Chalcogen Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/177)
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Patent number: 7767672Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: November 3, 2006Date of Patent: August 3, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Patent number: 7745463Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: June 15, 2009Date of Patent: June 29, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Ying Han, John F. Kadow, Zhongxing Zhang, Nicholas A. Meanwell
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Publication number: 20100160357Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: October 30, 2009Publication date: June 24, 2010Inventors: Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Publication number: 20100120856Abstract: The invention relates to compounds of the animated hydroxyquinoline type capable of preventing the migration of metastases or tumoral cells. Such compounds are useful for treating cancers.Type: ApplicationFiled: March 25, 2008Publication date: May 13, 2010Applicant: BIOPHARMEDInventors: Jean-Louis Kraus, Olivier Blin, Frederic Champavere
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Publication number: 20100029643Abstract: The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.Type: ApplicationFiled: November 8, 2007Publication date: February 4, 2010Applicant: ASTRAZENECA ABInventors: Gurmit Grewal, Edward Hennessy, Victor Kamhi, Danyang Li, Paul Lyne, Vibha Oza, Jamal Carlos Saeh, Qibin Su, Bin Yang
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Patent number: 7655801Abstract: The present invention relates to new substituted carbamic acid quinoline-6-yl esters of formulae 1 and 2 where R1=alkyl, aryl; R2=H, alkyl, aralkyl useful as acetylcholinesterase inhibitors, and which show potent antiacetylcholinesterase activity and have potential therapeutic use for prevention or cure of acetylcholinesterase related disorders including peripheral as well as central nervous system.Type: GrantFiled: December 28, 2004Date of Patent: February 2, 2010Assignee: Council of Scientific and Industrial ResearchInventors: Neeraj Shakya, Zeeshan Fatima, Chandishwar Nath, Anil Kumar Saxena
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Patent number: 7649094Abstract: The present invention provides a method of kinetic optical resolution of carboxylic acid derivatives using specific optically active catalysts. A racemic or diastereomeric mixture of carboxylic acid derivatives of the formula (A) is reacted with a nucleophile in the presence of an optically active catalyst to form an optically active nucleophile derivative of the formula (B). The catalyst is an optically active compound represented by the formula (C) or (D) [wherein R1 is a substituted or unsubstituted, saturated or unsaturated, straight-chain, branched or alicyclic aliphatic hydrocarbon group which can have a heteroatom, R2 is ethyl or vinyl, and R5 is hydrogen or methoxy respectively].Type: GrantFiled: January 31, 2003Date of Patent: January 19, 2010Assignee: Daiso Co., Ltd.Inventors: Yutaka Ishii, Yasushi Miki, Yoshiro Furukawa, Satoshi Murakami
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Publication number: 20090305285Abstract: Asymmetric cyanine compounds represented by general formula I are provided, wherein X, n, R1, R2, R3, R4 and Y? are as defined in the specification. They have a maximum absorption peak at about 640 nm which may not change with ambient temperature. When the compounds bind a nucleic acid to form a dye/nucleic acid complex, the fluorescence intensity of the complexes will increased rapidly, so that they can be used as a staining agent for nucleic acids in flow cytometers. Their spectra are in the near-infrared region, which can effectively reduce the interference from background fluorescence and improve the accuracy of detection. Moreover, the compounds provided can also be used as a staining agent for blood reticulocytes.Type: ApplicationFiled: June 10, 2009Publication date: December 10, 2009Applicant: SHENZHEN MINDRAY BIO-MEDICAL ELECTRONICS CO., LTD.Inventor: Shao Jianhui
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Publication number: 20090253741Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: ApplicationFiled: June 15, 2009Publication date: October 8, 2009Inventors: Tao Wang, Ying Han, John F. Kadow, Zhongxing Zhang, Nicholas A. Meanwell
