Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Quinoline Ring System Patents (Class 546/168)
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Patent number: 7193086Abstract: A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde important as intermediate for the synthesis of pharmaceuticals, efficiently from an unnecessary antipode, is provided. A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde represented by the formula (III): which comprises treating a compound represented by the formula (I) or (II): (wherein A is —CHOH or —C(O)—, and R is a hydrogen atom, a C1-4 alkyl group which may be branched, a phenyl group, an alkali metal ion or an alkaline earth metal ion) with ozone, followed by reduction with an inorganic sulfur compound or by hydrogenation for reduction decomposition.Type: GrantFiled: May 15, 2002Date of Patent: March 20, 2007Assignees: Nissan Chemical Industries, Ltd., Daicel Chemical Industries, Ltd.Inventors: Hiroo Matsumoto, Takanori Shimizu
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Patent number: 7186841Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.Type: GrantFiled: August 26, 2004Date of Patent: March 6, 2007Assignees: Amgen Inc., Syntex (U.S.A.) LLCInventors: Michelle F. Browner, David L. Clark, Timothy D. Cushing, Xiaolin Hao, Ronald C. Hawley, Xiao He, Juan C. Jaen, Sharada S. Labadie, Marie-Louise Smith, Francisco X. Talamas, Nigel P. C. Walker, Marc Labelle
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Patent number: 7148237Abstract: A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.Type: GrantFiled: February 27, 2002Date of Patent: December 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Fuji, Hidenori Mikamiyama, Hitoshi Murai
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Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7067533Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.Type: GrantFiled: April 13, 2001Date of Patent: June 27, 2006Assignee: Daiichi Asubio Pharma Co., Ltd.Inventors: Naohiro Takemoto, Hirokazu Annoura, Norihito Murayama
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Patent number: 7056931Abstract: The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: May 9, 2002Date of Patent: June 6, 2006Assignee: Eli Lilly and CompanyInventor: Owen Brendan Wallace
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Patent number: 7053105Abstract: This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: September 18, 2001Date of Patent: May 30, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René Angibaud, Marc Gaston Venet, Isabelle Noëlle Constance Pilatte
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Patent number: 7041664Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.Type: GrantFiled: June 14, 2004Date of Patent: May 9, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, George Maynard, Alan Hutchison
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Patent number: 6930104Abstract: The object of the present invention is to provide soluble ?-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: [wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group, etc., Ar1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].Type: GrantFiled: April 25, 2002Date of Patent: August 16, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Kakihana, Kaneyoshi Kato, Masaaki Mori, Toshiro Yamashita
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Patent number: 6903103Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): wherein: X represents carbonyl, sulphonyl or sulphoxide, G1, G2 and G3 are as defined in the description, T represents a fused phenyl group or a fused pyridyl group, R1 represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, R2a and R2b, which are the same or different, are as defined in the description, R3 represents aryl or heteroaryl-A as defined in the description, each of which groups may optionally be substituted, Y represents aryloxy, heteroaryloxy or heteroaryl-B as defined in the description, each of which groups may optionally be substituted, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically aType: GrantFiled: February 20, 2003Date of Patent: June 7, 2005Assignee: Les Laboratories ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6897319Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: December 10, 2002Date of Patent: May 24, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Ellen E. Codd, Philip M. Pitis
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Patent number: 6875769Abstract: This invention relates to compounds of the formula wherein A, B, D, E, K, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.Type: GrantFiled: January 6, 2003Date of Patent: April 5, 2005Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 6855711Abstract: Use of a compound of formula (I), wherein R1 is H or hydrocarbyl; R2 is a hydrophobic radical; R3 is 3-(C2-C6)acyl-4-hydroxyphenyl, 3-hydroxyimino (C2-C6)-alkyl-4-hydroxyphenyl, or COOZ, wherein Z is H, (C1-C6) alkyl, aryl, aryl or ar(C1-C6) alkyl; and n is 1-20; and of a compound of formula (II), wherein R4 is (C1-C6) alkyl, cyano (C1-C6) alkyl, (C1-C6) alkoxy (C1-C6) alkyl or —CH2NR7R8, wherein R7 and R8, the same or different, is each H or (C1-C6) alkyl, or together with the N atom form a saturated or unsaturated 5-7 membered ring optionally containing a further heteroatom selected from N, O or S, the further N atom being optionally substituted, and either R5 is H and R6 is (C2-C6) acyl or hydroxyimino (C2-C6) alkyl, or R5 and R6 together with the phenyl ring form a quinoline, a 1,2,3,4-tetrahydroquinoline or a perhydroquinoline ring, for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease or stroke.Type: GrantFiled: June 7, 2000Date of Patent: February 15, 2005Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.Inventors: Rivka Warshawsky, Moussa B. H. Youdim, Dorit Ben-Shachar, Abraham Warshawsky
