Pyridine Ring Or Partially Hydrogenated Pyridine Ring Patents (Class 546/193)
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Patent number: 7125887Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: October 9, 2001Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: Jeffrey J. Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Yuan Cheng, legal representative, Christopher A. Willoughby, deceased
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Patent number: 7122666Abstract: Compounds having activity against production of an inflammatory cytokine of formula (I)?: A? is pyrrole; R1? is phenyl or naphthyl; R2? is pyridyl or pyrimidinyl; R3? is (IIa)?, (IIb)? or (IIc)?: m? is 1; E? is nitrogen; D? is >C(R5?)—, R5? is hydrogen, Substituent ?? or Substituent ??; B? is nitrogen-containing 5-membered heterocyclic; R4? is 1 to 3 substituents from Substituent ??, Substituent ?? and Substituent ??; R1? and R3? are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2?; Substituent ?? is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa?Rb?; Ra? and Rb? are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra? and Rb? with the nitrogen atom form a heterocyclyl; Substituent ?? is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent ?? is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.Type: GrantFiled: January 30, 2003Date of Patent: October 17, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Akira Nakao, Nobuyuki Ohkawa, Takayoshi Nagasaki, Takanori Yamazaki
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Patent number: 7122551Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: February 26, 2004Date of Patent: October 17, 2006Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Robert Ian Dowell, Maurice Raymond Verschoyle Finlay, Nicholas John Newcombe, Howard Tucker, David Waterson
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Patent number: 7119098Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the ???3 and/or the ???5 integrin without significantly antagonizing the IIb/IIIa integrin.Type: GrantFiled: June 15, 2001Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
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Patent number: 7109215Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.Type: GrantFiled: June 27, 2001Date of Patent: September 19, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patricia McCaffrey, Perry M Novak, Michael Mullican
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Patent number: 7109216Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1–R4 have the meanings given in the specification.Type: GrantFiled: August 6, 2004Date of Patent: September 19, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Arnoldus H. J. Herremans, Herman H. van Stuivenberg
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Patent number: 7105505Abstract: Disclosed are novel compounds of the formula wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substituted aryl or heteroaryl; M1 and M2 are C(R3) or N; and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.Type: GrantFiled: April 16, 2003Date of Patent: September 12, 2006Assignee: Schering CorporationInventors: Qingbei Zeng, Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Jianhua Cao, Joseph A. Kozlowski, Pietro Mangiaracina, Kevin D. McCormick, Mwangi W. Mutahi, Stuart B. Rosenblum, Neng-Yang Shih, Daniel M. Solomon, Wing C. Tom
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7091353Abstract: The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-? in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.Type: GrantFiled: December 21, 2001Date of Patent: August 15, 2006Assignee: Celgene CorporationInventors: Michael J. Robarge, Roger Shen-Chu Chen, George W. Muller, Hon-Wah Man
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Patent number: 7084159Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, Ra, R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; Lck and Src kinase. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 14, 2003Date of Patent: August 1, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Young-Choon Moon, Jian Wang, Mark Ledeboer, Edmund Harrington, Huai Gao
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Patent number: 7084145Abstract: The invention provides compounds of formula (I), the pharmaceutically acceptable salts and solvates thereof, wherein A, B, R1, R2, and R7 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof as vasopressin V1A antagonists.Type: GrantFiled: October 24, 2003Date of Patent: August 1, 2006Assignee: Pfizer Inc.Inventors: Robert Duncan Armour, Andrew Douglas Baxter, Justin Stephen Bryans, Kevin Neil Dack, Patrick Stephen Johnson, Russell Andrew Lewthwaite, Julie Newman, David James Rawson, Thomas Ryckmans
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Patent number: 7077873Abstract: A subject-matter of the disclosure is a novel composition for the dyeing of human keratinous fibres, for example, the hair, comprising a monocationic monoazo dye of formula (I) W1-N?N—W2-NW3-W4-W5, the dyeing processes employing it, the use of the dyes of formula (I) as direct dyes and the novel compounds of formula (I).Type: GrantFiled: September 10, 2003Date of Patent: July 18, 2006Assignee: L'Oréal, SAInventors: Hervé David, Nathalie Berteuil, Laurent Vidal