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Publication number: 20090227626Abstract: The invention relates to compounds of general formula (I), to the process for the preparation thereof and to the use thereof as a therapeutic agent.Type: ApplicationFiled: August 4, 2006Publication date: September 10, 2009Applicant: PALUMED S.A.Inventors: Céline Deraeve, Marguerite Pitie, Christophe Boldron, Bernard Meunier
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Patent number: 7572810Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: May 16, 2007Date of Patent: August 11, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Ying Han, John F. Kadow, Zhongxing Zhang, Nicholas A. Meanwell
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Publication number: 20090176745Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: December 29, 2008Publication date: July 9, 2009Applicant: Emory UniversityInventor: Jack L. Arbiser
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Patent number: 7550482Abstract: The invention relates to ethynyl-substituted tetrahydroquinolinone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.Type: GrantFiled: August 24, 2005Date of Patent: June 23, 2009Assignee: Merz Pharma GmbH & Co. KGAAInventors: Valerjans Kauss, Ieva Jaunzeme, Aigars Jirgensons, Ivars Kalvinsh, Maksims Vanejevs, Markus Henrich, Wojciech Danysz, Claudia Jatzke, Christopher Graham Raphael Parsons, Tanja Weil
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Patent number: 7541467Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1, R2, R3, and R4 independently represent 2-quinolyl group which may be substituted, 1-isoquinolyl group which may be substituted, or 3-isoquinolyl group which may be substituted; m, n, p, and q independently represent 1 or 2; and L represents a single bond, or an alkylene group having 1 to 5 carbon atoms wherein said alkylene group may contain one or more heteroatoms in the main chain, and may have one or more substituents on the main chain, which is useful as a fluorescent zinc ion sensor.Type: GrantFiled: July 30, 2004Date of Patent: June 2, 2009Assignees: Sekisui Medical Co., Ltd.Inventors: Shigenobu Yano, Yuji Mikata
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Patent number: 7491714Abstract: Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.Type: GrantFiled: December 3, 2003Date of Patent: February 17, 2009Assignee: Glaxo Group LimitedInventors: Jeffrey Michael Axten, Catherine Genevieve Yvette Dartois, Guy Marguerite Marie Gerard Nadler, Neil David Pearson
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Publication number: 20080312273Abstract: The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH— or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.Type: ApplicationFiled: November 29, 2007Publication date: December 18, 2008Inventor: Laurent Francois Andre Hennequin
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Patent number: 7456196Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 5, 2006Date of Patent: November 25, 2008Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Marlon D. Cowart, Huaqing Liu
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Publication number: 20080221161Abstract: Disclosed herein are compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.Type: ApplicationFiled: February 5, 2008Publication date: September 11, 2008Applicant: KALYPSYS, INC.Inventors: Anthony B. Pinkerton, Ayman Kabakibi, Mark R. Herbert, Dana Siegel
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Patent number: 7317102Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: March 31, 2004Date of Patent: January 8, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Publication number: 20070287730Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: ApplicationFiled: May 16, 2007Publication date: December 13, 2007Inventors: Tao Wang, Ying Han, John F. Kadow, Zhongxing Zhang, Nicholas A. Meanwell
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Publication number: 20070270461Abstract: 5,7-Dibromo-8-(2-hydroxyethoxy) quinoline, 5,7-dibromo-8-(2-methoxycarbonylethoxy) quinoline, fungicidal compositions containing these compounds and methods of treating plant diseases with these compounds.Type: ApplicationFiled: May 18, 2006Publication date: November 22, 2007Inventors: Daniel F. Heiman, Peter D. Petracek, Judith A. Fugiel, Prem Warrior
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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: 7223776Abstract: The present invention describes novel anti-bacterial compounds of formula (I).Type: GrantFiled: October 9, 2003Date of Patent: May 29, 2007Assignee: Morphochem AGInventors: Jean Phillippe Surivet, Cornelia Zumbrunn, Christian Hubschwerlen, Annabelle Perez Frutos Honer
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Patent number: 7183299Abstract: The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero ring-substituted oxime derivative. A tetrazoyloxime derivative represented by the general formula (1): X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a cyano group, a methanesulfonyl group, a nitro group, a trifluoromethyl group, or an aryl group; A represents a 1-alkyltetrazoyl-5-yl group or a 5-alkyltetrazoyl-1-yl group; and Het represents a pyridyl group having a substituent or a thiazoyl group having a substituent, and a plant disease controlling agent containing the same as an active ingredient are disclosed.Type: GrantFiled: August 16, 2002Date of Patent: February 27, 2007Assignee: Nippon Soda Co., Ltd.Inventors: Takeo Kobori, Hitoshi Kondo, Hiroyuki Tsuboi, Kumiko Akiba, Akihiro Koiso, Tsuneyuki Otaguro, Hidetoshi Nakayama, Hiroyuki Hamano, Akira Ohno, Toru Asada
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Patent number: 7122672Abstract: Fungicidal compounds of the general formula (1) wherein one of X and Y is N or N-oxide and the other is CR or both of X and Y are NType: GrantFiled: October 27, 2003Date of Patent: October 17, 2006Assignee: Syngenta LimitedInventors: Roger Salmon, Patrick Jelf Crowley
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Patent number: 7105537Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I wherein Ar1, X, n, R1, R2, R3 and Q are as defined herein.Type: GrantFiled: January 27, 2004Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Roy J. Vaz, John K. Dickson, Jr., Jacques Y. Roberge, Wu Yang, Timur Gungor, James R. Corte, David P. Rotella, Yufeng Wang
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Patent number: 7009055Abstract: A dibromomethyl moiety is converted to a sulfonylmethyl moiety by treatment with a sulfinic acid salt. For example, (methyl-sulfonyl)methyl bromo-quinoline is prepared by the treatment of dibromomethyl bromo-quinoline with a sulfinic acid salt.Type: GrantFiled: July 19, 2002Date of Patent: March 7, 2006Assignee: Merck & Co., Inc.Inventors: Feng Xu, Kimberly A. Savary, John M. Williams
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Patent number: 6982334Abstract: The present invention comprises crystalline forms of 3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, represented by the structure: and as characterized herein by powder X-ray diffraction patterns as form A and form B, processes for preparing form A from the purified amorphous form of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, a processes for preparing form A by heating monohydrated form C of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, a pharmaceutical composition comprising form A, a pharmaceutical composition comprising form A and form B or monohydrated form C, a pharmaceutical composition comprising form A, form B and monohydrated form C, a method for treating a bacterial infection with form A, a method for treating a bacterial infection with form A and form B or monohydrated form C, and a method fType: GrantFiled: December 18, 2003Date of Patent: January 3, 2006Assignee: Aventis Pharma S.A.Inventors: Jacques Bourget, Marc Antoine Perrin, Serge Mignani, Bernd Janocha, Michel Cheve, Carole Neves, Pascal Billot, Michel Tabart, Sylvaine Lafont
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Patent number: 6958349Abstract: This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.Type: GrantFiled: March 31, 2003Date of Patent: October 25, 2005Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: John R. Carson, Michele C. Jetter, Jung S. Lee, Mark A. Youngman
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Patent number: 6939970Abstract: The present invention comprises monohydrated form C of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, represented by the structure and as herein defined by powder X-ray diffraction, processes for preparing monohydrated form C from amorphorous (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid or form A of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, pharmaceutical compositions comprising monohydrated form C and form A or form B of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, form A and form B, methods for treating bacterial infection with monohydrated form C, methods for treating bacterial infection with monohydrated formType: GrantFiled: December 18, 2003Date of Patent: September 6, 2005Assignee: Aventis Pharma S. A.Inventors: Jacques Bourget, Marc Antoine Perrin, Bernd Janocha, Carole Neves, Pascal Billot, Sylvaine Lafont
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Patent number: 6841562Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their pType: GrantFiled: September 10, 2003Date of Patent: January 11, 2005Assignee: Aventis Pharma S.A.Inventors: Eric Bacqué, Antony Bigot, Youssef El Ahmad, Jean-Luc Malleron, Serge Mignani, Baptiste Ronan, Michel Tabart, Fabrice Viviani
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Patent number: 6815547Abstract: Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.Type: GrantFiled: March 14, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma S.A.Inventors: Eric Bacque, Serge Mignani, Jean-Luc Malleron, Michel Tabart, Michel Evers, Fabrice Viviani, Youssef El Ahmad, Stéphane Mutti, Christophe Daubié
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Patent number: 6806277Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substitutedType: GrantFiled: July 18, 2003Date of Patent: October 19, 2004Assignee: Aventis, Pharma S.A.Inventors: Eric Bacqué, Jean-Luc Malleron, Serge Mignani, Michel Tabart
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Publication number: 20040176604Abstract: A dibromomethyl moiety is converted to a sulfonylmethyl moiety by treatment with a sulfinic acid salt. For example, (methyl-sulfonyl)methyl bromo-quinoline is prepared by the treatment of dibromomethyl bromo-quinoline with a sulfinic acid salt.Type: ApplicationFiled: January 20, 2004Publication date: September 9, 2004Inventors: Feng Xu, Kimberly A Savary, John M Williams
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Patent number: 6777427Abstract: Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acting excessively on the prostate as AR agonists, but by showing potent action on skeletal muscle tissue and bone tissue; and pharmaceutical compositions comprising the compounds or the salts as active ingredients:Type: GrantFiled: March 13, 2003Date of Patent: August 17, 2004Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Motonori Miyakawa, Seiji Amano, Misa Kamei, Keigo Hanada, Kazuyuki Furuya, Noriko Yamamoto
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Patent number: 6734306Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein X1 and X2 are halo; R1 and R2 are independently hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen or halo; and R5 is (a) —C3-9 diazacycloalkyl optionally substituted with C5-11 azabicycloalkyl; (b) —C3-9 azacycloalkyl-NH—(C5-11 azabicycloalkyl optionally substituted with C1-4 alkyl); (c) —NH—C1-3 alkyl-C(O)—C5-11 diazabicycloalkyl; (d) —NH—C1-3 alkyl-C(O)—NH—C5-11 azabicycloalkyl, the C5-11 azabicycloalkyl being optionally substituted with C1-4 alkyl; (e) —C3-9 azacycloalkyl optionally substituted with C3-9 azacycloalkyl; or (f) —NH—C1-5 alkyl-NH—C(O)—C4-9 cycloalkyl-NH2. These compounds are useful for the treatment of medical conditions mediated by bradykinin such as inflammation, allergic rhinitis, pain, etc.Type: GrantFiled: December 5, 2001Date of Patent: May 11, 2004Assignee: Pfizer, Inc.Inventors: Yasuhiro Katsu, Makoto Kawai, Hiroki Koike, Seiji Nukui
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Patent number: 6689792Abstract: Compounds of formula (1) are provided: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by C, CR4, [[CHR4]] and CHCH2; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or A and B may be concatenated together to form indole, benzimidazole, indolone or indoline moieties; oType: GrantFiled: October 12, 2001Date of Patent: February 10, 2004Assignee: WyethInventors: Michael G. Kelly, Young H. Kang
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Patent number: 6653312Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.Type: GrantFiled: March 16, 2001Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
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Patent number: 6653308Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 15, 2002Date of Patent: November 25, 2003Assignees: Sugen, Inc., Pharmacia & Upjohn CompanyInventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
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Publication number: 20030181724Abstract: Compounds of formula (I), wherein R1 is hydrogen or chlorine and R2 is hydrogen, C1-C8alkyl, or C1-C8alkyl substituted by C1-C6alkoxy or by C3-C6alkenyloxy, can be prepared by: a) introducing the major portion of the amount to be reacted of a compound of formula (II) into a solvent mixture comprising at least one organic solvent capable of forming an azeotrope with water, and at least one aprotic-dipolar solvent; b) metering in an aqueous strong base in an amount equivalent to that major portion of the total amount of the compound of formula (II); c) adding the remaining portion of the amount to be reacted of the compound of formula (II); d) adding a weak base in an amount that is at least equivalent to that remaining portion; e) removing the water from the reaction mixture by azeotropic distillation; f) adding a compound of formula (III), wherein R2 is as defined for formula (I); and g) isolating the resulting compound of formula (I) from the reaction mixture.Type: ApplicationFiled: December 20, 2002Publication date: September 25, 2003Inventor: Karl Scheuzger
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Patent number: 6608066Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.Type: GrantFiled: October 27, 2000Date of Patent: August 19, 2003Assignee: Sunol Molecular CorporationInventors: Jin-An Jiao, Lawrence K. Luepschen, Esperanza L. Nieves, Hing C. Wong, Dean P. Taylor
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Patent number: 6602884Abstract: Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.Type: GrantFiled: March 13, 2002Date of Patent: August 5, 2003Assignee: Aventis Pharma S.A.Inventors: Eric Bacqué, Serge Mignani, Jean-Luc Malleron, Michel Tabart, Michel Evers, Fabrice Viviani, Youssef El Ahmad, Stéphane Mutti, Christophe Daubié
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Publication number: 20020156054Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: ApplicationFiled: March 28, 2001Publication date: October 24, 2002Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Patent number: 6429213Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: June 17, 1999Date of Patent: August 6, 2002Inventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
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Patent number: 6410562Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: GrantFiled: December 8, 2000Date of Patent: June 25, 2002Assignee: Eli Lilly and CompanyInventors: Michael R. Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten, Kumiko Takeuchi, Wolfgang Stenzel
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Patent number: 6403610Abstract: Quinolylpropylpiperidine derivatives of formula (I) which are particularly advantageous antimicrobial agents, their compositions, and their use.Type: GrantFiled: September 18, 2000Date of Patent: June 11, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Luc Malleron, Michel Tabart, Jean-Christophe Carry, Michel Evers, Youssef El Ahmad, Serge Mignani, Fabrice Viviani, Michel Cheve
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Patent number: 6391064Abstract: The use of derivatives of quinoline- or quinoxaline-5,8-diones or -diols in cosmetics, especially for the dyeing of keratinous matter and, in particular, the hair. It also relates to novel compounds of this class. The invention is also directed to dyeing compositions comprising the said compounds and to the method of dyeing keratinous fibers.Type: GrantFiled: August 31, 1999Date of Patent: May 21, 2002Assignee: L'Oreal S.A.Inventors: Richard Baudry, Jean Maignan, Sylvie Genard
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Patent number: 6340697Abstract: Various oxime derivatives are provided, which do not cause any chemical damage to plants and which exhibit sufficient effectiveness against various plant diseases. The oxime derivatives are expressed by two general chemical formulas (1) and (2), as follows. Agricultural chemicals and plant disease control chemicals are also provided which contain the above mentioned oxime derivatives as active ingredients. Test results of these agricultural chemicals and the plant disease control chemicals are proved to be very effective for downey mildews and late blights or Phytophthora rot etc.Type: GrantFiled: June 12, 2000Date of Patent: January 22, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takeo Kobori, Tomoko Goto, Hitoshi Kondo, Hiroyuki Tsuboi, Mika Iiyama, Toru Asada, Takashi Goto
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Patent number: 6310211Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).Type: GrantFiled: September 5, 1997Date of Patent: October 30, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Valerie Ann Vaillancourt, Karen Rene Romines, Arthur Glenn Romero, John Alan Tucker, Joseph Walter Strohbach, Olivier Bezencon, Suvit Thaisrivongs