The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen (e.g., 2 Benzamidomethyl - Pyrrolidines, Etc.) Patents (Class 548/567)
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Patent number: 11040943Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents.Type: GrantFiled: September 5, 2019Date of Patent: June 22, 2021Assignee: LB Pharmaceuticals Inc.Inventors: Andrew R. Vaino, Vincent T. Grattan, Zachary Prensky
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Patent number: 10689338Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents.Type: GrantFiled: September 5, 2019Date of Patent: June 23, 2020Assignee: LB Pharmaceuticals Inc.Inventors: Andrew R. Vaino, Vincent T. Grattan, Zachary Prensky
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Patent number: 9608680Abstract: An electronic messaging device includes a receiver configured to receive a message at one of a first operational frequency and second operational frequency. The messaging device can operate using a time synchronous protocol and can receive commands through over-the-internet-programming (OTIP) and over-the-air-programming (OTAP).Type: GrantFiled: August 19, 2014Date of Patent: March 28, 2017Assignee: American Messaging Services, LLCInventors: John F. Nagel, J. Roy Pottle, Peter C. Barnett, David Andersen, Jamie Gordon Nlchol, Sangsoo Kim
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Publication number: 20150148549Abstract: The present disclosure sets forth incorporating microfluidic chips Interfaces for use with digital microfluidic processes. Methods and devices according to the present disclosure utilize compact, integrated platforms that interface with a chip upstream and downstream of the reaction, as well as between intermediate reaction steps if needed. In some embodiments these interfaces are automated, including automation of a multiple reagent process. Various reagent delivery systems and methods are also disclosed.Type: ApplicationFiled: June 10, 2013Publication date: May 28, 2015Inventors: R. Michael Van Dam, Gaurav Shah, Pei-Yuin Keng
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Patent number: 9040508Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: GrantFiled: December 8, 2009Date of Patent: May 26, 2015Assignee: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Patent number: 8853392Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: June 3, 2008Date of Patent: October 7, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20140294978Abstract: The present invention provides a cationic lipid and the like. The cationic lipid is for delivering a medicament containing a cationic lipid which facilitates the introduction of a nucleic acid into a cell or the like, and is represented by formula (I).Type: ApplicationFiled: March 12, 2014Publication date: October 2, 2014Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Takeshi KUBOYAMA, Kaori YAGI, Tomoyuki NAOI, Tomohiro ERA
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Publication number: 20140275086Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
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Publication number: 20140243374Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.Type: ApplicationFiled: October 4, 2012Publication date: August 28, 2014Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
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Patent number: 8735604Abstract: The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: GrantFiled: September 16, 2010Date of Patent: May 27, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
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Publication number: 20140107335Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.Type: ApplicationFiled: October 10, 2013Publication date: April 17, 2014Applicant: H. Lundbeck A/SInventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
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Publication number: 20140073803Abstract: A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (Bu3Sn) that is easy to be replaced. Thus a dopamine receptor radiotracer 123I-IBZM can be produced at high yield rate by a substitution reaction of the precursor. At the same time, both the method for preparing the precursor SnBZM and a method for preparing a reference standard IBZM are simplified. Moreover, stability of each product is improved.Type: ApplicationFiled: September 11, 2012Publication date: March 13, 2014Applicant: ATOMIC ENERGY COUNCIL - INSTITUTE OF NUCLEAR ENERGY RESEARCHInventors: SHOW-WEN LIU, YU CHANG, CHENG-FANG HSU, MING-CHE TSAI, TSUNG-HSIEN CHIANG, YUEH-FENG DENG, KUEI-LIN LU, CHIH-YUAN LIN, DA-MING WANG, CHING-YUN LI
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Patent number: 8624039Abstract: A method for preparing [18F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0˜25 ?L of 40% TBAHCO3 or K2.2.2./K2CO3 (5˜25 mg/0.5˜3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water (1.0/0.2 (v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [18F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH3CN as a solvent into a reactor and by reacting the same for 5˜35 minutes at 50˜120° C.; and a fourth step for preparing a pure [18F]fallypride by purifying the prepared [18F]fallypride product.Type: GrantFiled: March 4, 2010Date of Patent: January 7, 2014Assignee: SNU R&DB FoundationInventors: Sang Eun Kim, Byung Chul Lee, Byung Seok Moon, Yu Kyeong Kim
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Publication number: 20130303757Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.Type: ApplicationFiled: February 25, 2013Publication date: November 14, 2013Inventors: Duncan H. HUNTER, Mustafa JANABI
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Publication number: 20130296279Abstract: The invention in one embodiment is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to a composition comprising the compound of formula I or a pharmaceutically acceptable salt, and methods of treating the indications listed herein.Type: ApplicationFiled: May 10, 2013Publication date: November 7, 2013Inventor: Adam Morgan
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Publication number: 20130231319Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.Type: ApplicationFiled: November 16, 2011Publication date: September 5, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130096319Abstract: The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.Type: ApplicationFiled: June 9, 2011Publication date: April 18, 2013Applicant: Lupin LimitedInventors: Dinesh Jayntibhai Paghdar, Mahesh Ramkumar Kolekar, Tushar Nandkumar Deshpande, Suryaprakash Pandurang Patil, Yuvraj Atmaram Chavan, Purna Chandra Ray, Girij Pal Singh
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Publication number: 20130030184Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naCbH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C3H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg—and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substitute containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: PERKINELMER HEALTH SCIENCES, INC.Inventor: PerkinElmer Health Sciences, Inc.
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Publication number: 20130004518Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: Merck, Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: 8314139Abstract: The present invention is directed to the tosylate salt of trans-N-ethyl-3- fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.Type: GrantFiled: January 18, 2008Date of Patent: November 20, 2012Assignee: Pfizer Inc.Inventors: Todd W Butler, Travis T Wager
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Publication number: 20120264949Abstract: A method is provided to label dopamine D2 receptors at striatum and areas outside of striatum. A radiosynthesized ligand of iodine(I)-123-Epidepride is used. The I-123-Epidepride can be strongly bonded to the D2 receptor and has a rare characteristic of non-specificity. Hence, it is suitable for developing a tracer for areas outside of striatum, where D2 receptor densities are low. Besides, I-123-Epidepride can be passed through blood brain barrier and has a high affinity to an animal's brain, so it can be used to develop medicines for diagnosing schizophrenia.Type: ApplicationFiled: April 13, 2011Publication date: October 18, 2012Applicant: ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCHInventors: Shih-Ying Lee, Kang-Wei Chang, Chia-Chieh Chen
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Patent number: 8283478Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.Type: GrantFiled: April 19, 2006Date of Patent: October 9, 2012Assignee: Janssen Pharmaceutica NVInventors: Ahmed F. Abdel-Magid, Steven J. Mehrman
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Publication number: 20120178920Abstract: A method for preparing [18F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0˜25 ?L of 40% TBAHCO3 or K2.2.2./K2CO3 (5˜25 mg/0.5˜3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water (1.0/0.2 (v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [18F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH3CN as a solvent into a reactor and by reacting the same for 5˜35 minutes at 50˜120° C.; and a fourth step for preparing a pure [18F]fallypride by purifying the prepared [18F]fallypride product.Type: ApplicationFiled: March 4, 2010Publication date: July 12, 2012Applicant: Snu R&DB FoundationInventors: Sang Eun Kim, Byung Chul Lee, Byung Seok Moon, Yu Kyeong Kim
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Patent number: 8202866Abstract: The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.Type: GrantFiled: August 19, 2009Date of Patent: June 19, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu
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Publication number: 20120142659Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: ASTRAZENECA ABInventors: Jonas Bostrõm, Hans Emtenäs, Kenneth Granberg, Mickael Mogemark, Antonio Llinas
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Patent number: 8188296Abstract: The present invention relates to stabilized 123I-labelled radiopharmaceutical compositions having a stabilizer which comprises gentisic acid or a salt thereof with a biocompatible cation. Methods of preparation of the stabilized radioiodine compositions as well as the use of gentisic acid to stabilize 123I-labelled radiopharmaceutical at a specified radioactive concentration range are also described.Type: GrantFiled: March 31, 2006Date of Patent: May 29, 2012Assignee: GE Healthcare LimitedInventors: Ton Janssen, Jan Van Den Bos
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Patent number: 8173700Abstract: The present invention relates to salts of substituted allophanates, methods for their production, medicaments containing said compounds and the use of said compound for the production of medicaments.Type: GrantFiled: May 17, 2006Date of Patent: May 8, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel
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Patent number: 8158673Abstract: This invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility andType: GrantFiled: October 13, 2006Date of Patent: April 17, 2012Assignee: Pfizer Inc.Inventors: Travis T. Wager, Ramalakshmi Y Chandrasekaran, Todd William Butler
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Publication number: 20120035154Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).Type: ApplicationFiled: September 1, 2011Publication date: February 9, 2012Applicant: SARcode Bioscience, Inc.Inventors: Wang SHEN, Kenneth BARR, Johan D. OSLOB, Min ZHONG
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Publication number: 20120004413Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naC5bH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C1H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg— and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substituent containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.Type: ApplicationFiled: September 13, 2011Publication date: January 5, 2012Applicant: PerkinElmer Health Sciences, Inc.Inventor: Jerry Scot Pounds
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Publication number: 20110301133Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: ApplicationFiled: December 8, 2009Publication date: December 8, 2011Applicant: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Patent number: 8063098Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.Type: GrantFiled: August 14, 2009Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
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Patent number: 8058475Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.Type: GrantFiled: June 20, 2008Date of Patent: November 15, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Beatrix Merla, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Achim Kless, Petra Bloms-Funke, Babette-Yvonne Koegel, Heinze Graubaum
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Patent number: 8030502Abstract: This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.Type: GrantFiled: October 17, 2007Date of Patent: October 4, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, David Oare, Junning Lee, Weijiang Zhang
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Publication number: 20110224256Abstract: The invention features methods, kits, and compositions for the treatment of psychiatric disorders using therapeutic imprinting in pre-pubescent subjects.Type: ApplicationFiled: June 12, 2009Publication date: September 15, 2011Inventor: Susan L. Andersen
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Patent number: 8013241Abstract: Disclosed is a novel ionic liquid gel electrolyte having high photoelectric conversion efficiency. Also disclosed are a novel dye-sensitized photoelectric conversion device using such an ionic liquid gel electrolyte, and a solar cell composed of such a dye-sensitized photoelectric conversion device. Specifically disclosed is an ionic liquid gel electrolyte obtained by gelling a liquid electrolyte by using an ionic organic oligomer gelling agent represented by the general formulae (1) and (2) below. Also specifically disclosed are a dye-sensitized photoelectric conversion device, wherein the ionic liquid gel electrolyte is arranged between a counter electrode and a dye-absorbed semiconductor substrate which is arranged in contact with a transparent conductive substrate, and a solar cell.Type: GrantFiled: October 16, 2006Date of Patent: September 6, 2011Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Nagatoshi Koumura, Koujirou Hara, Zhong-Sheng Wang, Masaru Yoshida, Nobuyuki Tamaoki
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20110207739Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG -
Publication number: 20110160176Abstract: The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2Type: ApplicationFiled: August 25, 2010Publication date: June 30, 2011Applicant: Abbott GmbH & Co. KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Publication number: 20100298299Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: October 27, 2007Publication date: November 25, 2010Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
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Publication number: 20100222581Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: May 14, 2010Publication date: September 2, 2010Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
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Patent number: 7745642Abstract: The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.Type: GrantFiled: December 21, 2005Date of Patent: June 29, 2010Assignee: Glaxo Group LimitedInventors: Daniel Marcus Bradley, Roderick Alan Porter
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Publication number: 20100144720Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.Type: ApplicationFiled: December 11, 2009Publication date: June 10, 2010Applicant: ChemoCentryx, Inc.Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, John J. Wright
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Publication number: 20100056805Abstract: An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidine or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields.Type: ApplicationFiled: November 6, 2009Publication date: March 4, 2010Inventors: Takayuki Gotoh, Ichirou Araya
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Publication number: 20100048531Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.Type: ApplicationFiled: August 14, 2009Publication date: February 25, 2010Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
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Patent number: 7652153Abstract: The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.Type: GrantFiled: February 28, 2005Date of Patent: January 26, 2010Inventors: Jean Damien Charrier, Steven Durrant, Michael Mortimore, Michael O'Donnell, Alistair Rutherford, Sharn Ramaya, John Studley, Martin Trudeau, Adam Looker