The -c(=x)- Group And The Piperidine Ring Are Bonded Directly To The Same Chalcogen Patents (Class 546/222)
  • Patent number: 9035061
    Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: May 19, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Pierre-Jean Colson
  • Patent number: 8952036
    Abstract: The present invention provides a MDM2 inhibitor compound, or a pharmaceutically acceptable salt thereof, which compound is useful as a therapeutic agent, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contains the MDM2 inhibitor.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 10, 2015
    Assignee: Amgen Inc.
    Inventor: Yosup Rew
  • Publication number: 20150038719
    Abstract: This invention provides a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect. The agent for ameliorating chronic obstructive pulmonary disease contains mepenzolate bromide as an active ingredient. More preferably the mode of administration of the agent for ameliorating chronic obstructive pulmonary disease is airway administration or inhalation administration, and furthermore the mode of administration thereof is oral administration or rectal administration. This invention is a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect of mepenzolate bromide.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Toru Mizushima, Hongxing Liu
  • Publication number: 20140371270
    Abstract: An acetic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted deuterated lower alkyl, is disclosed.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 18, 2014
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masato Nanri, Yoshikazu Iwasawa, Fukumitsu Sakakibara, Shinichi Aoki
  • Patent number: 8822679
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: California Institute of Technology
    Inventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
  • Patent number: 8754225
    Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: June 17, 2014
    Assignee: Theravance, Inc.
    Inventor: Pierre-Jean Colson
  • Patent number: 8633225
    Abstract: Cosmetic or dermatological compositions which comprise at least one piperidinium salt, preferably a 4-[(2-cyclopentyl-2-hydroxyphenylacetyl)oxy]-1,1-dimethyl-piperidinium salt, and the use thereof, particularly as antiperspirants. This Abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: January 21, 2014
    Assignee: Beiersdorf AG
    Inventors: Michael Woehrmann, Lara Terstegen, Annette Martin, Melanie Sulzberger
  • Patent number: 8623238
    Abstract: The present invention relates to compounds represented by the following Formula Ic, in which R2-R6 can each independently be selected from hydrogen or hydrocarbyl (e.g., methyl); L1 and L4 are each independently a divalent linking group, such as a bond or —OC(O)—R8—C(O)O—, where R8 can be divalent hydrocarbyl (e.g., —CH2CH2—); each L2 and each L5 each independently represent a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 and each L6 each independently represent a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t and s are each independently from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; q and r are each independently from 0 to 4 for each s, provided that the sum of q and r is at least 1 for each s; and E1 and E2 can each independently be hydrogen or hydrocarbyl.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: January 7, 2014
    Assignee: Transitions Optical, Inc.
    Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
  • Patent number: 8519138
    Abstract: A novel process for the preparation of the compound of formula (II): which process comprises reacting a compound of formula (VI): with a compound of formula (IV): in a suitable solvent.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: August 27, 2013
    Assignee: Glaxo Group Limited
    Inventors: Dean David Edney, Matthew Peter John
  • Patent number: 8507529
    Abstract: The present invention provides a dermatological and/or cosmetic composition which includes a methoxycinnamate, and a cyclic nitroxide. The present invention further provides a method of synthesizing photo absorbing-antioxidant compounds and their use in dermatological and/or cosmetic compositions. In addition, the present invention relates to the use of methoxycinnamate, and nitroxide compounds for the preparation of a composition for the dermatological and/or cosmetic treatment of skin.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: August 13, 2013
    Assignee: Jarrow Formulas, Inc.
    Inventors: Elisabetta Damiani, Paola Astolfi, Lucedio Greci
  • Publication number: 20130196978
    Abstract: 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: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130012384
    Abstract: The present invention relates to novel compounds of the formula (I), in which W, X, Y, Z, G, A and t have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the spiroheterocyclic tetronic acid derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner Fischer, Stefan Lehr, Olga Malsam, Arnd Voerste
  • Publication number: 20130012701
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Application
    Filed: June 22, 2012
    Publication date: January 10, 2013
    Applicant: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Patent number: 8349210
    Abstract: The present invention relates to compounds represented by the following Formula I, in which R1-R6 can each independently be selected from hydrogen or hydrocarbyl (e.g., methyl); L1 is a divalent linking group, such as a bond or —OC(O)—R8—C(O)O—, where R8 can be divalent hydrocarbyl (e.g., —CH2CH2—); each L2 independently represents a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 independently represents a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t is from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; and E can be hydrogen or hydrocarbyl. The present invention also relates to compositions, such as liquid crystal compositions, and articles, such as optical elements, that include the compound represented by Formula I.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: January 8, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
  • Patent number: 8334306
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: December 18, 2012
    Assignee: The Trustees of California State University
    Inventors: Yong Ba, Errol V. Mathias
  • Patent number: 8309732
    Abstract: What is described is a process for preparing compounds of the general formula (I) in which R1, R2 and R3 independently of one another represent hydrogen, an alkyl group or an aryl group, wherein compounds of the general formula (II) in which R1 and R2 have the meaning given for formula (I), are reacted with an alkylating agent of the general formula (III) R3X??(III), in which X represents a halogen atom and R3 has the meaning given for formula (I), if appropriate in a solvent.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: November 13, 2012
    Assignee: Saltigo GmbH
    Inventors: Andreas Job, Denys Baskakov, Ralf Krahwinkel, Antje Hieronymi
  • Publication number: 20120263650
    Abstract: Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
    Type: Application
    Filed: April 5, 2012
    Publication date: October 18, 2012
    Applicants: Wake Forest University, and Human Services
    Inventors: David A. Wink, Wilmarie Flores-Santana, S. Bruce King, Murali Krishna Cherukuri, James B. Mitchell
  • Patent number: 8198304
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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: Grant
    Filed: September 9, 2011
    Date of Patent: June 12, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20120122850
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 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: Application
    Filed: January 11, 2012
    Publication date: May 17, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Publication number: 20120071319
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Application
    Filed: May 21, 2010
    Publication date: March 22, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Patent number: 8134006
    Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 13, 2012
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
  • Publication number: 20120046469
    Abstract: A novel process for the preparation of the compound of formula (II): which process comprises reacting a compound of formula (VI): with a compound of formula (IV): in a suitable solvent.
    Type: Application
    Filed: April 14, 2010
    Publication date: February 23, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Dean David Edney, Matthew Peter John
  • Publication number: 20120027960
    Abstract: The present invention relates to compounds represented by the following Formula Ic, in which R2-R6 can each independently be selected from hydrogen or hydrocarbyl (e.g., methyl); L1 and L4 are each independently a divalent linking group, such as a bond or —OC(O)—R8—C(O)O—, where R8 can be divalent hydrocarbyl (e.g., —CH2CH2—); each L2 and each L5 each independently represent a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 and each L6 each independently represent a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t and s are each independently from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; q and r are each independently from 0 to 4 for each s, provided that the sum of q and r is at least 1 for each s; and E1 and E2 can each independently be hydrogen or hydrocarbyl.
    Type: Application
    Filed: August 8, 2011
    Publication date: February 2, 2012
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
  • Publication number: 20120029021
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 2, 2012
    Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITY
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20120016130
    Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
    Type: Application
    Filed: June 30, 2011
    Publication date: January 19, 2012
    Inventor: Pierre-Jean COLSON
  • Publication number: 20120003401
    Abstract: The present invention relates to compounds represented by the following Formula I, in which R1-R6 can each independently be selected from hydrogen or hydrocarbyl (e.g., methyl); L1 is a divalent linking group, such as a bond or —OC(O)—R8—C(O)O—, where R8 can be divalent hydrocarbyl (e.g., —CH2CH2—); each L2 independently represents a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 independently represents a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t is from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; and E can be hydrogen or hydrocarbyl. The present invention also relates to compositions, such as liquid crystal compositions, and articles, such as optical elements, that include the compound represented by Formula I.
    Type: Application
    Filed: August 8, 2011
    Publication date: January 5, 2012
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Ruisong XU, Xiao-Man DAI, Anil KUMAR, Meng HE, Chenguang LI, Rachael L. YOEST
  • Publication number: 20110281851
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 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: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Publication number: 20110201583
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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: Application
    Filed: April 28, 2011
    Publication date: August 18, 2011
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Patent number: 7960385
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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: Grant
    Filed: September 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Patent number: 7910607
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Grant
    Filed: March 12, 2007
    Date of Patent: March 22, 2011
    Assignee: The Trustees of California State University
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20110027203
    Abstract: The present invention provides a dermatological and/or cosmetic composition which includes a methoxycinnamate, and a cyclic nitroxide. The present invention further provides a method of synthesizing photo absorbing-antioxidant compounds and their use in dermatological and/or cosmetic compositions. In addition, the present invention relates to the use of methoxycinnamate, and nitroxide compounds for the preparation of a composition for the dermatological and/or cosmetic treatment of skin.
    Type: Application
    Filed: October 11, 2010
    Publication date: February 3, 2011
    Inventors: Elisabetta Damiani, Paola Astolfi, Lucedio Greci
  • Patent number: 7880010
    Abstract: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: February 1, 2011
    Assignee: Theravance, Inc.
    Inventors: Jennifer Bolton, Robert S. Chao, Miroslav Rapta, Lisa Williams, Richard D. Wilson
  • Patent number: 7851633
    Abstract: Cosmetic or dermatological compositions which comprise at least one piperidinium salt, preferably a 4-[(2-cyclopentyl-2-hydroxyphenylacetyl)oxy]-1,1-dimethyl-piperidinium salt, and the use thereof, particularly as antiperspirants. This Abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: December 14, 2010
    Assignee: Beiersdorf AG
    Inventors: Michael Woehrmann, Lara Terstegen, Annette Martin, Melanie Sulzberger
  • Publication number: 20100305159
    Abstract: The present invention is to provide a crystalline form of (2R,4S)-1-{N-(3,5-bistrifluoromethylbenzyl)-N-methyl}aminocarbonyl-2-(4-fluoro-2-methylphenyl)-4-(2-hydroxyethylaminocarbonyloxy)piperidine or a solvate thereof.
    Type: Application
    Filed: November 28, 2008
    Publication date: December 2, 2010
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Ryo Kobayashi, Satoru Kuraoka
  • Publication number: 20100197667
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 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: Application
    Filed: April 14, 2010
    Publication date: August 5, 2010
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Publication number: 20100173880
    Abstract: 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: Application
    Filed: December 22, 2009
    Publication date: July 8, 2010
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
  • Publication number: 20100137603
    Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: February 5, 2010
    Publication date: June 3, 2010
    Applicant: THERAVANCE, INC.
    Inventors: Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
  • Publication number: 20100125079
    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: Application
    Filed: January 25, 2010
    Publication date: May 20, 2010
    Applicant: THERAVANCE, INC.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Patent number: 7709503
    Abstract: Compounds of Formula (1) and their pharmaceutically acceptable salts are described: Formula (1) Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Oluyinka Morenike Green, Kenneth Gregory Hull, Haihong Ni, Sheila Irene Hauck, George Byron Mullen, Alexander Louis Breeze, Neil James Hales, David Timms
  • Publication number: 20100093753
    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: Application
    Filed: December 17, 2009
    Publication date: April 15, 2010
    Applicant: THERAVANCE, INC.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Publication number: 20100063096
    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: Application
    Filed: November 12, 2009
    Publication date: March 11, 2010
    Applicant: THERAVANCE, INC.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Eric L. Stangeland
  • Publication number: 20100016366
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.
    Type: Application
    Filed: July 1, 2009
    Publication date: January 21, 2010
    Inventors: Paul Alan Glossop, Charlotte Alice Louise Lane
  • Publication number: 20090306134
    Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
    Type: Application
    Filed: September 30, 2008
    Publication date: December 10, 2009
    Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
  • Publication number: 20090270629
    Abstract: What is described is a process for preparing compounds of the general formula (I) in which R1, R2 and R3 independently of one another represent hydrogen, an alkyl group or an aryl group, wherein compounds of the general formula (II) in which R1 and R2 have the meaning given for formula (I), are reacted with an alkylating agent of the general formula (III) R3X ??(III) in which X represents a halogen atom and R3 has the meaning given for formula (I), if appropriate in a solvent.
    Type: Application
    Filed: April 6, 2009
    Publication date: October 29, 2009
    Applicant: SALTIGO GMBH
    Inventors: Andreas Job, Denys Baskakov, Ralf Krahwinkel, Antje Hieronymi
  • Publication number: 20090233965
    Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5 and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions and their use in therapy (I).
    Type: Application
    Filed: April 23, 2007
    Publication date: September 17, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Andrew Bailey, Antonio Mete, Garry Pairaudeau, Michael Stocks, Mark Wenlock
  • Patent number: 7338965
    Abstract: The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure: where Z is CR or N, and R1, R2 and R3 are as described in the specification.
    Type: Grant
    Filed: November 19, 2002
    Date of Patent: March 4, 2008
    Assignees: Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.
    Inventors: Joseph B. Moon, Shon R. Pulley, Daniel H. Rich, David L. Brown, Barbara Jagodzinska, Varghese John, John Jacobs
  • Patent number: 7199245
    Abstract: The present invention relates to selected 4-imino-N-alkoxy-polyalkyl-peperidine compounds preparation, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 4-imino-N-alkoxy-polyalkyl-piperidine compound. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 4-imino-N-alkoxy-polyalkyl-piperidine compounds for controlled polymerization.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: April 3, 2007
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Peter Nesvadba, Tobias Hintermann, Andreas Kramer, Marie-Odile Zink, Lucienne Bugnon
  • Patent number: 7084140
    Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: August 1, 2006
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
  • Patent number: 6849626
    Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
  • Publication number: 20040167163
    Abstract: A biocatalytic process to obtain optically enriched precursors of trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidines, based on the enzymatic resolution of racemic derivatives of general formula III (where R3 is preferably phenyl or benzyl) using cyclic anhydrides or the Meldrum's acid (2,2-dimethyl-1,3-dioxane-4,6-dione) as acylating agents of the hydroxyl group. Depending on the enzyme and the chosen reaction conditions, either of the two enantiomers may be obtained with high enantiomeric purity. These compounds are important intermediates in the synthesis of the paroxetine anti-depressive agent.
    Type: Application
    Filed: December 18, 2003
    Publication date: August 26, 2004
    Inventors: Miguel Bayod Jasanada, Victor M. Sanchez Pedregal, Vicente Gotor Santamaria, Gonzalo De Gonzalo Calvo, M. Rosario Brieva Collado