Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
Type:
Application
Filed:
July 8, 2011
Publication date:
November 17, 2011
Inventors:
Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.
Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for creating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.
Type:
Grant
Filed:
July 18, 2003
Date of Patent:
October 4, 2011
Assignee:
The General Hospital Corporation
Inventors:
Mikhail I. Papisov, Alexander Yurkovetskiy
Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Type:
Grant
Filed:
May 10, 2010
Date of Patent:
September 27, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
Abstract: Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
Type:
Grant
Filed:
June 9, 2010
Date of Patent:
September 27, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
Abstract: Aamantane dipyrromethane derivatives are obtained by reacting adamantane carbonyl derivatives with pyrrole or pyrrole derivative, in the presence of acid. Adamantane-dipyrromethanes are used to bind anions of the group consisting of: F—, Cl—, Br—, acetate, HSO4-NO3-, and H2PO4-, and particularly F—.
Type:
Grant
Filed:
September 16, 2009
Date of Patent:
September 20, 2011
Assignee:
Rudjer Boskovic Institute
Inventors:
Nikola Basaric, Marija Aleskovic, Kata Majerski
Abstract: The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Grant
Filed:
December 3, 2009
Date of Patent:
September 6, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Joe Timothy Bamberg, Johannes Cornelius Hermann, Remy Lemoine, Michael Soth
Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Grant
Filed:
February 20, 2009
Date of Patent:
August 30, 2011
Assignee:
Roche Palo Alto
Inventors:
Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
Abstract: The present invention provides dipyrrin substituted porphyrinic macrocycles, intermediates useful for making the same, and methods of making the same. Such compounds may be used for purposes including the making of molecular memory devices, solar cells and light harvesting arrays.
Type:
Application
Filed:
April 14, 2011
Publication date:
August 18, 2011
Inventors:
Lianhe Yu, Kannan Muthukumaran, Prathapan Sreedharan, Jonathan S. Lindsey
Abstract: The present invention provides a method for transferring a gene into cells, which is practically useful and can achieve high transfer efficiency, and also a composition for use in the method. By bringing a mixture of a composition comprising a diallylamine sulfur dioxide copolymer having a repeating unit represented by the formula (1) or a salt thereof and a gene into contact with a cell, a gene such as DNA and RNA can be transferred into a target cell safely and conveniently, and into a cell at a specific site with high gene transfer efficiency.
Abstract: A method of making a metalloporphyrin is carried out by reacting (i) a linear tetrapyrrole, said linear tetrapyrrole having a 19-acyl group and a 1-protecting group, with (ii) a metal salt under basic conditions to produce the metalloporphyrin. Products produced by such methods and intermediates useful for carrying out such methods are also described.
Type:
Grant
Filed:
February 11, 2008
Date of Patent:
August 9, 2011
Assignee:
North Carolina State University
Inventors:
Jonathan S. Lindsey, Dilek Dogutan Kiper
Abstract: The present invention provides a novel intermediate which enable to prepare tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3?-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and a process for preparing the same. That is, the present invention provides a process for preparing a compound of the following formula (I) wherein R1 is an amino group protected with a protecting group, etc., and R2 is a lower alkyl group, etc.
Abstract: A heterocycle-containing aromatic compound represented by the formula: A-B, and an electrically conductive polymer obtained by oxidative polymerization of the heterocycle-containing aromatic compound as a monomer are provided. In the above formula, A represents a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; B represents a substituted or unsubstituted hydrocarbon aromatic ring group, a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; the ring represented by A and the ring represented by B are directly linked; however, A and B represent structures that are different from each other. The compound can be produced by a coupling reaction using a hypervalent iodine reactant.
Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heterocyclic group bound by a carbon atom, a heterocyclic-(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; X is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(0)p group; and p is 0 to 2. The invention also relates to a method for preparing same and to the therapeutic application thereof.
Type:
Application
Filed:
August 13, 2009
Publication date:
July 28, 2011
Applicant:
SANOFI-AVENTIS
Inventors:
Florian Auger, Patrick Bernardelli, Jean-François Sabuco, Corinne Terrier
Abstract: A method of making a compound of Formula I? comprises reacting a compound of the formula DLCHO, with a compound of the formula to produce the compound of Formula I?. Methods of using the compounds are also described, particularly as intermediates for the synthesis of porphyrin rods, which porphyrin rods are in turn useful for (among other things) the production of molecular memory devices.
Type:
Application
Filed:
March 29, 2011
Publication date:
July 28, 2011
Inventors:
Jonathan S. Lindsey, Lianhe Yu, Patchanita Thamyongkit, Anil D. Bhise
Abstract: Disclosed herein is a compound represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
Type:
Application
Filed:
January 14, 2011
Publication date:
July 21, 2011
Applicant:
Gilead Sciences, Inc.
Inventors:
Eda CANALES, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman, Philip A. Morganelli, William J. Watkins
Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.
Type:
Grant
Filed:
October 17, 2008
Date of Patent:
July 19, 2011
Assignee:
Avila Therapeutics, Inc.
Inventors:
Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
Abstract: A compound of Formula 1.1A: 1.1A or salt thereof, as well as methods of making compounds of Formula 1.1A, methods of using compounds of Formula 1.1A to treat proliferative disorders such as cancer, and related compounds, composition, and methods.
Type:
Application
Filed:
June 26, 2009
Publication date:
July 14, 2011
Applicant:
Aegera Therapeutics, Inc.
Inventors:
Alain Laurent, Melanie Proulx, Yannick Rose, James B. Jaquith, Stephen Morris
Abstract: The invention provides compounds of Formula I wherein A, Y, R1, R1a, R2, and R2a are as described in the specification. Compounds of Formula I are useful in treating and/or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of preparing compounds of Formula I, and methods of treating cognitive disorders, such as Alzheimer's disease.
Type:
Grant
Filed:
May 21, 2008
Date of Patent:
July 12, 2011
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Darren Dressen, Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Matthew N. Mattson
Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.
Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.
Type:
Grant
Filed:
December 9, 2008
Date of Patent:
June 28, 2011
Assignee:
Gruenenthal GmbH
Inventors:
Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
Type:
Application
Filed:
December 16, 2010
Publication date:
June 23, 2011
Inventors:
Ara MERMERIAN, Bo Peng, Colleen Hudson, Charles Kim, Joel Moore, Jason Rohde, Kevin Sprott, Regina Graul, Takashi Nakai, James Jia, Wilmin Bartolini
Abstract: The present invention relates to 2,2?-di-substituted dipyrrins. The invention also relates to methods for the preparation of 2,2?-disubstituted dipyrrins, and to the use of 2,2?-disubstituted dipyrrins in, for example, sensing, imaging and laser applications.
Type:
Application
Filed:
October 12, 2010
Publication date:
June 16, 2011
Inventors:
Mikhail Filatov, Andrei Cheprakov, Sergei A. Vinogradov, Artem Y. Lebedev
Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
Type:
Application
Filed:
December 7, 2010
Publication date:
June 16, 2011
Inventors:
Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
Abstract: Methods of identifying NS5A inhibitors are provided. Novel binding sites are identified on NS5A dimers, and these binding sites can be used to design and/or identify new NS5A inhibitors.
Type:
Application
Filed:
December 3, 2010
Publication date:
June 9, 2011
Applicant:
ABBOTT LABORATORIES
Inventors:
CHARLES W. HUTCHINS, DAVID A. DEGOEY, WARREN M. KATI, ALLAN C. KRUEGER, JOHN T. RANDOLPH, ROLF WAGNER, PAMELA L. DONNER
Abstract: The invention relates to a method of developing a main proteinase SARS inhibitor. Human coronaviruses are major causes of upper respiratory tract illnesses in humans, in particular, the common cold. Recent investigations have shown that a novel coronavirus causes the Severe Acute Respiratory Syndrome (SARS), a disease that is characterized by high fever, malaise, rigor, headache, non-productive cough or dyspnea, which is rapidly spreading. Within the scope of the invention, based on the structural analysis of the binding mode of the SARS Mpro enzyme, a group of prototype inhibitors is provided that acts as suitable drugs targeting a majority of viral infections of the respiratory tract, including SARS.
Type:
Grant
Filed:
November 10, 2005
Date of Patent:
June 7, 2011
Assignee:
Universitat zu Luebeck
Inventors:
Rolf Hilgenfeld, Kanchan Anand, John Ziebuhr, Jeroen R. Mesters, Parvesh Wadhwani
Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Type:
Grant
Filed:
March 13, 2006
Date of Patent:
May 31, 2011
Assignee:
Eli Lilly and Company
Inventors:
Lisa Selsam Beavers, Don Richard Finley, Robert Alan Gadski, Philip Arthur Hipskind, Cynthia Darshini Jesudason, Richard Todd Pickard, Freddie Craig Stevens, Takako Takakuwa
Abstract: A compound comprising one or more polyfunctionalized pyrrolyl anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-pyrrolyl anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
Abstract: A compound of Formula (1) or a salt thereof, methods for the preparation and use of such a compound, especially as an IAP inhibitor, and related compounds, compositions, and methods.
Type:
Application
Filed:
May 5, 2009
Publication date:
May 19, 2011
Applicant:
Aegera Therapeutics, Inc.
Inventors:
Alain Laurent, Melanie Proulx, James Jaquith
Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Type:
Application
Filed:
June 24, 2009
Publication date:
April 28, 2011
Inventors:
Hong Lin, Meagan B. Rouse, Mark A. Seefeld, Ren Xie
Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.
Type:
Application
Filed:
September 21, 2010
Publication date:
April 7, 2011
Applicant:
ChemoCentryx, Inc.
Inventors:
Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
Abstract: A method of making a 5-formylporphyrin, comprises the steps of: condensing a 5-acetaldipyrromethane with a dipyrromethane-1,9-dicarbinol to produce a porphyrin having an acetal group substituted thereon at the 5 position; and then hydrolyzing said porphyrin to produce said 5-formylporphyrin. Products and intermediates useful in such methods, along with methods of making such intermediates, are also described.
Type:
Grant
Filed:
January 30, 2009
Date of Patent:
April 5, 2011
Assignee:
North Carolina State University
Inventors:
Arumugham Balakumar, Kannan Muthukumaran, Jonathan S. Lindsey
Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.
Type:
Application
Filed:
April 29, 2008
Publication date:
March 31, 2011
Applicant:
Genentech, Inc.
Inventors:
John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
Abstract: A photorefractive dendron compound, a photorefractive dendrimer compound and applications thereof, and more particularly, a photorefractive dendron compound, including a non-linear chromophore containing a tricyanopyrroline-based electron-withdrawing group and a carbazole derivative having excellent charge transport properties, a method of preparing the photorefractive dendrimer compound, a photorefractive device including the photorefractive dendrimer compound, and a method of manufacturing the photorefractive device. In the photorefractive dendrimer compound, dendron has the non-linear optical chromophore and carbazole introduced thereto to thus impart one molecule with both photoconductivity and non-linear optical properties, thereby solving conventional problems caused by poor compatibility between photoconductive material and chromophores in conventional photorefractive material.
Type:
Grant
Filed:
October 8, 2007
Date of Patent:
March 29, 2011
Assignees:
Samsung Electronics Co., Ltd., Seoul National University Industry Foundation, Korea University Industrial & Academic Collaboration Foundation
Inventors:
Dong Hoon Choi, Min Ju Cho, Kyung Moon Jung
Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
Type:
Application
Filed:
September 10, 2010
Publication date:
March 17, 2011
Inventors:
Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
Type:
Grant
Filed:
April 27, 2005
Date of Patent:
March 15, 2011
Assignee:
Rottapharm S.p.A.
Inventors:
Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Claudio Rovati
Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
Type:
Grant
Filed:
February 6, 2008
Date of Patent:
March 15, 2011
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Kevin M. Cottrell, John Maxwell, Robert B. Perni, Janos Pitlik
Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.
Type:
Application
Filed:
October 20, 2008
Publication date:
March 10, 2011
Inventors:
Matthew ColinThor Fyfe, William Gattrell, Colin Peter Sambrook-Smith, Simon Andrew Swain
Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.
Type:
Grant
Filed:
February 22, 2005
Date of Patent:
March 8, 2011
Assignee:
Eli Lilly and Company
Inventors:
Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Cynthia Darshini Jesudason, Karen Lynn Lobb, Richard Todd Pickard, Craig William Lindsley
Abstract: The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
Type:
Application
Filed:
January 16, 2009
Publication date:
February 24, 2011
Inventors:
David Hook, Bernhard Riss, Daniel Kaufmann, Matthias Napp, Erhard Bappert, Phillippe Polleux, Jonathan Medlock, Antonio Zanotti-Gerosa
Abstract: The present invention relates to compounds of general formula I wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
Type:
Application
Filed:
February 5, 2009
Publication date:
February 24, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.
Type:
Grant
Filed:
May 16, 2006
Date of Patent:
February 22, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
Abstract: The present invention discloses pyrido[2,3-B]pyrazinones having the structure of Formula I for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
February 22, 2011
Assignee:
Gilead Palo Alto, Inc.
Inventors:
Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrei Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov, Jeffrey Chisholm
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.
Type:
Application
Filed:
May 3, 2005
Publication date:
February 17, 2011
Applicants:
Novo Nordisk A/S
Inventors:
Zdenék Polivka, Karel Sindelar, Per Sauerberg, Ingrid Pettersson
Abstract: The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
Type:
Grant
Filed:
July 13, 2007
Date of Patent:
February 1, 2011
Assignee:
LG Life Sciences Ltd.
Inventors:
Sung Pil Choi, In Ae Ahn, Sang Hyup Lee, Sang Dae Lee, Mi Sook Shin, Koo Lee, Deog Young Choi, Dong Sup Shim, Hyeon Joo Yim, Min Kyung Yoon, Soo Yong Chung, Jung Ae Lee, Yong Hwa Ha, Young Kwan Kim, Oeuk Park, Hyun Min Lee, Youn Hoa Kim