Additional Hetero Ring Containing Patents (Class 546/135)
  • Patent number: 9453014
    Abstract: The present invention relates amide compounds of formula (I): wherein R1, R1a, Ar, A, B, W1, W2, D, a, b, and c are defined herein, and pharmaceutical acceptable salts thereof. These compounds have the ability to inhibit 11-?-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: September 27, 2016
    Assignee: Connexios Life Sciences Pvt. Ltd.
    Inventors: Jagannath Madanahalli Ranganath Rao, Uppala Venkatesham, Jenson George, George Fernand, Sivanageswara Rao Doppalapudi, G R Madhavan, Nagarajan Arumugam, Mohammed Ansari, K Murugavel, Jidugu Pradeep, Sulthan Allavuddeen, K Vijayaramalingam, Hampelingaiah Shiva Prasad, Augustine Michael Raj, S Gnanavel, Ramamoorthy Kottamalai, Naresh M P S Babu, Bommegowda Yadaganahalli Kenchegowda
  • Patent number: 9040706
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 26, 2015
    Assignee: GENENTECH, INC.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • Publication number: 20150139916
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Fabio RANCATI, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Publication number: 20150133491
    Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Fabio RANCATI, Ian LINNEY
  • Patent number: 8987299
    Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 24, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney
  • Patent number: 8980913
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: March 17, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Patent number: 8952165
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: February 10, 2015
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Patent number: 8877774
    Abstract: Compounds of formula(I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 4, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Andrea Rizzi, Gabriele Amari, Matteo Biagetti, Ian Linney
  • Publication number: 20140206633
    Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.
    Type: Application
    Filed: February 3, 2011
    Publication date: July 24, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
  • Patent number: 8785474
    Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: July 22, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
  • Publication number: 20140163066
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio RANCATI, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Publication number: 20140161736
    Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A
    Inventors: Fabio Rancati, Ian Linney
  • Patent number: 8618131
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthmas.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: December 31, 2013
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham, Adam D. Hughes, Craig Husfeld, Eric L. Stangeland
  • Patent number: 8609845
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: December 17, 2013
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • Publication number: 20130296340
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Application
    Filed: January 30, 2012
    Publication date: November 7, 2013
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Patent number: 8476296
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: July 2, 2013
    Assignee: Targacept, Inc.
    Inventors: Merouane Bencherif, Nikolai Fedorov, Terry Hauser, Kristen Jordan, Sharon Rae Letchworth, Anatoly Mazurov, Julio A. Munoz, Jason Speake, Daniel Yohannes
  • Patent number: 8476432
    Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: July 2, 2013
    Assignee: Yuhan Corporation
    Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
  • Publication number: 20130045169
    Abstract: Compounds of formula (I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.
    Type: Application
    Filed: June 8, 2012
    Publication date: February 21, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Fabio Rancati, Andrea Rizzi, Gabriele Amari, Matteo Biagetti, Ian Linney
  • Patent number: 8354536
    Abstract: The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic ?-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: January 15, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Thomas Cleary, Yaohui Ji, Thimma Rawalpally
  • Publication number: 20120277216
    Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.
    Type: Application
    Filed: December 29, 2009
    Publication date: November 1, 2012
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
  • Patent number: 8252811
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: August 28, 2012
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Truc Nguyen, Carla Gauss, Ashok Tehim
  • Patent number: 8242135
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: August 14, 2012
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Eric Stangeland
  • Patent number: 8137582
    Abstract: Disclosed is the chemical synthesis of chiral alkaloid monomers, liquid crystal compositions comprising the chiral alkaloid monomers, and polymerization of the liquid crystal compositions to provide polymer networks with useful cholesteric optical properties and stability.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: March 20, 2012
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Marc B. Goldfinger, Kai Qi
  • Patent number: 8134003
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: March 13, 2012
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Truc Nguyen, Carla Gauss, Ashok Tehim
  • Patent number: 8101766
    Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: January 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • Publication number: 20120004412
    Abstract: The present invention provides novel methods for preparing N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic ?-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.
    Type: Application
    Filed: June 23, 2011
    Publication date: January 5, 2012
    Inventors: Jodie Brice, Miall Cedilote, Zhiming Dong, Pingsheng Zhang
  • Patent number: 8088794
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: January 3, 2012
    Assignee: Amgen Inc.
    Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessandro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
  • Patent number: 8071601
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I).
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: December 6, 2011
    Assignee: Sanofi-Aventis
    Inventors: Peter Aranyi, Sandor Batori, Geza Timari, Kinga Boer, Zoltan Kapui, Endre Mikus, Katalin Urban-Szabo, Katalin Gerber, Judit Vargane Szeredi, Michel Finet
  • Patent number: 8044068
    Abstract: Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: October 25, 2011
    Assignees: Taisho Pharmaceutical Co., Ltd, Nissan Chemical Industries, Ltd.
    Inventors: Taketoshi Okubo, Toshihito Kumagai, Takaaki Ishii, Toshio Nakamura, Kumi Abe, Yuri Amada, Tomoko Ishizaka, Xiang-Min Sun, Yoshinori Sekiguchi, Shigetada Sasako, Takanori Shimizu, Takayuki Nagatsuka
  • Patent number: 8039482
    Abstract: A solid pharmaceutical preparation of solifenacin or a salt thereof, the preparation being stable and inhibited from decomposing with time when supplied to clinical fields. In a pharmaceutical preparation containing solifenacin or a salt thereof, the compound in an amorphous form was revealed to be causative of cardinal-drug decomposition with time. The composition for a solid pharmaceutical preparation of solifenacin or a salt thereof contains solifenacin or its salt each in a crystalline from, and the content provided are: a process for producing the composition; and a medicinal composition for solid pharmaceutical preparations which contains solifenacin and an amorphization inhibitor.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: October 18, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Akio Sugihara, Takehiko Yasuji, Katsuhiro Masaki, Daisuke Murayama
  • Patent number: 7951940
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: May 31, 2011
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Patent number: 7888510
    Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: February 15, 2011
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
  • Publication number: 20100317842
    Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
    Type: Application
    Filed: August 25, 2010
    Publication date: December 16, 2010
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
  • Publication number: 20100267712
    Abstract: Disclosed is a compound of Formula (I) in which W and R1-R6 are defined herein. Also disclosed is a method of treating spinal muscular atrophy, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced directly or indirectly by mutation or frameshift.
    Type: Application
    Filed: September 26, 2008
    Publication date: October 21, 2010
    Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,
    Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
  • Patent number: 7807694
    Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: October 5, 2010
    Assignee: Genzyme Corporation
    Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
  • Patent number: 7767670
    Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: August 3, 2010
    Assignee: Ambit Biosciences Corporation
    Inventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
  • Patent number: 7767193
    Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: August 3, 2010
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Lan Miao
  • Patent number: 7696242
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
    Type: Grant
    Filed: July 19, 2005
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Murray D. Bailey, Punit Bhardwaj, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Montse Llinas-Brunet, Marc-André Poupart, Jean Rancourt
  • Patent number: 7618961
    Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: November 17, 2009
    Assignee: Biovitrum AB
    Inventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
  • Patent number: 7595327
    Abstract: This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-?, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.
    Type: Grant
    Filed: March 16, 2006
    Date of Patent: September 29, 2009
    Assignee: Wyeth
    Inventors: Jeremy I. Levin, Zhong Li, George Diamantidis, Frank E. Lovering, Weiheng Wang, Jeffrey S. Condon, Yang-I Lin, Jerauld S. Skotnicki, Kaapjoo Park
  • Patent number: 7582657
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: September 1, 2009
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Elizabeth M. Doherty, Michael G. Kelly
  • Patent number: 7557212
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are provided as well as processes for the manufacture of such compounds. The compounds are useful in the treatment or prevention of inflammatory and allergic diseases.
    Type: Grant
    Filed: November 11, 2003
    Date of Patent: July 7, 2009
    Assignee: Laboratorios Almirall, S.A.
    Inventors: Carlos Puig Duran, Daniel Perez Crespo, Jordi Bach Tana, Hamish Ryder
  • Patent number: 7531662
    Abstract: One aspect of the present invention relates to cinchona-alkaloid-based catalysts. A second aspect of the invention relates to a method of preparing a derivatized cinchona alkaloid catalyst by reacting a cinchona-alkaloid with base and a compound that has a suitable leaving group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral cyclic anhydride or a meso cyclic anhydride, comprising the step of: reacting a prochiral cyclic anhydride or a meso cyclic anhydride with a nucleophile in the presence of a catalyst; wherein said prochiral cyclic anhydride or meso cyclic anhydride comprises an internal plane of symmetry or point of symmetry or both; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized cinchona-alkaloid.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: May 12, 2009
    Assignee: Brandeis University
    Inventors: Li Deng, Xiaofeng Liu
  • Patent number: 7521558
    Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: April 21, 2009
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • Patent number: 7482370
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.
    Type: Grant
    Filed: July 13, 2005
    Date of Patent: January 27, 2009
    Assignee: Schering Corporation
    Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar
  • Patent number: 7449478
    Abstract: This invention relates to treating peroxisome proliferator-activated receptors related diseases with certain indole compounds. The indole compounds are of formula (I) below. Each variable is defined in the specification.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: November 11, 2008
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Neeraj Mahindroo, Tsu-An Hsu, Chien-Fu Huang, Xin Chen, Yu-Sheng Chao
  • Patent number: 7439256
    Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R5 and J are defined herein, are useful in the treatment of cancer.
    Type: Grant
    Filed: September 15, 2005
    Date of Patent: October 21, 2008
    Inventors: Arlindo Castelhano, Andrew Crew, Hanqing Dong, An-Hu Li, Li Qiu, Alun Smith
  • Patent number: 7378421
    Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: May 27, 2008
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Teresa Mujica-Fernaud, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
  • Patent number: 7375219
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: May 20, 2008
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Patent number: 7355046
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: April 8, 2008
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes, Yan Chen