The Hetero Ring Contains Plural Nitrogens Patents (Class 540/470)
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Patent number: 9932407Abstract: The present application disclose a method for treating a patient who would benefit from stimulation of the patient's stem cells, comprising administering to the patient an antibody that specifically binds to an epitope of the MUC1 protein expressed on human undifferentiated stem cells.Type: GrantFiled: February 13, 2015Date of Patent: April 3, 2018Assignee: Minerva Biotechnologies CorporationInventor: Cynthia Bamdad
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Patent number: 9305476Abstract: Methods for removing, reducing or treating the trace metal contaminants and the smaller fine sized cerium oxide particles from cerium oxide particles, cerium oxide slurry or chemical mechanical polishing (CMP) compositions for Shallow Trench Isolation (STI) process are applied. The treated chemical mechanical polishing (CMP) compositions, or the CMP polishing compositions prepared by using the treated cerium oxide particles or the treated cerium oxide slurry are used to polish substrate that contains at least a surface comprising silicon dioxide film for STI (Shallow trench isolation) processing and applications. The reduced nano-sized particle related defects have been observed due to the reduced trace metal ion contaminants and reduced very smaller fine cerium oxide particles in the Shallow Trench Isolation (STI) CMP polishing.Type: GrantFiled: May 12, 2015Date of Patent: April 5, 2016Assignee: Air Products and Chemicals, Inc.Inventors: Xiaobo Shi, John Edward Quincy Hughes, Hongjun Zhou, Daniel Hernandez Castillo, II, Jae Ouk Choo, James Allen Schlueter, Jo-Ann Theresa Schwartz, Laura Ledenbach, Steven Charles Winchester, Saifi Usmani, John Anthony Marsella, Martin Kamau Ngigi Mungai
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Patent number: 9062230Abstract: Methods for removing, reducing or treating the trace metal contaminants and the smaller fine sized cerium oxide particles from cerium oxide particles, cerium oxide slurry or chemical mechanical polishing (CMP) compositions for Shallow Trench Isolation (STI) process are applied. The treated chemical mechanical polishing (CMP) compositions, or the CMP polishing compositions prepared by using the treated cerium oxide particles or the treated cerium oxide slurry are used to polish substrate that contains at lease a surface comprising silicon dioxide film for STI (Shallow trench isolation) processing and applications. The reduced nano-sized particle related defects have been observed due to the reduced trace metal ion contaminants and reduced very smaller fine cerium oxide particles in the Shallow Trench Isolation (STI) CMP polishing.Type: GrantFiled: September 10, 2014Date of Patent: June 23, 2015Assignee: Air Products and Chemicals, Inc.Inventors: Xiaobo Shi, John Edward Quincy Hughes, Hongjun Zhou, Daniel Hernandez Castillo, II, Jae Ouk Choo, James Allen Schlueter, Jo-Ann Theresa Schwartz, Laura Ledenbach, Steve Charles Winchester, Saifi Usmani, John Anthony Marsella, Martin Kamau Ngigi Mungai
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Publication number: 20150140489Abstract: Disclosed and claimed herein is a composition of matter having a general structure chosen from (I), (II), (III) or (IV); wherein X and Y are the same or different, wherein at least one of X and Y comprises an acid labile group, wherein R1 is a saturated or unsaturated group having from 1-4 carbon atoms, R2 is chosen from hydrogen or a saturated or unsaturated group having from 1-4 carbon atoms, R3 is a saturated or unsaturated group having from 1-4 carbon atoms, and R4 is a saturated or unsaturated group having from 1-4 carbon atoms.Type: ApplicationFiled: October 21, 2014Publication date: May 21, 2015Inventors: Alex Philip Graham Robinson, Dongxu Yang, Andreas Frommhold, Thomas Lada, John L. Roth, Xiang Xue
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Patent number: 8951997Abstract: The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH?CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.Type: GrantFiled: June 18, 2010Date of Patent: February 10, 2015Assignee: D. Western Therapeutics Institute, Inc.Inventors: Hiroyoshi Hidaka, Kouichi Takahashi, Yoshihiro Inoue, Kengo Sumi, Ryohei Nakamura
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Patent number: 8722881Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.Type: GrantFiled: October 13, 2010Date of Patent: May 13, 2014Assignee: Board of Trustees of the University of ArkansasInventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
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Patent number: 8716475Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: February 13, 2013Date of Patent: May 6, 2014Assignee: Janssen Pharmaceutica NVInventors: Frank Chavez, James P. Edwards, Brad M. Savall, Jennifer D. Venable
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Patent number: 8628978Abstract: A compound of formula (I) is provided: wherein: R1 is an optionally substituted 2-(1-azathiaxanthone); each —R2 is independently of the formula —CH2—C(?O)—R4, wherein R4 is an amino acid or a salt thereof, attached to the remainder of R2 through the nitrogen atom of the amino group; and R3 is hydrogen or a C1-6 alkyl group; or wherein: R1 is an optionally substituted 2-(1-azaxanthone); each R2 is independently an optionally substituted glutaric or succinic acid, or a salt or ester thereof; and R3 is hydrogen or a C1-6 alkyl group.Type: GrantFiled: January 29, 2010Date of Patent: January 14, 2014Assignee: University of DurhamInventors: David Parker, Robert Pal
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Patent number: 8592403Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, L and n are as defined in the specification. These compounds are useful as MC4 agonists.Type: GrantFiled: July 30, 2009Date of Patent: November 26, 2013Assignee: Pfizer LimitedInventors: Mark David Andrews, Christopher Gordon Barber
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Patent number: 8420626Abstract: The present invention relates to arene connected polyamine macrocyclic derivatives represented by general formula I, pharmaceutically acceptable salts or hydrates thereof which have anti-HIV activities, in which the definitions of substituents are as defined in the description; to preparation methods of the compounds of formula I; to pharmaceutical compositions containing the compounds of formula I or their pharmaceutically acceptable salts or hydrates; to the use of the compounds of formula I or their pharmaceutically acceptable salts or hydrates for the preparation of a medicament for the treatment and prevention of HIV-associated diseases.Type: GrantFiled: May 30, 2008Date of Patent: April 16, 2013Assignee: Beijing Molecule Science and Technology Co., Ltd.Inventors: Song Li, Jing Su, Yao Liu, Junhai Xiao, Lili Wang, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Guoming Zhao, Xiaokui Wang, Xinbo Zhou, Hongying Liu
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Patent number: 8415336Abstract: The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, Ra, R10, R20, R30, R40, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.Type: GrantFiled: January 19, 2012Date of Patent: April 9, 2013Assignee: SanofiInventors: Henning Steinhagen, Bodo Scheiper, Hans Matter, Gary McCort, Guillaume Begis, Pascale Goberville, Berangere Thiers
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Patent number: 8394789Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: February 6, 2009Date of Patent: March 12, 2013Assignee: MSD Oss B.V.Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
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Patent number: 8362164Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.Type: GrantFiled: October 12, 2011Date of Patent: January 29, 2013Assignee: Bridgestone CorporationInventor: Yan Yan-Yong
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Patent number: 8329771Abstract: The object of the present invention is to provide a photobase generator capable of efficiently generating amines (tertiary amines and amidine) high in catalytic activity by sensing light with a wavelength of from 350 to 500 nm (especially, from 400 to 500 nm). The present invention is a photobase generator characterized in being represented by general formula (1) or (2). Y+ is a quaternary ammonio group of general formula (3) to (5), and X? is a counter anion selected from among a borate anion, a phenolate anion, and a carboxylate anion.Type: GrantFiled: March 18, 2009Date of Patent: December 11, 2012Assignee: San-Apro LimitedInventors: Atsushi Shiraishi, Hideki Kimura
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Publication number: 20120220566Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: August 30, 2012Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
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Patent number: 8193174Abstract: The invention provides a compound comprising a xanthone or thiaxanthone sensitizing moiety, capable of coordinating to a lanthanide ion by the nitrogen atom of an integral pyridyl group or a related group able to bind a lanthanide ion.Type: GrantFiled: May 11, 2006Date of Patent: June 5, 2012Assignee: University of DurhamInventors: Parker David, Robert Pal, Junhua Yu
