Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/156)
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Patent number: 7531656Abstract: Provided are a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a suspension in a dipolar aprotic solvent.Type: GrantFiled: August 14, 2003Date of Patent: May 12, 2009Assignee: Teva Pharmaceuticals USA, Inc.Inventors: Valerie Niddam-Hildesheim, Ben-Zion Dolitzky, Gideon Pilarski, Greta Sterimbaum
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Publication number: 20090118324Abstract: Compounds are provided for use with MEK that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 17, 2008Publication date: May 7, 2009Inventors: Qing DONG, Toufiko Kanounl, Michael B. Wallace
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Publication number: 20090111851Abstract: Compounds having the general structure: which are effective antimicrobial agents.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Benoit Ledoussal, Ji-In Kim Almstead, Jeffery Lyle Gray
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Publication number: 20090105272Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: December 21, 2006Publication date: April 23, 2009Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Ann Hazlewood, Hayley Binch
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Patent number: 7521560Abstract: The present disclosure provides 2-substituted-quinoline compounds that inhibit the IgE receptor signaling cascade that leads to the release of chemical mediators, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and/or prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE receptor signaling cascade.Type: GrantFiled: June 29, 2005Date of Patent: April 21, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Rajinder Singh
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Publication number: 20090099230Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.Type: ApplicationFiled: September 15, 2008Publication date: April 16, 2009Inventors: John DeMattei, Yushi Feng, Cristian Harrison, Adam Looker, Praveen Mudunuri, Stefanie Roeper, Yuegang Zhang
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Publication number: 20090099366Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: September 11, 2008Publication date: April 16, 2009Applicant: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Patent number: 7514451Abstract: To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe.Type: GrantFiled: September 8, 2004Date of Patent: April 7, 2009Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yoshikazu Asahina, Masaya Takei
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Patent number: 7498442Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 13, 2008Date of Patent: March 3, 2009Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul Fatheree, Roland Gendron, Adam A Goldblum, Lan Jiang, Daniel D Long, Daniel Marquess
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Patent number: 7498343Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen.Type: GrantFiled: December 8, 2004Date of Patent: March 3, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Jozef Frans Elisabetha Van Gestel, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Hervé Jean Joseph Poignet, Laurence Françoise Bernadette Decrane, Daniel F. J. Vernier, Frank Christopher Odds
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Publication number: 20090054643Abstract: The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.Type: ApplicationFiled: May 22, 2008Publication date: February 26, 2009Inventors: Laurence BERTHON-CEDILLE, Marie-Emmanuelle Leguern, Gilles Renaud, Francis Tombret
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Publication number: 20090054445Abstract: Compounds of Formula I wherein R1, A, R2, n, R3, m, R4, R5 and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: January 25, 2007Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Jeffrey Albert, Cristobal Alhambra, James Kang, Gerard Koether, Yan Li, Thomas Simpson, James Woods
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Patent number: 7495103Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: June 24, 2005Date of Patent: February 24, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazelwood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20090042819Abstract: The invention describes novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.Type: ApplicationFiled: February 16, 2006Publication date: February 12, 2009Applicant: NitroMed, Inc.Inventors: James L. Ellis, David S. Garvey, Chia-En Lin
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Patent number: 7488739Abstract: A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.Type: GrantFiled: July 22, 2004Date of Patent: February 10, 2009Assignee: Astellas Pharma Inc.Inventors: Susumu Watanuki, Yuji Koga, Hiroyuki Moritomo, Issei Tsukamoto, Daisuke Kaga, Takao Okuda, Fukushi Hirayama, Yumiko Moritani, Jun Takasaki
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Publication number: 20090036684Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2?): wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.Type: ApplicationFiled: March 6, 2007Publication date: February 5, 2009Inventors: Koji Matsuda, Koji Ando, Shigeki Ohki, Jun-ichi Hoshi, Takahiro Yamasaki
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Publication number: 20090029980Abstract: The present invention relates to C-7 isoxazolyl quinoline/naphthyridine derivatives useful as antimicrobial compounds, pharmaceutical compositions comprising said derivatives and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.Type: ApplicationFiled: July 28, 2008Publication date: January 29, 2009Inventors: Mark J. Macielag, Michele A. Weidner-Wells, Shu-Chen Lin
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Patent number: 7482458Abstract: NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.Type: GrantFiled: March 21, 2006Date of Patent: January 27, 2009Assignee: SmithKline Beecham Farmaceutica S.p.A.Inventors: Carlo Farina, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Luca Francesco Raveglia
