Plural Ring Hetero Atoms In The Bicyclo Ring System, Or Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System Patents (Class 548/453)
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Patent number: 7820675Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: GrantFiled: December 20, 2004Date of Patent: October 26, 2010Assignee: Biovitrum ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Publication number: 20100252112Abstract: Disclosed are semiconducting compounds having one or more phthalimide units and/or one or more head-to-head (H-H) substituted biheteroaryl units. Such compounds can be monomeric, oligomeric, or polymeric, and can exhibit desirable electronic properties and possess processing advantages including solution-processability and/or good stability at ambient conditions.Type: ApplicationFiled: April 6, 2010Publication date: October 7, 2010Inventor: Mark D. Watson
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Patent number: 7808691Abstract: Green electrochromic (EC) materials based on thiophene, and a green EC material based on pyrazine are disclosed. A first thiophene derivative (2,3-Di-thiophen-2-yl-thieno[3,4-b]pyrazine), which was previously investigated as a nonlinear optical material, is here disclosed for its use as an EC material and for its incorporation into an EC device. Synthesis of two new thiophene derivatives (2,5-di(thien-2-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene and 2,5-(2,3-dihydro-thieno[3,4-b][1,4]dioxin-5-yl)-3,4-di(2,2,2-trifluoro-ethoxy)-thiophene), and a new pyrazine derivative (2,3-dibenzyl-5,7-di(thien-2-yl)thieno[3,4-b]pyrazine) are also disclosed, since these materials are all able to selectively change state to appear a green color and can be polymerized to achieve a green EC polymer.Type: GrantFiled: October 22, 2007Date of Patent: October 5, 2010Assignee: University of WashingtonInventors: Lu Liu, Chunye Xu, Minoru Taya
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Patent number: 7799932Abstract: A family of N-substituted 3,4-alkylenedioxypyrrole includes monomers for of formula (I) electropolymerization to conjugated polymers and key intermediates for the preparation of the monomers. The preparation of the //-substituted 3,4-alkylenedioxypyrroles is carried out via a synthetic intermediate, an ester substituted dihydroxypyrrole. The synthetic method to prepare the //-substituted 3,4-alkylenedioxypyrrole intermediates and ultimately the N-substituted 3,4-alkylenedioxypyrrole monomers begins with a reaction to form the ester substituted dihydroxypyrrole.Type: GrantFiled: October 6, 2006Date of Patent: September 21, 2010Assignee: University of Florida Research Foundation, Inc.Inventors: John R. Reynolds, Ryan M. Walczak, John Sigure Cowart, II
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Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100235950Abstract: This invention relates to a pesticidal compositions containing at least one pyrrolizidine alkaloid compound derived from a plant and endophyte combination, and applying the pesticidal compositions to another plant without pesticidal protection, where upon application of the composition, the plant confers pest protection. The pyrrolizidine alkaloid compound is of Formula wherein: R?H or CH3 and R??H, CH3, CHO, COCH3.Type: ApplicationFiled: March 12, 2008Publication date: September 16, 2010Applicant: GRASSLANZ TECHNOLOGY LTDInventor: Christopher Gerald Lee Pennell
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Publication number: 20100222326Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2008Publication date: September 2, 2010Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
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Publication number: 20100222358Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: ApplicationFiled: March 2, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G.Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Patent number: 7786163Abstract: Certain constrained cyano compounds are useful as inhibitors of post-proline/alanine cleaving amino-dipeptidases. Accordingly, these compounds can be employed, alone or with another therapeutic agent, to treat diabetes (especially, Type II diabetes), hyperglycemia, Syndrome X, diabetic complications, hyperinsulinemia, obesity, atherosclerosis and related diseases, as well as various immunomodulatory diseases and chronic inflammatory bowel disease.Type: GrantFiled: July 12, 2005Date of Patent: August 31, 2010Inventors: David Alan Campbell, Juan Manuel Betancort, David T. Winn
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Patent number: 7786313Abstract: The present invention relates to a process for the preparation of a mixture comprising at least two structurally different diketopyrrolopyrrole pigments of formula wherein A1 and A2 are each independently of the other an aromatic or heteroaromatic radical, by reacting a succinic acid ester with at least one unsubstituted or substituted aromatic or heteroaromatic nitrile, which process comprises carrying out the reaction in the presence of at least one compound of formula wherein A is an aromatic or heteroaromatic radical, R3 is hydrogen, halogen, methyl, methoxy, —CF3 or —CN, R4 is a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, X is —S—, —O—, —CR5R5?—, —COO—, —CONR5—, —SO—, SO2—, —SO2NR5— or —NR5— and R5 and R5? are each independently of the other hydrogen or a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, to the use of such a mixture in the coloring of organic material and in cosmetics, and alType: GrantFiled: July 17, 2008Date of Patent: August 31, 2010Assignee: Ciba Specialty Chemicals Corp.Inventors: Olof Wallquist, Roman Lenz, Leonhard Feiler, Mathias Düggeli, Taher Yousaf, Gerardus De Keyzer
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Patent number: 7781431Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: September 7, 2004Date of Patent: August 24, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
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Publication number: 20100210856Abstract: The invention discloses a dithiolopyrrolone compound represented by formula I or its pharmaceutically acceptable salts, wherein X1, R1, R2, R3, R4 are defined as in the description. The invention also discloses the preparation of such compounds, and the use of such compounds in preparation of medicaments for increasing peripheral white blood cells and in preparation of ancillary medicaments for inhibiting the decrease of peripheral white blood cells in radiotherapy or chemotherapy.Type: ApplicationFiled: August 29, 2008Publication date: August 19, 2010Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, SHANGHAI MODERN PHARMACEUTICAL CO., LTDInventors: Guoping Wang, Quanhai Liu, Haiyan Sun, Wei Wu, Jian Hou, Lin Yao, Chungang Li, Minyu Liu, Fei Li, Xuejun Wu, Shuai Zhao
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Publication number: 20100204224Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.Type: ApplicationFiled: July 7, 2006Publication date: August 12, 2010Applicant: VERNALIS R & D LIMITEDInventors: Richard Hamlyn, Glyn Addison, Christopher Geoffrey Earnshaw, Harry Finch, Mike Huckstep, Rosemary Lynch, Sarah Mellor
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Publication number: 20100184794Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: October 17, 2007Publication date: July 22, 2010Inventors: Tsuneo Yasuma, Yasufumi Miyamoto
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Publication number: 20100179189Abstract: Compounds represented by Formula (I) or Formula (II) against cell releasing TNF?, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH2, CO, SO, or SO2; D represents S, NH, or NC1-6 alkyl; R1 represents H, or one or two same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)2.Type: ApplicationFiled: October 16, 2007Publication date: July 15, 2010Inventor: Hesheng Zhang
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Publication number: 20100173932Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Yun-De Xiao, Philip S. Hammond, Craig H. Miller, Srinivisa Rao Akireddy, V. Srinivasa Murthy, Regina C. Whitaker, Scott R. Breining, Matt S. Melvin
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Patent number: 7750034Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: GrantFiled: January 19, 2007Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Publication number: 20100160323Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Publication number: 20100144826Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: ApplicationFiled: December 15, 2009Publication date: June 10, 2010Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Publication number: 20100144700Abstract: A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?402 subtype in the central nervous system (CNS).Type: ApplicationFiled: March 12, 2008Publication date: June 10, 2010Applicant: TARGACEPT, INC.Inventors: Philip S. Hammond, Anatoly A. Mazurov, Lan Miao, Yun-De Xiao, Balwinder Singh Bhatti, Jon-Paul Strachan, V. Srinivasa Murthy, David C. Kombo, Srinivisa Rao Akireddy
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Patent number: 7732477Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: GrantFiled: December 16, 2002Date of Patent: June 8, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Timo Fleβner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100137397Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt: possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity such as 2 diabetes. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.Type: ApplicationFiled: February 2, 2006Publication date: June 3, 2010Applicant: ASTRAZENECA ABInventors: Alan Martin Birch, Craig Johnstone, Alleyn Thomas Plowright, Iain Simpson, Paul Robert Owen Whittamore
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Patent number: 7728031Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands, Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: GrantFiled: February 13, 2007Date of Patent: June 1, 2010Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Lawrence Kolaczkowski
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Patent number: 7728139Abstract: The present application relates to compounds of formula A(D)x(E)y, (I), compounds of formula (III), compounds of formula (X), as well as processes for the preparation thereof, processes where the compounds (I) are converted to pigments of formula (II) and the use of the compounds (I).Type: GrantFiled: June 24, 2003Date of Patent: June 1, 2010Assignee: MCA Technologies GmbHInventor: Bansi Lal Kaul
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Patent number: 7723530Abstract: The present invention relates to the use of polymerisable diketopyrrolopyrroles in colour filters, which can themselves be used for example in electro-optical systems such as TV screens, liquid crystal displays, charge coupled devices, plasma displays or electroluminescent displays and the like. In contrast to conventional pigments the polymerisable diketopyrrolopyrroles do not tend to aggregate and, hence, show very good dispersibility. Color filters prepared by using the polymerisable diketopyrrolopyrroles have high transparence and pure hue. In addition, they facilitate adjustment of color points and enable a large choice of shades.Type: GrantFiled: January 3, 2008Date of Patent: May 25, 2010Assignee: Ciba Specialty Chemicals CorporationInventors: Jean-Marie Adam, Gerardus De Keyzer