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Patent number: 7071177Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 26, 2001Date of Patent: July 4, 2006Assignee: Syntex (U.S.A.) LLCInventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
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Patent number: 7071201Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 2, 2001Date of Patent: July 4, 2006Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 7067533Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.Type: GrantFiled: April 13, 2001Date of Patent: June 27, 2006Assignee: Daiichi Asubio Pharma Co., Ltd.Inventors: Naohiro Takemoto, Hirokazu Annoura, Norihito Murayama
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Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
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Patent number: 7064135Abstract: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: GrantFiled: October 9, 2002Date of Patent: June 20, 2006Assignee: Novo Nordisk Inc.Inventor: Florencio Zaragoza Dörwald
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Patent number: 7057042Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.Type: GrantFiled: May 23, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
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Patent number: 7030141Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: October 23, 2002Date of Patent: April 18, 2006Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Patent number: 7022716Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: December 27, 2002Date of Patent: April 4, 2006Assignee: WyethInventors: Baihua Hu, Fuk-Wah Sum, Michael Sotirios Malamas
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Patent number: 7005437Abstract: The present invention relates to new substituted aryl and heteroaryl derivatives of general formula wherein A, Ar, n, X, Y1, Y2, Y3, Y4, R1 and R5 are defined as in claim 1, the prodrugs, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. Thus, the compounds of the above general formula I wherein R5 does not contain a cyano group have, in particular, an antithrombotic effect and a selective factor Xa-inhibiting effect with generally improved compatibility. The compounds of the above general formula I wherein R5 contains a cyano group are valuable intermediate products for preparing the antithrombotic compounds of general formula I.Type: GrantFiled: May 10, 2002Date of Patent: February 28, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Henning Priepke, Uwe Ries, Herbert Nar, Wolfgang Wienen, Jean-Marie Stassen
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Patent number: 6998401Abstract: There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1 and E2 are oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is pheny group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins.Type: GrantFiled: March 24, 2003Date of Patent: February 14, 2006Assignee: Suntory LimitedInventors: Hirokazu Annoura, Naohiro Takemoto, Hiroshi Uramoto
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Patent number: 6995268Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: June 14, 2001Date of Patent: February 7, 2006Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6989448Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: September 25, 2002Date of Patent: January 24, 2006Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
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Patent number: 6989393Abstract: The invention concerns compounds of formula (I), wherein the variables are defined herein; processes for preparing them, compositions comprising them and their use in modulating CCR5 receptor activity.Type: GrantFiled: March 6, 2001Date of Patent: January 24, 2006Assignee: AstraZeneca ABInventors: Jeremy Burrows, John Cumming, Thomas Mcinally
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Patent number: 6984649Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: March 28, 2003Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 6984652Abstract: Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylaxis of bacterial infections in mammals. The compounds are believed to function by inhibiting gyrase B.Type: GrantFiled: May 17, 2004Date of Patent: January 10, 2006Assignee: Warner-Lambert Company LLCInventors: Kraig Yager, Shaosong Chu, Krzysztof Appelt, Xiaoming Li
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Patent number: 6979690Abstract: This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2 and R3 are independently hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen or C1-6 alkyl; R6 is hydrogen, C1-12 alkyl, C1-6 alkoxy (C1-6)alkyl or C1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R7 and R8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R9 is C1-6 alkyl or C3-8 cycloalkyl; R10 is C1-6 alkyl or NR11R12; L is (CR11R12)n or NR11; M is NR11 or (CR11R12)n; R11 and R12 are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C1-6 alkyl; with the proviso that when R9 iType: GrantFiled: January 7, 2003Date of Patent: December 27, 2005Assignee: Pfizer Inc.Inventors: Geoffrey Gymer, Kiyoshi Kawamura, Sachiko Mihara, Mikio Morita, Alan Stobie, Chikara Uchida, Seiji Nukui
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Patent number: 6977263Abstract: Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.Type: GrantFiled: April 26, 2001Date of Patent: December 20, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Peter C. Astles, Paul R. Eastwood, Olivier Houille, Julian Levell, Heinz Pauls, Mark Czekaj, Guyan Liang, Yong Gong, James Pribish, Kent Neuenschwander
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Patent number: 6977260Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6958331Abstract: The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.Type: GrantFiled: June 2, 2000Date of Patent: October 25, 2005Assignee: Novartis AGInventors: Christopher Thomas Brain, William Cantrell, Andrew James Culshaw, Edward Karol Dziadulewicz, Terance William Hart, Timothy John Ritchie, Liladhar Waykole
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Patent number: 6949547Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: May 28, 2003Date of Patent: September 27, 2005Assignee: Chiron CorporationInventors: John M. Nuss, Savithri Ramurthy
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Patent number: 6932960Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.Type: GrantFiled: March 18, 2004Date of Patent: August 23, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Shuang Liu
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Patent number: 6930116Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.Type: GrantFiled: March 24, 2003Date of Patent: August 16, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, Dean Stamos, Michael Badia, Anne Laure Grillot, Steven Ronkin, Martin Trudeau
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Patent number: 6927295Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X? derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: April 24, 2003Date of Patent: August 9, 2005Assignee: Ciba Specialty Chemicals Corp.Inventors: Andreas Kramer, Peter Nesvadba
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Patent number: 6924296Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: August 6, 2001Date of Patent: August 2, 2005Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, John Joseph Masters, Jason Scott Sawyer, Robert Theodore Shuman, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6906084Abstract: The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.Type: GrantFiled: November 21, 2002Date of Patent: June 14, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Marc Nazaré, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
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Patent number: 6903085Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditionsType: GrantFiled: August 18, 2000Date of Patent: June 7, 2005Assignee: AstraZeneca, ABInventors: Stephen Thom, Andrew Baxter, Nicholas Kindor, Thomas McInally, Brian Springthorpe, Matthew Perry, David Harden, Richard Evans, David Marriott
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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: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
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Patent number: 6878725Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: June 12, 2001Date of Patent: April 12, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6875767Abstract: The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: June 19, 2002Date of Patent: April 5, 2005Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, George D. Hartman
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Patent number: 6867220Abstract: The invention relates to compounds of formula (I) where R1 represents a hydrogen or halogen atom or an —S(O)z—(C1-C4)alkyl, —S(O)z—(C1-C4)R3, —SO2—NH—(C1-C4)alkyl, —NHCO(C1-C4) alkyl, —CO(C1-C4)alkyl or —NHSO2—(C1-C4)alkyl group; m and n independently represent 0, 1 or 2; A represents a group of formula (a) or (b): where X is N or CH; R2 represents an —SO2—R3, —CO—R3 or —CO—(C1-C4)—alkyl group; R3 represents a phenyl group, optionally substituted by a (C1-C4)alkyl or (C1-C4)alkoxy group, one or two halogen atoms or a heterocycle; R4 represents a hydrogen or halogen atom or a (C1-C6)alkyl, (C1-C4)alkoxy, —COOH, —COO(C1-C4)alkyl, —CN, —CONR5R6, —NO2, —NHSO2(C1-C4)alkyl or —SO2NR5R6 group; z is 1 or 2; R5 and R6 independently represent a hydrogen atom or a (C1-C4)alkyl, phenyl or phenyl (C1-C4)alkyl group; and their salts or solvates, to a process for their preparation, to synthetic intermediates and to the pharmaceutical compositions comprising them.Type: GrantFiled: December 14, 2000Date of Patent: March 15, 2005Assignee: Sanofi-SynthelaboInventor: Roberto Cecchi
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Patent number: 6867217Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: March 15, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Qingping Zeng, Ashton T. Hamme, II, Melvin L. Rueppel
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Patent number: 6864252Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: March 8, 2005Assignee: Pfizer, Inc.Inventors: Subas M. Sakya, Bryson Rast