Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/566)
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Patent number: 11589583Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: GrantFiled: May 17, 2019Date of Patent: February 28, 2023Assignee: FMC CorporationInventors: Andrew Duncan Satterfield, Thomas Paul Selby, David Andrew Travis, Kanu Maganbhai Patel, Andrew Edmund Taggi
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Patent number: 11528906Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: GrantFiled: January 18, 2022Date of Patent: December 20, 2022Assignee: FMC CorporationInventors: Andrew Duncan Satterfield, Thomas Paul Selby
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Patent number: 9108915Abstract: The present invention provides an inexpensive and industrially advantageous method for producing an optically active form of an anti-(3S,4R)-3-alkylcarbamoyl-4-hydroxypyrrolidine derivative or it's enantiomer, which is a key intermediate for producing a high-quality optically active form of (3R,4S)-3-alkylaminomethyl-4-fluoropyrrolidine or it's enantiomer useful as an intermediate for producing pharmaceuticals. The present invention relates to a method for producing an optically active anti-(3S,4R)-4-hydroxypyrrolidine-3-carboxamide derivative, or it's enantiomer by carrying out asymmetric hydrogenation using an optically active catalyst of a 4-oxopyrrolidine-3-carboxamide derivative represented by the general formula (I). [in the formula (I), PG1 represents a protective group for an amino group, and R1 represents hydrogen, a C1 to C6 alkyl group which may be substituted, or a C3 to C8 cycloalkyl group which may be substituted].Type: GrantFiled: October 24, 2011Date of Patent: August 18, 2015Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Ichiro Araya, Koichi Kiyota, Muneki Nagao
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Publication number: 20140371176Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
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Patent number: 8877754Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: August 17, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
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Patent number: 8865741Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: GrantFiled: February 18, 2012Date of Patent: October 21, 2014Assignee: Asana Biosciences, LLCInventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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Patent number: 8802856Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: October 22, 2013Date of Patent: August 12, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Patent number: 8791076Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.Type: GrantFiled: August 31, 2011Date of Patent: July 29, 2014Inventors: Pablo Villoslada, Angel Messeguer
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Publication number: 20140171439Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Publication number: 20140161830Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: Massachusetts Institute of TechnologyInventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
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Patent number: 8637568Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: July 8, 2013Date of Patent: January 28, 2014Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Publication number: 20140024679Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.Type: ApplicationFiled: December 31, 2012Publication date: January 23, 2014Applicant: Reviva Pharmaceuticals, Inc.Inventor: Reviva Pharmaceuticals, Inc.
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Publication number: 20130331397Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.Type: ApplicationFiled: February 23, 2012Publication date: December 12, 2013Applicant: IRM LLCInventors: Valentina Molteni, Yi Fan, Jon Loren, Jeffrey M. Smith, Brenton T. Flatt
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Patent number: 8592453Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: October 6, 2010Date of Patent: November 26, 2013Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Publication number: 20130310529Abstract: Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a group 4 metal and a Salan ligand in the polymerization of alpha-olefins, is disclosed. The Salan ligand is characterized by a sequential diamino-containing skeleton unit which is non-symmetric, and the pre-catalysts can also be such that are devoid of a symmetry element. The disclosed polymerization results in alpha-olefin polymers such as polypropylene which are characterized by high levels of tacticity. Also disclosed are novel Salan ligands and novel complexes thereof with group 4 metals.Type: ApplicationFiled: January 19, 2012Publication date: November 21, 2013Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Moshe Kol, Konstantin Press
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Publication number: 20130296322Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Patent number: 8536201Abstract: The present invention relates to novel pesticidal arylpyrrolidine compounds (arylpyrrolidines) having the general formula (I) wherein A, X1, X2, X3, X4, R1, R2, R3, R4, and G are as defined in the application and their use as pesticide, in particular for combating animal pests which occur in the agricultural and/or the veterinary field, as well as to a preparation methods for preparing such compounds.Type: GrantFiled: December 23, 2010Date of Patent: September 17, 2013Assignee: Bayer Intellectual Property GmbHInventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Norio Sasaki, Tetsuya Murata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Hidetoshi Kishikawa, Ulrich Görgens
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Patent number: 8501965Abstract: An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.Type: GrantFiled: May 30, 2011Date of Patent: August 6, 2013Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Masashi Suzuki, Muneki Nagao
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Patent number: 8501964Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: December 1, 2011Date of Patent: August 6, 2013Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Patent number: 8455646Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 22, 2009Date of Patent: June 4, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Publication number: 20130123243Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Inventor: Celtaxsys, Inc.
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Publication number: 20130109854Abstract: The present invention includes a method of preparing a composition comprising (+)-doxapram or a salt thereof, wherein the composition is essentially free of (?)-doxapram or a salt thereof.Type: ApplicationFiled: April 19, 2012Publication date: May 2, 2013Inventors: Scott L. Dax, Vita Ozola, Andrejs Krasikovs, Edgars Suna
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Publication number: 20130096271Abstract: Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a Group IV metal and a salalen ligand in the polymerization of alpha-olefins, is disclosed. The alpha-olefin polymers obtained are characterized by controlled levels of tacticity. Also disclosed are novel salalen ligands and novel complexes thereof with Group IV metals.Type: ApplicationFiled: June 16, 2011Publication date: April 18, 2013Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Moshe Kol, Konstantin Press, Ad Cohen
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Publication number: 20130085282Abstract: An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.Type: ApplicationFiled: May 30, 2011Publication date: April 4, 2013Inventors: Masashi Suzuki, Muneki Nagao
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Patent number: 8404728Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).Type: GrantFiled: July 29, 2010Date of Patent: March 26, 2013Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material CommandInventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
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Patent number: 8378121Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: October 6, 2010Date of Patent: February 19, 2013Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Patent number: 8354445Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: GrantFiled: May 11, 2011Date of Patent: January 15, 2013Assignee: MethylGene Inc.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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Publication number: 20130005988Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20120283448Abstract: Provided is an inexpensive and industrially advantageous method for preparing (3R,4S)-3-(N-substituted aminomethyl)-4-fluoropyrrolidine or an enantiomer thereof which can be an intermediate for producing pharmaceuticals. It relates to a method for preparing (3R,4S)-3-(N-substituted cyclopropylaminomethyl)-4-fluoropyrrolidine derivative or ait's enantiomer, or their salts, comprising a step of fluorinating a 4-hydroxy-3-(N-substituted aminomethyl)pyrrolidine derivative represented by the general formula (1) or an enantiomer thereof using a sulfur tetrafluoride derivative. [In the formula (1), PG represents a protective group for the amino group, and R1 represents a C1 to C6 alkyl group which may be substituted, or a C3 to C8 cycloalkyl group which may be substituted.Type: ApplicationFiled: January 7, 2011Publication date: November 8, 2012Inventors: Ichiro Araya, Kazuo Orita
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Publication number: 20120214809Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine.Type: ApplicationFiled: February 18, 2012Publication date: August 23, 2012Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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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: 20120149660Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R2, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.Type: ApplicationFiled: December 9, 2011Publication date: June 14, 2012Inventors: Jin-Jun Liu, Tina Morgan Ross
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Publication number: 20120142689Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Applicant: THERAVANCE, INC.Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
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Patent number: 8193184Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.Type: GrantFiled: April 20, 2008Date of Patent: June 5, 2012Assignee: Unimed Pharma, SPOL, S.R.O.Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
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Publication number: 20120128592Abstract: A compound for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) and a method of forming the compound is provided. The compound has Formula I: wherein W is selected from the group consisting of an optionally substituted aryl group and an optionally substituted heteroaryl group; each Y independently is NR1R2, wherein R1 and R2 are independently selected from the group consisting of H and C1-C6 alkyl, or R1 and R2 combine to form together with the nitrogen to which they are attached a heterocyclic group with 4 to 5 carbon atoms, is used to denote a single or a double bond, and Z is NH, NH2, NH—(C?O)—(CH2)n—SH, wherein n=1 to 10, or or a tautomer or stereoisomer thereof, or a salt thereof. A method and device for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) is also provided.Type: ApplicationFiled: October 12, 2011Publication date: May 24, 2012Inventors: Young-Tae CHANG, Kaustabh Kumar Maiti, Dinish Unnimadhava Kurup Soudamini Amma, Chit Yaw Fu, Malini Olivo, Kiat Seng Jason Soh, Seong-Wook Yun
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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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Publication number: 20110257243Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 30, 2011Publication date: October 20, 2011Applicant: THERAVANCE, INC.Inventors: Eric Stangeland, Daisuke Roland Saito, Adam Hughes, Jane Schmidt, Priscilla Van Dyke, Lori Jean Patterson
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Patent number: 8030344Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: GrantFiled: March 6, 2008Date of Patent: October 4, 2011Assignee: MethylGene Inc.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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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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Patent number: 8022203Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.Type: GrantFiled: May 31, 2007Date of Patent: September 20, 2011Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
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Patent number: 8017791Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.Type: GrantFiled: March 17, 2008Date of Patent: September 13, 2011Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 8017558Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 13, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 7994344Abstract: A process for producing an optically active compound represented by formula (4) or a salt thereof: the process including reacting a cyclization reagent with an optically active compound represented by formula (3) or its salt: optionally in the presence of a Lewis acid, to form the compound of formula (4) or its salt, wherein, in the compounds of formula (3) and formula (4) and their salts, R1 is a protecting group, and wherein the cyclization reagent is prepared from a titanium (IV) reagent and an alkylmetal compound.Type: GrantFiled: April 24, 2009Date of Patent: August 9, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Masao Fujita, Yutaka Kitagawa, Makoto Muto
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Patent number: 7968734Abstract: The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-selective reactions, and the method of their synthesis and use.Type: GrantFiled: June 30, 2005Date of Patent: June 28, 2011Assignee: STC.UNMInventors: Wei Wang, Jian Wang, Hao Li
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Patent number: 7834185Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: February 21, 2008Date of Patent: November 16, 2010Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Publication number: 20100280024Abstract: The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: October 13, 2008Publication date: November 4, 2010Inventors: Jigar Desai, Pravin S. Thombare, Mukul R. Jain, Pankaj Ramanbhai Patel
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Patent number: 7812180Abstract: The invention relates to an electropolymerizable monomer, intended to be polymerized in aqueous solution, comprising a single electropolymerizable unit and an electron-donating group, characterized in that it also comprises at least one arm ionizable in aqueous solution. The invention also relates to the polymerization process, to the electroactive probe thus obtained and to the method for the detection of a target ligand in a biological sample.Type: GrantFiled: July 7, 2006Date of Patent: October 12, 2010Assignees: Biomerieux, Centre National de la Recherche ScientifiqueInventors: Aurelie Bouchet, Carole Chaix, Bernard Mandrand
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Patent number: 7807709Abstract: The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesisType: GrantFiled: March 21, 2006Date of Patent: October 5, 2010Assignee: Novartis AGInventors: Claus Ehrhardt, Osamu Irie, Edwige Liliane Lorthiois, Juergen Klaus Maibaum, Nils Ostermann, Holger Sellner
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Publication number: 20100210630Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: April 30, 2010Publication date: August 19, 2010Inventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Patent number: 7776903Abstract: Pharmaceutical preparations containing substituted 2,5-diaminomethyl-1H-pyrrole compounds corresponding to formula I, and the use of these compounds for the production of pharmaceutical preparations and in related treatment methods.Type: GrantFiled: June 20, 2005Date of Patent: August 17, 2010Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Corinna Sundermann, Utz-Peter Jagusch, Werner Englberger, Hagen-Heinrich Hennies