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Patent number: 6852748Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 15, 2003Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz
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Patent number: 6831089Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.Type: GrantFiled: October 8, 2002Date of Patent: December 14, 2004Assignee: Schering CorporationInventors: Yuguang Wang, Samuel Chackalamannil
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Patent number: 6831083Abstract: Using a compound selected from compounds represented by the following formula (1) (which include 3-phenyl-2-pyrazoline derivatives and 3-phenyl-tetrahydropyridazine derivatives) and pharmacologically acceptable salts thereof, an agent is provided which can activate glutamic acid transporter and which is useful for prevention and/treatment of cerebral ischemia (cerebral infarct and brain edema), amyotrophic lateral sclerosis (ALS), etc., all caused by glutamic acid toxicity.Type: GrantFiled: September 20, 2002Date of Patent: December 14, 2004Assignee: Mitsui Chemicals, Inc.Inventors: Junya Fujiwara, Kazuya Sakai, Kenji Kibayashi, Fumiki Shimada, Yoshio Shiga, Shiro Takagi
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Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors
Patent number: 6825352Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: August 30, 2002Date of Patent: November 30, 2004Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan -
Patent number: 6780868Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: February 20, 2003Date of Patent: August 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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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: 6770648Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: July 30, 2002Date of Patent: August 3, 2004Assignee: Tularik Inc.Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
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Publication number: 20040147750Abstract: A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde important as intermediate for the synthesis of pharmaceuticals, efficiently from an unnecessary antipode, is provided.Type: ApplicationFiled: December 1, 2003Publication date: July 29, 2004Inventors: Hiroo Matsumoto, Takanori Shimizu
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Publication number: 20040122234Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: ApplicationFiled: June 3, 2003Publication date: June 24, 2004Inventors: Kenneth Lee Hauser, Jeffrey Alan Dodge, Mark Louis Heiman, Scott Alan Jones, Charles Arthur Alt, Henry Uhlman Bryant, Jeffrey Daniel Cohen, James Densmore Copp, Kennan Joseph Fahey, William Harlan Gritton, Louis Nickolaus Jungheim, Joseph Henry Kennedy, Charles Willis Lugar, Brian Stephen Muehl, Alan David Palkowitz, Andrew Michael Ratz, Gary Anthony Rhodes, Roger Lewis Robey, David Edward Seyler, Timothy Alan Shepherd, Kenneth Jeff Thrasher, William George Trankle
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Publication number: 20040073034Abstract: A process for producing quinoline-3-carboxylic acid represented by formula 1Type: ApplicationFiled: September 24, 2003Publication date: April 15, 2004Inventors: Susumu Nishizawa, Sadanobu Yoshikawa
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Publication number: 20040063758Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.Type: ApplicationFiled: October 25, 2002Publication date: April 1, 2004Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanandan E. Velu
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Patent number: 6710056Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: GrantFiled: June 5, 2002Date of Patent: March 23, 2004Assignee: Ajinomoto Co., Inc.Inventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Publication number: 20040048867Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: May 2, 2003Publication date: March 11, 2004Applicant: Neurogen CorporationInventors: Guolin Cai, Jun Yuan, Kevin Currie, Pamela Albaugh, Alan Hutchison
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Publication number: 20040049031Abstract: This invention relates to novel intermediates and processes for preparing pharmaceutically active quinoline compounds, including (−)-(S)-N-(&agr;-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide.Type: ApplicationFiled: May 20, 2003Publication date: March 11, 2004Applicant: SmithKline Beecham CorporationInventors: Mark Mellinger, Conrad Kowalski
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Publication number: 20040034011Abstract: Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: July 9, 2003Publication date: February 19, 2004Inventors: Reijo Bckstrm, Jarmo Pystynen, Timo Lotta, Martti Ovaska, Jyrki Taskinen
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Patent number: 6689769Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: GrantFiled: November 29, 2001Date of Patent: February 10, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Publication number: 20030232989Abstract: A new process for the preparation of specific aromatic aldehydes by ozonolysis of aromatic alkenes is provided. This new process can be advantageously integrated into a synthesis of specific chiral diols using aromatic aldehydes of this type.Type: ApplicationFiled: April 14, 2003Publication date: December 18, 2003Inventors: Stefan Antons, Joachim Rehse, Herbert Diehl, Christian Laue
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Publication number: 20030232988Abstract: Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described. Also described are methods for making an alpha amino ketone synthon that enables facile syntheses of bisindole compounds, including topsentins and dragmacidins.Type: ApplicationFiled: December 5, 2002Publication date: December 18, 2003Inventors: David A. Horne, Kenichi Yakushijin
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Publication number: 20030212101Abstract: A compound, or a solvate or a salt thereof, of formula (I): 1Type: ApplicationFiled: February 5, 2003Publication date: November 13, 2003Applicant: SmithKline Beecham S.p.A.Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Marcel Morvan, Guy Marguerite Marie Gerard Nadler, Luca Francesco Raveglia
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20030195227Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: September 18, 2002Publication date: October 16, 2003Applicant: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Publication number: 20030181481Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: ApplicationFiled: December 10, 2002Publication date: September 25, 2003Inventors: John R. Carson, Ellen E. Codd, Philip M. Pitis
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Patent number: 6620947Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: August 26, 2002Date of Patent: September 16, 2003Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
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Patent number: 6605615Abstract: Hydrazones and hydrazone analogs are provided which are useful as upregulators of LDL receptors and can be used in the treatment of hypercholesterolemia and related disorders and conditions.Type: GrantFiled: March 1, 2001Date of Patent: August 12, 2003Assignee: Tularik Inc.Inventors: Julio C. Medina, Hirohiko Hasegawa
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Publication number: 20030149046Abstract: Using a compound selected from compounds represented by the following formula (1) 1Type: ApplicationFiled: September 20, 2002Publication date: August 7, 2003Inventors: Junya Fujiwara, Kazuya Sakai, Kenji Kibayashi, Fumiki Shimada, Yoshio Shiga, Shiro Takagi
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Patent number: 6596735Abstract: The invention relates to compounds of the formula: and to pharmaceutically acceptable salts and solvates thereof wherein Y, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings defined in the specification. The invention also relates to pharmaceutical compositions comprising said compounds and to the use of said compounds for inhibiting abnormal cell growth in mammals. The compounds of the above formula have activity as farnesyl protein transferase inhibitors.Type: GrantFiled: November 28, 2000Date of Patent: July 22, 2003Assignee: Pfizer IncInventor: Bingwei V. Yang
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Publication number: 20030134874Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: September 16, 2002Publication date: July 17, 2003Inventors: Francine S. Grant, Bradley S. Johnson, Michael A. Pleiss, Eugene D. Thorsett
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Publication number: 20030114680Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enal is prepared in a high yield by reducing 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrite with Raney nickel either in the presence of formic acid and 0.25 to 1 part by volume of water per part by volume of formic acid or in the presence of both an amine salt of formic acid and an organic acid.Type: ApplicationFiled: November 20, 2002Publication date: June 19, 2003Inventors: Katsumasa Harada, Shigeyoshi Nishino, Hidetaka Shima, Takashi Harada, Naoako Okada
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Publication number: 20030109517Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.Type: ApplicationFiled: September 16, 2002Publication date: June 12, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan Jose Marugan Sanchez, Kristin D. Haslow, Jonathan Hall
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Publication number: 20030109547Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: ApplicationFiled: June 5, 2002Publication date: June 12, 2003Applicant: AJINOMOTO CO. INCInventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Publication number: 20030105088Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: ApplicationFiled: January 17, 2002Publication date: June 5, 2003Applicant: GUILFORD PHARMACEUTICALS INC.Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
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Publication number: 20030096828Abstract: The invention relates to compounds represented by the following general formula (1): 1Type: ApplicationFiled: June 19, 2002Publication date: May 22, 2003Applicant: KOWA CO., LTD.Inventors: Hiroyuki Ishiwata, Seiichi Sato, Mototsugu Kabeya, Soichi Oda, Yukio Hattori, Makoto Suda, Manabu Shibasaki, Hiroshi Nakao, Takao Nagoya
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Patent number: 6562977Abstract: The present invention is concerned with mixed anhydrides. The mixed anhydrides are prepared by adding an adjuvant base to a mixture of acid and reactive acid derivative. The mixed anhydrides play an role primarily in activating and coupling reactions.Type: GrantFiled: December 6, 2001Date of Patent: May 13, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6562976Abstract: The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by customary methods. The tetrahydroquinolines are suitable as active compounds in medicaments, in particular in medicaments. for the treatment of arteriosclerosis and dyslipidaemias.Type: GrantFiled: April 15, 2002Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Jürgen Stoltefuss, Michael Lögers, Arndt Brandes, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt
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Patent number: 6559163Abstract: Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: August 16, 2001Date of Patent: May 6, 2003Assignee: Neurogen CorporationInventors: Guolin Cai, Jun Yuan, Kevin Currie, Pamela Albaugh, Alan Hutchison
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Publication number: 20030083523Abstract: A compound represented by the following general formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: May 1, 2003Applicant: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe