Abstract: The present invention provides an optical recording composition comprising at least one compound denoted by general formula (I) and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one compound denoted by general formula (I). In general formula (I), each of A1 and A2 independently denotes —CR4R5—, —O—, —NR6—, —S—, or —C(?O)—, each of R4, R5, and R6 independently denotes a hydrogen atom or a substituent, R1 denotes a substituent, n denotes an integer ranging from 0 to 4, each of R2 and R3 independently denotes a substituent having a Hammett substituent constant, ?p value, of greater than 0, R2 and R3 do not form a ring structure by bonding together, and at least one from among R1, R2, R3, A1, and A2 comprises at least one polymerizable group.
Abstract: A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) wherein
Type:
Application
Filed:
December 4, 2006
Publication date:
August 6, 2009
Applicants:
OSAKA UNIVERSITY, TAKASAGO INTERNATIONAL CORPORATION
Abstract: A merocyanine dye is provided. The merocyanine dye is represented by formula (1). In the formula (1), A1 represents a divalent atomic group, n represents an integer of 1 to 3, A2 and A3 each independently represent an aromatic hydrocarbon ring or a heterocyclic ring having 3 to 18 carbon atoms, and R11 and R12 each independently represent a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, an aryl group having 6 to 18 carbon atoms, or a heterocyclic group having 3 to 18 carbon atoms.
Abstract: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays.
Type:
Grant
Filed:
January 25, 2006
Date of Patent:
July 21, 2009
Assignee:
Roche Diagnostics Operations, Inc.
Inventors:
Dieter Heindl, Rupert Herrmann, Wolfgang Jenni
Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.
Abstract: To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1): (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.
Type:
Application
Filed:
November 30, 2006
Publication date:
June 25, 2009
Applicants:
Fujifilm RI Pharma Co., Ltd., Daiichi Sankyo Company, Limited
Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.
Type:
Application
Filed:
April 15, 2008
Publication date:
June 18, 2009
Applicant:
Gruenenthal GmbH
Inventors:
Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Derek SAUNDERS, Bernd SUNDERMANN, Jeewoo LEE
Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, especially an antifungal that contains the compound, its salt or their hydrate.
Abstract: The invention concerns the use as cdc25 phosphatase inhibitors, in particular cdc25-C phosphatase, and CD45 phosphatase, of compounds of general formula (I), wherein: W represents O or S. In accordance with the invention, the compounds of general formula (I) can in particular be used for preparing a medicine for cancer treatment.
Type:
Application
Filed:
October 6, 2008
Publication date:
May 21, 2009
Applicant:
Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)
Abstract: The present application provides benzoxazole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
Abstract: 5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses.
Type:
Application
Filed:
January 12, 2009
Publication date:
May 7, 2009
Applicant:
LABORATOIRES FOURNIER S.A.
Inventors:
Didier THOMAS, Michel Bondoux, Veronique Barberousse, Vincent Peyrou
Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
Type:
Application
Filed:
January 6, 2009
Publication date:
May 7, 2009
Inventors:
Andrew Thomas Bach, Prasad Koteswara Kapa, George Tien-San Lee, Eric M. Loeser, Michael Lloyd Sabio, James Lawrence Stanton, Thalaththani Ralalage Vedananda
Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.
Type:
Application
Filed:
October 30, 2008
Publication date:
April 30, 2009
Inventors:
Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. McClure, Taraneh Mirzadegan, Alejandro Santillan, JR.
Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
May 3, 2007
Date of Patent:
April 7, 2009
Assignee:
Cephalon, Inc.
Inventors:
Robert L. Hudkins, Dandu R. Reddy, Ming Tao, Theodore L. Underiner, Allison L. Zulli
Abstract: The present invention relates to the identification of compounds that are suitable for imaging amyloid deposits in living patients. The invention relates, in part, to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease. The present invention also relates to therapeutic uses for such compounds, as exemplified by compounds of the formula (1) in which Y is independently S, O, or N and m is 1, 2, or 3.
Type:
Application
Filed:
July 15, 2005
Publication date:
April 2, 2009
Applicants:
The General Hospital Corporation, Massachusetts Institute of Technology, University of Pittsburg of the Commonwealth System of Higher Education
Inventors:
Brian Bacskai, Bradley T. Hyman, William E. Klunk, Chester A. Mathis, Timothy Swager, Evgueni Nesterov, Ivory Hills
Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.
Abstract: A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II?). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II?), the bond between L? and T? is a double or conjugated double bond. L?: carbon atom. T?: carbon, oxygen, nitrogen atom. s?: 0-4. Ring containing L? and T?: 5-membered ring, may contain a heteroatom.
Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
Type:
Application
Filed:
January 19, 2007
Publication date:
February 12, 2009
Inventors:
Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Type:
Application
Filed:
May 22, 2006
Publication date:
January 29, 2009
Applicant:
ASTRAZENECA AB
Inventors:
Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
Type:
Application
Filed:
May 1, 2008
Publication date:
January 29, 2009
Applicant:
BIOTA SCIENTIFIC MANAGEMENT PTY. LTD.
Inventors:
Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
Type:
Application
Filed:
October 24, 2007
Publication date:
January 8, 2009
Applicant:
BIODIEM LTD.
Inventors:
Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
Abstract: A quaternary nitrogen-containing corrosion inhibitor of formula wherein is an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof, Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.
Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.
Type:
Application
Filed:
February 23, 2006
Publication date:
December 11, 2008
Inventors:
Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
Abstract: The invention is directed to heterocyclic indene derivatives useful for ?-amyloid plaque imaging, their radiolabeled compounds and their preparation methods. The compounds of the invention are easily labeled with radioisotopes and have high affinities to ?-amyloid depositions, thus they facilitate diagnosis of Alzheimer's disease by imaging the distribution of ?-amyloid depositions.
Type:
Application
Filed:
May 28, 2008
Publication date:
December 4, 2008
Applicant:
SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATION
Inventors:
Jae Min JEONG, Dong Soo LEE, June-Key CHUNG, Myung Chul LEE
Abstract: The present invention is directed to novel cyclohexylglycine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
June 10, 2004
Date of Patent:
November 25, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Scott D. Edmondson, Anthony Mastracchio, Emma R. Parmee
Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
Type:
Application
Filed:
March 19, 2008
Publication date:
November 13, 2008
Applicant:
SANOFI-AVENTIS
Inventors:
Agnes PAPPNE BEHR, Zoltan KAPUI, Peter ARANYI, Sandor BATORI, Veronika BARTANE BODOR, Lajos T. NAGY, Mihalyne Santa, Marton VARGA, Endre MIKUS, Katalin URBAN-SZABO, Judit VARGANE SZEREDI, Tibor SZABO, Edit SUSAN, Marianna KOVACS
Abstract: The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4?-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.
Type:
Application
Filed:
April 28, 2008
Publication date:
October 30, 2008
Applicant:
The General Hospital Corporation
Inventors:
David R. Elmaleh, Timothy M. Shoup, Alan J. Fischman
Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen a
Type:
Application
Filed:
June 24, 2008
Publication date:
October 23, 2008
Applicant:
SANOFI-AVENTIS
Inventors:
Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
Type:
Application
Filed:
October 20, 2005
Publication date:
October 23, 2008
Applicant:
Bayer CropScience AG
Inventors:
Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also 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.
Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is optionally substituted 4-6-membered heterocyclic ring containing one or more N atoms, or RC forms together with the phenyl ring to which it is attached a benzodioxolyl group, or RC is —NR1R2, RA is a group having the formula RB is hydrogen or alkyl. The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (I).
Type:
Application
Filed:
July 12, 2004
Publication date:
October 16, 2008
Inventors:
David Smith, Anne Marjamaki, Marika Ojala, Marjo Pihlavisto, Jyrki Heino, Jarmo Kapyla, Olli Pentikainen, Tommi Nyronen, Mark Johnson, Mikko Huhtala
Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
Type:
Grant
Filed:
January 27, 2006
Date of Patent:
September 9, 2008
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
Abstract: This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6, R7, R8 and X have the meanings that are indicated in more detail in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials.
Type:
Grant
Filed:
August 10, 1998
Date of Patent:
August 5, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann
Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.
Type:
Grant
Filed:
June 20, 2007
Date of Patent:
August 5, 2008
Assignee:
Sanofi-Aventis
Inventors:
Laurent Dubois, Yannick Evanno, Andre Malanda
Abstract: Disclosed herein is a method for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising applying to the keratin fibers a dye composition comprising at least one compound chosen from styryl and imine compounds comprising a heterocycle that can undergo opening and/or dyes corresponding to these compounds whose heterocycles are open. The compositions and methods of the present disclosure may produce a coloration of keratin fibers that is chromatic and fast with respect to external factors such as shampooing, does not stain, and/or allows simultaneous dyeing and bleaching of keratin fibers.
Abstract: The cyanine compound of the present invention is represented by general formula (I) below and suitable as an optical recording material used in a recording layer of optical recording media on which recording and play-back are conducted with laser beam. The cyanine compound of the present invention particularly exhibits appropriate thermal decomposition behavior to attain sensitivity compatible with high-speed recording.
Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
Type:
Grant
Filed:
August 18, 2004
Date of Patent:
June 10, 2008
Assignee:
Sloan-Kettering Institute for Cancer Research
Inventors:
Samuel J. Danishefsky, Alexey Rivkin, Fumihiko Yoshimura, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong, Kaida Wu, Malcolm A. S. Moore, David Dorn
Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U ia an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3) (R4) A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.
Type:
Grant
Filed:
December 31, 2003
Date of Patent:
June 10, 2008
Assignee:
Eli Lilly and Company
Inventors:
Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
Abstract: The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA).
Type:
Application
Filed:
May 25, 2007
Publication date:
May 29, 2008
Inventors:
Dinesh U. Chimmanamada, Chi-Wan Lee, David James, Shijie Zhang, Weiwen Ying, Junghyun Chae, Teresa Przewloka
Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds of Formula (I) wherein the variables R, R?, RP, RP3, LP1, LP2, ZP, RB, RB?, LXB and ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and methods of use.
Type:
Application
Filed:
December 19, 2005
Publication date:
May 22, 2008
Inventors:
Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee
Abstract: A reversible recording material is disclosed. The reversible recording material includes one or more kinds of compounds having a structure shown in Chemical Formula (1) on a surface of metal oxide particles. In Chemical Formula (1), X shows a linkage including an element selected from Si, Ti, and Al; Y shows a linkage including a structure selected from Chemical Formula (2); Z shows a methylene group or a sulfide group capable of having a substituent group; Ar shows an aromatic group capable of having a substituent group; R1 and R2 show corresponding alkylene groups; R3 shows an alkylene group capable of forming a ring structure linked with —N—C—O— and able to have a substituent group; and “n” is an integer which is 1 or more.
Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
Type:
Application
Filed:
July 19, 2005
Publication date:
May 8, 2008
Applicant:
MERCK & CO., INC.
Inventors:
Linda Brockunier, Jian Guo, Rui Liang, Emma R. Parmee, Subharekha Raghavan, George Scott Tria, Yusheng Xiong
Abstract: The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.
Abstract: A compound of Formula (I): wherein R1 is selected from the group consisting of an aliphatic functionality having 2 to 12 carbons, an aromatic functionality having 3 to 20 carbons, and a cycloaliphatic functionality having 3 to 20 carbons; with the proviso that R1 is not —C6H5 or —NH—C10H7; R2 and R3 are independently selected from the group consisting of a hydroxyl group, a halogen atom, an aliphatic functionality having 2 to 12 carbons, an aromatic functionality having 3 to 20 carbons, and a cycloaliphatic functionality having 3 to 20 carbons; X is either an oxygen atom or a sulfur atom; “n” has a value of 0 to 4; and “m” has a value of 0 to 3.
Type:
Application
Filed:
September 29, 2006
Publication date:
April 3, 2008
Applicant:
General Electric Company
Inventors:
Yogendrasinh Bharatsinh Chauhan, Adil Minoo Dhalla, Sriramakrishna Maruvada, Shantaram Narayan Naik, Vandita Pai-Paranjape, Kiran Puthamane, Philippe Schottland
Abstract: 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle around (1)} a hydrogen atom, {circle around (2)} an aroylamino group, {circle around (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle around (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle around (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle around (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; l is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5.