Piperidines Patents (Class 546/184)
  • Patent number: 7714089
    Abstract: Rubbery polymers can be formed having the general formula: R1R2N—(CH2)n—X—CH2—CHR3R4 wherein R1 and R2 are independently selected from a group consisting of alkyls, cycloalkyls, alkenyls, cycloalkenyls, aryls, phenyls, heterocycles, acyls, and silanes, or R1 in combination with R2 forms a heterocyclic ring; n is an integer from 1 to 20; X is selected from a group consisting of sulfur, a phosphorus moiety, and a silicon moiety; R3 and R4 are one of hydrogen, alkyls, alkenyls, and at least one of which includes reactive unsaturation such as an alkenyl group. Moreover, this invention discloses a process of making functionalized rubbery polymers from the functionalized monomers.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: May 11, 2010
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Adel Farhan Halasa, Wen-Liang Hsu, Leh-Yeh Hsu, legal representative, Shingo Futamura, Joe Zhou, Chad Aaron Jasiunas
  • Patent number: 7704409
    Abstract: A compound represented by formula (1): wherein R1 is hydrogen or alkyl having 1 to 20 carbons, in which in the alkyl, arbitrary —CH2— may be replaced by —O—, —S—, —COO—, —CH?CH— or —C?C—, and arbitrary hydrogen may be replaced by halogen or alkyl having 1 to 3 carbons; ring A1, ring A2, ring A3, ring A4 and ring A5 are each independently a benzene ring, a piperidine ring, a tetrahydropyrane ring or a dioxane ring, in which in the rings, arbitrary hydrogen may be replaced by halogen, alkyl having 1 to 3 carbons, alkoxy having 1 to 3 carbons or halogenated alkyl having 1 to 3 carbons, and —CH? may be replaced by —N?; Z1, Z2, Z4, Z5 and Z6 are each independently a single bond, —COO— or —CF2O—; Z3 is a single bond or —CF2O—, and in the case where Z3 is a single bond, ring A3 is a ring represented by formula (RG-5), or L1 and L2 are both fluorine, or at least one of Z1, Z2, Z4, Z5 and Z6 is —CF2O—; L1, L2, L3 and L4 are each independently hydrogen or halogen; X1 is hydrogen, halogen, —C?N, —N?C?S, —C?C—C?N, —S
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: April 27, 2010
    Assignees: Chisso Corporation, Chisso Petrochemical Corporation
    Inventors: Yasuhiro Haseba, Masayuki Saito
  • Patent number: 7705020
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: April 27, 2010
    Assignee: Pfizer Inc.
    Inventors: Koji Ando, Saturu Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Patent number: 7687518
    Abstract: 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: March 30, 2010
    Assignee: Purdue Pharma L.P.
    Inventor: Zhengming Chen
  • Patent number: 7683091
    Abstract: The present invention relates generally to substituted indoles and methods of using them.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: March 23, 2010
    Assignee: Wyeth
    Inventors: Baihua Hu, James W. Jetter
  • Patent number: 7683070
    Abstract: It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: March 23, 2010
    Assignee: FMC Corporation
    Inventors: Ping Ding, Robert N. Henrie, II, Daniel H. Cohen, John W. Lyga, David S. Rosen, George Theodoridis, Qun Zhang, Walter H. Yeager, Stephen F. Donovan, Stephen Shunxiang Zhang, Inna Shulman, Seong Jae Yu, Guozhi Wang, Y. Larry Zhang, Ariamala Gopalsamy, Dennis L. Warkentin, Paul E. Rensner, Ian R. Silverman, Thomas G. Cullen
  • Publication number: 20100069420
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 21, 2009
    Publication date: March 18, 2010
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20100056567
    Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: November 9, 2009
    Publication date: March 4, 2010
    Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jorgen Scheel-Krûger
  • Patent number: 7659403
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: February 9, 2010
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Patent number: 7659286
    Abstract: N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: February 9, 2010
    Assignee: AstraZeneca AB
    Inventors: Cathy Dantzman, Glen Ernst, Megan Murphy King
  • Patent number: 7655653
    Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: February 2, 2010
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozens
  • Patent number: 7649004
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
    Type: Grant
    Filed: July 12, 2005
    Date of Patent: January 19, 2010
    Assignee: Pfizer, Inc.
    Inventors: Charlotte Alice Louise Lane, Graham Nigel Maw, David James Rawson, Lisa Rosemary Thompson
  • Patent number: 7649009
    Abstract: Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: January 19, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Patent number: 7642355
    Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: January 5, 2010
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Eric L. Stangeland
  • Patent number: 7638639
    Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: December 29, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
  • Publication number: 20090312304
    Abstract: 3,4-substituted piperidine compounds, these 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; the use of a compound of that class 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; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.
    Type: Application
    Filed: December 28, 2005
    Publication date: December 17, 2009
    Inventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen K. Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
  • Patent number: 7632847
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: December 15, 2009
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Publication number: 20090306391
    Abstract: The invention relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by contacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a solid proton source under conditions sufficient to form the corresponding amine. The invention also relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by a) reacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material, and b) subsequently reacting the reaction product from step a) with an electrophile or a proton source. Preferred Stage 0 or Stage I alkali metal-silica gel materials include Na, K2Na, and Na2K.
    Type: Application
    Filed: February 13, 2007
    Publication date: December 10, 2009
    Applicant: SIGNA CHEMISTRY, LLC
    Inventors: Michael Lefenfeld, James L. Dye, Partha Nandi, James Jackson
  • Patent number: 7629336
    Abstract: The invention provides compounds of formula I: wherein a, b, c, d, n, R1, R2, R3, R6, R7, W, and A are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: December 8, 2009
    Assignee: Theravance, Inc.
    Inventors: Yu-Hua Ji, Craig Husfeld, Li Li, Mathai Mammen, YongQi Mu, Eric L. Stangeland
  • Patent number: 7615566
    Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: November 10, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
  • Patent number: 7612105
    Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: November 3, 2009
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
  • Patent number: 7598269
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: October 6, 2009
    Assignee: Bellus Health (International) Limited
    Inventors: Xianqi Kong, Walter A. Szarek, Francine Gervais
  • Patent number: 7598249
    Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Grant
    Filed: December 29, 2005
    Date of Patent: October 6, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, Mark Seierstad, Wei Xiao
  • Patent number: 7598386
    Abstract: Novel sulphones of Formula I are disclosed: wherein A completes a 4-7 membered ring optionally comprising up to two heteroatoms. The compounds modulate the action of ?-secretase and are therefore useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: October 6, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
  • Patent number: 7595329
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: September 29, 2009
    Assignee: Pfizer Inc
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Publication number: 20090239907
    Abstract: Therapeutic and prophylactic treatments of aquatic species and aquatic diseases through the controlled introduction of a heterocyclic N-halamine into an aquatic habitat.
    Type: Application
    Filed: February 28, 2007
    Publication date: September 24, 2009
    Applicant: HALOSOURCE, INC.
    Inventors: Michael A. Bridges, Christine M. Palczewski, James R. Scott, Jeremy Suess, Everett J. Nichols
  • Publication number: 20090227571
    Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Application
    Filed: June 30, 2006
    Publication date: September 10, 2009
    Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
  • Patent number: 7585856
    Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.
    Type: Grant
    Filed: August 12, 2003
    Date of Patent: September 8, 2009
    Assignee: The Brigham and Women's Hospital, Inc.
    Inventor: Charles N. Serhan
  • Publication number: 20090215764
    Abstract: Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.
    Type: Application
    Filed: May 3, 2006
    Publication date: August 27, 2009
    Inventors: Biswajit Das, Jasbir Singh Arora, Shahadat Ahmed, Anish Bandyopadhyay, Rita Katoch, Santosh Haribhau Kurhade, Sujata Rathy, Soma Ghosh, Abhijit Datta Khoje, Arti Gujrati, Dilip J. Upadhyay
  • Patent number: 7579465
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: August 25, 2009
    Assignee: Biota Scientific Managment Pty. Ltd.
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Patent number: 7576110
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: August 18, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 7572792
    Abstract: The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: April 25, 2005
    Date of Patent: August 11, 2009
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
  • Patent number: 7569588
    Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: August 4, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
  • Patent number: 7566716
    Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: July 28, 2009
    Assignee: Array Biopharma Inc.
    Inventors: Ellen Laird, George Topalov, Joseph P. Lyssikatos, Mike Welch, Jonas Grina, Josh Hansen, Brad Newhouse
  • Patent number: 7560549
    Abstract: A compound having the formula (I) wherein R1 is a substituted phenyl, R2 is a phenyl substituted with halogen atoms, R3 is a substituted phenyl, D is an oxygen or a methylene, and n is 0 or 1. The compound is a synthetic intermediate for a neurokinin receptor antagonist.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: July 14, 2009
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Tomori, Hiroshi Miyamoto, Keijiro Kobayashi
  • Publication number: 20090176988
    Abstract: The present application relates to mixed Mg/Li amides of the general formula R1R2N—Mg(NR3R4)mX,m zLiY (II) wherein R1, R2, R3, and R4 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together, or R3 and R4 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 and at least one of R3 and R is other than H; X and Y are, independently, selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; HalOn, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx, wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containi
    Type: Application
    Filed: January 18, 2007
    Publication date: July 9, 2009
    Inventors: Paul Knochel, Arkady Krasovskiy, Valeria Krasovskaya, Christoph Josef Rohbogner, Giuliano Cesar Clososki
  • Patent number: 7557104
    Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: July 7, 2009
    Assignee: Schering Corporation
    Inventors: Lianyun Zhao, Panduranga Adulla P. Reddy, Neng-Yang Shih, Kamil Paruch, Timothy J. Guzi, M. Arshad Siddiqui
  • Patent number: 7553837
    Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), (B-2) or (B-3); A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a); X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.
    Type: Grant
    Filed: July 30, 2004
    Date of Patent: June 30, 2009
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Mitsumasa Takada, Seiichi Ikeyama, Shiro Tsubokura, Yasuyuki Shiinoki, Fumie Shirato, Hiroko Momoe
  • Publication number: 20090156824
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: October 14, 2008
    Publication date: June 18, 2009
    Applicant: BOARD OF TRUSTEES OF UNIVERSITY OF ILLINOIS
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Publication number: 20090124806
    Abstract: To provide an industrially-useful and environmentally-friendly novel oxidation reaction.
    Type: Application
    Filed: May 6, 2008
    Publication date: May 14, 2009
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Yoshiharu IWABUCHI, Masatoshi Shibuya, Masaki Tomizawa, Takahisa Sato, Susumu Sato
  • Patent number: 7531656
    Abstract: Provided are a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a suspension in a dipolar aprotic solvent.
    Type: Grant
    Filed: August 14, 2003
    Date of Patent: May 12, 2009
    Assignee: Teva Pharmaceuticals USA, Inc.
    Inventors: Valerie Niddam-Hildesheim, Ben-Zion Dolitzky, Gideon Pilarski, Greta Sterimbaum
  • Patent number: 7524867
    Abstract: The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB1 receptor modulators, in particular CB1 receptor antagonists or inverse agonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: April 28, 2009
    Assignee: Solvay Pharmaceuticals, B.V.
    Inventors: Josephus H. M Lange, Henderik C. Wals, Cornelis G. Kruse
  • Patent number: 7517990
    Abstract: The present invention relates to a method for deuteration of a heterocyclic ring, which comprises subjecting a compound having a heterocyclic ring to sealed refluxing state in a deuterated solvent in the presence of an activated catalyst selected form a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. In accordance with a method of the present invention, a hydrogen atom belonging to a heterocyclic ring of a compound having a heterocyclic ring can be very efficiently deuterated because temperature of deuteration reaction can be maintained at higher than boiling point of the solvent. Further, a method for deuteration of the present invention can be applied widely to deuteration of various compounds having a heterocyclic ring which are liable to decomposition under supercritical conditions or acidic conditions, leading to industrial and efficient deuteration of a compound having a heterocyclic ring.
    Type: Grant
    Filed: November 7, 2003
    Date of Patent: April 14, 2009
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Nobuhiro Ito, Tsuneaki Maesawa, Kazushige Muto, Kosaku Hirota, Hironao Sajiki
  • Patent number: 7517989
    Abstract: The present invention provides a compound of formula (I), wherein: Z is (A) OR (B) and wherein the remaining variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of achemokine (such as CCR3) or H1 mediated disease state.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: April 14, 2009
    Assignee: AstraZeneca AB
    Inventors: Christopher Luckhurst, Matthew Perry, Hitesh Sanganee, Brian Springthorpe
  • Publication number: 20090093493
    Abstract: The invention relates to a new class of compounds, which are 1-phenylalcoxy-2-?-phenylethyl derivatives, as P-glycoprotein (P-GP) inhibitors. These compounds are useful in drug resistance events. They have been shown able to inhibit in a dose-dependent manner Glycoprotein-P (P-gp) activity in cell lines in which the expression of said glycoprotein is very high, like Caco-2 (human colon cancer) cells and MCF7/Adr (adriamycin-resistant human breast carcinoma) cells. The invention also relates to methods of production and the utilization of such compounds as medicaments useful in the treatment of states linked to the difficulty for some drugs to cross the blood-brain barrier (BBB) and generally within the context of the problems of drug resistance induced by chemotherapy agents.
    Type: Application
    Filed: October 9, 2007
    Publication date: April 9, 2009
    Inventors: Francesco Berardi, Nicola Antonio Colabufo, Roberto Perrone, Aldo Balsamo, Simona Rapposelli, Maria Digiacomo
  • Publication number: 20090082203
    Abstract: It has now been found that certain novel bis(substituted phenyl)-1 {[4-(saturated heterocyclyl-substituted)phenyl-methyl](4-piperidyl)}methane derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I); where R through R15, m, n, s, A, B, D and W are defined herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: December 9, 2005
    Publication date: March 26, 2009
    Applicant: Bayer Cropscience AG
    Inventors: John W. Lyga, David S. Rosen, Y. Larry Zhang, Ping Ding, Robert N. Henrie, II, Frank J. Zawacki, Charles E. Hatch, III, Shunxiang Zhang, Jaidev S. Goudar
  • Publication number: 20090065739
    Abstract: A compound represented by formula (1): wherein R1 is hydrogen or alkyl having 1 to 20 carbons, in which in the alkyl, arbitrary —CH2— may be replaced by —O—, —S—, —COO—, —CH?CH— or —C?C—, and arbitrary hydrogen may be replaced by halogen or alkyl having 1 to 3 carbons; ring A1, ring A2, ring A3, ring A4 and ring A5 are each independently a benzene ring, a piperidine ring, a tetrahydropyrane ring or a dioxane ring, in which in the rings, arbitrary hydrogen may be replaced by halogen, alkyl having 1 to 3 carbons, alkoxy having 1 to 3 carbons or halogenated alkyl having 1 to 3 carbons, and —CH? may be replaced by —N?; Z1, Z2, Z4, Z5 and Z6 are each independently a single bond, —COO— or —CF2O—; Z3 is a single bond or —CF2O—, and in the case where Z3 is a single bond, ring A3 is a ring represented by formula (RG-5), or L1 and L2 are both fluorine, or at least one of Z1, Z2, Z4, Z5 and Z6 is —CF2O—; L1, L2, L3 and L4 are each independently hydrogen or halogen; X1 is hydrogen, halogen, —C?N, —N?C?S, —C?C—C?N, —S
    Type: Application
    Filed: August 21, 2008
    Publication date: March 12, 2009
    Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATION
    Inventors: Yasuhiro HASEBA, Masayuki SAITO
  • Publication number: 20090062261
    Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: February 21, 2007
    Publication date: March 5, 2009
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
  • Patent number: 7495012
    Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:
    Type: Grant
    Filed: April 20, 2005
    Date of Patent: February 24, 2009
    Assignee: Amgen Inc.
    Inventors: Michael R. DeGraffenreid, Jay P. Powers, Daqing Sun, Xuelei Yan