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Patent number: 7482457Abstract: The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR?R? or C1-6 alkyl-NR?R? where R? and R? are independently chosen from hydrogen and C1-4 alkyl and where R? and R?, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR?R? as defined above or R2 is C1-6 alkoxy substituted by NR?R? as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; oType: GrantFiled: February 3, 2004Date of Patent: January 27, 2009Assignee: Merck Sharp & DohmeInventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod
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Patent number: 7482454Abstract: This invention relates to novel antimicrobial compounds of formula; wherein X, R1, R3, R5, R6, and R8 are defined in the claims, and to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides and imides thereof, and to compositions and uses of such compounds. The invention also relates to compounds derived from these compounds having antimicrobial uses.Type: GrantFiled: December 13, 2005Date of Patent: January 27, 2009Assignee: The Procter & Gamble CompanyInventors: Benoit Ledoussal, Ji-In Kim Almstead, Jeffrey Lyle Gray
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Patent number: 7482455Abstract: 3-carboxy quinoline derivatives, which are useful as YAK3 inhibitors are described herein. The described invention also includes methods of making such 3-carboxy quinoline derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate YAK3 activity.Type: GrantFiled: October 15, 2003Date of Patent: January 27, 2009Assignee: SmithKline Beecham CorporationInventors: Joelle L. Burgess, James F. Callahan, Toshihiro Hamajima, Satoru Ida, Ichiro Mori, Jun Tang
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Publication number: 20090012118Abstract: The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.Type: ApplicationFiled: July 21, 2005Publication date: January 8, 2009Inventors: István Borza, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
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Publication number: 20090012119Abstract: This invention relates to a compound represented by the following formula (1): [F.1] its salt or a hydrate thereof.Type: ApplicationFiled: January 20, 2006Publication date: January 8, 2009Applicant: DAIICHI SANKYO COMPANY LIMITEDInventors: Hisashi Takahasi, Rie Miyauchi, Makoto Takemura
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Patent number: 7468378Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1—R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.Type: GrantFiled: February 3, 2005Date of Patent: December 23, 2008Assignee: Pfizer Inc.Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
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Patent number: 7465799Abstract: The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.Type: GrantFiled: November 9, 2004Date of Patent: December 16, 2008Assignee: WyethInventors: Neelu Kaila, Silvano L. Debernardo, Kristin M. Jantz, Raymond T. Camphausen, Patricia W. Bedard
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080306110Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: September 19, 2006Publication date: December 11, 2008Applicant: ASTRAZENECA ABInventors: Jeffrey S. Albert, Cristobal Alhambra, James Kang, Gerard M. Koether, Thomas R. Simpson, James Woods, Yan Li
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Publication number: 20080300403Abstract: The present invention is directed to a lyophilized preparation which contains a synthetic quinolone antibacterial compound and, as a solo additive, a pH-adjusting agent, and which exhibits an excellent reconstituting property. The invention provides a method for producing a lyophilized preparation containing a synthetic quinolone antibacterial compound as an active ingredient, characterized by including, sequentially, cooling an aqueous solution containing a synthetic quinolone antibacterial compound and a pH-adjusting agent to yield a frozen product, elevating the temperature of the frozen product, and re-cooling the resultant to prepare the lyophilized preparation.Type: ApplicationFiled: September 28, 2006Publication date: December 4, 2008Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: Norihiro Nishimoto
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Patent number: 7456279Abstract: Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.Type: GrantFiled: March 26, 2007Date of Patent: November 25, 2008Assignee: The Procter & Gamble CompanyInventor: Michael Reilly
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Publication number: 20080280902Abstract: The instant invention provides for compounds which comprise substituted quinolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 24, 2006Publication date: November 13, 2008Inventors: Mark E. Fraley, Robert M. Garbaccio, Shaei Y. Huang, Justin T. Steen
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 7442793Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 11, 2003Date of Patent: October 28, 2008Assignee: SmithKline Beecham CorporationInventors: Jinhwa Lee, Siegfried B. Christensen, IV
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Publication number: 20080255190Abstract: To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe. A compound represented by the following formula (1): (wherein R1 represents a C3-C6 cycloalkyl group which may have a substituent or the like; R2 represents a hydrogen atom or the like; R3 and R4 each independently represent a hydrogen atom or a C1-C6 alkyl group, or a substituted carboxyl group derived from an amino acid, a dipeptide, or a tripeptide, and, in the case where each of R3 and R4 represents a C1-C6 alkyl group, the alkyl group may be substituted by one or more atoms or groups selected from among a hydroxyl group, a halogen atom, a C1-C6 alkylthio group, and a C1-C6 alkoxy group; and n denotes an integer of 1 to 3), a salt thereof, and a hydrate of the compound or the salt. Also, antibacterial drugs and therapeutic agents for infectious diseases are prepared.Type: ApplicationFiled: September 29, 2004Publication date: October 16, 2008Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Hisashi Takahashi, Rie Miyauchi, Makoto Takemura
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Publication number: 20080255113Abstract: This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents ?1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1,Type: ApplicationFiled: November 10, 2004Publication date: October 16, 2008Inventors: Tomoki Kato, Kiyoshi Kawamura, Mikio Morita, Chikara Uchida
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Patent number: 7423153Abstract: Provided are novel crystalline forms of gatifloxacin denominated forms A, B, C, D, E1, F, G, H, I, and J, and methods for their preparation. Also provided are methods for making known crystalline forms of gatifloxacin, in particular forms omega and T2RP.Type: GrantFiled: May 12, 2003Date of Patent: September 9, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Valerie Niddam-Hildesheim, Shlomit Wizel, Greta Sterimbaum, Ehud Amir
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Publication number: 20080214605Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: September 19, 2006Publication date: September 4, 2008Applicant: AstraZeneca ABInventors: Jeffrey S. Albert, Gerard M. Koether, Cristobal Alhambra, James Kang, Thomas R. Simpson, James Woods, Yan Li
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Publication number: 20080207618Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.Type: ApplicationFiled: June 22, 2007Publication date: August 28, 2008Inventors: Motohide SATOH, Hisateru Aramaki, Masaki Yamashita, Masafumi Inoue, Hiroshi Kawakami, Hisashi Shinkai, Hiroshi Nakamura, Yuji Matsuzaki, Shuichi Wamaki
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Publication number: 20080194622Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5 n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: June 21, 2006Publication date: August 14, 2008Applicant: AstraZeneca ABInventors: Thomas R. Simpson, James Kang, Jeffrey S. Albert, Cristobal Alhambra, Gerard M. Koether, James Woods, Yan Li
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Publication number: 20080194623Abstract: This invention relates to novel intermediates and processes for preparing pharmaceutically active quinoline compounds, including (?)-(S)—N-(?-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide.Type: ApplicationFiled: August 2, 2006Publication date: August 14, 2008Inventors: Clifford S. Labaw, Peng Liu
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Patent number: 7411067Abstract: Provided are two novel crystalline forms of gatifloxacin, denominated form O and form V, and methods for their preparation.Type: GrantFiled: June 16, 2003Date of Patent: August 12, 2008Assignee: Teva Pharmaceutical Industries LtdInventors: Valerie Niddam-Hildesheim, Shlomit Wizel, Greta Sterimbaum, Ehud Amir
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Patent number: 7402674Abstract: 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments The invention relates to 7-phenylamino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.Type: GrantFiled: January 25, 2005Date of Patent: July 22, 2008Assignee: Sanofi-Aventis Deutschland GmbH,Inventors: Elisabeth Defossa, Dieter Kadereit, Sven Ruf, Thomas Klabunde, Dieter Schmoll, Andreas Herling, Karl-Ulrich Wendt
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Patent number: 7399862Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 4, 2005Date of Patent: July 15, 2008Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul Fatheree, Adam A Goldblum, Lan Jiang, Daniel D Long, Daniel Marquess, S. Derek Turner
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Patent number: 7399434Abstract: An article of manufacture marked with compositions comprising rare earth metal compounds which, due to their luminescence when irradiated with UV light, are suitable in particular for the marking of security-relevant items, such as documents or data carriers.Type: GrantFiled: November 8, 2006Date of Patent: July 15, 2008Assignee: Honeywell International IncInventors: Thomas Potrawa, Joachim Schulz
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Patent number: 7396839Abstract: Provided are novel crystalline forms of gatifloxacin, denominated forms L, M, P, Q, S, and T1, and methods for making them. Also provided are methods of transforming the novel crystalline forms of gatifloxacin of the present invention to other crystalline forms of gatifloxacin.Type: GrantFiled: August 6, 2003Date of Patent: July 8, 2008Assignee: Teva Pharmaceuticals USA, Inc.Inventors: Valerie Niddam-Hildesheim, Shlomit Wizel, Greta Sterimbaum
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Patent number: 7396933Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 4, 2005Date of Patent: July 8, 2008Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul Fatheree, Roland Gendron, Adam A Goldblum, Lan Jiang, Daniel D Long, Daniel Marquess
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Publication number: 20080161340Abstract: Tetrahydroquinolinone and tetrahydronaphthyridone cannabinoid receptor ligand compounds and stereoisomers, mixtures of stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, solvates, acid salt hydrates, and isomorphic crystalline forms thereof are described.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Applicant: CARA THERAPEUTICS, INC.Inventors: Gary R. Gustafson, R. Paul Beckett
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Patent number: 7393957Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: September 20, 2004Date of Patent: July 1, 2008Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Patent number: 7393958Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.Type: GrantFiled: October 30, 2006Date of Patent: July 1, 2008Assignee: Pfizer, Inc.Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
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Publication number: 20080139558Abstract: The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.Type: ApplicationFiled: February 23, 2007Publication date: June 12, 2008Applicant: KALYPSYS, INC.Inventors: Nicholas D. Smith, Jeffrey R. Roppe, Celine Bonnefous, Joseph E. Payne, Hui Zhuang, Xiaohong Chen, Andrew K. Lindstrom, Sergio G. Duron, Christian A. Hassig, Stewart A. Noble
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Publication number: 20080125594Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: September 11, 2007Publication date: May 29, 2008Applicant: Gilead Sciences, Inc.Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer