Nitrogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/557)
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Publication number: 20090088464Abstract: Merged compounds of ion channel modulating compounds, including, for example, merged compounds of the ion channel modulating compound of the following formula: (I) are described herein, as well as methods of making and using such merged compounds and pharmaceutical compositions containing such merged compounds.Type: ApplicationFiled: April 1, 2005Publication date: April 2, 2009Applicant: Cardiome Pharma Corp.Inventors: Lewis S.L. Choi, Doug Ta Hung Chou, Grace Jung, Bertrand M.C. Plouvier
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Patent number: 7507760Abstract: The invention relates to novel 3-amino pyrrolidine derivatives, as well as methods for modulating calcium channel activity and for treating conditions associated with calcium channel function. In particular, the compounds generally contain at least one benzhydril moiety, and are useful in treating conditions which benefit from blocking calcium ion channels.Type: GrantFiled: January 22, 2004Date of Patent: March 24, 2009Assignee: Neuromed Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Terrance P. Snutch
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Publication number: 20090076062Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 13, 2007Publication date: March 19, 2009Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
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Patent number: 7504521Abstract: A method for preparing a compound having the formula: including the steps of: (a) cyclizing a compound of formula II: to form a compound of formula I: (b) deprotecting the nitrogen atom of the compound of formula I by amination or hydrogenation to form compound III.Type: GrantFiled: August 5, 2005Date of Patent: March 17, 2009Assignee: Bristol-Myers Squibb Co.Inventor: Paul C. Lobben
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Publication number: 20090068120Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.Type: ApplicationFiled: November 6, 2007Publication date: March 12, 2009Inventors: Hiroaki Suga, Jun Igarashi
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Publication number: 20090062373Abstract: The present application describes deuterium-enriched PF-184298, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 25, 2008Publication date: March 5, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20090042851Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.Type: ApplicationFiled: July 21, 2008Publication date: February 12, 2009Applicant: SANOFI-AVENTISInventors: Pierre DESPEYROUX, Evelyne Fontaine, Gilles Courtemanche, Pierrick Rochard, Claudine Serradeil-Le Gal
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Patent number: 7485665Abstract: The present invention relates to an ameliorant for improving the movement of the digestive tract comprising, as an active ingredient, 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-2-hydroxymethyl-4-pyrrolidinyl]benzamide or an acid addition salt thereof which is a metabolite of 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4-pyrrolidinyl]benzamide or an acid addition salt thereof, having high biding affinity for a serotonin receptor 4 (5HT4) and causing no arteritis and thrombus formation; a medicinal composition for improving the movement of the digestive tract comprising the said ameliorant and a pharmaceutically acceptable carrier; and a treating method for promoting the movement of the digestive tract, which comprises using the said medicinal composition for improving the movement of the digestive tract.Type: GrantFiled: September 12, 2002Date of Patent: February 3, 2009Assignee: Nagase Chemtex CorporationInventors: Akihiko Kitajima, Osamu Kamoda, Akihiro Ohsako, Toshiharu Yanagi
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Publication number: 20090030212Abstract: A process for the preparation of a nucleophilic addition product of an aziridine and a nucleophile, the process comprising treating the arizidine with the nucleophile in the presence of a biaryl phosphoric acid catalystType: ApplicationFiled: June 30, 2008Publication date: January 29, 2009Inventors: Jon C. Antilla, Emily B. Rowland, Gerald B. Rowland
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Patent number: 7479357Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: September 13, 2002Date of Patent: January 20, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
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Publication number: 20080300266Abstract: The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.Type: ApplicationFiled: October 13, 2005Publication date: December 4, 2008Applicant: Eli Lilly And CompanyInventors: Thomas Charles Britton, Veronique Dehlinger, Colin Peter Dell, Bruce Anthony Dressman, Jason Kenneth Myers, Eric Samuel Nisenbaum
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Publication number: 20080287523Abstract: The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: June 10, 2005Publication date: November 20, 2008Inventor: Craig A. Coburn
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Publication number: 20080275087Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: June 24, 2008Publication date: November 6, 2008Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx
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Patent number: 7446115Abstract: One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize ? opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize ?-opioid receptors.Type: GrantFiled: August 29, 2006Date of Patent: November 4, 2008Assignee: Sepracor, Inc.Inventors: Paul E. Persons, Joanne M. Holland, James R. Hauske
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Publication number: 20080262073Abstract: The invention describes new compounds derived from formula I pyrroles, methods for obtaining them and their application as drugs in pharmaceutical compositions for the treatment of cancer due to their inhibitory activity on certain histone deacetylases.Type: ApplicationFiled: December 27, 2005Publication date: October 23, 2008Inventors: Fernando Pedro Cossio Mora, Manel Esteller Badosa, Aizpea Zubia Olascoaga, Dorleta Otaegui Ansa
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Publication number: 20080255371Abstract: The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-aminopyrrolidine that is used in the method.Type: ApplicationFiled: August 3, 2007Publication date: October 16, 2008Applicant: Kaneka CorporationInventors: Fumihiko Kano, Natsuki Mori
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Publication number: 20080255205Abstract: The present invention relates to compounds of Formulas I and II, wherein B1, B2, B3, B4, C1, C2, ring D, L1, L2 and R1-4 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and Aurora and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.Type: ApplicationFiled: October 25, 2007Publication date: October 16, 2008Applicant: Amgen Inc.Inventors: Brian L. Hodous, Stephanie D. Geuns-Meyer, Philip R. Olivieri, Vinod F. Patel, Paul A. Tempest
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Publication number: 20080242653Abstract: Compounds of formula (I) wherein R1, R2, R3, R3a, R3b, R4, and R5 are defined in the description, 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: December 14, 2007Publication date: October 2, 2008Inventors: Huaqing Liu, Lawrence A. Black, Youssef L. Bennani, Marlon D. Cowart, Zhenping Tian, Paul J. Brackemeyer
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Publication number: 20080227826Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: ApplicationFiled: March 6, 2008Publication date: September 18, 2008Applicant: METHYLGENE INC.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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Patent number: 7425631Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 12, 2004Date of Patent: September 16, 2008Assignees: Amgen Inc., Array BioPharma Inc.Inventors: Robert D. Groneberg, Benny C. Askew, Jr., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Publication number: 20080214646Abstract: This invention provides a prodrug that help arthritis patients without increasing cardiovascular and gastrointestinal risk. A novel group of hybrid nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs), moiety attached via a one -carbon methylene spacer to the carboxylic acid group of the traditional NSAIDs aspirin, ibuprofen and indomethacin were synthesized. The ester prodrugs showed equipotent anti-inflammatory activities in vivo to that of the parent aspirin, ibuprofen and indomethacin. The simultaneous release of parent drug and nitric oxide from the NO- prodrugs constitutes a potentially beneficial property for the prophylactic prevention of thrombus formation and adverse cardiovascular events such as stroke and myocardial infarction. Data acquired in an in vivo ulcer index (UI) assay showed that this group of ester prodrugs in which no lesions were observed when compared to the parent drugs at equivalent doses.Type: ApplicationFiled: May 16, 2006Publication date: September 4, 2008Inventors: Edward E. Knaus, Carlos Velazquez
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Publication number: 20080207908Abstract: Disclosed are processes for the synthesis of piperidinyl-substituted urea compounds. This invention further relates to novel intermediates prepared during this synthesis.Type: ApplicationFiled: January 28, 2008Publication date: August 28, 2008Inventor: Richard D. Gless
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Patent number: 7405307Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: September 13, 2007Date of Patent: July 29, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7388112Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 each is a hydrogen or a C1 to C20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; and wherein, a, b and c are integers from 0 to 12; R1, R2, R3, and R4 each is a hydrogen or a C1 to C20; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.Type: GrantFiled: July 1, 2005Date of Patent: June 17, 2008Assignee: MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Maralee McVean, Kevin Kennedy, Arthur Yeung, Bruce H. Devens
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Publication number: 20080139805Abstract: A process for the preparation of carbapenem-type antibacterial agents involving the following reaction: wherein R1 is a C1-C3 alkyl group, n is 0, 1 or 2, A is a C1-C3 alkylene group, L is a leaving group, R3 is a hydrogen atom, a C1-C3 alkyl group or an amino protecting group, and the hydroxyl or carboxyl groups are optionally independently protected. In such process, amine compound (1) or a salt thereof acts as a synthetic intermediate. Such process is a less expensive and highly safe synthetic route for carbapenem-type antibacterial agents suitable for large-scale synthesis.Type: ApplicationFiled: September 19, 2007Publication date: June 12, 2008Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Makoto MICHIDA, Masaki HAYASHI, Satoshi KOBAYASHI
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Patent number: 7381741Abstract: 3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed.Type: GrantFiled: May 25, 2005Date of Patent: June 3, 2008Assignee: Pfizer IncInventors: John Michael Humphrey, Thomas Allen Chappie
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Patent number: 7378436Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S oType: GrantFiled: June 17, 2004Date of Patent: May 27, 2008Assignee: Pfizer Inc.Inventors: Paul Vincent Fish, Michael Jonathan Fray, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock, Mark David Andrews, Alan Daniel Brown, Mark Ian Lansdell
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Patent number: 7368572Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: August 19, 2004Date of Patent: May 6, 2008Assignee: Pharmacyclics, Inc.Inventor: Martin Sendzik
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Patent number: 7329685Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: June 17, 2004Date of Patent: February 12, 2008Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Chuen Chan, Henry Anderson Kelly, Savvas Kleanthous, Andrew McMurtrie Mason, Nigel Stephen Watson
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Patent number: 7326729Abstract: The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.Type: GrantFiled: May 11, 2005Date of Patent: February 5, 2008Assignee: Schering CorporationInventors: Jianhua Chao, Arthur G. Taveras, Cynthia J. Aki
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Patent number: 7304167Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: January 24, 2006Date of Patent: December 4, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7300934Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 1, 2004Date of Patent: November 27, 2007Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Nancy Elisabeth Krauss
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Patent number: 7291615Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: April 29, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventor: Robert J. Cherney
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Patent number: 7291621Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: January 3, 2006Date of Patent: November 6, 2007Assignee: Neurogen CorporationInventors: Yang Gao, Andrew Thrukauf, He Zhao
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Patent number: 7271272Abstract: The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.Type: GrantFiled: March 6, 2004Date of Patent: September 18, 2007Assignee: LG Life Sciences Ltd.Inventors: Gyo-Hyun Hwang, Yeong-Dae Kim, Hyun Nam, Jay-Hyok Chang, Hyun-Ik Shin, Young-Keun Kim, Kyung Hee Lee, Jae Sung Lee
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Patent number: 7268236Abstract: The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-aminopyrrolidine that is used in the method.Type: GrantFiled: March 28, 2003Date of Patent: September 11, 2007Assignee: Kaneka CorporationInventors: Fumihiko Kano, Natsuki Mori
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Patent number: 7250443Abstract: New pyrrole 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 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: August 21, 2003Date of Patent: July 31, 2007Assignee: Chiron CorporationInventors: Manoj C. Desai, Simon Ng, Zhi-Jie Ni, Keith B. Pfister, Savithri Ramurthy, Sharadha Subramanian, Allan S. Wagman
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Patent number: 7223788Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.Type: GrantFiled: February 17, 2004Date of Patent: May 29, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Petra Stahl, Dirk Gretzke
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Patent number: 7183298Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.Type: GrantFiled: September 30, 2004Date of Patent: February 27, 2007Assignee: Topotarget UK LimitedInventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Vija Gailite, Maxim Vorona, Irina Piskunova, Igor Starchenkov, Victor Andrianov, C. John Harris, James E. S. Duffy
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7148225Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: November 19, 2004Date of Patent: December 12, 2006Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchinson, Wallace C. Pringle, Taeyoung Yoon, He Zhao
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Patent number: 7132534Abstract: The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions. The present invention makes it possible in particular to obtain a chromatic, strong, relatively unselective and resistant coloration of keratin fibers.Type: GrantFiled: July 7, 2003Date of Patent: November 7, 2006Assignee: L'OrealInventors: Stéphane Sabelle, Laure Ramos, Madeleine LeDuc
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Patent number: 7132543Abstract: The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenylene derivative as at least one oxidation base, and to a process for dyeing keratin fibers and a multi-compartment kit using the claimed dye composition. Such a composition makes it possible to obtain a chromatic, powerful, unselective and fast coloration of keratin fibers.Type: GrantFiled: March 29, 2004Date of Patent: November 7, 2006Assignee: L'Oreal S.A.Inventors: Laure Ramos, Stéphane Sabelle
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Patent number: 7126007Abstract: A process for synthesizing para-phenylenediamine derivative compounds containing a pyrolidinyl group, and substituted by a nitrogenous radical, wherein the para-phenylenediamine derivative compounds are chosen from those of formula (I): Intermediates containing a pyrrolidinyl group bearing a nitrogenous radical are also disclosed herein.Type: GrantFiled: November 24, 2004Date of Patent: October 24, 2006Assignee: L'Oreal S.A.Inventors: Thierry Bordier, Jinzhu Xu
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Patent number: 7126010Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: January 21, 2005Date of Patent: October 24, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III., Daniel S Gardner
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Patent number: 7122683Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; provided that at least one of R1, R2 and R3 are other than H.Type: GrantFiled: November 15, 2005Date of Patent: October 17, 2006Assignee: Pfizer Inc.Inventors: Paul Vincent Fish, Thomas Ryckmans, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock
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Patent number: 7115754Abstract: The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1–C6-alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrheaType: GrantFiled: July 4, 2003Date of Patent: October 3, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Catherine Jorand-Lebrun, Jerome Dorbais, Anna Quattropani, Matthias Schwarz, Delphine Valognes
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Patent number: 7105546Abstract: The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 30, 2002Date of Patent: September 12, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mullican, David Lauffer, Roger Tung
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Patent number: 7064218Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.Type: GrantFiled: December 24, 2002Date of Patent: June 20, 2006Assignee: Genelabs Technologies, Inc.Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
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Patent number: 7045521Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: November 12, 2003Date of Patent: May 16, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Robert Cherney