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Publication number: 20120035159Abstract: The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH?CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.Type: ApplicationFiled: June 18, 2010Publication date: February 9, 2012Applicant: D. WESTERN THERAPEUTICS INSTITUTE, INCInventors: Hiroyoshi Hidaka, Kouichi Takahashi, Yoshihiro Inoue, Kengo Sumi, Ryohei Nakamura
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Patent number: 8105567Abstract: Compounds of the formula: Wherein R is selected from the group consisting of H, NH2, and NHBoc; and R? is selected from the group consisting of H, CH2Ph and tBu, optionally de-protected. Such compounds may be conjugated with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi, 213Bi, 214Bi, 105Rh, 109Pd, 117mSn, 177Sn and 199Au, as well as the salts thereof with physiologically compatible bases or acids.Type: GrantFiled: September 3, 2009Date of Patent: January 31, 2012Assignee: Bracco Imaging SpAInventors: Kondareddiar Ramalingam, Rolf E. Swenson
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Publication number: 20120004206Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: August 25, 2011Publication date: January 5, 2012Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Patent number: 8034898Abstract: Diagnostic compositions and methods for imaging and/or assessing collagen are described. The diagnostic compositions can include collagen binding peptides.Type: GrantFiled: December 29, 2006Date of Patent: October 11, 2011Assignee: Collagen Medical, LLCInventors: Peter D. Caravan, Andrew Kolodziej, Zhaoda Zhang, Stephane Dumas, Biplab Kumar Das, Vincent Jacques, Richard Looby, Steffi K. Koerner, Wei-Chuan Sun, David R. Buckler, Aida Abujoub, Aaron K. Sato
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Patent number: 8012969Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.Type: GrantFiled: January 11, 2006Date of Patent: September 6, 2011Assignee: GE Healthcare LimitedInventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Sobolov-Jaynes, Timothy James McCarthy
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Patent number: 7960181Abstract: The invention relates to methods of determining potassium ions in a sample, wherein the ions are contacted with a compound having chromophoric moiety and an ionophoric moiety, where the ionophoric moiety interacts with the potassium ions present in the sample, resulting in the chromophoric moiety changing its radiation absorption properties in the ultraviolet and visible regions of the spectrum. For example, a change in an intensity of an absorption maximum is measured and the ion concentration is determined accordingly.Type: GrantFiled: May 2, 2007Date of Patent: June 14, 2011Assignee: OPTI Medical SystemsInventors: Huarui He, Chao Lin, Neeta Raje, Chuseng Liu
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Publication number: 20110136814Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, L and n are as defined in the specification. These compounds are useful as MC4 agonists.Type: ApplicationFiled: July 30, 2009Publication date: June 9, 2011Inventors: Mark David Andrews, Christopher Gordon Barber
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Publication number: 20110073331Abstract: The present invention relates to the use of ionic liquids as flame retardants. The compounds of the invention may be used as flame retardants in various materials without causing damage to the environment and or health of humans or animals. Ionic liquid flame retardants maybe applied alone or in combination with traditional flame retardants. Ionic liquid flame retardants can be applied to finish textile, plastic, leather, paper, rubber or as wild fire flame retardants.Type: ApplicationFiled: November 16, 2010Publication date: March 31, 2011Inventor: Yanjie Xu
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Publication number: 20110039832Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: N.V. OrganonInventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
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Publication number: 20110039467Abstract: The present invention relates to the use of ionic liquids as flame retardants. The compounds of the invention may be used as flame retardants in various materials without causing damage to the environment and or health of humans or animals. Ionic liquid flame retardants maybe applied alone or in combination with traditional flame retardants. Ionic liquid flame retardants can be applied to finish textile, plastic, leather, paper, rubber, or as wild fire flame retardants.Type: ApplicationFiled: August 9, 2010Publication date: February 17, 2011Applicant: H&C ChemicalInventor: Yanjie Xu
