Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/375)
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Publication number: 20100113430Abstract: The present invention is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for treatment of infectious diseases. The invention furthermore relates to compositions comprising said anti-infective agents.Type: ApplicationFiled: January 7, 2008Publication date: May 6, 2010Applicant: BKG PHARMA APSInventor: Birgit Kjældgaard Giwercman
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Publication number: 20100081203Abstract: The present invention provides novel reactive fluorescent compounds that incorporate stable isotopic (deuterium, 13-carbon, 15-nitrogen, 18-oxygen) substitutions. The invention includes the use of these compounds, in combination with non-isotopically substituted analogs, for the purification, identification and relative quantification of proteins, peptides, saccharides, metabolites, and other biologically important compounds by combining liquid chromatography (LC) and mass spectrometry (MS). Fluorescent labeling of target compounds in this manner provides orders-of-magnitude sensitivity enhancement over traditional stable isotope labels, and also affords the possibility of simultaneous multiplexed analysis due to the multiwavelength nature of different fluorophores.Type: ApplicationFiled: June 19, 2009Publication date: April 1, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Brian Agnew, Kyle Richard Gee
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Publication number: 20100074973Abstract: The present invention relates to new thioxanthene modulators of dopamine D2 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: August 21, 2009Publication date: March 25, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz, Sepehr Sarshar
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Publication number: 20090309076Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.Type: ApplicationFiled: December 5, 2008Publication date: December 17, 2009Applicant: TRANSITIONS OPTICAL, INC.Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Terry A. Kellar, II
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Publication number: 20090312317Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.Type: ApplicationFiled: June 10, 2009Publication date: December 17, 2009Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Jang-Yang Chang, Ching-Chuan Kuo, Yu-Sheng Chao
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Publication number: 20090170870Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu, Cameron Smith
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Publication number: 20090032782Abstract: Various non-limiting embodiments disclosed herein relate to photochromic materials having extended pi-conjugated systems, such as an indeno-fused naphthopyran, which comprises a group that extends the pi-conjugated system of the indeno-fused naphthopyran bonded at the 11-position thereof. Further, the photochromic materials according to certain non-limiting embodiments disclosed herein may display hyperchromic absorption of electromagnetic radiation as compared to conventional photochromic materials and/or may have a closed-form absorption spectrum that is bathochromically shifted as compared to conventional photochromic materials. Other non-limiting embodiments relate to photochromic compositions and photochromic articles, such as optical elements, made using the disclosed photochromic materials, and methods of making the same.Type: ApplicationFiled: June 10, 2008Publication date: February 5, 2009Applicant: TRANSITIONS OPTICAL, INC.Inventors: Beon-Kyu Kim, Jun Deng, Wenjing Xiao, Barry Van Gemert, Anu Chopra
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Publication number: 20090017546Abstract: The present invention provides novel reactive fluorescent compounds that incorporate stable isotopic (deuterium, 13-carbon, 15-nitrogen, 18-oxygen) substitutions. The invention includes the use of these compounds, in combination with non-isotopically substituted analogs, for the purification, identification and relative quantification of proteins, peptides, saccharides, metabolites, and other biologically important compounds by combining liquid chromatography (LC) and mass spectrometry (MS). Fluorescent labeling of target compounds in this manner provides orders-of-magnitude sensitivity enhancement over traditional stable isotope labels, and also affords the possibility of simultaneous multiplexed analysis due to the multiwavelength nature of different fluorophores.Type: ApplicationFiled: July 21, 2008Publication date: January 15, 2009Applicant: INVITROGEN CORPORATIONInventors: Brian Agnew, Kyle Richard Gee
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Publication number: 20080275237Abstract: The invention relates to a method for obtaining pure tetrahydrocannabinol from reaction mixtures containing tetrahydrocannabinol compounds or from raw products containing tetrahydrocannabinol compounds. According to said method, the tetrahydrocannabinol compounds in the reaction mixture or in the raw product are converted into crystallisable derivatives, preferably using a suitable solvent, said derivatives are then crystallised and isolated, and the pure tetrahydrocannabinol compounds are then obtained from the crystallised derivatives. The invention also related to the use of compounds produced in this way for the production of a medicament for human therapy, and to the medicaments thus produced.Type: ApplicationFiled: July 19, 2004Publication date: November 6, 2008Inventors: Enver Arslantas, Ulrich Weigl
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Patent number: 7390898Abstract: Included within the scope of the present invention are potent taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.Type: GrantFiled: February 21, 2003Date of Patent: June 24, 2008Assignee: Immunogen Inc.Inventors: Erkan Baloglu, Michael Miller, Ravi V. J. Chari
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Publication number: 20080146574Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: February 12, 2008Publication date: June 19, 2008Inventors: Darren Whitehouse, Shaojing Hu, Haiquan Fang, Kerry Combs, Michael C. Van Zandt
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Publication number: 20080146545Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: August 10, 2007Publication date: June 19, 2008Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20080064679Abstract: Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.Type: ApplicationFiled: June 23, 2005Publication date: March 13, 2008Inventors: Billy R. Martin, Raj K. Razdan, Anu Mahadevan
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Publication number: 20080027049Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.Type: ApplicationFiled: July 26, 2007Publication date: January 31, 2008Applicant: WYETHInventors: Gregory S. WELMAKER, Matthew A. WILSON, Geraldine R. McFARLANE, Joan E. SABALSKI, John A. BUTERA, Eugene J. Trybulski, David R. HERBST
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Publication number: 20080015200Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: July 10, 2007Publication date: January 17, 2008Inventors: Frank Chavez, Michael P. Curtis, James P. Edwards, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Brad M. Savall
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Patent number: 7271168Abstract: The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and bipolar disorders.Type: GrantFiled: November 8, 2002Date of Patent: September 18, 2007Assignee: Novartis AGInventors: Thomas J. Troxler, Daniel Hoyer
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Patent number: 7223789Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.Type: GrantFiled: April 9, 2004Date of Patent: May 29, 2007Assignee: Glenmark Pharmaceuticals S.A.Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karaunakaran
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Patent number: 7186752Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.Type: GrantFiled: April 26, 2005Date of Patent: March 6, 2007Assignee: SCRASInventors: Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
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Patent number: 7119214Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: April 12, 2005Date of Patent: October 10, 2006Assignee: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Pyrano-quinolines, pyrano-quinolinones, combinations thereof, photochromic compositions and articles
Patent number: 7094368Abstract: Described are compositions of at least one material represented by a pyrano[3,2-c]quinoline structure, a pyrano[3,2-c]quinolinone structure or mixtures thereof. The pyrano[3,2-c]quinoline structure is characterized by having a nitrogen atom at the 6-position ring atom and an oxy-substituent at the 5-position ring atom. The pyrano[3,2-c]quinolinone structure is characterized by having a substituted nitrogen atom at the 6-position ring atom and an oxo-substituent at the 5-position ring atom, the nitrogen atom substituents being hydrogen, aliphatic substituents, cycloaliphatic substituents, aromatic substituents, heteroaromatic substituents or a combination thereof. Both of the pyrano[3,2-c]quinoline and pyrano[3,2-c]quinolinone structures are characterized by having two substituents at the 2-position ring atom. Also described are photochromic articles that contain or that have coatings or films containing at least one of the novel compositions or combinations thereof with other photochromic materials.Type: GrantFiled: December 10, 2003Date of Patent: August 22, 2006Assignee: Transitions Optical, Inc.Inventors: Beon-Kyu Kim, Anil Kumar, Barry Van Gemert -
Patent number: 7074782Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: August 21, 2003Date of Patent: July 11, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
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Patent number: 6821967Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: October 9, 2002Date of Patent: November 23, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Patent number: 6777414Abstract: Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases.Type: GrantFiled: October 5, 2001Date of Patent: August 17, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoto Ohkura, Yukiko Hiraiwa, Tetsuya Matsushima, Kazue Sasaki, Takehiro Yamamoto, Masaharu Shiotani, Shigeki Suzuki, Yuuko Nakatani, Chizuko Kuroda, Mieko Nagasawa, Kiyoaki Katano
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Publication number: 20040097734Abstract: The invention relates to novel aryl- and heteroarylcarboxamides of the general formula (1), their preparation and use as medicaments, in particular for the treatment of tumors.Type: ApplicationFiled: June 27, 2003Publication date: May 20, 2004Inventors: Matthias Gerlach, Peter Emig, Emmanuel Polymeropoulos, Gilbert Muller, Peter Schmidt, Silke Baasner, Eckhard Gunther
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Publication number: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Patent number: 6716987Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z representsType: GrantFiled: December 20, 2001Date of Patent: April 6, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Publication number: 20040058877Abstract: Compounds according to the formula: 1Type: ApplicationFiled: September 8, 2003Publication date: March 25, 2004Applicant: Pfizer IncInventors: Bruce A. Hay, Anthony P. Ricketts, Bridget M. Cole
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Publication number: 20030229083Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1Type: ApplicationFiled: November 27, 2002Publication date: December 11, 2003Applicant: DR. REDDY'S LABORATORIES LIMITEDInventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
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Publication number: 20030212061Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: ApplicationFiled: March 12, 2002Publication date: November 13, 2003Inventor: Simon N. Haydar
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Publication number: 20030199493Abstract: New compounds of general formula I 1Type: ApplicationFiled: March 18, 2002Publication date: October 23, 2003Inventors: Ulrich Jordis, Johannes Frohlich, Matthias Treu, Manfred Hirnschall, Laszlo Czollner, Beate Kalz, Stefan Welzig
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Patent number: 6613762Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined in the specification.Type: GrantFiled: February 6, 2002Date of Patent: September 2, 2003Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Shailaja Kasibhatla, Federico C. Gaeta
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Publication number: 20030114442Abstract: The present invention relates to substituted piperazine derivatives of general formula 1Type: ApplicationFiled: October 8, 2002Publication date: June 19, 2003Inventors: Armin Heckel, Thorsten Lehmann-Lintz, Leo Thomas, Michael Mark
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Patent number: 6514996Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CType: GrantFiled: November 19, 1997Date of Patent: February 4, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Patent number: 6511976Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.Type: GrantFiled: April 6, 2000Date of Patent: January 28, 2003Assignee: Jannsen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
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Patent number: 6492368Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.Type: GrantFiled: March 31, 2000Date of Patent: December 10, 2002Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Hanns Wurziger, Guido Melzer, Horst Juraszyk, Sabine Bernotat-Danielowski
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Publication number: 20020169164Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: ApplicationFiled: March 27, 2002Publication date: November 14, 2002Applicant: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
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Publication number: 20020151552Abstract: The compounds of the formulas described herein, wherein X, R0, R1, R2, n and m have the meanings given in the specification, are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of said compounds as a medicament and for the manufacture of a medicament for the treatment of erectile dysfunction.Type: ApplicationFiled: December 17, 2001Publication date: October 17, 2002Inventor: Adnan Badwan
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Patent number: 6429312Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: March 19, 2001Date of Patent: August 6, 2002Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 6391882Abstract: A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3 to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: February 2, 2001Date of Patent: May 21, 2002Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Ivan Mikkelsen, Christian Korg-Jensen
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Patent number: 6372738Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: August 21, 2001Date of Patent: April 16, 2002Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blatter
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Patent number: 6353102Abstract: Described are novel photochromic naphtho[1,2-b]pyran compounds having certain substituents at the 2 position of the pyran ring, certain substituents at the 5 and 6 positions and optionally at the 7, 8, 9 and 10-positions of the naphtho portion of the compound. These compounds may be represented by the following graphic formula: Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or contact lenses that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: December 17, 1999Date of Patent: March 5, 2002Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6333324Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 26, 1999Date of Patent: December 25, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masahiro Neya, Hitoshi Yamazaki, Natsuko Kayakiri, Kentaro Sato, Teruo Oku
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Patent number: 6323206Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1998Date of Patent: November 27, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Patent number: 6214827Abstract: Novel compounds of Formula are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: June 23, 1998Date of Patent: April 10, 2001Assignee: Schering CorporationInventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
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Patent number: 6156790Abstract: The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.Type: GrantFiled: December 30, 1997Date of Patent: December 5, 2000Assignees: Hauser, Inc., Johns Hopkins UniversityInventors: Gary H. Posner, Soon Hyung Woo, Poonsakdi Ploypradith, Michael H. Parker, Theresa A. Shapiro, Qun Y. Zheng, Christopher Murray, Randall J. Daughenbaugh
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Patent number: 6130101Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.Type: GrantFiled: September 23, 1997Date of Patent: October 10, 2000Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
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Patent number: 6096740Abstract: The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow.Type: GrantFiled: September 28, 1998Date of Patent: August 1, 2000Assignees: Ramot University Authority for Applied Research and Industrial Development Ltd., Yissum Research Develpoment Company of the Hebrew University in JersusalemInventors: Raphael Mechoulam, Emil Pop, Mordechai Sokolovsky, Yoel Kloog, Anat Biegon
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Patent number: 6060468Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6057441Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.Type: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6054458Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and m are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: June 23, 1998Date of Patent: April 25, 2000Assignee: NovoNordiskalsInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Rolf Hohlweg, Uffe Bang Olsen, Erik Fischer, Zdenek Polivka, Kaler Sindelar