At 2-position Patents (Class 544/315)
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20100004233Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: February 9, 2007Publication date: January 7, 2010Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Patent number: 7629346Abstract: The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.Type: GrantFiled: May 30, 2007Date of Patent: December 8, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Hans Iding, Matthias Heinrich Nettekoven, Ulrike Obst Sander, Stephan Roever, Urs Weiss, Beat Wirz
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Patent number: 7579362Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: June 26, 2007Date of Patent: August 25, 2009Assignee: Novartis AGInventors: Dominik Feuerbach, Konstanze Hurth, Timothy J Ritchie
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Publication number: 20090197901Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.Type: ApplicationFiled: January 7, 2009Publication date: August 6, 2009Applicant: PHARMA MAR, S.A.Inventors: Modesto Remuinan, Juan Jose Gonzalez, Carlos del Pozo, Andres Francesh, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Regan James Anderson, Jonathan Charles Morris
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Publication number: 20090192179Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: February 26, 2009Publication date: July 30, 2009Inventors: Bing Wang, Jian Chen
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Publication number: 20090176766Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.Type: ApplicationFiled: January 5, 2009Publication date: July 9, 2009Applicant: National Health Research InstitutesInventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yen-Shian Wu, Sheng-Ju Hsu, Yueh Andrew Yueh, Yu-Sheng Chao
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Patent number: 7547704Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: December 6, 2004Date of Patent: June 16, 2009Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, Universita Degli Studi di CagliariInventors: Paola LaColla, Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
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Patent number: 7538072Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1-C7 alkoxy, C3-C7 alkenyloxy, C3-C7 alkynyloxy, C5-C7 cycloalkoxy, {(C1-C7 alkoxy)carbonyl} C1-C3 alkoxy, (C1-C7 alkylamino)oxy, {di(C1-C7 alkyl)amino}oxy, (C3-C7 alkylideneamino)oxy, C1-C7 alkylamino, di(C1-C7 alkyl)amino, C3-C7 alkenylamino, C3-C7 alkynylamino, C5-C7 cycloalkylamino, {(C1-C7 alkoxy)carbonyl} C1-C3 alkylamino, or (C1-C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1-C3 alkyl, or C1-C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.Type: GrantFiled: June 16, 2006Date of Patent: May 26, 2009Assignee: Sumitomo Chemical Company, LimitedInventor: Nobuaki Mito
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Publication number: 20090111820Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Inventors: Kenneth GRANBERG, Bjorn HOLM
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090069355Abstract: The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: ApplicationFiled: November 6, 2008Publication date: March 12, 2009Inventors: Michael Philip Clark, Steven Karl Laughlin, Adam Golebiowski, Todd Andrew Brugel, Mark Sabat
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Patent number: 7482356Abstract: The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2?]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2?]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: GrantFiled: November 5, 2004Date of Patent: January 27, 2009Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Steven Karl Laughlin, Adam Golebiowski, Todd Andrew Brugel, Mark Sabat
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Patent number: 7473695Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 maybe the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 20, 2004Date of Patent: January 6, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Patent number: 7470686Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.Type: GrantFiled: July 18, 2007Date of Patent: December 30, 2008Assignee: Laboratoires Serono SAInventors: Serge Halazy, Dennis Church, Monstserrat Camps, Pascale Gaillard, Jean-Pierre Gotteland
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Patent number: 7462619Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.Type: GrantFiled: April 1, 2005Date of Patent: December 9, 2008Assignee: Merck & Co., Inc.Inventors: Nicholas D. Cosford, Jeffrey R. Roppe, Lida R. Tehrani, Nicholas D. Smith, Brian Stearns, Dehua Huang, Bowei Wang, Thomas J. Seiders
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Publication number: 20080221127Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: March 5, 2008Publication date: September 11, 2008Inventors: Jack Lin, Patrick Womack, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Publication number: 20080096220Abstract: An affinity ligand-matrix conjugate comprises the matrix and conjugated thereto by the group Z, a ligand having general formula (I): wherein one X is N and the other X is N, CCL or CCn; A1 and A2 are each independently O, S or N-R1 and R1 is H, C1-6 alkyl, C1-6 hydroxyalkyl, benzyl or ?-phenylethyl; B1 and B2 are each independently an optionally substituted hydrocarbon linkage containing from 1 to 10 carbon atoms; D1 is H or a primary amino, secondary amino, tertiary amino, quaternary ammonium, imidazole, guanidine or amidino group; and D2 is a secondary amino, tertiary amino, quaternary ammonium, imadazole, guanidine or amidino group; or B2-D2 is —CHCOOH—(CH2)3-4—NH2; and p is 0 or 1. Such conjugates are useful for the separation, isolation, purification, characterization, identification or quantification of an endotoxin.Type: ApplicationFiled: August 14, 2006Publication date: April 24, 2008Inventors: Christopher Robin Lowe, Kim Hilary Lawden
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Patent number: 7351700Abstract: The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.Type: GrantFiled: February 23, 2005Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Pari Malherbe, Raffaello Masciadri, Eric Prinssen, Will Spooren, Andrew William Thomas
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Patent number: 7317014Abstract: The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them.Type: GrantFiled: July 21, 2003Date of Patent: January 8, 2008Assignees: Orchid Research Laboratories, Ltd., Bexel Pharmaceuticals Inc.Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Patent number: 7312329Abstract: An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to theType: GrantFiled: December 3, 2004Date of Patent: December 25, 2007Assignee: Glenmark Pharmaceuticals LimitedInventors: Narendra Joshi, Shekhar Bhaskar Bhirud, Batchu Chandrasekhar, K. Eswara Rao, Subhash Damle
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Patent number: 7312209Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.Type: GrantFiled: December 20, 2002Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 7304156Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: GrantFiled: July 12, 2002Date of Patent: December 4, 2007Assignee: AstraZeneca UK LimitedInventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Patent number: 7301021Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: May 17, 2002Date of Patent: November 27, 2007Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ralph F. Hall
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Patent number: 7297694Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 20, 2007Assignee: SmithKline Beechum P.L.C.Inventors: David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
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Patent number: 7288544Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally.Type: GrantFiled: March 14, 2003Date of Patent: October 30, 2007Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Kayo Otani, Seiji Niwa, Satoshi Iwayama, Akira Takahara, Hajime Koganei, Yukitsugu Ono, Shinichi Fujita, Tomoko Takeda, Masako Hagihara, Akiko Okajima
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7259162Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.Type: GrantFiled: December 20, 2000Date of Patent: August 21, 2007Assignee: Applied Research Systems Ars Holding N.V.Inventors: Serge Halazy, Dennis Church, Montserrat Camps, Pascale Gaillard, Jean-Pierre Gotteland
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Patent number: 7244692Abstract: The invention relates to novel substituted benzoylcyclohexanediones of formula (I) in which A1 represents a single bond or represents alkanediyl (alkylene) having 1 to 3 carbon atoms, A2 represents alkanediyl (alkylene) having 1 to 3 carbon atoms, and R1, R2, R3, R4 and R5 are each as defined in the disclosure, and to novel intermediates, to processes for their preparation and to their use as herbicides.Type: GrantFiled: September 20, 2004Date of Patent: July 17, 2007Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Hans-Georg Schwarz, Stefan Lehr, Otto Schallner, Dorothee Hoischen, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 7238697Abstract: The present invention relates to novel pyridylpyrimidines of the formula in which R1, R2, X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing these compounds, and to their use for controlling pests. This invention further relates to novel intermediates and process for their preparation.Type: GrantFiled: February 11, 2002Date of Patent: July 3, 2007Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Mazen Es-Sayed, Rüdiger Fischer, Fritz Maurer, Christoph Erdelen, Peter Lösel
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Patent number: 7232905Abstract: The present invention provides a process for the preparation of substituted dihydropyrimidinones using polyaniline salts as reusable catalysts, which comprises reacting an aldehyde, a ?-keto ester and urea/thiourea in the presence of a polyaniline salt catalyst and separating the substituted dihydropyrimidinone obtained.Type: GrantFiled: March 26, 2004Date of Patent: June 19, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Palaniappan Srinivasan, Vaidya J. Rao, Gangadasu Banda
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Patent number: 7192572Abstract: A composition comprising (a) from 0.005% to 0.5% by weight of a cooling compound; (b) from 0.1% to 10% by weight of an emulsifiable substance; (c) from 0.15% to 15% by weight of a surfactant; (d) optionally up to 5% by weight, preferably from 0.05% to 5% by weight of a cosurfactant.Type: GrantFiled: December 18, 2003Date of Patent: March 20, 2007Assignee: Conopco, Inc.Inventors: Ingrid Anne Marie Appelqvist, Mark Emmett Malone, Asish Nandi
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Patent number: 7179806Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests.Type: GrantFiled: November 22, 2001Date of Patent: February 20, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Thomas Seitz, Johannes Rudolf Jansen, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7166597Abstract: Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, R2, and R4 are various substituent groups, are protein kinase inhibitorsType: GrantFiled: August 22, 2001Date of Patent: January 23, 2007Assignee: Glaxo Group LimitedInventors: Michael John Alberti, Ian Robert Baldwin, Mui Cheung, Stuart Cockerill, Stephen Flack, Philip Anthony Harris, David Kendall Jung, Gregory Peckham, Michael Robert Peel, Jennifer Gabriel Badiang, Kirk Stevens, James Marvin Veal
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Patent number: 7144888Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 8, 2003Date of Patent: December 5, 2006Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7141569Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: March 21, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham CorporationInventors: Mui Cheung, Kristjan Gudmundsson, Brian A. Johns
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Patent number: 7119097Abstract: A compound of the formula pharmaceutically acceptable salts and enantiomers thereof and pharmaceutical compositions containing this compound, its pharmaceutically acceptable salts and enantiomers are claimed.Type: GrantFiled: March 16, 2006Date of Patent: October 10, 2006Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 7109205Abstract: Carboxylic acid derivatives where R–R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: June 24, 2003Date of Patent: September 19, 2006Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Müller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 7109148Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl} C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl} C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.Type: GrantFiled: May 31, 2001Date of Patent: September 19, 2006Assignee: Sumitomo Chemical Company, LimitedInventor: Nobuaki Mito
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Patent number: 7098331Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.Type: GrantFiled: March 5, 2003Date of Patent: August 29, 2006Assignee: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve
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Patent number: 7067664Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: May 30, 2000Date of Patent: June 27, 2006Assignees: Pfizer Inc., Pfizer Products Inc.Inventor: Yuhpyng L. Chen
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Patent number: 7064136Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: December 20, 2001Date of Patent: June 20, 2006Assignee: AstraZeneca ABInventor: Ashokkumar Bhikkappa Shenvi
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Patent number: 7060707Abstract: Isoquinoline derivatives of the general formula (I) in which X, Y, Z, R1, R2 and n are as defined in Patent Claim (1), and physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammation, tumors, osteoporosis, infections and restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.Type: GrantFiled: February 7, 2003Date of Patent: June 13, 2006Assignee: Merck Patent GmbHInventors: Matthias Wiesner, Simon Goodman, Horst Kessler, Georgette Thumshirn, Dirk Weber, Dirk Gottschling
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Patent number: 7026478Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1-M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.Type: GrantFiled: May 10, 2002Date of Patent: April 11, 2006Assignee: Studiengesellschaft Kohle mbHInventors: Alois Fürstner, Andreas Leitner, María Méndez
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Patent number: 7026327Abstract: The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and B(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of where defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkylType: GrantFiled: May 23, 2002Date of Patent: April 11, 2006Assignee: Glaxo Group LimitedInventors: Alan Naylor, Jeremy John Payne, Neil Anthony Pegg
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Patent number: 6936616Abstract: Selective MMP-13 inhibitors are pyrimidine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R2 is hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.Type: GrantFiled: February 13, 2002Date of Patent: August 30, 2005Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, William Chester Patt
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Patent number: 6919346Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.Type: GrantFiled: December 2, 2003Date of Patent: July 19, 2005Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
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Patent number: 6878717Abstract: This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally subsType: GrantFiled: November 1, 1999Date of Patent: April 12, 2005Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken