1,4-benzothiazines Patents (Class 544/51)
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Publication number: 20080260754Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: ApplicationFiled: March 21, 2008Publication date: October 23, 2008Inventors: Hui Li, Vanessa Taylor, Somasekhar Bhamidipati, John Ramphal, Kin Tso, Avinder Sran, Holger Keim, Vadim Markovtsov, David Carroll, Sambaiah Thota, Ankush Argade, Jeffrey Wayne Clough, Rajinder Singh, Robin Cooper
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Publication number: 20080255102Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: June 23, 2008Publication date: October 16, 2008Applicant: WyethInventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
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Patent number: 7348426Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: April 25, 2000Date of Patent: March 25, 2008Assignees: Dr. Reddy's Laboraties Limited, Dr. Reddy's Research FoundationInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Ranga Madhavan Gurram, Ramanujam Rajagopalan, Chakrabarti Ranjan
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Publication number: 20080058320Abstract: The invention relates to novel amino alcohols of the general formula (I) where X, R1, R2, R3, R4, R5 and R6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.Type: ApplicationFiled: March 17, 2005Publication date: March 6, 2008Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Michael Quirmbach, Dirk Behnke, Christiane Marti
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Publication number: 20070265252Abstract: The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.Type: ApplicationFiled: May 10, 2007Publication date: November 15, 2007Inventors: Gee-Hong Kuo, Aihua Wang, Thomas Rano, Catherine Prouty, Keith T. Demarest, Patricia Pelton
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Patent number: 7141564Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7049312Abstract: Q is —N=or CR2 X is S, O or NOR3 Y is —O—, —S—, —SO— or —SO2— R and R1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl group R2 is H or a substituent R3 is H, or —C(O)R4 R4 is a substituted or unsubstituted aliphatic or aromatic group n is an integer from 0 to 1 Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.Type: GrantFiled: June 2, 2000Date of Patent: May 23, 2006Assignee: Abbott GmbH & Co. KGInventors: Paul Rafferty, David Calderwood, Lee Arnold, Beatriz Gonzalez Pascual, Jose L. Ortego Martinez, Maria J. Perez de Vega, Isabel Fernandez
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6919332Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 28, 2003Date of Patent: July 19, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
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Patent number: 6914059Abstract: Compounds of formula I, their tautomeric and isomeric forms and salts, as well as the process for their production and their use in pharmaceutical agents are described.Type: GrantFiled: April 12, 2001Date of Patent: July 5, 2005Assignee: Schering AGInventors: Hartmut Rehwinkel, Peter Hoelscher, Stefan Jaroch, Detlev Suelzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdonald McDonald
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Patent number: 6897305Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities thereof.Type: GrantFiled: December 8, 1999Date of Patent: May 24, 2005Assignee: Theravance, Inc.Inventors: Yu-Hua Ji, Maya Natarajan, John H. Griffin, Thomas E. Jenkins
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Patent number: 6809095Abstract: A method for preventing or treating complications of diabetes by administering a compound of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates.Type: GrantFiled: March 29, 2001Date of Patent: October 26, 2004Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Publication number: 20040138214Abstract: Disclosed are substituted xanthines of general formula 1Type: ApplicationFiled: October 28, 2003Publication date: July 15, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Patent number: 6716851Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 12, 2001Date of Patent: April 6, 2004Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, Bao Nguyen, Azra Pervin
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Publication number: 20040058915Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or &agr;v&bgr;5 integrin. The ring A-B, is selected from the group consisting of the formula II all optionally substituted and bonded to X and Z1 at any position.Type: ApplicationFiled: August 18, 2003Publication date: March 25, 2004Inventors: Ish Kumar Khanna, Yi Yu, Devadas Balekudra, Hwang-Fun Lu, Nizal S. Chandrakumar
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Patent number: 6696435Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines.Type: GrantFiled: May 23, 2002Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040005986Abstract: Novel pyridazin-3-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is haloalkyl; R2 and R3 are the same or different and are hydrogen, alkyl, haloalkyl, or alkoxyalkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4], or [Q-5]. Also provided are their use and intermediates for their production.Type: ApplicationFiled: October 3, 2002Publication date: January 8, 2004Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
