The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen (e.g., 2 Benzamidomethyl - Pyrrolidines, Etc.) Patents (Class 548/567)
  • Patent number: 9608680
    Abstract: 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: Grant
    Filed: August 19, 2014
    Date of Patent: March 28, 2017
    Assignee: American Messaging Services, LLC
    Inventors: John F. Nagel, J. Roy Pottle, Peter C. Barnett, David Andersen, Jamie Gordon Nlchol, Sangsoo Kim
  • Publication number: 20150148549
    Abstract: 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: Application
    Filed: June 10, 2013
    Publication date: May 28, 2015
    Inventors: R. Michael Van Dam, Gaurav Shah, Pei-Yuin Keng
  • Patent number: 9040508
    Abstract: 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: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 8853392
    Abstract: 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: Grant
    Filed: June 3, 2008
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Publication number: 20140294978
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: October 2, 2014
    Applicant: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Takeshi KUBOYAMA, Kaori YAGI, Tomoyuki NAOI, Tomohiro ERA
  • Publication number: 20140275086
    Abstract: 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: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: 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
  • Publication number: 20140243374
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
  • Patent number: 8735604
    Abstract: 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: Grant
    Filed: September 16, 2010
    Date of Patent: May 27, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
  • Publication number: 20140107335
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20140073803
    Abstract: 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: Application
    Filed: September 11, 2012
    Publication date: March 13, 2014
    Applicant: ATOMIC ENERGY COUNCIL - INSTITUTE OF NUCLEAR ENERGY RESEARCH
    Inventors: 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
  • Patent number: 8624039
    Abstract: 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: Grant
    Filed: March 4, 2010
    Date of Patent: January 7, 2014
    Assignee: SNU R&DB Foundation
    Inventors: Sang Eun Kim, Byung Chul Lee, Byung Seok Moon, Yu Kyeong Kim
  • Publication number: 20130303757
    Abstract: 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: Application
    Filed: February 25, 2013
    Publication date: November 14, 2013
    Inventors: Duncan H. HUNTER, Mustafa JANABI
  • Publication number: 20130296279
    Abstract: 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: Application
    Filed: May 10, 2013
    Publication date: November 7, 2013
    Inventor: Adam Morgan
  • Publication number: 20130231319
    Abstract: 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: Application
    Filed: November 16, 2011
    Publication date: September 5, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
  • Publication number: 20130217660
    Abstract: 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: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20130190338
    Abstract: 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: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130096319
    Abstract: 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: Application
    Filed: June 9, 2011
    Publication date: April 18, 2013
    Applicant: Lupin Limited
    Inventors: Dinesh Jayntibhai Paghdar, Mahesh Ramkumar Kolekar, Tushar Nandkumar Deshpande, Suryaprakash Pandurang Patil, Yuvraj Atmaram Chavan, Purna Chandra Ray, Girij Pal Singh
  • Publication number: 20130030184
    Abstract: 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: Application
    Filed: October 4, 2012
    Publication date: January 31, 2013
    Applicant: PERKINELMER HEALTH SCIENCES, INC.
    Inventor: PerkinElmer Health Sciences, Inc.
  • Publication number: 20130004518
    Abstract: 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: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: 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
  • Patent number: 8314139
    Abstract: 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: Grant
    Filed: January 18, 2008
    Date of Patent: November 20, 2012
    Assignee: Pfizer Inc.
    Inventors: Todd W Butler, Travis T Wager
  • Publication number: 20120264949
    Abstract: 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: Application
    Filed: April 13, 2011
    Publication date: October 18, 2012
    Applicant: ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCH
    Inventors: Shih-Ying Lee, Kang-Wei Chang, Chia-Chieh Chen
  • Patent number: 8283478
    Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: October 9, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ahmed F. Abdel-Magid, Steven J. Mehrman
  • Publication number: 20120178920
    Abstract: 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: Application
    Filed: March 4, 2010
    Publication date: July 12, 2012
    Applicant: Snu R&DB Foundation
    Inventors: Sang Eun Kim, Byung Chul Lee, Byung Seok Moon, Yu Kyeong Kim
  • Patent number: 8202866
    Abstract: 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: Grant
    Filed: August 19, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu
  • Publication number: 20120142659
    Abstract: 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: Application
    Filed: November 29, 2011
    Publication date: June 7, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Jonas Bostrõm, Hans Emtenäs, Kenneth Granberg, Mickael Mogemark, Antonio Llinas
  • Patent number: 8188296
    Abstract: 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: Grant
    Filed: March 31, 2006
    Date of Patent: May 29, 2012
    Assignee: GE Healthcare Limited
    Inventors: Ton Janssen, Jan Van Den Bos
  • Patent number: 8173700
    Abstract: 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: Grant
    Filed: May 17, 2006
    Date of Patent: May 8, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel
  • Patent number: 8158673
    Abstract: 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 and
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: April 17, 2012
    Assignee: Pfizer Inc.
    Inventors: Travis T. Wager, Ramalakshmi Y Chandrasekaran, Todd William Butler
  • Publication number: 20120035154
    Abstract: 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: Application
    Filed: September 1, 2011
    Publication date: February 9, 2012
    Applicant: SARcode Bioscience, Inc.
    Inventors: Wang SHEN, Kenneth BARR, Johan D. OSLOB, Min ZHONG
  • Publication number: 20120004413
    Abstract: 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: Application
    Filed: September 13, 2011
    Publication date: January 5, 2012
    Applicant: PerkinElmer Health Sciences, Inc.
    Inventor: Jerry Scot Pounds
  • Publication number: 20110301133
    Abstract: 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: Application
    Filed: December 8, 2009
    Publication date: December 8, 2011
    Applicant: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 8063098
    Abstract: 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: Grant
    Filed: August 14, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
  • Patent number: 8058475
    Abstract: 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: Grant
    Filed: June 20, 2008
    Date of Patent: November 15, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Beatrix Merla, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Achim Kless, Petra Bloms-Funke, Babette-Yvonne Koegel, Heinze Graubaum
  • Publication number: 20110275615
    Abstract: 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 un
    Type: Application
    Filed: October 29, 2010
    Publication date: November 10, 2011
    Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
  • Publication number: 20110275797
    Abstract: 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: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Patent number: 8030502
    Abstract: 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: Grant
    Filed: October 17, 2007
    Date of Patent: October 4, 2011
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, David Oare, Junning Lee, Weijiang Zhang
  • Publication number: 20110224256
    Abstract: The invention features methods, kits, and compositions for the treatment of psychiatric disorders using therapeutic imprinting in pre-pubescent subjects.
    Type: Application
    Filed: June 12, 2009
    Publication date: September 15, 2011
    Inventor: Susan L. Andersen
  • Patent number: 8013241
    Abstract: 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: Grant
    Filed: October 16, 2006
    Date of Patent: September 6, 2011
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventors: Nagatoshi Koumura, Koujirou Hara, Zhong-Sheng Wang, Masaru Yoshida, Nobuyuki Tamaoki
  • Publication number: 20110207739
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Publication number: 20110160176
    Abstract: 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, 2
    Type: Application
    Filed: August 25, 2010
    Publication date: June 30, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
  • Publication number: 20100324046
    Abstract: 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: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20100298299
    Abstract: 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: Application
    Filed: October 27, 2007
    Publication date: November 25, 2010
    Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
  • Publication number: 20100222581
    Abstract: 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: Application
    Filed: May 14, 2010
    Publication date: September 2, 2010
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
  • Patent number: 7745642
    Abstract: 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: Grant
    Filed: December 21, 2005
    Date of Patent: June 29, 2010
    Assignee: Glaxo Group Limited
    Inventors: Daniel Marcus Bradley, Roderick Alan Porter
  • Publication number: 20100144720
    Abstract: 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: Application
    Filed: December 11, 2009
    Publication date: June 10, 2010
    Applicant: ChemoCentryx, Inc.
    Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, John J. Wright
  • Publication number: 20100056805
    Abstract: 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: Application
    Filed: November 6, 2009
    Publication date: March 4, 2010
    Inventors: Takayuki Gotoh, Ichirou Araya
  • Publication number: 20100048531
    Abstract: 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: Application
    Filed: August 14, 2009
    Publication date: February 25, 2010
    Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
  • Patent number: 7652153
    Abstract: 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: Grant
    Filed: February 28, 2005
    Date of Patent: January 26, 2010
    Inventors: Jean Damien Charrier, Steven Durrant, Michael Mortimore, Michael O'Donnell, Alistair Rutherford, Sharn Ramaya, John Studley, Martin Trudeau, Adam Looker
  • Publication number: 20100016374
    Abstract: Compounds of formula (I) and salts and solvates are provided: wherein R2 is selected from phenyl substituted with n R1 groups, and pyridyl substituted with n R1 groups; n=0, 1 or 2; each R1 is independently selected from the group consisting of halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and cyano; R3 is selected from hydrogen and C1-2 alkyl; R4 is selected from the group consisting of ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C1-4alkyl, and haloC1-4alkyl; R12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R13 is selected from hydrogen, chloro and trifluoromethyl; R14 is selected from hydrogen, trifluoromethyl and chloro; R15 is selected from hydrogen, chloro and trifluoromethyl; R16 is selected
    Type: Application
    Filed: April 3, 2007
    Publication date: January 21, 2010
    Inventors: Steven Coulton, Martin Gilpin, Roderick Alan Porter
  • Patent number: 7649011
    Abstract: 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: Grant
    Filed: December 22, 2003
    Date of Patent: January 19, 2010
    Assignee: Chemocentryx, Inc.
    Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, J. J. Wright