Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
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Patent number: 7141567Abstract: 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: GrantFiled: May 24, 2004Date of Patent: November 28, 2006Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann, Bernhard Kohl
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Patent number: 7132429Abstract: 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: GrantFiled: February 28, 2005Date of Patent: November 7, 2006Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Bryon A. Merrill, Ralph R. Roberts, Ai-Ping Wei
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Patent number: 7132428Abstract: 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: GrantFiled: July 3, 2003Date of Patent: November 7, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Tahir Nadeem Majid, Corey Hopkins, Brian Leslie Pedgrift, Nicola Collar, Friederike Wirtz-Brugger, Jean Merrill
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Patent number: 7125990Abstract: 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: GrantFiled: February 4, 2004Date of Patent: October 24, 2006Assignee: Bristol-Myers Squibb COmpanyInventors: Xiaojun Han, Gene M. Dubowchik, John E. Macor
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Patent number: 7105676Abstract: 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: GrantFiled: February 23, 2004Date of Patent: September 12, 2006Assignee: Altana Pharma AGInventor: Jörg Senn-Bilfinger
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Patent number: 7091214Abstract: 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: GrantFiled: December 18, 2003Date of Patent: August 15, 2006Assignee: 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
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Patent number: 7081456Abstract: 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: GrantFiled: November 21, 2003Date of Patent: July 25, 2006Assignee: Active Biotech ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
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Patent number: 7078523Abstract: 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: GrantFiled: October 7, 2003Date of Patent: July 18, 2006Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, George W. Griesgraber, Philip D. Heppner, Bryon A. Merrill
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Patent number: 7060710Abstract: 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: GrantFiled: November 22, 2002Date of Patent: June 13, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 7053211Abstract: 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: GrantFiled: December 11, 2001Date of Patent: May 30, 2006Assignee: Merck Patent GmbHInventors: Thorsten Hartig, Steffen Enke
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Patent number: 7053093Abstract: 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: GrantFiled: January 28, 2003Date of Patent: May 30, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
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Patent number: 7049439Abstract: 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: GrantFiled: October 7, 2003Date of Patent: May 23, 2006Assignee: 3M Innovative Properties Co.Inventors: Stephen L. Crooks, George W. Griesgraber, Philip D. Heppner, Bryon A. Merrill
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Patent number: 7049437Abstract: 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: GrantFiled: March 29, 2001Date of Patent: May 23, 2006Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Matsubara, Takashi Ohya, Masaaki Uenaka
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Patent number: 7038051Abstract: 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: GrantFiled: July 25, 2005Date of Patent: May 2, 2006Assignee: 3M Innovative Properties CompanyInventors: 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
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Patent number: 7030131Abstract: 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: GrantFiled: April 16, 2004Date of Patent: April 18, 2006Inventors: Stephen L. Crooks, Bryon A. Merrill
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Patent number: 7018840Abstract: The present invention is directed, in part, to fluorescent metal sensors for detecting metal ions, and methods of making and using the same.Type: GrantFiled: April 17, 2002Date of Patent: March 28, 2006Assignee: Massachusetts Institute of TechnologyInventors: Stephen J. Lippard, Shawn Burdette
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Patent number: 6989389Abstract: 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: GrantFiled: October 29, 2003Date of Patent: January 24, 2006Assignee: 3M Innovative Properties Co.Inventors: Philip D. Heppner, Leslie J. Charles, Joseph F. Dellaria, Bryon A. Merrill, John W. Mickelson
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Patent number: 6987187Abstract: 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: GrantFiled: July 15, 2002Date of Patent: January 17, 2006Assignee: Shionogi & Co., Ltd.Inventors: Toshiaki Masui, Kyozo Kawata, Takayuki Kasai, Makoto Kakinuma
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Patent number: 6974824Abstract: 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: GrantFiled: January 8, 2001Date of Patent: December 13, 2005Assignee: Research Triangle InstituteInventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6967205Abstract: 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: GrantFiled: November 13, 2000Date of Patent: November 22, 2005Assignee: New Pharma Research Sweden ABInventor: Shoaá Abdul-Rahman
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Patent number: 6953804Abstract: 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: GrantFiled: October 29, 2003Date of Patent: October 11, 2005Assignee: 3M Innovative Properties Co.Inventors: Joseph F. Dellaria, John W. Mickelson
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Patent number: 6949648Abstract: 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: GrantFiled: March 27, 2001Date of Patent: September 27, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Keita Mitsui, Akiko Asakawa, Shigeru Morimoto, Masataka Yamamoto, Hiroyuki Kimura, Takeo Moriya, Masahiro Mizuno
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Patent number: 6949649Abstract: 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: GrantFiled: October 29, 2003Date of Patent: September 27, 2005Assignee: 3M Innovative Properties Co.Inventors: Jason D. Bonk, Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
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Patent number: 6943255Abstract: 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: GrantFiled: May 28, 2004Date of Patent: September 13, 2005Assignee: 3M Innovative Properties CompanyInventors: Kyle J. Lindstrom, Luke T. Dressel
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Patent number: 6927292Abstract: 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: GrantFiled: July 31, 2002Date of Patent: August 9, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Peter Jan Zimmermann
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Patent number: 6924293Abstract: 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: GrantFiled: September 23, 2003Date of Patent: August 2, 2005Assignee: 3M Innovative Properties CompanyInventor: Kyle J. Lindstrom
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Patent number: 6921826Abstract: 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: GrantFiled: October 29, 2003Date of Patent: July 26, 2005Assignee: 3M Innovative Properties Co.Inventors: Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
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Patent number: 6916810Abstract: 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: GrantFiled: September 7, 2001Date of Patent: July 12, 2005Assignee: Merck & Co., Inc.Inventors: John H. Hutchinson, Aiwen Li
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Patent number: 6916825Abstract: 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: GrantFiled: March 28, 2001Date of Patent: July 12, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr
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Patent number: 6916925Abstract: 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: GrantFiled: July 22, 2003Date of Patent: July 12, 2005Assignee: 3M Innovative Properties Co.Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
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Patent number: 6906063Abstract: 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: GrantFiled: August 2, 2001Date of Patent: June 14, 2005Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6900223Abstract: 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: GrantFiled: July 28, 2003Date of Patent: May 31, 2005Assignee: WyethInventors: Neal Jeffrey Green, Steve Yikkai Tam, Jason Shaoyun Xiang, Audrey Molina Davies, Lihren Chen, Gary Paul Stack
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Patent number: 6897221Abstract: 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: GrantFiled: February 17, 2004Date of Patent: May 24, 2005Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, Michael J. Rice
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Patent number: 6897314Abstract: 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: GrantFiled: July 21, 2003Date of Patent: May 24, 2005Assignee: 3M Innovative Properties CompanyInventors: John F. Gerster, Kyle J. Lindstrom
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Patent number: 6894165Abstract: 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: GrantFiled: April 14, 2004Date of Patent: May 17, 2005Assignee: 3M Innovative Properties CompanyInventors: 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
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Patent number: 6888000Abstract: 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: GrantFiled: December 12, 2003Date of Patent: May 3, 2005Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, George W. Griesgraber, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
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Patent number: 6888004Abstract: 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: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Gene M. Dubowchik, Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta, John E. Macor
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Patent number: 6869949Abstract: 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: GrantFiled: October 23, 2001Date of Patent: March 22, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr, Peter Zimmermann, Bernhard Kohl
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Patent number: 6858621Abstract: 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: GrantFiled: April 11, 2003Date of Patent: February 22, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso
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Patent number: 6852861Abstract: 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: GrantFiled: July 23, 2003Date of Patent: February 8, 2005Assignee: Biogal Gyogyszergyar Rt.Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
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Patent number: 6852730Abstract: 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: GrantFiled: February 7, 2003Date of Patent: February 8, 2005Assignee: Neurogen CorporationInventors: George Maynard, Jun Yuan, Stanislaw Rachwal
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Patent number: 6844089Abstract: 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: GrantFiled: May 10, 2002Date of Patent: January 18, 2005Assignee: Sensient Imaging Technologies GmbHInventors: Andreas Richter, Dietmar Keil, Gerhard Diener
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Patent number: 6841678Abstract: 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: GrantFiled: July 28, 2003Date of Patent: January 11, 2005Assignee: Biogal Gyogyszergyar Rt.Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
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Patent number: 6841556Abstract: 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: GrantFiled: July 3, 2003Date of Patent: January 11, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Stefanie Flohr, Thorsten Naumann
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Patent number: 6838193Abstract: 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: GrantFiled: November 14, 2002Date of Patent: January 4, 2005Assignee: Academia SinicaInventors: Yu-Tai Tao, Chung-Wen Ko, Chang-Hao Chuen, Jing-Wen Peng
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Publication number: 20040259904Abstract: Compounds having the formula (I) 1Type: ApplicationFiled: March 3, 2004Publication date: December 23, 2004Inventors: Yunsong Tong, Akiyo K. Claiborne, Gaoquan Li, Nan-Horng Lin, Hing L. Sham, Thomas J. Sowin, Zhi-Fu Tao
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Publication number: 20040249147Abstract: 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: ApplicationFiled: July 2, 2004Publication date: December 9, 2004Inventors: Jitendra Sattigeri, Jasbir Singh Arora, Sanjay Malhotra, Ashwani Kumar Verma, Mohammad Salman
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Patent number: 6825350Abstract: 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: GrantFiled: June 15, 2001Date of Patent: November 30, 2004Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, Byron A. Merrill
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Publication number: 20040235882Abstract: 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: ApplicationFiled: February 2, 2004Publication date: November 25, 2004Inventors: Jorg Senn-Bilfinger, Peter Jan Zimmermann
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Publication number: 20040235883Abstract: 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: ApplicationFiled: February 2, 2004Publication date: November 25, 2004Inventors: Jorg Senn-Bilfinger, Peter Jan Zimmermann