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Patent number: 7863440Abstract: Disclosed are a macrocyclic carbodiimide (MC-CDI) and a process for synthesizing the same through condensation of a molecule with multiple-isocyanate terminal functional groups under high dilution in the presence of a phospholene catalyst such as phospholene or arsenic catalyst. Also disclosed are MC-CDI derivatives, such as MC-urea (MC-U), MC-acylurea (MC-ACU), acid functionalized MC-ACU, and anhydride functionalized MC-ACU, processes for synthesizing the same, and the applications of such derivatives as hydrolysis stabilizers in organic polymeric materials, such as polyurethane (PU) and polyesters, as well as the applications in the syntheses of the amide- and imide-modified polyurethane by ring-opening reaction of the MC-ACU.Type: GrantFiled: December 28, 2006Date of Patent: January 4, 2011Assignee: Great Eastern Resins Industrial Co., Ltd.Inventors: Shenghong A. Dai, Chih-Chia Cheng, Chien-Wen Chen, Chih-Hung Chen
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Patent number: 7851621Abstract: A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.Type: GrantFiled: May 31, 2006Date of Patent: December 14, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Marzi, Maria Di Marzo
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Patent number: 7829563Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.Type: GrantFiled: February 27, 2008Date of Patent: November 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7754711Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: February 9, 2005Date of Patent: July 13, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Nagasree Chakka, Mikhail Chafeev, Sultan Chowdhury, Jian-Min Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Michael D. Winther, Zaihui Zhang, Melwyn Abreo, Mark W. Holladay, Wenbao Li, Sengen Sun, Chi Tu, Heinz W. Gschwend
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Patent number: 7745619Abstract: The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed.Type: GrantFiled: October 31, 2007Date of Patent: June 29, 2010Assignee: Albany Molecular Research, Inc.Inventors: Ian L. Scott, Jeffrey M. Ralph, Matthew E. Voss
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Publication number: 20100160626Abstract: There is provided processes for the preparation of various compounds, including compounds of formulae I, IV and VII, or salts and/or solvates thereof, which compounds are useful intermediates in the synthesis of certain oxabispidines having antiarrhythmic activity, such as compounds of formula XI wherein R1?, R15?, R16?, R18? and D have meanings given in the description.Type: ApplicationFiled: June 12, 2006Publication date: June 24, 2010Applicant: ASTRAZENECA ABInventors: Emma Anderson, David Cladingboel, Gareth Ensor, David Holmes, Mark Purdie
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Patent number: 7718658Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 31, 2005Date of Patent: May 18, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Lev Fanning, Paul Krenitsky, Joshua Boger
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Patent number: 7683168Abstract: Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.Type: GrantFiled: April 14, 2006Date of Patent: March 23, 2010Assignee: Mount Cook Bio Sciences, Inc.Inventors: Shyi-Tai Jan, Kwen-Jen Chang, Kestutis P. Biciunas, Xin Ma
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Patent number: 7659393Abstract: A method of preparing cyclene having formula (I) from triethylenetetraamine having formula (VIII) or ethylenediamine having formula (VIII?) includes a series of steps. The first series of steps (I) includes a step A (one-pot preparation of the compound having formula (IIa) from the compound having formula (VIII)), followed by a step B (transforming the compound having formula (IIa) into cyclene having formula (I)). The second series of steps (II) includes a step C (preparing the compound having formula (IIb) from the compound having formula (VIII)), followed by a step D (transforming the compound having formula (IIb) into cylcene having formula (I)). The third series of steps (III) includes a step E involving the onepot preparation of the compound having formula (IIa) from the compound having formula (VIII), followed by a step B involving the transformation of the compound having formula (IIa) into cyclene having formula (I).Type: GrantFiled: June 4, 2004Date of Patent: February 9, 2010Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Frederic Boschetti, Fanny Chaux, Franck Denat, Roger Guilard, Henry Ledon
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Patent number: 7632943Abstract: A novel reaction scheme is presented for making a 3,3,7,7-tetrakis(difluoramino)octahydro-1,5-diazocinium salt, such as HNFX, from a tetrahydro-1,5-diazocine-3,7(2H,6H)-dione that does not employ N-nitrolysis,—but that instead requires protolytic N-deprotection, or protolytic denosylation, (i.e., the nosyl N-protecting group is replaced with protons, forming the corresponding protonated amine or ammonium derivative). In summary, the present method subjects a suitably N-protected dione to difluoramination followed by protolytic N-deprotection by addition of a superacid and subsequent nitration utilizing an electrophilic nitrating agent to yield the diazocinium salt.Type: GrantFiled: December 10, 2004Date of Patent: December 15, 2009Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert D. Chapman, Thomas J. Groshens
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Patent number: 7618957Abstract: The invention relates to the subjects that are characterized in the claims, namely perfluoroalkyl-containing metal complexes with nitrogen-containing radicals of general formula I, process for their production and their use in NMR and x-ray diagnosis, radiodiagnosis, and radiotherapy, as well as in MRT lymphography and in blood-pool imaging.Type: GrantFiled: July 17, 2006Date of Patent: November 17, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heiko Schirmer, Hanns-Joachim Weinmann, Johannes Platzek, Ludwig Zorn, Bernd Misselwitz, Joerg Meding, Heribert Schmitt-Willich, Thomas Brumby
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Patent number: 7612055Abstract: The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: November 4, 2004Date of Patent: November 3, 2009Assignee: Novartis AGInventors: Yves Auberson, Claudia Betschart, Ralf Glatthar, Kurt Laumen, Rainer Machauer, Marina Tintelnot-Blomley, Thomas J. Troxler, Siem Jacob Veenstra
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Patent number: 7582280Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.Type: GrantFiled: July 8, 2008Date of Patent: September 1, 2009Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
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Patent number: 7563889Abstract: 3,3,7,7-Tetrakis(difluoramino)octahydro-1,5-diazocinium intermediate salts and method for making the salts, through difluoramination followed by N-denosylation or N-deprotection, which are valuable for use as precursor(s) to HNFX as well as to other members of the rare class of 3,3,7,7-tetrakis(difluoramino)octahydro-1,5-diazocines.Type: GrantFiled: December 10, 2004Date of Patent: July 21, 2009Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert D. Chapman, Thomas J. Groshens
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Patent number: 7538114Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: June 26, 2007Date of Patent: May 26, 2009Assignee: Amgen Inc.Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Patent number: 7531543Abstract: The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: May 12, 2009Assignee: WyethInventors: Paige Erin Mahaney, Eugene John Trybulski, Lori Krim Gavrin, An Thien Vu
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Patent number: 7514436Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: July 29, 2004Date of Patent: April 7, 2009Assignee: Xenon Pharmaceuticals Inc.Inventors: Heinz W. Gschwend, Vishnumurthy Kodumuru, Shifeng Liu, Rajender Kamboj
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Publication number: 20090075981Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 1, 2008Publication date: March 19, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
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Patent number: 7470469Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality. The functionalities can be carboxylate, amine, or sulfate groups and/or polyethylene glycol and can optionally include crosslinking groups.Type: GrantFiled: July 5, 2007Date of Patent: December 30, 2008Assignee: Advanced Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7468435Abstract: The present invention provides compound of the formula (I): in which at least two of R1, R2, R3, R4, R5, and R6 are N2O2M and related compounds substrates, compositions, and methods of using such compounds and compositions to treat biological disorders in which a polyphasic release of nitric oxide would be beneficial.Type: GrantFiled: November 5, 2004Date of Patent: December 23, 2008Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: David J. Waterhouse, Preeya Kapur, Larry K. Keefer, Joseph A. Hrabie, Frank De Rosa
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Publication number: 20080261938Abstract: The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, R14, R15, A, Ar, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: October 25, 2005Publication date: October 23, 2008Inventors: Caterina Ercolani, Joerg Habermann, Frank Narjes, Simona Ponzi, Michael Rowley, Ian Stansfield
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil