Nitrogen, Other Than As Nitro Or Nitroso, Attached Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/176)
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Publication number: 20090054420Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Applicant: ABBOTT LABORATORIESInventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
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Patent number: 7491733Abstract: The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1. These compounds may be used in the treatment of pathologies associated with insulin resistane syndrome.Type: GrantFiled: February 27, 2002Date of Patent: February 17, 2009Assignee: Merck Patent GmbHInventors: Gerard Moinet, Daniel Cravo
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Publication number: 20090041675Abstract: A medicament comprising, separately or together, (A) a compound of formula I in free or salt or solvate form, where W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 have the meanings as indicated in the specification, and (B) one or more of compounds selected from the group consisting of PDE4 inhibitors and PDE5 inhibitors, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.Type: ApplicationFiled: May 30, 2006Publication date: February 12, 2009Inventor: Alexandre Trifilieff
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Publication number: 20090042806Abstract: Transglutaminase inhibitors and methods of use thereof are provided.Type: ApplicationFiled: August 28, 2006Publication date: February 12, 2009Inventors: Chaitan Khosla, Richard Edward Watts, Matthew John Siegel, Daniel M. Pinkas, Kihang Choi, Keith M. Rich
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Publication number: 20090042875Abstract: The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.Type: ApplicationFiled: September 29, 2008Publication date: February 12, 2009Inventors: George W. Muller, Hon-Wah Man
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Patent number: 7476673Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 7456196Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 5, 2006Date of Patent: November 25, 2008Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Marlon D. Cowart, Huaqing Liu
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Publication number: 20080287399Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: December 12, 2005Publication date: November 20, 2008Applicant: AstraZeneca ABInventors: Jeffrey Scott Albert, Owen Callaghan, James Campbell, Robin Arthur Ellis Carr, Gianni Chessari, Suzanna Cowan, Miles Stuart Congreve, Phil Edwards, Martyn Frederickson, Christopher William Murray, Sahil Patel
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Publication number: 20080281105Abstract: The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.Type: ApplicationFiled: January 18, 2006Publication date: November 13, 2008Applicant: IMMUSOL INCORPORATEDInventors: James E. Macdonald, Michelle K. Hysell, Dehua Yu, Henry Li, Flossie Wong-Staal
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Publication number: 20080269283Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: June 27, 2008Publication date: October 30, 2008Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kukutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
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Publication number: 20080263785Abstract: The present disclosure relates to polycationic monochromophoric hydrazone compounds of following formula (I): wherein W1 is a heteroaromatic radical comprising 5 or 6 ring members, optionally condensed with an aromatic ring comprising 6 ring members, comprising a quaternized nitrogen atom and optionally another heteroatom which may or may not be identical to nitrogen; X, which may or may not be identical, is a nitrogen atom or a CR2 group; Z is a cationic group comprising at least one quaternized nitrogen atom. The present disclosure also relates to a composition for dyeing human keratin fibers comprising the polycationic compounds disclosed herein, and to a dyeing process using the composition of the present disclosure, and even further to multicompartment device.Type: ApplicationFiled: April 14, 2008Publication date: October 30, 2008Inventors: Herve David, Nadege Murguet
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Patent number: 7432282Abstract: Novel indole derivatives of the formula (I), in which X, Y, R1, R1?, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors.Type: GrantFiled: October 30, 2003Date of Patent: October 7, 2008Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Günter Hölzemann, Kai Schiemann, Timo Heinrich, Henning Böttcher, Joachim Leibrock, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20080221152Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: ApplicationFiled: May 20, 2008Publication date: September 11, 2008Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Patent number: 7423154Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.Type: GrantFiled: November 22, 2005Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: William Brown, Niklas Plobeck
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Publication number: 20080214607Abstract: The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.Type: ApplicationFiled: February 27, 2008Publication date: September 4, 2008Inventors: Patrick R. Verhoest, Christopher J. Helal, Dennis J. Hoover, John M. Humphrey
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Patent number: 7417062Abstract: Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.Type: GrantFiled: August 11, 2005Date of Patent: August 26, 2008Assignee: ChemoCentryx, Inc.Inventors: Anita Melikian, John J. Kim Wright
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Publication number: 20080199875Abstract: Embodiments of the present invention provide methods and nucleic acid reporter molecules for the detection of nucleic acid in a sample. The nucleic acid reporter molecule comprises two unsymmetrical cyanine monomer moieties, which may be the same or different, that are covalently attached by a linker comprising at least one aromatic, heteroaromatic, cyclic or heterocyclic moiety comprising 3-20 non-hydrogen atoms selected from the group consisting of O, N, S, P and C. The linker may be rigid, relatively flexible or some degree thereof. The unsymmetrical cyanine monomer moieties comprise a substituted or unsubstituted benzazolium moiety and a substituted or unsubstituted pyridinium or quinolinium moiety that is connected by a methine bridge that is monomethine, trimethine or pentamethine. The linkers form the cyanine dimer compounds by attaching to the pyridinium or quinolinium moiety of the monomer moieties.Type: ApplicationFiled: April 7, 2008Publication date: August 21, 2008Applicant: INVITROGEN CORPORATIONInventors: Stephen Yue, Ching-Ying Cheung
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Patent number: 7411068Abstract: The invention provides reporter compounds based on squaric, croconic, and/or rhodizonic acid, among others, reactive intermediates used to synthesize the reporter compounds, and methods of synthesizing and using the reporter compounds, among others. The reporter compounds relate generally to the following structure Here, Z is a four, five, or six-member aromatic ring, and A, B, C, D, E, and F are substituents of Z, where F is absent when Z is a five-member ring, and where E and F are absent when Z is a four-member ring. A, B, C, D, E, and F are selected from a variety of elements and groups, including but not necessarily limited to O, S, Se, Te, N—Ra, C(Rb)(Rc), W1, and W2.Type: GrantFiled: November 10, 2004Date of Patent: August 12, 2008Inventors: Ewald A. Terpetschnig, Anatoliy Tatarets, Olga Galkina, Iryna Fedyunyaeva, Leonid Patsenker
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Publication number: 20080188520Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.Type: ApplicationFiled: December 12, 2007Publication date: August 7, 2008Applicant: SANOFI-AVENTISInventors: Joachim BRENDEL, Heinrich Christian ENGLERT, Stefan PEUKERT, Klaus WIRTH, Michael WAGNER, Jean-Marie RUXER, Fabienne PILORGE
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Publication number: 20080182855Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines 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 a bacterial disease including a mycobacterial disease, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of bacterial diseases and a process for preparing the claimed compounds.Type: ApplicationFiled: July 26, 2006Publication date: July 31, 2008Inventors: Jerome Emile Georges Guillemont, David Francis Alain Lancois, Elisabeth Therese Jeanne Pasquier, Koenraad Jozef Lodewijk Andries, Anil Koul
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Publication number: 20080182875Abstract: N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof.Type: ApplicationFiled: October 19, 2007Publication date: July 31, 2008Applicant: ASTRAZENECA ABInventors: Khanh Bui, Cathy Dantzman, Glen Ernst, Valerie Hoesch, Thomas Hudzik, Megan Murphy King, Jie Liu, Jingbo Yan
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Publication number: 20080182873Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic residue.Type: ApplicationFiled: March 24, 2008Publication date: July 31, 2008Inventors: Murat Acemoglu, Bernhard Riss
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080153871Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: Abbott LaboratoriesInventors: Erol K. Bayburt, Jerome F. Daanen, Arthur R. Gomtsyan, Steven P. Latshaw, Chih-hung Lee, Robert G. Schmidt
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080146564Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; CI1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono- or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a —S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b1', R10b—C(?O)—O—; and R8 and/or R9 may also beType: ApplicationFiled: March 17, 2006Publication date: June 19, 2008Inventors: Jean-Francois Bonfanti, Jerome Michel Claude Portin, Ismet Dorange
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Publication number: 20080125423Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: July 18, 2007Publication date: May 29, 2008Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. Dewolf, Dalia R. Jakas
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Patent number: 7358261Abstract: This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.Type: GrantFiled: December 16, 2004Date of Patent: April 15, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Michele C. Jetter, Jung S. Lee, Mark A. Youngman
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Patent number: 7351807Abstract: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions.Type: GrantFiled: July 3, 2001Date of Patent: April 1, 2008Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Patent number: 7317102Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: March 31, 2004Date of Patent: January 8, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 7317024Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 12, 2006Date of Patent: January 8, 2008Assignee: Bristol-Myers Squibb Co.Inventor: Bingwei V. Yang
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Patent number: 7291631Abstract: The present invention relates to compounds that bind to chemokine receptors, and having the formula wherein each A, X, Y, R1, R2 and R3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.Type: GrantFiled: April 12, 2004Date of Patent: November 6, 2007Assignee: Genzyme CorporationInventors: Gary J. Bridger, Ernest J. McEachern, Renato Skerlj, Dominique Schols, Ian Baird, Al Kaller, Curtis Harwig, Yongbao Zhu, Gang Chen, Krystyna Skupinska
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Publication number: 20070232648Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where A, B, and R1-R3 are defined herein.Type: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventors: Russell Dahl, Sara Sabine Hadida-Ruah, Leslie A. Robinson
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7262282Abstract: The present invention provides a sensor and methods for determining kinase activity.Type: GrantFiled: April 6, 2004Date of Patent: August 28, 2007Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Melissa D. Shults
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Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
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Patent number: 7250517Abstract: The invention provides reporter compounds based on squaric, croconic, and/or rhodizonic acid, among others, reactive intermediates used to synthesize the reporter compounds, and methods of synthesizing and using the reporter compounds, among others. The reporter compounds relate generally to the following structure: Here, Z is a four, five, or six-member aromatic ring, and A, B, C, D, E, and F are substituents of Z, where F is absent when Z is a five-member ring, and where E and F are absent when Z is a four-member ring.Type: GrantFiled: November 28, 2003Date of Patent: July 31, 2007Inventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Anatoliy Tatarets
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Patent number: 7223776Abstract: The present invention describes novel anti-bacterial compounds of formula (I).Type: GrantFiled: October 9, 2003Date of Patent: May 29, 2007Assignee: Morphochem AGInventors: Jean Phillippe Surivet, Cornelia Zumbrunn, Christian Hubschwerlen, Annabelle Perez Frutos Honer
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7205408Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: GrantFiled: January 22, 2002Date of Patent: April 17, 2007Assignee: SmithKline Beecham, p.l.c.Inventors: David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, William Miller, Neil David Pearson
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Patent number: 7202383Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1–4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.Type: GrantFiled: September 14, 2004Date of Patent: April 10, 2007Assignee: The Hospital For Sick ChildrenInventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
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Patent number: 7189758Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: October 5, 2005Date of Patent: March 13, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David Thomson, Yan Zhang, Renee Michele Zindell
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Patent number: 7173027Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.Type: GrantFiled: January 29, 2002Date of Patent: February 6, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Hongfeng Deng
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Patent number: 7105537Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I wherein Ar1, X, n, R1, R2, R3 and Q are as defined herein.Type: GrantFiled: January 27, 2004Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Roy J. Vaz, John K. Dickson, Jr., Jacques Y. Roberge, Wu Yang, Timur Gungor, James R. Corte, David P. Rotella, Yufeng Wang
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Patent number: 7098222Abstract: Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X?, Y, Y?, Z, Z?, R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 6, 2005Date of Patent: August 29, 2006Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Michael P. Curtis
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7074806Abstract: A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: May 28, 2003Date of Patent: July 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, David Thomson
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Patent number: 7071192Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a diType: GrantFiled: June 20, 2000Date of Patent: July 4, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7041667Abstract: Compounds of Formula 1 [Region ?]—[Region ?]—[Region ?]—[Region ?]??(1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: May 9, 2006Assignee: Pfizer, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards