomas M. Stevenson
  • Production method of 1-substituted-1,2,3-triazole derivatives
    Publication number: 20040106803
    Abstract: A method for producing a compound of the formula: 1
    Type: Application
    Filed: November 4, 2003
    Publication date: June 3, 2004
    Inventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu, Yasuhiro Sawai, Hirohiko Nishiyama, Yasushi Isogami
  • Substituted fused pyrroleimines and pyrazoleimines
    Patent number: 6743817
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Neurogen Corporation
    Inventors: George Maynard, LingHong Xie, Stanislaw Rachwal
  • Method for producing 1-substituted-1,2,3-triazole derivative
    Patent number: 6743924
    Abstract: A method for producing a compound of the formula: (1) in a secondary or tertiary alcohol in the presence of a base, or (2) in the absence of a base is provided.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: June 1, 2004
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu, Yasuhiro Sawai, Hirohiko Nishiyama, Yasushi Isogami
  • Cytokine inhibitors
    Publication number: 20040102492
    Abstract: Disclosed are compounds of formula (I) 1
    Type: Application
    Filed: November 20, 2003
    Publication date: May 27, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Derek A. Cogan, Ming-Hong Hao, Kevin Chungeng Qian, Alan David Swinamer
  • Thia-and oxazoles and their use as ppars activators
    Publication number: 20040102493
    Abstract: A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0-3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3-5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5.
    Type: Application
    Filed: November 17, 2003
    Publication date: May 27, 2004
    Inventors: Paul John Beswick, Vipulkumar Patel, Michael Lawrence Sierra
  • Crystal modification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide and its use as antiepileptic
    Patent number: 6740669
    Abstract: The invention relates to the novel modification A or A′ of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of the formula its use and pharmaceutical preparations comprising this crystal modification.
    Type: Grant
    Filed: September 8, 1998
    Date of Patent: May 25, 2004
    Assignee: Novartis AG
    Inventors: Robert Portmann, Urs Christoph Hofmeier, Andreas Burkhard, Walter Scherrer, Martin Szelagiewicz
  • 1g(a)-Amino-n-hydroxy-acetamide derivatives
    Publication number: 20040082630
    Abstract: The invention relates to &agr;-amino-N-hydroxy-acetamide derivatives of formula (I), wherein R is di-lower alkyl amino, 1,2,3-triazol-2yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.
    Type: Application
    Filed: August 7, 2003
    Publication date: April 29, 2004
    Inventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
  • Nitrogen containing heterobicycles as factor Xa inhibitors
    Patent number: 6716841
    Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: April 6, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Irina C. Jacobson, Mimi L. Quan
  • &bgr;3 adrenergic receptor agonists and uses thereof
    Patent number: 6706743
    Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: March 16, 2004
    Assignee: Pfizer Inc
    Inventors: Robert F. Day, Jennifer A. Lafontaine