Sulfur Containing Patents (Class 554/42)
- Ring bonded directly to the sulfoxy (Class 554/45)
- Additional nitrogen containing (Class 554/46)
- The carboxamide nitrogen and a -S(=O)(=O)-O-X group attached to each other by an acyclic chain which consists of carbons, wherein X is hydrogen or a metal (e.g., taurides, etc.) (Class 554/49)
- Sulfoxy in acid moiety (Class 554/50)
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Patent number: 11349128Abstract: Disclosed is an electrically conductive substance which comprises a complex containing rubeanic acid ligands and copper ions. The copper ions contained in the complex comprise copper (I) ions. The electrically conductive substance is produced by a production method which comprises mixing a rubeanic acid compound and a copper (I) compound in the presence of a base.Type: GrantFiled: August 13, 2018Date of Patent: May 31, 2022Assignee: ZEON CORPORATIONInventors: Hiroyuki Yonemaru, Tsutomu Fujii
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Patent number: 11319285Abstract: A flavour composition comprising a compound of formula (I) and edible salts thereof, wherein R1 is an alkyl residue containing 2 to 18 carbon atoms, or an alkene residue containing from 9 to 25 carbon atoms with 1 to 6 double bonds, R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid.Type: GrantFiled: July 2, 2019Date of Patent: May 3, 2022Assignee: GIVAUDAN S.A.Inventor: Yili Wang
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Patent number: 8969354Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: GrantFiled: November 9, 2012Date of Patent: March 3, 2015Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20140323390Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.Type: ApplicationFiled: July 9, 2014Publication date: October 30, 2014Applicant: IRM LLCInventors: Tom Yao-Hsiang WU, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
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Patent number: 8871805Abstract: The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.Type: GrantFiled: April 6, 2013Date of Patent: October 28, 2014Assignee: Krisani Biosciences Pvt. Ltd.Inventor: Mahesh Kandula
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Patent number: 8741966Abstract: The present disclosure relates to lipid compounds of formula (I): wherein: R1 is chosen from a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and are chosen from hydrogen and a C1-C6 alkyl; X is chosen from O, S, SO, SO2, Si, and Se; n=1 or 3; and P1 is chosen from hydrogen; a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; a group of formula (II) or formula (III), wherein P2, P3, and P4 are chosen from hydrogen, an alkyl, an alkenyl, and an alkynyl, optionally substituted; and a group of formula (IV) or formula (V), wherein P5 is chosen from hydrogen and a C1-C6 alkyl; or a pharmaceutically acceptable salt, complex, or solvate thereof.Type: GrantFiled: November 6, 2008Date of Patent: June 3, 2014Assignee: Pronova Biopharma Norge ASInventor: Anne Kristin Holmeide
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Patent number: 8445707Abstract: The disclosure herein provides the compounds of Formulas 1, 2 and 3 and their pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.Type: GrantFiled: October 10, 2012Date of Patent: May 21, 2013Assignee: Krisani Biosciences (P) Ltd.Inventor: Mahesh Kandula
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Publication number: 20130065909Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20130059801Abstract: The invention relates to fatty acid amides; compositions comprising an effective amount of a fatty acid amide; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a fatty acid amide.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
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Publication number: 20120065394Abstract: The invention relates to the use of salts of compounds of the formula (1) and amines of the formula (2) where R1 is C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R2 is C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30alkylaryl, or an optionally heteroatom containing organic radical having from 1 to 30 carbon atoms, and R3 and R4 are each independently hydrogen, C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, or an optionally heteroatom containing organic radical having from 1 to 30 carbon atoms, where R3 and R4 can also form, with the inclusion of the nitrogen atom, a ring having from 5 to 7 ring atoms.Type: ApplicationFiled: November 18, 2011Publication date: March 15, 2012Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Dirk LEINWEBER, Michael FEUSTEL
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Patent number: 8049022Abstract: The present invention relates to fatty acid alkanolamides or polyolamides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.Type: GrantFiled: July 2, 2007Date of Patent: November 1, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Publication number: 20110082210Abstract: The invention relates to fatty acid fibrate derivatives; compositions comprising an effective amount of a fatty acid fibrate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid fibrate derivative.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20100234592Abstract: The invention relates to the use of salts of compounds of the formula (1) and amines of the formula (2) where R1 is C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R2 is C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, or an optionally heteroatom containing organic radical having from 1 to 30 carbon atoms, and R3 and R4 are each independently hydrogen, C1- to C30-alkyl, C2- to C30-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, or an optionally heteroatom containing organic radical having from 1 to 30 carbon atoms, where R3 and R4 can also form, with the inclusion of the nitrogen atom, a ring having from 5 to 7 ring atoms.Type: ApplicationFiled: January 10, 2007Publication date: September 16, 2010Inventors: Dirk Leinweber, Michael Feustel
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Publication number: 20090312432Abstract: The present invention relates to fatty acid alkanolamides or polyolamides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r— or (CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.Type: ApplicationFiled: July 2, 2007Publication date: December 17, 2009Inventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Patent number: 7582306Abstract: The present invention relates to a pseudoceramide represented by the following formula (I) and a cosmetic composition comprising the same: wherein Z represents —OH and Y represents —OH, ?with the proviso that X is Z represents —OH and X represents —OH, with the proviso that Y is Y represents —OH and X represents —OH, with the proviso that Z is R represents a linear or branched, saturated or unsaturated aliphatic hydrocarbon group; and when substituted, R has one or more —OH groups.Type: GrantFiled: February 26, 2002Date of Patent: September 1, 2009Assignee: Coreana Cosmetics Co., Ltd.Inventors: Jung-No Lee, Kang-Tae Lee, Jee-Hean Jeong, Byong-Kee Jo
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Patent number: 7544714Abstract: N-fatty acid-amino acid conjugates and J2 prostanoid-amino acid conjugates are disclosed along with methods for making such conjugates and methods of using these conjugates in the treatment of conditions that involve dysfunctional lipid metabolism, insulin sensitivity, glucose homeostasis, and/or inflammation.Type: GrantFiled: July 15, 2005Date of Patent: June 9, 2009Assignee: University of MassachusettsInventors: Sumner H. Burstein, Robert B. Zurier
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Patent number: 7235586Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-thiocarbamoyloxy and carbamoyloxy as therapeutic agents e.g. as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: wherein a wavy segments indicate either the alpha (?) or beta (?) configuration; the dashed bond represents a double bond or a single bond; U, Y, X, R1, Ar, n, x and y are as defined in the specification.Type: GrantFiled: September 9, 2003Date of Patent: June 26, 2007Assignee: Allergan, Inc.Inventors: David W. Old, Robert M. Burk
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Publication number: 20040186176Abstract: This invention provides methods for treating a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn-Z-CO—Y, where R is an alkyl group having 6-20 carbons; Z is a radical selected from —CH2—, —O—, and —NH—, two of these radicals coupled together, or —CH2═CH2—; Y is —NH2, O—CH2—C6H5, —CO—CO—O—CH3, or O—CH3; and n is 1 or 2. It has been discovered that these compounds inhibit growth of microbial cells which synthesize &agr;-substitued. &bgr;-hydroxy fatty acids, particularly corynemycolic acid, nocardic acid, and mycolic acid. These compounds may be used to inhibit growth of mycobacterial cells, such as Mycobacterium tuberculosis, drug-resistant M. tuberculosis, M. avium intracellulare, and M. leprae.Type: ApplicationFiled: January 27, 2004Publication date: September 23, 2004Applicant: The Johns Hopkins University of MedicineInventors: Craig A. Townsend, James D. Dick, Gary R. Pasternack, Francis P. Kuhajda, Nicole M. Parrish
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Patent number: 6511670Abstract: Novel pharmaceutically/cosmetically-active (poly)thiaalkynoic compounds have the structural formula (I): R1—Y—CH2—C≡C—CH2—S—CH2—R2 (I) and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example inflammation disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 13, 2000Date of Patent: January 28, 2003Assignee: Societe L'Oreal S.A.Inventors: Jean Maignan, Sylvie Genard, Serge Michel
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Publication number: 20020115723Abstract: Objects of the present invention are to provide an oxidative stress inhibitor which is capable of suppressing the expression of a cytotoxic protein and the activation of a gene transcriptional regulatory factor taking part such expression of a cytotoxic protein and exhibits good feeling upon use and safety; to provide a method for preventing, retarding, alleviating or treating a skin change due to aging or an undesirable aesthetic skin change, both caused or promoted by an oxidative stress; and to provide a cosmetic composition or dermatologic preparation for external use comprising the oxidative stress inhibitor as an effective ingredient, and for those purposes are employed an oxidative stress inhibiting agent which comprises, as an effective ingredient, at least one selected from cysteine or cystine derivatives and the salts thereof.Type: ApplicationFiled: January 22, 2002Publication date: August 22, 2002Applicant: AJINOMOTO CO., INC.Inventors: Keiji Iwasaki, Manabu Kitazawa, Eiji Shiojiri, Kazutami Sakamoto
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Patent number: 6407137Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: July 9, 2001Date of Patent: June 18, 2002Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6353032Abstract: Phospholipid-HETE derivatives, compositions and methods of use are disclosed. The compounds are particularly useful for treating dry eye.Type: GrantFiled: October 23, 2000Date of Patent: March 5, 2002Assignee: Alcon Universal Ltd.Inventors: Gustav Graff, Peter G. Klimko
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Patent number: 6288250Abstract: Compounds of the general formula wherein R represents a straight or branched chain alkyl group containing from 1 to 16 carbon atoms, pharmaceutically acceptable salts thereof and/or optical isomers thereof have an immunostimulating effect, and are useful in the treatment of arteriosclerosis.Type: GrantFiled: September 30, 1999Date of Patent: September 11, 2001Assignee: Astra AktiebolagInventors: Håkan Bergstrand, Jan Dahmén, Bengt Särnstrand
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Patent number: 6258836Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: November 29, 1999Date of Patent: July 10, 2001Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6057464Abstract: The invention relates to high-foaming zwitterionic and anionic surfactants which are prepared by sulfation of N,N-dialkylaminoalkyl-sugar amides, preferably using gaseous sulfur trioxide. The invention furthermore relates to compositions which comprise known surfactants and suitable solvents, in addition to the novel active compounds. The novel surfactants are particularly suitable for detergents and cosmetic formulations.Type: GrantFiled: December 23, 1998Date of Patent: May 2, 2000Assignee: Clariant GmbHInventor: Bernd Papenfuhs
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Patent number: 5990083Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: March 13, 1997Date of Patent: November 23, 1999Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5981580Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.Type: GrantFiled: October 20, 1998Date of Patent: November 9, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments
Patent number: 5955452Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 26, 1998Date of Patent: September 21, 1999Assignee: Roche Diagnostics GmbHInventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss -
Patent number: 5952377Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.Type: GrantFiled: October 20, 1998Date of Patent: September 14, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Patent number: 5948418Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.Type: GrantFiled: July 30, 1997Date of Patent: September 7, 1999Assignee: Estee Lauder, Inc.Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
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Patent number: 5929110Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.Type: GrantFiled: October 20, 1998Date of Patent: July 27, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Patent number: 5863750Abstract: The present invention describes methods for the detoxification of a mixture of nitrile compounds, or a mixture of nitrile and amide compounds by conversion of the nitrile compound(s) to the corresponding amide or acid compounds using a pure culture of an induced microorganism strain capable of converting a nitrile moiety to an amide or acid moiety. If an amide is formed or is present in the mixture, the amide can be further converted, using the present methods for detoxification, to the corresponding acid. The acid can then, if desired, be further degraded to CO.sub.2, H.sub.2 O and biomass. The induced pure cultures are able to detoxify a mixture of nitrites or a mixture of nitriles and amides which are typically present, in high concentration(s), in nitrile production waste streams.Type: GrantFiled: December 18, 1996Date of Patent: January 26, 1999Inventor: George E. Pierce
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Patent number: 5861520Abstract: The present invention provides a compound which is a glycolipid analog having a novel structure represented by the formula (1): ##STR1## wherein Z represents an imino group, an oxygen atom or a sulfur atom; m is an integer of from 3 to 12; and n is an integer of from 4 to 22; and shows a potent activity of inhibiting glycosidase and has potential physiological activities, for example, antiviral activity. The invention also provides a glycosidase inhibitor which comprises said glycolipid analog as an active ingredient.Type: GrantFiled: May 31, 1995Date of Patent: January 19, 1999Assignee: Seikagaku Kogyo Kabushiki Kaisha (Seikagaku Corporation)Inventors: Seiichiro Ogawa, Hidetoshi Tsunoda, Jinichi Inokuchi
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Patent number: 5830870Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: December 4, 1996Date of Patent: November 3, 1998Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5763481Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.Type: GrantFiled: July 10, 1996Date of Patent: June 9, 1998Assignee: Novartis CorproationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna, Henry Szczepanski
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Patent number: 5627056Abstract: An efficient method of producing phytosphingosine-containing ceramide one comprising: (a) obtaining a phytosphingosine base from tetraacetylphytosphingosine (TAPS) by a deacetylation reaction wherein the TAPS is produced by fermentation of cells of the F-60-10 mating type strain of Hansenula ciferrii using a fed-batch mode and a non-fermentable carbon source; and (b) coupling together the phytosphingosine base and a fatty acid/.omega.-hydroxy fatty acid component wherein the .omega.-hydroxy fatty acid component is prepared by a process which includes Kolbe synthesis.Type: GrantFiled: February 9, 1995Date of Patent: May 6, 1997Assignee: Elizabeth Arden Co., Division of Conopco, Inc.Inventors: John Casey, Peter S. Cheetham, Peter C. Harries, Della Hyliands, John T. Mitchell, Anthony V. Rawlings
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Patent number: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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Patent number: 5589588Abstract: A sulfated acid amide having heparin-like properties of the formula:(R.sub.1)--NH--R--NH--(R.sub.1)whereR.sub.1 is a di-, tri- or tetra-saccharide acid selected from cellobiose, cellotriose, cellotetrose, maltose, maltotriose and maltotetrose or mixtures thereof, andR is an alkylene of from 3 to 12 carbons, and is optionally substituted with one or more hydroxyls.Type: GrantFiled: March 30, 1993Date of Patent: December 31, 1996Assignee: Reliable Biopharmaceutical CorporationInventor: Joseph A. Toce
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Patent number: 5559111Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: September 24, 1996Assignee: Ciba-Geigy CorporationInventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
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Patent number: 5550262Abstract: Disclosed herein are inbibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: November 14, 1994Date of Patent: August 27, 1996Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5502225Abstract: This invention relates to perfluoroalkyl group terminated urethanes, thiourethanes and ureas of the general formula(R--X--CONH).sub.m Awhere m is 1, 2 or 3, R is R.sub.f -E and optionally R.sub.1 with the proviso that at least one R is R.sub.f -E, R.sub.f is a perfluoroalkyl group, R.sub.1 is a hydrocarbon group, E is a divalent linking group, X is --O--, --S--, --NR.sub.2 -- and R.sub.2 is H or lower alkyl and A is R.sub.f E or R.sub.1 if m is 1 and a divalent or trivalent linking group if m is 2 or 3 respectively.Compounds of this general formula are useful as solid lubricants or as additives for waxes and resins providing lubricating properties.Type: GrantFiled: November 9, 1992Date of Patent: March 26, 1996Assignee: Dynax CorporationInventors: Eduard K. Kleiner, Athanasios Karydas
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Patent number: 5498786Abstract: This invention relates to novel processes for synthesizing intermediates in the preparation of N-aryl and N-heteroarylamide inhibitors of the enzyme acyl coenzyme A: cholesterol acyltransferase (ACAT), and to novel intermediates used in such processes.Type: GrantFiled: September 13, 1993Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventors: Sarah E. Kelly, George Chang
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Patent number: 5424468Abstract: This specification provides a polymeric material useful for manufacturing contact lenses having improved oxygen permeability. The contact lenses prepared from the polymeric material of the invention show improved hydrophilicity and enhanced oxygen permeability as compared with that made of the conventional fluoroalkyl-containing polymeric materials.Type: GrantFiled: February 1, 1994Date of Patent: June 13, 1995Assignee: Korea Institute of Science and TechnologyInventors: Kwang U. Kim, Tae S. Park, Seung S. Hwang, Jong C. Lee, Moo S. Lee, Seong M. Cheong
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Patent number: 5352673Abstract: The present invention provides prodrugs that serve as useful therapeutics for various disease states and conditions mediated by underlying specific hydrolytic enzyme activity. The prodrugs hereof (additionally) impart a physiologically bioactive component thus providing prodrug compounds that are capable of imparting dual effect systemically.Type: GrantFiled: June 10, 1991Date of Patent: October 4, 1994Inventor: Edward A. Dennis
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Patent number: 5344949Abstract: Surface active anion-cation complexes are synthesized where an organic or organosilicon compound with at least one epoxide group is reacted with a quaternary ammonium hydrogen sulfite of the general formulaHN.sup.+ (R.sup.1).sub.3 SO.sub.3 H.sup.- IwhereinR.sup.1 within the molecule is the same or different and can be(1) an alkyl or hydroxyalkyl group with 1 to 18 carbon atoms,(2) a phenyl group, or(3) a group of the formula C.sub.n H.sub.2n+1 CONH--(CH.sub.2).sub.m --, in which n can be a number from 7 to 17 and m is 2 or 3,in the presence of a polar solvent in such amounts so that the molar ratio of the epoxide group to HN.sup.+ (R.sup.1).sub.3 SO.sub.3 H.sup.- is 2:1.Type: GrantFiled: July 14, 1993Date of Patent: September 6, 1994Assignee: Th. Goldschmidt AGInventors: Gotz Koerner, Klaus-Dieter Klein, Dietmar Schaefer
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Patent number: 5342977Abstract: Salts of aminosulfonic acid derivatives of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each independently of the others an aliphatic hydrocarbon radical having from 7 to 21 carbon atoms,n is 0 or 1,As is the amidically bonded residue of a (D)- or (L)-amino acid or of a (D)- or (L)-amino acid derivative from the group consisting of Gly, Ala, Ser, Thr, Asp, Asp(R.sup.5), Glu, Glu(R.sup.5), Gla, Gla(R.sup.5) and Gla(R.sup.5).sub.2, andR.sup.4 and R.sup.5 are each independently of the other the amidically bonded radical of an unsubstituted or carboxy-substituted .omega.-amino-C.sub.2 -C.sub.3 alkanesulfonic acid, are described.Those salts have an immunostimulating action and can be used as medicaments.Type: GrantFiled: December 17, 1992Date of Patent: August 30, 1994Assignee: Ciba-Geigy Corp.Inventors: Gerhard Baschang, Albert Hartmann
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Patent number: 5268494Abstract: Compounds corresponding to the formula: ##STR1## wherein A represents --CH.sub.2).sub.2 or --C.tbd.C--;n is equal to 0, 1 or 2;R represents hydroxyl, alkoxy having the formula --OR.sub.1, or amino having the formula ##STR2## R.sub.1 represents alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or aralkyl;R.sub.2 and R.sub.3 represent hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl;R.sub.2 and R.sub.3 form, with the nitrogen atom, a heterocyclic ring.Application of these compounds in pharmacy and cosmetics.Type: GrantFiled: June 4, 1992Date of Patent: December 7, 1993Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Christopher Hensby, Jean Maignan, Gerard Lang, Michel Colin
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Patent number: 5266713Abstract: Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.Type: GrantFiled: August 12, 1992Date of Patent: November 30, 1993Assignee: Miles Inc.Inventors: Trevor S. Abram, Peter Norman, Stephen R. Tudhope, Harold C. Kluender, Robert N. Schut, Heinrich Meier, Ulrich Rosentreter
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Patent number: 5182407Abstract: The present invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, denote a methyl or ethyl radical;R.sub.3 denotes a methyl, ethyl or hydroxyethyl radical;A denotes a ##STR2## radical or ##STR3## R denotes H or CH.sub.3 ; X denotes Cl.sup.-, BR.sup.-, I.sup.-, CH.sub.3 OSO.sub.3.sup.-, CH.sub.3 SO.sub.3.sup.-, ##STR4## p and q, which are identical or different, denote integers such that 1.ltoreq.p.ltoreq.15, 0.ltoreq.q.ltoreq.13 and 2.ltoreq.p+q.ltoreq.20;n denotes an integer equal to 2 or 3;m denotes 0 or 1, and m+q.noteq.0;as well as the salts from neutralization by bases, their preparation process and their utilization as an additive in compositions for treatment of keratinous materials.Type: GrantFiled: July 17, 1991Date of Patent: January 26, 1993Assignee: L'OrealInventor: Henri Sebag
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Patent number: 5162367Abstract: Insecticidal and acaricidal compounds of FormulaAR(CH.sub.2).sub.x O(CH.sub.2).sub.m A(CH.sub.2).sub.n (CE.sup.1 =CE.sup.2).sub.a (CE.sup.3 =CE.sup.4)CONR.sup.1 R.sup.2 (I)whereinAr is phenyl or naphthyl, in either case optionally substituted by one or more of optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.1-6 -alkylthio or C.sub.1-6 alkylthiooxy, halogen or optionally substituted C.sub.1-6 alkoxy,x=0 or 1m=1 to 7n=1 to 7A=CH.sub.2 or oxygena=0 or 1R.sup.1 and R.sup.2 are independently selected from hydrogen, C.sub.1-6 alkyl and C.sub.3-6 cycloalkyl (either of which may be substituted by one or more of halo, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, CF.sub.2-6 alkoxy, C.sub.2-6 alkynyl, dioxalanyl and C.sub.3-6 cycloalkyl)E.sup.1, E.sup.2, E.sup.3 and E.sup.4 are independently selected from hydrogen, C.sub.1-4 alkyl, optionally substituted by halo, and nitrile, provided that at least one of E.sup.1, E.sup.2, E.sup.3 and E.sup.Type: GrantFiled: October 23, 1989Date of Patent: November 10, 1992Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, John E. Robinson