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Publication number: 20100119966Abstract: The present invention relates to a pigment composition composed of compounds of the formula (I), (II) and (III) with a novel crystal modification, to their preparation and to the use of this novel product as a pigment. For many applications of organic pigments, for example the coloring of metallic lacquers or the use thereof in color filters, a very high transparency is required. To produce color filters, for example, particularly fine pigments are used, in order to substantially rule out the particle scattering which leads to a lowering of the contrast ratio. The commercially available products, however, do not always meet all requirements of the art. More particularly, there was a need for improvement with regard to the transparency and the associated fineness of the pigment crystals, and also the color purity (chroma).Type: ApplicationFiled: January 17, 2008Publication date: May 13, 2010Applicant: CLARIANT FINANCE (BVI) LIMITEDInventor: Matthias Ganschow
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Publication number: 20100121053Abstract: The invention relates to a method for directly producing fine-particle 1,4-diketopyrrolo[3,4-c]pyrrols of formula (1), wherein R1a, R1b, R2a and R2b independently represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, cyano or phenyl, said compounds being characterized by a maximum frequency distribution between 20 and 120 nm. According to the method, nitriles are reacted with succinic acid esters or lactames or enamines in an alkali medium to form a pigment salt, and then protolysis of the pigment alkali salt is carried out. Said method is characterized in that an effective quantity of a pigment dispersant of formula (II) is added during the protolysis of the pigment alkali salt. In formula (II), Q is a radical of an organic pigment from the group of perinone, quinacridone, quinacridonquinone, anthanthrone, indanthrone, dioxazine, diketopyrrolopyrrol, indigo, thioindigo, thiazineindigo, isoindoline, isoindolinone, pyranthrone, isoviolanthrone, flavanthrone or anthrapyrimidine pigments.Type: ApplicationFiled: February 20, 2008Publication date: May 13, 2010Applicant: CLARIANT FINANCE (BVI) LIMITEDInventor: Matthias Ganschow
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Publication number: 20100120740Abstract: The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.Type: ApplicationFiled: August 6, 2009Publication date: May 13, 2010Applicant: SEPRACOR INC.Inventors: Michele L. R. Heffernan, Richard Dennis, James M. Dorsey, Robert J. Foglesong, Michael L. Jones, Cyprian O. Ogbu, Mustapha Soukri, Kerry L. Spear, H. Scott Wilkinson, Michael Anthony Orsini
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Patent number: 7714018Abstract: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.Type: GrantFiled: December 11, 2006Date of Patent: May 11, 2010Assignee: Roche Palo Alto LLCInventors: Eun Kyung Lee, Chris Richard Melville, David Mark Rotstein
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Publication number: 20100099840Abstract: The present invention relates to dioxypyrrolo-heterocyclic compounds and an organic electronic device using the same. The compound of the present invention satisfies the requirements for use in an organic electronic device such as an organic light emitting device, an organic thin film transistor, and an organic solar cell, for example, suitable energy levels, and the electrochemical and thermal stability, by introducing various substituents to the core structure, and also have amorphous or crystalline property depending on the Mnd of the substituents, to satisfy the characteristics individually required for each of the devices. Further, an organic semi-conductor of p-type or n-type can be fabricated by introducing various substituents to the core structure having a property of n-type, thereby providing stability for the device.Type: ApplicationFiled: April 11, 2008Publication date: April 22, 2010Inventors: Jae-Min Moon, Hyeon Choi, Jae-Min Lee
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Publication number: 20100099730Abstract: The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e.g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same.Type: ApplicationFiled: July 30, 2007Publication date: April 22, 2010Applicant: MERCKLE GMBHInventors: Stefan Laufer, Tiziana Guarnieri, Simona Tavolari, Vittorio Tomasi, Ernesto Palazzini, Miriam Barbanti
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Publication number: 20100099874Abstract: The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C1-C6 alkyl group, a C1-C6 arylalkyl group, a C2-C6 alkenyl group, or a alkoxycarbonylalkyl group; Y is a —C(HR4)- group in which R4 is a hydrogen atom, a C1-C6 alkyl group, an aryl group, a C1-C6 arylalkyl group, or a C2-C6 alkenyl group; or an orthophenylene group.Type: ApplicationFiled: March 21, 2008Publication date: April 22, 2010Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRSInventors: Jean Martinez, Georges Dewynter, Daniel Farran
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Patent number: 7691896Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.Type: GrantFiled: February 8, 2008Date of Patent: April 6, 2010Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Binyuan Sun, Stona R Jackson
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Publication number: 20100081683Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).Type: ApplicationFiled: November 1, 2007Publication date: April 1, 2010Applicant: TARGCEPT INC.Inventors: Anatoly Mazurov, Lan Miao, Yun-De Xiao, Philip S. Hammond, Craig H. Miller, Srinivisa Rao Akireddy, V.Srinivasa Murthy, Regina C. Whitaker, Scott R. Breining, Matt S. Melvin
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Publication number: 20100075945Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.Type: ApplicationFiled: November 6, 2009Publication date: March 25, 2010Inventors: Woo-Baeg Choi, David S. Menaldino, Deog-II Kim, Martin Bouygues, Michael W. Hager
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Patent number: 7674794Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: November 15, 2006Date of Patent: March 9, 2010Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Publication number: 20100056495Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: March 4, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20100041729Abstract: The present invention provides dithiolopyrrolone compounds of the general formula I, and their salts, wherein A is sulfur or carbon, and R1, R2, and R3 are selected from groups defined herein, and wherein when A is sulfur, then B is oxygen, and n=1 or 2, and when A is carbon, then B is oxygen or sulfur, and n=1. The compounds are useful for the prevention and treatment of microbial infections such as HIV infection, and for the treatment of blood disorders, such as neutropenia. In particular, the compounds are useful for the manufacture of medicaments for increasing white blood cells.Type: ApplicationFiled: September 10, 2007Publication date: February 18, 2010Inventors: Yingping Guo, Genhui Chen, Bin Li
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Patent number: 7652020Abstract: 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.Type: GrantFiled: June 1, 2005Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
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Patent number: 7652058Abstract: The present invention is directed to certain hydropyranopyrrolidine 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 formations 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: GrantFiled: December 12, 2005Date of Patent: January 26, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Robert J. DeVita, Jinlong Jiang, Sander G. Mills, Jonathan R. Young
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Publication number: 20100009214Abstract: An ?-diketopyrrolopyrrole pigment characterized by giving an X-ray diffraction spectrum in which the ratio of the peak density (I020) for plane index (020) to the peak intensity (I?141) for plane index (?141), I020/I?141 is 0.40 or lower and the ratio of the peak intensity (I?141) for plane index (?141) to the peak intensity (I111) for plane index (111), I?141/I111 is 1.28 or lower. Also provided are: a coloring composition containing this pigment; and a red film formed with this coloring composition. In a color filter formed with ?-diketopyrrolopyrrole pigment, which has that property, the red filter segments have a high contrast ratio and a small absolute value of birefringence. Consequently, a color liquid-crystal display or the like having small viewing-angle dependence and showing excellent display characteristics can be produced.Type: ApplicationFiled: October 1, 2007Publication date: January 14, 2010Inventors: Takeshi Sato, Toru Omura, Taro Murohoshi, Yoshiko Takabatake, Yasushi Ariyoshi
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Patent number: 7638513Abstract: 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, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: December 1, 2005Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
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Publication number: 20090318529Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: ApplicationFiled: June 18, 2004Publication date: December 24, 2009Inventors: William H. Fenical, Paul R. Jensen, Tracy J. Mincer, Robert H.R. Feling
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Publication number: 20090306169Abstract: The present invention provides the use of fused pyrrole carboxylic acids of formula (I) for the manufacture of a medicament to inhibit D-amino acid oxidase, particularly for the treatment of neurodegenerative and psychiatric disorders or diseases; certain compounds of formula I being novel, pharmaceutical compositions containing them, their use in medicine and methods of treatment using them are also disclosed.Type: ApplicationFiled: October 5, 2006Publication date: December 10, 2009Inventors: Philip E. Brandish, Timothy Sparey, Alister Campbell, Andrew Pike, Nicholas Brandon, Wei Zheng
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Publication number: 20090298810Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (II-8).Type: ApplicationFiled: April 20, 2007Publication date: December 3, 2009Inventor: Jakob Busch-Petersen
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Publication number: 20090298906Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.Type: ApplicationFiled: May 12, 2009Publication date: December 3, 2009Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Venkat Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur, Ta-Hsiang Chao, Saskia Theodora Cornelia Neuteboom
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Patent number: 7612213Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.Type: GrantFiled: June 6, 2003Date of Patent: November 3, 2009Assignee: RikenInventors: Hiroyuki Osada, Hideaki Kakeya, Yujiro Hayashi
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Publication number: 20090270467Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: ApplicationFiled: January 19, 2007Publication date: October 29, 2009Applicant: MERCK & CO., INC.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber