Single Bond Between 1,2-positions And Single Bond Between 3,4-positions Patents (Class 546/165)
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Publication number: 20080227979Abstract: The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such quinazolines.Type: ApplicationFiled: March 12, 2008Publication date: September 18, 2008Applicant: NOVALED AGInventors: Josef Saalbeck, Manfred Kussler, Andrea Lux
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Publication number: 20080214823Abstract: A process for preparing amorphous montelukast sodium comprises removing solvent from a solution comprising montelukast sodium using agitated thin film drying.Type: ApplicationFiled: July 20, 2006Publication date: September 4, 2008Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Pratap Reddy Padi, Satyanarayana Bollikonda, Alok Kumar Srivastava, Ravi Kumar Kasturi, Rajender Reddy Jinna, Narsimha Naidu Mopidevi
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Publication number: 20080200451Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: June 2, 2006Publication date: August 21, 2008Inventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Frank Zenke
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Publication number: 20080182874Abstract: The invention provides compounds of formula (I), or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof, in which A, n, p, q, R1, R2, R3 and R4 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.Type: ApplicationFiled: November 28, 2005Publication date: July 31, 2008Applicant: ASTRAZENECA ABInventors: Richard Evans, Rhonan Ford, Toby Thompson, Paul Willis
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Publication number: 20080146611Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: September 14, 2007Publication date: June 19, 2008Applicant: Hydra Biosciences Inc.Inventors: Magdalene M. Moran, Jayhong A. Chong, Christopher Fanger, Amy Ripka, Glenn R. Larsen, Xiaoguang Zhen, Dennis John Underwood, Manfred Weigele
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Publication number: 20080105865Abstract: An object is to provide a pyrene based compound that is good in both properties of light emission and mobility when the compound is used as a light emitting transistor element; and a light emitting transistor element wherein this specific pyrene based compound is used. A pyrene based compound represented by the following chemical formula (1) is used as a main component of a light emitting layer in a light emitting transistor element: (wherein R1 represents a group selected from a heteroaryl group which may have a substituent, an aryl group which may have a substituent except a phenyl group which does not have any substituent, an alkyl group which may have a substituent and has a main chain having 1 to 20 carbon atoms, an alkenyl group which may have a substituent, an alkynyl group which may have a substituent, a silyl group which may have a substituent, and a halogen atom.Type: ApplicationFiled: November 25, 2005Publication date: May 8, 2008Inventors: Takahito Oyamada, Hiroyuki Uchiuzou, Chihaya Adachi, Seiji Akiyama, Takayoshi Takahashi
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Patent number: 7358220Abstract: A polyol polymeric structure comprising a bleach activating moiety to give benefits in detergent compositions such as bleaching action, soil suspension, increased surfactant availability in the presence of free hardness.Type: GrantFiled: February 3, 2005Date of Patent: April 15, 2008Assignee: Procter & Gamble CompanyInventors: Jeffrey John Scheibel, Julie Ann Menkhaus, George Douglas Hiler, II, Marc Eric Gustwiller
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Publication number: 20080081803Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: ApplicationFiled: October 15, 2004Publication date: April 3, 2008Inventors: Gabor Butora, Stephen D. Goble, Alexander Pastemak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
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Patent number: 7342113Abstract: Colorant compositions are useful for a wide variety of product applications. For example, colorants are used in tinting of polymers, providing colors to aqueous solution(s), and affording color to solid or semi-solid products such as detergents. Disclosed herein are colorant compositions having a triphenylmethane (“TPM”) structure having improved stability to alkaline conditions. Thus, the colorant compositions resist decolorization, even at relatively high pH levels.Type: GrantFiled: November 18, 2004Date of Patent: March 11, 2008Assignee: Milliken & CompanyInventors: Eric B. Stephens, Pat Moore
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Patent number: 7312230Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.Type: GrantFiled: September 30, 2005Date of Patent: December 25, 2007Assignee: Roche Palo Alto LLCInventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 7256291Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.Type: GrantFiled: January 22, 2004Date of Patent: August 14, 2007Assignee: Enzo Life Sciences, Inc.Inventors: Jannis G. Stavrianopoulos, Elazar Rabbani
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Patent number: 7226740Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: October 13, 2003Date of Patent: June 5, 2007Assignee: Invitrogen CorporationInventors: Richard P. Haugland, Stephen T. Yue
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Patent number: 7217297Abstract: Composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, which comprises at least one compound chosen from among the direct dyes of the heteroylarylmethane type defined herein, including diheteroylarylmethane and leuco precursors thereof. Furthermore, a method for dyeing keratin fibers, for example, human keratin fibers such as the hair, using the composition and a kit or device containing same.Type: GrantFiled: December 29, 2003Date of Patent: May 15, 2007Assignee: L'Oreal S.A.Inventors: Frédéric Guerin, Alain Lagrange
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Patent number: 7211117Abstract: A composition for dyeing keratin fibers, for example, human keratin fibers, such as hair, comprising at least one dye chosen from heteroyldiarylmethane type direct dyes, for example, monoheteroyidiarylmethane direct dyes, and the leuco precursors thereof; and also to methods for dyeing keratin fibers, for example, human keratin fibers, such as hair, using the composition, and multi-compartment devices.Type: GrantFiled: December 29, 2003Date of Patent: May 1, 2007Assignee: L'Oreal S.A.Inventors: Frédéric Guerin, Alain Lagrange
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Patent number: 7179921Abstract: Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours.Type: GrantFiled: February 22, 2002Date of Patent: February 20, 2007Assignee: School of Pharmacy, University of LondonInventors: Mark Searcey, Laurence Hylton Patterson
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Patent number: 7166617Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.Type: GrantFiled: February 26, 2001Date of Patent: January 23, 2007Assignee: Mitsubishi Pharma CorporationInventors: Haruko Yamabe, Masahiro Okuyama, Akira Nakao, Mitsuru Ooizumi, Ken-ichi Saito
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Patent number: 7145011Abstract: The invention relates to a method for the production of substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acids, i.e. 7,9-dichlor-3a,4,5,9b-tetrahydro-3H-cyclopental[c]quinoline-4-carboxylic acid.Type: GrantFiled: July 22, 2004Date of Patent: December 5, 2006Assignee: Grunenthal GmbHInventor: Michael Thomas Przewosny
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Patent number: 7102007Abstract: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: August 26, 2003Date of Patent: September 5, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller, Narendra Panday
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Patent number: 7084275Abstract: The present invention describes methods for the stereoselective synthesis of heterocyclic enantiomers. The methods of the present invention incorporate the stereo-preferred oxidation of quinolone thiomethyl intermediates by optically active camphor based oxaziridines to provide R(+) or S(?) quinolone methylsulfinyl derivatives.Type: GrantFiled: November 18, 2003Date of Patent: August 1, 2006Assignee: R. T. Alamo Ventures I, LLCInventors: Stefan Kwiatkowski, Miroslaw Golinski, Joseph Kupper
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 6949543Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.Type: GrantFiled: November 8, 2001Date of Patent: September 27, 2005Assignees: Yamanouchi Pharmaceutical Co., Ltd., Rational Drug Design LaboratoriesInventors: Toru Kontani, Junji Miyata, Wataru Hamaguchi, Yoji Miyazaki, Hiroshi Suzuki, Eiichi Nakai, Shunji Kageyama
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Patent number: 6943176Abstract: The present invention relates to methods for the treatment of epilepsy and irritable bowel syndrome.Type: GrantFiled: February 10, 2004Date of Patent: September 13, 2005Assignee: SmithKline Beecham CorporationInventor: Alessandra Orlandi
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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: 6903094Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.Type: GrantFiled: May 10, 2002Date of Patent: June 7, 2005Assignee: Japan Tabacco, Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: 6900319Abstract: The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Abbott GmbH & Co. KGInventors: Hans-Joachim Boehm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
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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: 6844344Abstract: The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotineType: GrantFiled: December 6, 2000Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Patent number: 6841561Abstract: Flavivirus, rhabdovirus and paramyxovirus infections may be treated by administering an inhibitor of the enzyme dihydroorotate dehydrogenase such as 6-fluoro-2-(2?-fluoro-1,1?-biphenyl-4-yl)-3-methyl-4-quinolinearcarboxylic acid sodium salt (Brequinar). A synergistic effect can be obtained if an interferon such as interferon ?2, interferon ?8 or interferon ?, or an inhibitor of a second enzyme selected from inosine monophosphate dehydrogenase, guanosine monophosphate synthetase, cytidine triphosphate synthetase and S-adenosylhomocysteine hydrolase, is also administered.Type: GrantFiled: September 29, 2000Date of Patent: January 11, 2005Assignee: Institute of Molecular and Cell BiologyInventors: Yin Hwee Tan, John Stanford Driscoll, Sim Mui Mui
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Patent number: 6831163Abstract: Disclosed is a molecule containing a first chromophore that exhibits a first absorption maximum above 700 nm and a second chromophore that exhibits a second absorption maximum different from the first absorption maximum, wherein the absorption of the first and second chromophores are substantially independent of each other. The molecule exhibits improved stability.Type: GrantFiled: December 26, 2002Date of Patent: December 14, 2004Assignee: Eastman Kodak CompanyInventors: Ruizheng Wang, Ann L. Carroll-Lee, Kevin W. Williams, Linda A. Kaszczuk, Charles H. Weidner
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Publication number: 20040215018Abstract: 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: ApplicationFiled: October 22, 2003Publication date: October 28, 2004Inventor: Owen Brendan Wallace
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Patent number: 6809107Abstract: This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.Type: GrantFiled: June 14, 2000Date of Patent: October 26, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ramesh M. Kanojia, Alfonzo D. Jordan, Allen B. Reitz, Mark J. Macielag, Boyu Zhao
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Patent number: 6800645Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —Type: GrantFiled: July 7, 2000Date of Patent: October 5, 2004Assignee: Aventis Pharma LimitedInventors: Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
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Publication number: 20040171835Abstract: A compound of formula (I) 1Type: ApplicationFiled: December 18, 2003Publication date: September 2, 2004Inventors: Hisao Tajima, Yoshisuke Nakayama, Tadashi Tatsumi, Daikichi Fukushima
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Patent number: 6784189Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.Type: GrantFiled: November 15, 2002Date of Patent: August 31, 2004Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Publication number: 20040157866Abstract: The present invention relates to compounds of the formula (I) wherein X1 is wherein R1, R2 and R10 are independently hydrogen or a suitable substituent; R11 and R12 are independently hydrogen or a suitable substituent; R is unsaturated 5 to 6-membered heteromonocyclic group; A is direct bond or —NH—; X2 is monocyclic arylene, unsaturated 5 to 6-membered heteromonocyclic group or cycloalkenylene; Y is bivalent group selected from ethylene, trimethylene and vinylene, wherein CH2 is optionally replaced by NH or O, and CH is optionally replaced by N; and Z is —(CH2)n—, —CO—(CH2)m—, —CH═CH— or —CO—NH—, wherein n is 1, 2 or 3 and m is 1 or 2, or a salt thereof. The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.Type: ApplicationFiled: October 30, 2003Publication date: August 12, 2004Inventors: Hisashi Takasugi, Takeshi Terasawa, Yoshikazu Inoue, Hideko Nakamura, Akira Nagayoshi, Yoshiro Furukawa, Masafumi Mikami, Kasumasa Hinoue, Makoto Ohtsubo
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Patent number: 6774086Abstract: There are described derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R1a, R1b, R1c, R2, R3, R4 and R5 are various radicals, X1 is a bridging atom, X2 a carbon chain and X3 a chalcogen atom.Type: GrantFiled: September 10, 2002Date of Patent: August 10, 2004Assignee: Bayer CropScience GmbHInventors: Thomas Seitz, Lothar Willms, Andreas van Almsick, Hermann Bieringer, Thomas Auler, Hubert Menne
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Publication number: 20040152724Abstract: Compounds of formula (I) 1Type: ApplicationFiled: August 12, 2003Publication date: August 5, 2004Inventors: Michael J. Dart, Xenia B. Searle, Karin R. Tietje, Richard B. Toupence
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Patent number: 6770672Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.Type: GrantFiled: February 11, 2000Date of Patent: August 3, 2004Assignee: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 6740649Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.Type: GrantFiled: September 16, 2002Date of Patent: May 25, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Patent number: 6734193Abstract: Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.Type: GrantFiled: June 3, 2003Date of Patent: May 11, 2004Assignee: Allergan, Inc.Inventors: Tien Duong, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 6699877Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I and salts thereof with pharmaceutically acceptable acids. Also disclosed are methods for making the derivative, and pharmaceutical compositions comprising the derivative. Methods for treating pain, migraine, and various other diseases using the pharmaceutical composition are also disclosed.Type: GrantFiled: August 7, 2002Date of Patent: March 2, 2004Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Michael Przewosny, Werner Englberger, Elke Reissmueller, Petra Bloms-Funke, Corinna Maul, Utz-Peter Jagusch
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Patent number: 6664047Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: April 24, 2000Date of Patent: December 16, 2003Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Stephen T. Yue
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Publication number: 20030225281Abstract: The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.Type: ApplicationFiled: September 9, 2002Publication date: December 4, 2003Inventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Publication number: 20030216432Abstract: The present invention relates to certain substituted heterocycles of Formula (200), 1Type: ApplicationFiled: March 6, 2003Publication date: November 20, 2003Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Mohamed Boudejelal, James W. Zapf
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Patent number: 6649764Abstract: The present invention describes methods for the stereoselective synthesis of heterocyclic enantiomers. The methods of the present invention incorporate the stereo-preferred oxidation of quinolone thiomethyl intermediates by optically active camphor based oxaziridines to provide R(+) or S(−) quinolone methylsulfinyl derivatives.Type: GrantFiled: October 25, 2001Date of Patent: November 18, 2003Assignee: R. T. Alamo Ventures I, LLCInventors: Stefan Kwiatkowski, Miroslaw Golinski, Joseph Kupper
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Patent number: 6642228Abstract: There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and &agr;1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for &agr;1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which &agr;1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by &agr;1B adrenoceptor.Type: GrantFiled: April 13, 2001Date of Patent: November 4, 2003Assignee: Toray Industries, Inc.Inventors: Ryoji Hayashi, Eiji Ohmori, Masafumi Isogaya, Mitsuhiro Moriwaki, Hiroki Kumagai
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Patent number: 6630463Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.Type: GrantFiled: July 23, 2001Date of Patent: October 7, 2003Assignee: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Publication number: 20030158178Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.Type: ApplicationFiled: October 30, 2002Publication date: August 21, 2003Applicant: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Publication number: 20030114679Abstract: This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.Type: ApplicationFiled: September 12, 2002Publication date: June 19, 2003Inventors: Ernest J. McEachern, Gary J. Bridger, Krystyna A. Skupinska, Renato T. Skerlj