Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
  • Patent number: 7141567
    Abstract: The invention relates to imidazopyridines of a certain formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion-inhibiting properties.
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: November 28, 2006
    Assignee: Altana Pharma AG
    Inventors: Jörg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann, Bernhard Kohl
  • Patent number: 7132429
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and sulfonamide or sulfamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: November 7, 2006
    Assignee: 3M Innovative Properties Company
    Inventors: George W. Griesgraber, Bryon A. Merrill, Ralph R. Roberts, Ai-Ping Wei
  • Patent number: 7132428
    Abstract: Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.
    Type: Grant
    Filed: July 3, 2003
    Date of Patent: November 7, 2006
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Tahir Nadeem Majid, Corey Hopkins, Brian Leslie Pedgrift, Nicola Collar, Friederike Wirtz-Brugger, Jean Merrill
  • Patent number: 7125990
    Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: October 24, 2006
    Assignee: Bristol-Myers Squibb COmpany
    Inventors: Xiaojun Han, Gene M. Dubowchik, John E. Macor
  • Patent number: 7105676
    Abstract: Compounds of formula (1) in which the substituents have the meanings mentioned in the description, are suitable for the prevention and treatment of gastrointestinal diseases.
    Type: Grant
    Filed: February 23, 2004
    Date of Patent: September 12, 2006
    Assignee: Altana Pharma AG
    Inventor: Jörg Senn-Bilfinger
  • Patent number: 7091214
    Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: August 15, 2006
    Assignee: 3M Innovative Properties Co.
    Inventors: David S. Hays, Shri Niwas, Tushar Kshirsagar, Philip D. Heppner, Bryon A. Merrill, Michael E. Danielson, John F. Gerster, Chad A. Haraldson, Maureen A. Kavanagh, Michael J. Rice, Sarah A. Strong, Joshua R. Wurst
  • Patent number: 7081456
    Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: July 25, 2006
    Assignee: Active Biotech AB
    Inventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
  • Patent number: 7078523
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: July 18, 2006
    Assignee: 3M Innovative Properties Company
    Inventors: Stephen L. Crooks, George W. Griesgraber, Philip D. Heppner, Bryon A. Merrill
  • Patent number: 7060710
    Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: June 13, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
  • Patent number: 7053211
    Abstract: The invention relates to a process for the preparation of ?-aminosubstituted carboxylic acid amide compounds and/or their salts comprising reacting a carboxylic acid amide of a primary amine with a nitrosylating agent in the presence of a base followed by hydrolysis to give a hydroxy imino derivative followed by hydrogenation and if necessary converting a base or acid of the ?-aminosubstituted carboxylic acid amide into one of its salts.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: May 30, 2006
    Assignee: Merck Patent GmbH
    Inventors: Thorsten Hartig, Steffen Enke
  • Patent number: 7053093
    Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
    Type: Grant
    Filed: January 28, 2003
    Date of Patent: May 30, 2006
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
  • Patent number: 7049439
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: May 23, 2006
    Assignee: 3M Innovative Properties Co.
    Inventors: Stephen L. Crooks, George W. Griesgraber, Philip D. Heppner, Bryon A. Merrill
  • Patent number: 7049437
    Abstract: The present invention provides a process of a compound of the formula (I): wherein R is heteroaryl or the like, ring A is a heteroalicyclic group or the like comprising reacting a compound of the formula (II): wherein Hal is halogen and the other symbols are the same as the above, in the presence of a sulfinic acid salt and further in the presence of an acid or a salt with an organic base, and a novel crystal form of 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine phosphate monohydrate.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: May 23, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Fumihiko Matsubara, Takashi Ohya, Masaaki Uenaka
  • Patent number: 7038051
    Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: May 2, 2006
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
  • Patent number: 7030131
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: April 16, 2004
    Date of Patent: April 18, 2006
    Inventors: Stephen L. Crooks, Bryon A. Merrill
  • Patent number: 7018840
    Abstract: The present invention is directed, in part, to fluorescent metal sensors for detecting metal ions, and methods of making and using the same.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: March 28, 2006
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen J. Lippard, Shawn Burdette
  • Patent number: 6989389
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: January 24, 2006
    Assignee: 3M Innovative Properties Co.
    Inventors: Philip D. Heppner, Leslie J. Charles, Joseph F. Dellaria, Bryon A. Merrill, John W. Mickelson
  • Patent number: 6987187
    Abstract: A process for producing amidine derivatives represented by the following reaction scheme, characterized in that the reactions of steps 1 and 3 are conducted in acetonitrile and the reaction of step 2 is conducted in acetone.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: January 17, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiaki Masui, Kyozo Kawata, Takayuki Kasai, Makoto Kakinuma
  • Patent number: 6974824
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: January 8, 2001
    Date of Patent: December 13, 2005
    Assignee: Research Triangle Institute
    Inventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
  • Patent number: 6967205
    Abstract: There are provided novel compounds which have both antibacterial and antiparasitic properties, thereby reducing the need for using several compounds in combined antibacterial and antiparasitic treatment of livestock. The present novel compounds are especially well suited for treatment of coccidiosis, and they are represented by general formula (I) wherein R1-R6, X and A are as defined in the specification.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 22, 2005
    Assignee: New Pharma Research Sweden AB
    Inventor: Shoaá Abdul-Rahman
  • Patent number: 6953804
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: October 11, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Joseph F. Dellaria, John W. Mickelson
  • Patent number: 6949648
    Abstract: Novel pharmaceutical compositions for inhibiting Th2-selective immune response and pharmaceutical compositions for inhibiting cyclooxygenase comprising condensed pyrazole derivatives represented by the general formula (I): or salts thereof.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: September 27, 2005
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Uchikawa, Keita Mitsui, Akiko Asakawa, Shigeru Morimoto, Masataka Yamamoto, Hiroyuki Kimura, Takeo Moriya, Masahiro Mizuno
  • Patent number: 6949649
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: September 27, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Jason D. Bonk, Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
  • Patent number: 6943255
    Abstract: A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-?]pyridine and converting a 7H-imidazo[4,5-c]tetrazolo[1,5-?]pyridine to a 1H-imidazo[4,5-c]pyridin-4-amine.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: September 13, 2005
    Assignee: 3M Innovative Properties Company
    Inventors: Kyle J. Lindstrom, Luke T. Dressel
  • Patent number: 6927292
    Abstract: The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: August 9, 2005
    Assignee: Altana Pharma AG
    Inventors: Jörg Senn-Bilfinger, Peter Jan Zimmermann
  • Patent number: 6924293
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: September 23, 2003
    Date of Patent: August 2, 2005
    Assignee: 3M Innovative Properties Company
    Inventor: Kyle J. Lindstrom
  • Patent number: 6921826
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: July 26, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
  • Patent number: 6916810
    Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as ?v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: July 12, 2005
    Assignee: Merck & Co., Inc.
    Inventors: John H. Hutchinson, Aiwen Li
  • Patent number: 6916825
    Abstract: Compounds of the formula 1 in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: July 12, 2005
    Assignee: Altana Pharma AG
    Inventors: Jörg Senn-Bilfinger, Wilm Buhr
  • Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Patent number: 6906063
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: June 14, 2005
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
  • Patent number: 6900223
    Abstract: The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.
    Type: Grant
    Filed: July 28, 2003
    Date of Patent: May 31, 2005
    Assignee: Wyeth
    Inventors: Neal Jeffrey Green, Steve Yikkai Tam, Jason Shaoyun Xiang, Audrey Molina Davies, Lihren Chen, Gary Paul Stack
  • Patent number: 6897221
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain urea, thiourea, acylurea, or sulfonylurea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: February 17, 2004
    Date of Patent: May 24, 2005
    Assignee: 3M Innovative Properties Company
    Inventors: Stephen L. Crooks, Michael J. Rice
  • Patent number: 6897314
    Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: May 24, 2005
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom
  • Patent number: 6894165
    Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: May 17, 2005
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
  • Patent number: 6888000
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: May 3, 2005
    Assignee: 3M Innovative Properties Company
    Inventors: Stephen L. Crooks, George W. Griesgraber, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
  • Patent number: 6888004
    Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: May 3, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gene M. Dubowchik, Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta, John E. Macor
  • Patent number: 6869949
    Abstract: The invention relates to imidazopyridines of a certain formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion-inhibiting properties.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: March 22, 2005
    Assignee: Altana Pharma AG
    Inventors: Jörg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann, Bernhard Kohl
  • Patent number: 6858621
    Abstract: The present invention is directed to novel 2-(quinolonyl)-fused heterocyclyl derivatives of the general formula (I) wherein R1, R2, R3, R3a, R4, R5, R6 and R7 are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: February 22, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso
  • Patent number: 6852861
    Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: February 8, 2005
    Assignee: Biogal Gyogyszergyar Rt.
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
  • Patent number: 6852730
    Abstract: Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. 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 treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided.
    Type: Grant
    Filed: February 7, 2003
    Date of Patent: February 8, 2005
    Assignee: Neurogen Corporation
    Inventors: George Maynard, Jun Yuan, Stanislaw Rachwal
  • Patent number: 6844089
    Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1; R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R9 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, —OR16, —COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R9 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or —COOR16. The compounds I are partly new.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: January 18, 2005
    Assignee: Sensient Imaging Technologies GmbH
    Inventors: Andreas Richter, Dietmar Keil, Gerhard Diener
  • Patent number: 6841678
    Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.
    Type: Grant
    Filed: July 28, 2003
    Date of Patent: January 11, 2005
    Assignee: Biogal Gyogyszergyar Rt.
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
  • Patent number: 6841556
    Abstract: Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.
    Type: Grant
    Filed: July 3, 2003
    Date of Patent: January 11, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Stefanie Flohr, Thorsten Naumann
  • Patent number: 6838193
    Abstract: This invention features a dipyrazolo-pyridine compound of formula (I): each of R1, R2, R3, and R4, independently, is H, alkyl, alkenyl, cycloalkyl, aryl, or heteroaryl; and each of R5 and R6, independently, is aryl or heteroaryl, or R5 and R6, together with the N atom they are attached to, are heteroaryl. The dipyrazolo-pyridine compound can be used in an electro-luminescence device.
    Type: Grant
    Filed: November 14, 2002
    Date of Patent: January 4, 2005
    Assignee: Academia Sinica
    Inventors: Yu-Tai Tao, Chung-Wen Ko, Chang-Hao Chuen, Jing-Wen Peng
  • Publication number: 20040259904
    Abstract: Compounds having the formula (I) 1
    Type: Application
    Filed: March 3, 2004
    Publication date: December 23, 2004
    Inventors: Yunsong Tong, Akiyo K. Claiborne, Gaoquan Li, Nan-Horng Lin, Hing L. Sham, Thomas J. Sowin, Zhi-Fu Tao
  • Publication number: 20040249147
    Abstract: Methods for producing azole compounds useful as intermediates for antifungal compounds and compositions including reaction of epoxy alcohols with reactants having active hydrogen attached to nitrogen, oxygen or sulfur in the presence of redox coupling agents. In some embodiments, a procedure known as a Mitsunobu reaction is utilized for the transformations.
    Type: Application
    Filed: July 2, 2004
    Publication date: December 9, 2004
    Inventors: Jitendra Sattigeri, Jasbir Singh Arora, Sanjay Malhotra, Ashwani Kumar Verma, Mohammad Salman
  • Patent number: 6825350
    Abstract: The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selected from the group of immune response modifiers comprising imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines and 1,2-bridged imidazoquinoline amines.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: November 30, 2004
    Assignee: 3M Innovative Properties Company
    Inventors: Stephen L. Crooks, Byron A. Merrill
  • Publication number: 20040235882
    Abstract: Compounds of the formula (I), in which the substituents and symbols are as defined in the description are suitable for preventing and treating gastrointestinal disorders.
    Type: Application
    Filed: February 2, 2004
    Publication date: November 25, 2004
    Inventors: Jorg Senn-Bilfinger, Peter Jan Zimmermann
  • Publication number: 20040235883
    Abstract: Compounds of the formula 1, in which the substituents and symbols are as defined in the description are suitable for pre-venting and treating gastrointestinal disorders.
    Type: Application
    Filed: February 2, 2004
    Publication date: November 25, 2004
    Inventors: Jorg Senn-Bilfinger, Peter Jan Zimmermann