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Patent number: 6667302Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, 0, (C1-C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: June 13, 2001Date of Patent: December 23, 2003Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. La Voie, Jung Sun Kim, Leroy Fong Liu
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Uracil derivatives as inhibitors of TNF-alpha converting enzyme (TACE) and matrix metalloproteinases
Publication number: 20030229081Abstract: The present application describes novel uracil derivatives of formula I:Type: ApplicationFiled: March 14, 2003Publication date: December 11, 2003Inventor: Thomas P. Maduskuie -
Publication number: 20030203907Abstract: The present invention relates to a compound of the general formula (I): 1Type: ApplicationFiled: January 31, 2003Publication date: October 30, 2003Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Publication number: 20030187256Abstract: This invention discloses benzoxazinone and benzothiazinone compounds which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: ApplicationFiled: November 12, 2002Publication date: October 2, 2003Inventors: Kent Alan Berryman, Dennis Michael Downing, Danette Andrea Dudley, Jeremy John Edmunds, Lakshmi Sourirajan Narasimhan, Stephen Taras Rapundalo
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Patent number: 6620809Abstract: The invention relates to compound of formula (I): wherein: G represents an alkylene chain containing from 1 to 4 carbon atoms, A represents X represents oxygen or sulphur and R2 and R1 are as defined in the description and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: December 5, 2000Date of Patent: September 16, 2003Assignee: Les Laboratoires ServierInventors: Marie-Claude Viaud, Gérald Guillaumet, Philippe Daubos, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Publication number: 20030139399Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: ApplicationFiled: February 4, 2003Publication date: July 24, 2003Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
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Publication number: 20030139400Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: ApplicationFiled: February 6, 2003Publication date: July 24, 2003Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
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Patent number: 6573218Abstract: A compound of the formula (Ia): or its salts, in which the variables are as described in the disclosure; herbicidal compositions of said compounds, herbicidal processes using said compounds, defoliant processes using said compounds, and processes for preparing said compounds.Type: GrantFiled: July 5, 2001Date of Patent: June 3, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Masamitsu Tsukamoto, Sandeep Gupta, Shao-Yong Wu, Bai-Ping Ying, David A. Pulman
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Patent number: 6566520Abstract: A method for the preparation and purification of compounds using a novel support, a tetrabenzo [a, c, g, i]-fluorene group (Tbf) comprising reacting a building block (A) containing a Tbf group (Tbf-A), with a second building block (B), to afford an intermediate compound (Tbg-A-B) followed by purifying the intermediate compound by adsorption on a carbon support, removing the intermediate compound from the support with a solvent and repeating the previous reactions using the required number of building blocks to synthesize the compounds followed by removal of the Tbf group to afford the desired compounds.Type: GrantFiled: April 14, 1999Date of Patent: May 20, 2003Assignee: Warner-Lambert CompanyInventors: Sheila Helen DeWitt, Robert Ramage, Alasdair Arthur MacDonald
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Publication number: 20030073127Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities thereof.Type: ApplicationFiled: December 8, 1999Publication date: April 17, 2003Inventors: YU-HUA JI, MAYA NATARAJAN, JOHN H. GRIFFIN, THOMAS E. JENKINS
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Publication number: 20030065173Abstract: Pyridone-fused azabicyclic compounds of the formula 1Type: ApplicationFiled: February 14, 2001Publication date: April 3, 2003Inventor: Brian T. O'Neill
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Publication number: 20020165226Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: ApplicationFiled: April 11, 2002Publication date: November 7, 2002Inventors: Frank P. DiNinno, Jane Y. Wu, Seongkon Kim, Helen Y. Chen
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Publication number: 20020156276Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.Type: ApplicationFiled: April 23, 2002Publication date: October 24, 2002Inventors: Naoto Ohkura, Takashi Tsuruoka, Takayuki Usui, Yukiko Hiraiwa, Tetsuya Matsushima, Masaharu Shiotani, Tetsutaro Niizato, Yuuko Nakatani, Shigeki Suzuki, Chidsuko Kuroda, Kiyoaki Katano
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Publication number: 20020143009Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1Type: ApplicationFiled: March 4, 2002Publication date: October 3, 2002Applicant: Pharmacia & UpjohnInventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Paul D. Johnson
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Publication number: 20020142993Abstract: The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: ApplicationFiled: October 10, 2001Publication date: October 3, 2002Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Om Reddy Gaddam, Chandra Sekhar Batchu, Ramabhadra Sarma Mamillapalli, Prasad Sivarama Addanki
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Patent number: 6455519Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N- disubstituted fused-heterocyclo amines.Type: GrantFiled: November 15, 2001Date of Patent: September 24, 2002Assignee: G.D. SEarle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6448246Abstract: Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. 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: May 25, 2000Date of Patent: September 10, 2002Assignee: Neurogen CorporationInventors: Guolin Cai, Gang Liu, Pamela A. Albaugh
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Patent number: 6448241Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.Type: GrantFiled: May 24, 2001Date of Patent: September 10, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-François Peyronel
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Patent number: 6444615Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Dow AgroSciences LLCInventors: Bin Li, Ying Man, Zongjian Zhang, Adam Chi-Tung Hsu
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Patent number: 6437141Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: April 2, 2001Date of Patent: August 20, 2002Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
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Patent number: 6432946Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: Ar represents aryl or heteroaryl; R1 and R2 are the same or different and represent organic or inorganic substituents; R5 is hydrogen or C1-C6 alkyl; W represents CH or nitrogen; X is oxygen or sulfur; and A represents an alkylene group, which compounds bind selectively with high affinity to the dopamine D4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.Type: GrantFiled: August 4, 2000Date of Patent: August 13, 2002Assignee: Neurogen corporationInventor: Xiao-shu He
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Publication number: 20020082258Abstract: A method for preventing or treating complications of diabetes by administering a compound of formula (I) 1Type: ApplicationFiled: March 29, 2001Publication date: June 27, 2002Applicant: DR. REDDY'S RESEARCH FOUNDATION & REDDY- CHEMINOR, INC.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6380235Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitutType: GrantFiled: April 19, 2000Date of Patent: April 30, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20010051619Abstract: Compounds of formula (I) 1Type: ApplicationFiled: March 23, 2001Publication date: December 13, 2001Applicant: DR. REDDY'S RESEARCH FOUNDATION AND REDDY-CHEMINOR, INC.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Publication number: 20010047018Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: March 27, 2001Publication date: November 29, 2001Inventors: Michael J. Genin, Fred L. Ciske
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Patent number: 6300342Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.Type: GrantFiled: December 9, 1999Date of Patent: October 9, 2001Assignee: Boehringer Ingelheim Pharm KGInventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
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Publication number: 20010021709Abstract: Compounds of the formula I 1Type: ApplicationFiled: April 26, 2001Publication date: September 13, 2001Applicant: Merck Patent Gesellschaft mit Beschrankt PatentsInventors: Beate Diefenbach, Simon L. Goodman, Joachim Marz, Peter Raddatz, Friedrich Rippmann, Matthias Wiesner
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Publication number: 20010020098Abstract: A cyanine dye having the formula 1Type: ApplicationFiled: April 2, 2001Publication date: September 6, 2001Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, David George Ahern, Mark Norman Bobrow
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Patent number: 6265401Abstract: Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.Type: GrantFiled: May 27, 1998Date of Patent: July 24, 2001Assignees: Reddy-Cheminor, Inc., Dr. Reddy's Research FoundationInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6232310Abstract: The present invention relates to fused 1,4-thiazine-2-carbonitrile derivatives, compositions thereof and methods for preparing the compounds. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.Type: GrantFiled: March 8, 2000Date of Patent: May 15, 2001Assignee: Novo Nordisk A/SInventors: Holger Claus Hansen, Tina Møller Tagmose, John Bondo Hansen
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Patent number: 6224644Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: May 1, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
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Patent number: 6204389Abstract: A cyanine dye having the formula wherein R1--R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: March 20, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow