The -c(=x)- Group And The Piperidine Ring Are Bonded Directly To The Same Chalcogen Patents (Class 546/222)
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Patent number: 9035061Abstract: 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: GrantFiled: November 26, 2013Date of Patent: May 19, 2015Assignee: Theravance Biopharma R&D IP, LLCInventor: Pierre-Jean Colson
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Patent number: 8952036Abstract: 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: GrantFiled: February 27, 2014Date of Patent: February 10, 2015Assignee: Amgen Inc.Inventor: Yosup Rew
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Publication number: 20150038719Abstract: 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: ApplicationFiled: February 28, 2013Publication date: February 5, 2015Inventors: Toru Mizushima, Hongxing Liu
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Publication number: 20140371270Abstract: 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: ApplicationFiled: January 25, 2013Publication date: December 18, 2014Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Masato Nanri, Yoshikazu Iwasawa, Fukumitsu Sakakibara, Shinichi Aoki
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Patent number: 8822679Abstract: 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: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: California Institute of TechnologyInventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8754225Abstract: 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: GrantFiled: June 30, 2011Date of Patent: June 17, 2014Assignee: Theravance, Inc.Inventor: Pierre-Jean Colson
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Patent number: 8633225Abstract: 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: GrantFiled: November 5, 2010Date of Patent: January 21, 2014Assignee: Beiersdorf AGInventors: Michael Woehrmann, Lara Terstegen, Annette Martin, Melanie Sulzberger
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Patent number: 8623238Abstract: 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: GrantFiled: August 8, 2011Date of Patent: January 7, 2014Assignee: Transitions Optical, Inc.Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
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Patent number: 8519138Abstract: 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: GrantFiled: April 14, 2010Date of Patent: August 27, 2013Assignee: Glaxo Group LimitedInventors: Dean David Edney, Matthew Peter John
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Patent number: 8507529Abstract: 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: GrantFiled: October 11, 2010Date of Patent: August 13, 2013Assignee: Jarrow Formulas, Inc.Inventors: Elisabetta Damiani, Paola Astolfi, Lucedio Greci
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Publication number: 20130196978Abstract: 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: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130012384Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Reiner Fischer, Stefan Lehr, Olga Malsam, Arnd Voerste
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Publication number: 20130012701Abstract: 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: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8349210Abstract: 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: GrantFiled: August 8, 2011Date of Patent: January 8, 2013Assignee: Transitions Optical, Inc.Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
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Patent number: 8334306Abstract: 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: GrantFiled: March 21, 2011Date of Patent: December 18, 2012Assignee: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Patent number: 8309732Abstract: 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: GrantFiled: April 6, 2009Date of Patent: November 13, 2012Assignee: Saltigo GmbHInventors: Andreas Job, Denys Baskakov, Ralf Krahwinkel, Antje Hieronymi
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Publication number: 20120263650Abstract: 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: ApplicationFiled: April 5, 2012Publication date: October 18, 2012Applicants: Wake Forest University, and Human ServicesInventors: David A. Wink, Wilmarie Flores-Santana, S. Bruce King, Murali Krishna Cherukuri, James B. Mitchell
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Patent number: 8198304Abstract: 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: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20120122850Abstract: 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: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20120071319Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.Type: ApplicationFiled: May 21, 2010Publication date: March 22, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
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Patent number: 8134006Abstract: 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: GrantFiled: February 5, 2010Date of Patent: March 13, 2012Assignee: Theravance, Inc.Inventors: Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
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Publication number: 20120046469Abstract: 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: ApplicationFiled: April 14, 2010Publication date: February 23, 2012Applicant: GLAXO GROUP LIMITEDInventors: Dean David Edney, Matthew Peter John
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Publication number: 20120029021Abstract: 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: ApplicationFiled: January 17, 2011Publication date: February 2, 2012Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITYInventors: Yong Ba, Errol V. Mathias
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Publication number: 20120027960Abstract: 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: ApplicationFiled: August 8, 2011Publication date: February 2, 2012Applicant: TRANSITIONS OPTICAL, INC.Inventors: Ruisong Xu, Xiao-Man Dai, Anil Kumar, Meng He, Chenguang Li, Rachael L. Yoest
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Publication number: 20120016130Abstract: 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: ApplicationFiled: June 30, 2011Publication date: January 19, 2012Inventor: Pierre-Jean COLSON
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Publication number: 20120003401Abstract: 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: ApplicationFiled: August 8, 2011Publication date: January 5, 2012Applicant: TRANSITIONS OPTICAL, INC.Inventors: Ruisong XU, Xiao-Man DAI, Anil KUMAR, Meng HE, Chenguang LI, Rachael L. YOEST
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Publication number: 20110281851Abstract: 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: ApplicationFiled: July 29, 2011Publication date: November 17, 2011Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20110201583Abstract: 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: ApplicationFiled: April 28, 2011Publication date: August 18, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Patent number: 7960385Abstract: 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: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Patent number: 7910607Abstract: 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: GrantFiled: March 12, 2007Date of Patent: March 22, 2011Assignee: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Publication number: 20110027203Abstract: 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: ApplicationFiled: October 11, 2010Publication date: February 3, 2011Inventors: Elisabetta Damiani, Paola Astolfi, Lucedio Greci
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Patent number: 7880010Abstract: 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: GrantFiled: April 24, 2007Date of Patent: February 1, 2011Assignee: Theravance, Inc.Inventors: Jennifer Bolton, Robert S. Chao, Miroslav Rapta, Lisa Williams, Richard D. Wilson
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Patent number: 7851633Abstract: 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: GrantFiled: June 9, 2006Date of Patent: December 14, 2010Assignee: Beiersdorf AGInventors: Michael Woehrmann, Lara Terstegen, Annette Martin, Melanie Sulzberger
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Publication number: 20100305159Abstract: 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: ApplicationFiled: November 28, 2008Publication date: December 2, 2010Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Ryo Kobayashi, Satoru Kuraoka
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Publication number: 20100197667Abstract: 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: ApplicationFiled: April 14, 2010Publication date: August 5, 2010Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20100173880Abstract: 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: ApplicationFiled: December 22, 2009Publication date: July 8, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Publication number: 20100137603Abstract: 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: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Applicant: THERAVANCE, INC.Inventors: Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
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Publication number: 20100125079Abstract: 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: ApplicationFiled: January 25, 2010Publication date: May 20, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Patent number: 7709503Abstract: 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: GrantFiled: September 10, 2004Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Oluyinka Morenike Green, Kenneth Gregory Hull, Haihong Ni, Sheila Irene Hauck, George Byron Mullen, Alexander Louis Breeze, Neil James Hales, David Timms
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Publication number: 20100093753Abstract: 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: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20100063096Abstract: 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: ApplicationFiled: November 12, 2009Publication date: March 11, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Eric L. Stangeland
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Publication number: 20100016366Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.Type: ApplicationFiled: July 1, 2009Publication date: January 21, 2010Inventors: Paul Alan Glossop, Charlotte Alice Louise Lane
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Publication number: 20090306134Abstract: 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: ApplicationFiled: September 30, 2008Publication date: December 10, 2009Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20090270629Abstract: 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: ApplicationFiled: April 6, 2009Publication date: October 29, 2009Applicant: SALTIGO GMBHInventors: Andreas Job, Denys Baskakov, Ralf Krahwinkel, Antje Hieronymi
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Publication number: 20090233965Abstract: 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: ApplicationFiled: April 23, 2007Publication date: September 17, 2009Applicant: ASTRAZENECA ABInventors: Andrew Bailey, Antonio Mete, Garry Pairaudeau, Michael Stocks, Mark Wenlock
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Patent number: 7338965Abstract: 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: GrantFiled: November 19, 2002Date of Patent: March 4, 2008Assignees: 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
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Patent number: 7199245Abstract: 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: GrantFiled: June 4, 2002Date of Patent: April 3, 2007Assignee: Ciba Specialty Chemicals Corp.Inventors: Peter Nesvadba, Tobias Hintermann, Andreas Kramer, Marie-Odile Zink, Lucienne Bugnon
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Patent number: 7084140Abstract: 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: GrantFiled: September 5, 2002Date of Patent: August 1, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Patent number: 6849626Abstract: 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: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Publication number: 20040167163Abstract: 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: ApplicationFiled: December 18, 2003Publication date: August 26, 2004Inventors: Miguel Bayod Jasanada, Victor M. Sanchez Pedregal, Vicente Gotor Santamaria, Gonzalo De Gonzalo Calvo, M. Rosario Brieva Collado