Cyclopentyl In Acid Moiety (e.g., Prostaglandins, Etc.) Patents (Class 560/121)
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Patent number: 10870621Abstract: The present invention relates to a process for preparing latanoprostene bunod and an intermediate therefor. In accordance with the preparation process of the present invention, latanoprostene bunod can be efficiently and cost-effectively prepared while reducing side reactions.Type: GrantFiled: August 3, 2018Date of Patent: December 22, 2020Assignee: YONSUNG FINE CHEMICAL CO., LTD.Inventors: Eun Jeong Ko, Hyun Ik Shin, Kee Young Lee, Chang Young Oh
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Patent number: 10781221Abstract: The present disclosure is directed at methods of forming an N—Si silyl bond, the method comprising contacting an organic substrate comprising an aromatic amine having at least one N—H bond with a mixture comprising of (a) at least one hydrosilane or hydrosiloxane and (b) at least one hydroxide or alkoxide, under conditions sufficient to form the N—Si bond. The disclosure is further directed to the compositions involved in these methods and the products that result therefrom.Type: GrantFiled: January 10, 2019Date of Patent: September 22, 2020Assignee: California Institute of TechnologyInventors: Anton A. Toutov, Kerry N. Betz, Andrew M. Romine, Robert H. Grubbs
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Patent number: 9994543Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.Type: GrantFiled: July 17, 2015Date of Patent: June 12, 2018Assignee: CHIROGATE INTERNATIONAL INC.Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
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Patent number: 9796653Abstract: Copper(II) bromide mediated oxidation of acylated enol and use of the reaction in the synthesis of ?,?-unsaturated or ?-bromo ketones or aldehydes are disclosed. The method provides an efficient and practical process for manufacturing dehydrohedione (DHH) and many other versatile ?,?-unsaturated or ?-bromo ketones or aldehydes in large scales to avoid using precious metal compounds.Type: GrantFiled: December 19, 2016Date of Patent: October 24, 2017Assignee: INTERNATIONAL FLAVORS & FRAGRANCES INC.Inventors: Ian R Baxendale, James S Sharley, Amadeo Fernández Miranda, Ana Maria Collado Pérez
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Patent number: 9499478Abstract: Provided herein, inter alia, are, methods of using esters of bimatoprost with the Formula (I):Type: GrantFiled: September 16, 2014Date of Patent: November 22, 2016Assignee: ALLERGAN, INC.Inventors: David F. Woodward, Jenny W. Wang, Neil J. Poloso, Todd S. Gac, Robert M. Burk, Michael E. Garst
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Patent number: 9370530Abstract: The present invention is directed to a composition or a kit comprising a combination of a prostaglandin analog and an adenosine receptor A1 agonist and to a method of reducing intraocular pressure (IOP) in a subject using such combination or kit.Type: GrantFiled: October 17, 2014Date of Patent: June 21, 2016Assignee: Inotek Pharmaceuticals CorporationInventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley, Rudolf A. Baumgartner
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Patent number: 9115109Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.Type: GrantFiled: August 15, 2013Date of Patent: August 25, 2015Assignee: CHIROGATE INTERNATIONAL INC.Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
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Publication number: 20150126764Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.Type: ApplicationFiled: January 12, 2015Publication date: May 7, 2015Inventors: Robert R. HOGAN, Ronald Rossi
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Patent number: 9005874Abstract: There are provided a novel compound, a polymeric compound, a resist composition, an acid generator and a method of forming a resist pattern the compound represented by general formula (1-1): wherein each of R1 and R3 independently represents a single bond or a divalent linking group; A represents a divalent linking group; each of R2 and R4 independently represents a hydroxyl group, a hydrocarbon group which may have a substituent, or a group represented by general formula (1-an1), (1-an2) or (1-an3), provided that at least one of R2 and R4 represents a group represented by general formula (1-an1), (1-an2) or (1-an3); and n0 is preferably 0 or 1, and wherein Y1 represents a single bond or —SO2—; R5 represents a linear or branched monovalent hydrocarbon group of 1 to 10 carbon atoms, cyclic monovalent hydrocarbon group of 3 to 20 carbon atoms or monovalent hydrocarbon group of 3 to 20 carbon atoms having a cyclic partial structure which may be substituted with a fluorine atom; and M+ represents an organic caType: GrantFiled: April 18, 2012Date of Patent: April 14, 2015Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Yoshitaka Komuro, Yoshiyuki Utsumi, Akiya Kawaue, Masatoshi Arai
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Patent number: 8957240Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.Type: GrantFiled: July 29, 2013Date of Patent: February 17, 2015Assignee: Johnson Matthey Public Limited CompanyInventors: Robert R. Hogan, Ronald Rossi
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Publication number: 20150044114Abstract: An acid gas absorbent according to an embodiment includes at least one kind of amino acid salt represented by the following general formula (1). In the above-described formula (1), R1 indicates a cyclic alkyl group having 3 to 8 carbon atoms, R2 indicates a cyclic alkyl group having 3 to 8 carbon atoms, a chain alkyl group having 1 to 8 carbon atoms, or a hydrogen atom, R3 indicates a methylene group, an alkylene group having 2 to 4 carbon atoms, an alkylidene group having 2 to 4 carbon atoms, or a polymethylene group having 3 to 4 carbon atoms, and M indicates alkali metal.Type: ApplicationFiled: August 4, 2014Publication date: February 12, 2015Applicant: KABUSHIKI KAISHA TOSHIBAInventors: Shinji MURAI, Yasuhiro KATO, Yukishige MAEZAWA, Takehiko MURAMATSU, Daigo MURAOKA, Satoshi SAITO
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Publication number: 20150031898Abstract: A convergent synthesis of the prostaglandin F2? analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ?-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.Type: ApplicationFiled: March 8, 2013Publication date: January 29, 2015Applicant: INSTYTUT FARMACEUTYCZNYInventors: Iwona Dams, Andrzej Kutner, Michal Chodynski, Malgorzata Krupa, Anita Pietraszek, Marta Zezula, Piotr Cmoch, Monika Kosinska
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Publication number: 20150025250Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of catType: ApplicationFiled: October 2, 2014Publication date: January 22, 2015Inventors: Susana AYESA, Urszula GRABOWSKA, Ellen HEWITT, Daniel JONSSON, Bjorn KLASSON, Pia KAHNBERG, Stina LUNDGREN, Jan TEJBRANT, Daniel WIKTELIUS
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Publication number: 20150005528Abstract: Intermediates of the following formulae for the preparation of lubiprostone:Type: ApplicationFiled: August 21, 2014Publication date: January 1, 2015Inventors: Julian Paul HENSCHKE, Yuanlian LIU, Lizhen XIA, Yung-Fa CHEN
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Publication number: 20140371304Abstract: A method for suppressing tumorigenicity of stem cells in a mammalian subject, which comprises administering an effective amount of a fatty acid derivative and a method for suppressing tumorigenicity of stem cells of a mammalian subject, which comprises contacting said stem cell with an effective amount of a fatty acid derivative, are provided.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Applicant: SUCAMPO AGInventors: Ryuji UENO, Sachiko KUNO, John CUPPOLETTI
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Patent number: 8895040Abstract: The present invention relates to cosmetic and/or personal care formulations and/or compounds. In one embodiment, the present invention relates to ester compounds that can be used in various personal care formulations and/or compounds. In another embodiment, the present invention relates to branced ester compounds having a molecular weight of at least about 1,500 daltons that can be used in various personal care formulations and/or compounds.Type: GrantFiled: June 4, 2009Date of Patent: November 25, 2014Assignee: Lubrizol Advanced Materials, Inc.Inventors: Brian J. Vondruska, Peter Frank, Anchuu Wu
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Publication number: 20140288230Abstract: The present invention provides methylene beta-ketoester monomers, methods for producing the same, and compositions and products formed therefrom. In the method for producing the methylene beta-ketoesters of the invention, a beta-ketoester is reacted with a source of formaldehyde in a modified Knoevenagel reaction optionally in the presence of an acidic or basic catalyst, and optionally in the presence of an acidic or non-acidic solvent, to form reaction complex. The reaction complex may be an oligomeric complex. The reaction complex is subjected to further processing, which may be vaporization by contact with an energy transfer means in order to isolate the beta-ketoester monomer. The present invention further compositions and products formed from methylene beta-ketoester monomers of the invention, including monomer-based products (e.g., inks, adhesives, coatings, sealants or reactive molding) and polymer-based products (e.g., fibers, films, sheets, medical polymers, composite polymers and surfactants).Type: ApplicationFiled: October 18, 2012Publication date: September 25, 2014Inventors: Bernard M. Malofsky, Adam G. Malofsky, Tanmoy Dey
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Patent number: 8828967Abstract: New low molecular weight complexes between iron and maltobionic acid that can be administered parenterally, preferably intramuscularly or subcutaneously, in the treatment of anemic states, caused by iron deficiencies, and new pharmaceutical compositions adapted for this use. In particular, the invention provides a new complex between preferably trivalent iron and maltobionic acid that is characterized by a molecular weight Mw between 10,000 and 30,000 Da, by a polydispersity of 1.0-1.8 and by an iron content between 25% and 40% by weight.Type: GrantFiled: June 8, 2011Date of Patent: September 9, 2014Assignee: Biofer S.p.A.Inventors: Michele Autuori, Dario Bosi, Alessandro Lapini Sacchetti, Egidio Marchi
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Patent number: 8742143Abstract: A process for preparing a prostaglandin analogue comprising a step of converting a compound of formula (8?): to the prostaglandin analogue, wherein R3 represents hydrogen or a hydroxyl protecting group.Type: GrantFiled: March 27, 2013Date of Patent: June 3, 2014Assignee: Scinopharm Taiwan, Ltd.Inventors: Julian P. Henschke, Yuanlian Liu, Yung-Fa Chen, Dechao Meng, Ting Sun
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Patent number: 8728978Abstract: Suggested are biocide compositions, comprising (a) esters based on ketocarboxylic acids, (b) biocides, and optionally (c) oil components or co-solvents and/or (d) emulsifiers. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. over a longer period.Type: GrantFiled: August 24, 2010Date of Patent: May 20, 2014Assignee: Cognis IP Management GmbHInventors: Joaquin Bigorra Llosas, Stéphanie Merlet, Ramon Valls, Stefan Busch
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Patent number: 8664429Abstract: The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.Type: GrantFiled: November 8, 2012Date of Patent: March 4, 2014Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20140051874Abstract: The present invention provides a method that allows production of stereospecific and asymmetrical five-membered ring-containing compounds serving as synthetic intermediates for formation of five-membered rings of prostaglandins and the like, with high yield and excellent stereoselectivity in terms of diastereoselectivity and enantioselectivity in a short process without requiring troublesome procedures such as optical resolution.Type: ApplicationFiled: April 27, 2012Publication date: February 20, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventor: Yujiro Hayashi
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Patent number: 8648213Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.Type: GrantFiled: October 4, 2005Date of Patent: February 11, 2014Assignee: Allergan, Inc.Inventors: David F. Woodward, Robert M. Burk
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Publication number: 20140031423Abstract: The present invention is directed to novel amino acid prostaglandin salts and methods of making and using them.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: NOVAER HOLDINGS, INC.Inventors: Mitchell A. deLong, Jill Marie Sturdivant
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Publication number: 20130274329Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.Type: ApplicationFiled: August 11, 2011Publication date: October 17, 2013Applicant: NABRIVA THERAPEUTICS AGInventors: Rosemarie Riedl, Klaus Thirring, Werner Heilmayer
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Patent number: 8546603Abstract: Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: GrantFiled: March 19, 2012Date of Patent: October 1, 2013Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 8530519Abstract: Provided is a method for promoting upper gastrointestinal bicarbonate secretion in a mammalian subject, which comprises administering an effective amount of a compound of Formula (I): to a subject in need thereof, wherein W1, W2, R1, R2, x1, x2, Y and A are herein defined. The compound is also useful for protecting the upper gastrointestinal tract of a mammal from mucosal damage.Type: GrantFiled: November 23, 2010Date of Patent: September 10, 2013Assignee: Sucampo AGInventor: Ryuji Ueno
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Patent number: 8519178Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.Type: GrantFiled: June 22, 2010Date of Patent: August 27, 2013Assignee: Johnson Matthey Public Limited CompanyInventors: Robert R. Hogan, Ronald Rossi
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Publication number: 20130217767Abstract: The present invention concerns a cosmetic composition comprising the following fluorinated analog of prostaglandin F2?: The cosmetic composition may further comprise a complexing agent and/or a humectant. The present invention further relates to a cosmetic kit, comprising the cosmetic composition and an applicator for application thereof.Type: ApplicationFiled: March 21, 2013Publication date: August 22, 2013Applicant: S & V Technologies AGInventor: S & V Technologies AG
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USE OF MEXIPROSTIL IN THE TREATMENT OF INFLAMMATORY BOWEL DISEASE AND/OR OF IRRITABLE BOWEL SYNDROME
Publication number: 20130202704Abstract: The invention relates to the use of mexiprostil in the treatment and/or prevention of inflammatory bowel disease and of irritable bowel syndrome, to the combinations of mexiprostil with other drugs, and also to a novel method for the synthesis of mexiprostil.Type: ApplicationFiled: October 18, 2011Publication date: August 8, 2013Applicant: COSMO TECHNOLOGIES LTD.Inventors: Alessandro Assandri, Luigi Moro -
Patent number: 8476471Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.Type: GrantFiled: July 13, 2010Date of Patent: July 2, 2013Assignee: Irix Pharmaceuticals, Inc.Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephanie Bosse Abernathy
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Patent number: 8466309Abstract: The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 13, 2009Date of Patent: June 18, 2013Inventors: Marie-Claude Fournie-Zaluski, Hervé Poras, Bernard Roques
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Publication number: 20130072695Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.Type: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: Alphora Research Inc.Inventor: Alphora Research Inc.
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Patent number: 8389748Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.Type: GrantFiled: April 19, 2010Date of Patent: March 5, 2013Assignees: Sucampo AG, R-Tech Ueno, Ltd.Inventors: Ryu Hirata, Tatsuya Matsukawa, Kazuhiro Masuzaki, Ryuji Ueno
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Patent number: 8343972Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.Type: GrantFiled: July 26, 2006Date of Patent: January 1, 2013Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Heinz Berner
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Publication number: 20120270155Abstract: There are provided a novel compound, a polymeric compound, a resist composition, an acid generator and a method of forming a resist pattern the compound represented by general formula (1-1): wherein each of R1 and R3 independently represents a single bond or a divalent linking group; A represents a divalent linking group; each of R2 and R4 independently represents a hydroxyl group, a hydrocarbon group which may have a substituent, or a group represented by general formula (1-an1), (1-an2) or (1-an3), provided that at least one of R2 and R4 represents a group represented by general formula (1-an1), (1-an2) or (1-an3); and n0 is preferably 0 or 1, and wherein Y1 represents a single bond or —SO2—; R5 represents a linear or branched monovalent hydrocarbon group of 1 to 10 carbon atoms, cyclic monovalent hydrocarbon group of 3 to 20 carbon atoms or monovalent hydrocarbon group of 3 to 20 carbon atoms having a cyclic partial structure which may be substituted with a fluorine atom; and M+ represents an organic caType: ApplicationFiled: April 18, 2012Publication date: October 25, 2012Applicant: TOKYO OHKA KOGYO CO., LTD.Inventors: Yoshitaka Komuro, Yoshiyuki Utsumi, Akiya Kawaue, Masatoshi Arai
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Publication number: 20120209011Abstract: This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.Type: ApplicationFiled: December 21, 2009Publication date: August 16, 2012Inventors: Chandrashekar Aswathanarayanappa, Pullela Venkata Srinivas, Divya Kangath, Thilak Gregory Soundararajan, Anegondi Sreenivasa Prasad, Suriyan Masinaickenpatty Raghavendran
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Publication number: 20120065409Abstract: There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds.Type: ApplicationFiled: January 22, 2010Publication date: March 15, 2012Applicant: APOTEX PHARMACHEM INC.Inventors: Kiran Kumar Kothakonda, Fan Wang, Bhaskar Reddy Guntoori, Minh T. N. Nguyen, Alfredo Paul Ceccarelli, Yajun Zhao, Uma Kotipalli, Sammy Chris Duncan, Kaarina K. Milnes, Kevin Wade Kells, Laura Kaye Montemayor
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Patent number: 8063240Abstract: A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.Type: GrantFiled: November 14, 2008Date of Patent: November 22, 2011Assignee: Cayman Chemical Company, IncorporatedInventors: Nancy S. Barta, Stephen D. Barrett, Gregory W. Endres, Andriy M. Kornilov, Kirk M. Maxey, Adam Uzieblo
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Patent number: 8052894Abstract: A compound having a structural unit of Formula: (I). A polymer having a structural unit of Formula: (II). A conjugated polymer having one or more side groups of the following Formula: (III). Additionally, compositions, polymer blends, films, coatings, and electronic devices prepared from such polymers.Type: GrantFiled: December 1, 2005Date of Patent: November 8, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Yang Cheng, Michael Inbasekaran, Chun Wang
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Publication number: 20110184192Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.Type: ApplicationFiled: April 7, 2011Publication date: July 28, 2011Applicant: ALPHORA RESEARCH INC.Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
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Publication number: 20110172435Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.Type: ApplicationFiled: November 12, 2010Publication date: July 14, 2011Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
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Publication number: 20110082111Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 7, 2010Publication date: April 7, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Publication number: 20110071218Abstract: The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: PHARMALEADSInventors: Marie-Claude Fournie-Zaluski, Hervé Poras, Bernard Roques
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Publication number: 20110052513Abstract: The present patent application relates to novel surface-active cationic compounds, to their use, in particular as hair conditioning agent, to a cosmetic treatment method, in particular for the hair, employing the said compounds, and to the cosmetic or pharmaceutical compositions, in particular hair compositions, comprising the said surfactants.Type: ApplicationFiled: February 3, 2009Publication date: March 3, 2011Applicant: L' OrealInventors: Laure Ramos-Stanbury, Herve Andrean, Christian Blaise
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Patent number: 7897793Abstract: The invention relates to a process for the preparation of 13,14-dihydro-PGF2? derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2?, i.e., latanoprost.Type: GrantFiled: October 18, 2007Date of Patent: March 1, 2011Assignee: Instytut FarmaceutycznyInventors: Jacek Martynow, Julita Szyc, Wieslaw Szelejewski, Osman Achmatowicz, Andrzej Kutner, Krzysztof Wiśniewski, Jerzy Winiarski, Oliwia Zegrocka-Stendel, Piotr Golebiewski
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Patent number: 7897795Abstract: The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6): R1 represents H, C1-C5-alkyl, or benzyl, in particular isopropyl.Type: GrantFiled: April 9, 2009Date of Patent: March 1, 2011Assignee: Scinopharm Taiwan Ltd.Inventors: Julian P. Henschke, Yuanlian Liu, Yung-Fa Chen, Dechao Meng, Ting Sun
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Patent number: 7875688Abstract: The invention is based on the discovery that certain polyester compounds bearing are useful as b-stageable and/or liquid adhesives for the microelectronic packaging industry.Type: GrantFiled: October 15, 2007Date of Patent: January 25, 2011Assignee: Designer Molecules, Inc.Inventors: Stephen M. Dershem, Farhad G. Mizori
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Patent number: 7868113Abstract: The invention is based on the discovery that a certain polyester compounds are useful as b-stageable adhesives for the microelectonic packaging industry. The polyester compounds described herein contain ring-opening or ring-forming polymerizable moieties and therefore exhibit little to no shrinkage upon cure. In addition, there are provided well-defined b-stageable adhesives useful in stacked die assemblies. In particular, there are provided assemblies wherein the b-stageable adhesive encapsulates a portion of the wiring members contained within the bondline gap between the stacked die.Type: GrantFiled: April 11, 2007Date of Patent: January 11, 2011Assignee: Designer Molecules, Inc.Inventor: Stephen M Dershem
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Patent number: 7812182Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.Type: GrantFiled: February 7, 2007Date of Patent: October 12, 2010Assignees: Sucampo AG, R-Tech Ueno, Ltd.Inventors: Ryu Hirata, Tatsuya Matsukawa, Kazuhiro Masuzaki, Ryuji Ueno