The -c(=x)- Group Is Bonded Directly To The Thiazole Ring Patents (Class 548/188)
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Publication number: 20090198054Abstract: The present disclosure is directed to a process for the preparation of a compound having the formula: wherein R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a selected leaving group that is not halogen, and may specifically be methylsulfonate, trifluoromethylsulfonate, and p-toluenesulfonate. These compounds are valuable intermediates useful in the synthesis of compounds having pesticidal activity.Type: ApplicationFiled: April 16, 2009Publication date: August 6, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony Cornelius O'Sullivan
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Publication number: 20090137611Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: (I)Type: ApplicationFiled: April 5, 2007Publication date: May 28, 2009Inventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stephane Carbonne, Stephanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
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Publication number: 20090124676Abstract: Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: November 5, 2008Publication date: May 14, 2009Inventor: Yariv Donde
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Publication number: 20090042885Abstract: An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof.Type: ApplicationFiled: June 13, 2008Publication date: February 12, 2009Applicant: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke TANI, Kaoru KOBAYASHI, Toru MARUYAMA, Tohru KAMBE, Mikio OGAWA, Tsutomu SHIROYA
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080300269Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: August 6, 2008Publication date: December 4, 2008Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20080287683Abstract: The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.Type: ApplicationFiled: July 30, 2008Publication date: November 20, 2008Inventors: Jonathan B. DeCamp, Paul S. Watson, Jin She
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Publication number: 20080269498Abstract: Therapeutic compounds, compositions, medicaments, and methods are disclosed herein.Type: ApplicationFiled: March 17, 2008Publication date: October 30, 2008Inventor: David W. Old
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Patent number: 7414137Abstract: The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.Type: GrantFiled: March 22, 2007Date of Patent: August 19, 2008Assignee: Inspire Pharmaceuticals, Inc.Inventors: Jonathan B. DeCamp, Paul S. Watson, Jin She
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Patent number: 7402600Abstract: Compounds or their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.Type: GrantFiled: September 26, 2005Date of Patent: July 22, 2008Assignee: NicOx S.A.Inventor: Piero Del Soldato
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Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 6987120Abstract: Compounds of their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.Type: GrantFiled: April 11, 2000Date of Patent: January 17, 2006Assignee: Nicox, S.A.Inventor: Piero Del Soldato
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Patent number: 6809107Abstract: This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.Type: GrantFiled: June 14, 2000Date of Patent: October 26, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ramesh M. Kanojia, Alfonzo D. Jordan, Allen B. Reitz, Mark J. Macielag, Boyu Zhao
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Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Patent number: 6569874Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 17, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6559168Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biType: GrantFiled: January 31, 2002Date of Patent: May 6, 2003Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Publication number: 20020123520Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1Type: ApplicationFiled: January 31, 2002Publication date: September 5, 2002Applicant: Pfizer Inc.Inventors: Anthony Marfat, Michael William McKechney
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Publication number: 20020115863Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.Type: ApplicationFiled: December 13, 2000Publication date: August 22, 2002Inventors: Dinesh Patel, Jeffrey W. Jacobs, Rakesh Jain, Zhi-Jie Ni, Zhengyu Yuan
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Publication number: 20020107390Abstract: Compounds of the formula 1Type: ApplicationFiled: August 16, 2001Publication date: August 8, 2002Inventor: Paivi J. Kukkola
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Patent number: 6403612Abstract: A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.Type: GrantFiled: January 30, 2001Date of Patent: June 11, 2002Assignee: Merck & Co., Inc.Inventors: Philippe G. Nantermet, James C. Barrow, Harold G. Selnick
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Patent number: 6399783Abstract: The invention relates to a method for preparing an ester, by admixing a compound having the structure I or IV: with a base and an alcohol to produce an ester, wherein the alcohol is a precursor to Taxol and its analogs. The present invention also relates to compounds having the structure I and IV and methods of main them therefor. The invention also relates to the esterification of an alcohol by adding an alkoxide to a compound having the structure, VII: The invention further relates to compounds having the structure I, IV, and VII and methods of making them therefor. The invention further relates to alcohols, and in particular, alcohols that are synthetic precursors to Taxol and analogs thereof.Type: GrantFiled: August 25, 2000Date of Patent: June 4, 2002Assignee: Emory UniversityInventors: Dennis C. Liotta, Hariharan Venkatesan, Laura Captain, Michael V. Voronkov, James P. Snyder, Marcus A. Schestopol
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Patent number: 6372913Abstract: 2-substituted 5-formylthiazoles are prepared in an advantageous manner by reacting halogenomalonaldehydes in the presence of a solvent and a C1-compound of the formula (III) in which X represents oxygen or sulfur and R1 is as defined in the description, the reaction mixture comprising less than 5% by weight of water.Type: GrantFiled: August 17, 1998Date of Patent: April 16, 2002Assignee: Bayer AGInventor: Helmut Kraus
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6331639Abstract: A compound represented by the formula (1) which is useful as an agricultural fungicide or an intermediate thereof can be obtained by reacting a compound of the general formula (2) with a compound of the general formula (3) in the presence of an acid and reducing the resulted reaction mixture. wherein, each of R1 to R4 and R1a to R4a independently represents a hydrogen atom or an alkyl group, and R represents an alkyl group, alkoxy group, phenyl group or 5-membered or 6-membered heterocyclic group.Type: GrantFiled: February 20, 2001Date of Patent: December 18, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hiroyuki Katsuta, Seiichi Ishii, Kanji Tomiya, Kenji Kodaka
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Patent number: 6255330Abstract: The heterocyclically substituted phenylglycinolamides are obtained by reaction of heterocyclically substituted phenylacetic acids with appropriate phenylglycinols. The heterocyclically substituted phenylglycinolamides are suitable as active compounds in medicaments, in particular in antiatherosclerotically active medicaments.Type: GrantFiled: April 20, 2000Date of Patent: July 3, 2001Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck
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Patent number: 6184386Abstract: A compound for photography is described, which is represented by following formula (I): wherein R1, R2, and R3 each represents a hydrogen atom or a group capable of being substituted; A and B each represents a hydrogen atom or a group which can be removed with an alkali; “time” represents a group releasing PUG after released from an oxidation product of the hydroquinone mother nucleus; m represents 0 or 1; and PUG represents a group represented by following formula (II): wherein X represents a hydrogen atom, an alkyl group, a carboxyl group, an alkoxycarbonyl group, a cyano group, or a carbamoyl group; Y represents a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, a carbamoyl group, or an alkoxycarbonyl group; L represents an alkylene group or an arylene group; and n represents 0 or 1.Type: GrantFiled: August 26, 1998Date of Patent: February 6, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Takeuchi, Shinichi Ichikawa, Keisuke Matsumoto
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Patent number: 6124455Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: January 25, 2000Date of Patent: September 26, 2000Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 6080760Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 17, 1998Date of Patent: June 27, 2000Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Mark G. Bock
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Patent number: 6037354Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 17, 1998Date of Patent: March 14, 2000Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Harold G. Selnick, Mark G. Bock
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6004543Abstract: The invention relates to novel compounds of formula (I): ##STR1## where R1 is chosen from hydrogen, saturated or unsaturated linear or branched C1 to C8 alkyl groups which are optionally substituted with a substituent, and optionally substituted benzyl groups, and R2 is chosen from hydrogen, saturated or unsaturated linear or branched C1 to C24 alkyl groups which are optionally substituted with a substituent, aromatic groups which are optionally substituted with a substituent, and saturated or unsaturated heterocyclic groups; and the use of these derivatives for skincare.Type: GrantFiled: December 23, 1996Date of Patent: December 21, 1999Assignee: L'OrealInventor: Jean-Baptiste Galey
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Patent number: 5973161Abstract: Methods of synthesizing compounds of the Formula V: ##STR1## wherein X.sub.c is a chiral auxiliary, m is from 1 to 4, and R.sub.8 is hydrogen or --OH, are provided.Additionally, methods of synthesizing compounds of the Formula XII: ##STR2## wherein m is from 1-4; B is hydrogen or a blocking group; and R.sub.13 is a leaving group or a compound of formula R.sub.14 --N--R.sub.15 ;wherein R.sub.14 is hydrogen or branched or straight-chain C1-C6 alkyl; and R.sub.15 is hydrogen, C3-C8 cycloalkyl, or branched or straight-chain alkyl;are also provided. Novel compounds useful in the synthesis of cyclopentenes and carbocyclic nucleosides are further provided.Type: GrantFiled: March 17, 1997Date of Patent: October 26, 1999Assignee: The University of North Carolina at Chapel HillInventor: Michael T. Crimmins
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5925658Abstract: An optically active thiazolidinone derivative having the general formula: ##STR1## wherein: R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a phenyl group, a substituted phenyl group (said substituent represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen), a phenyl-C.sub.1 -C.sub.2 alkyl group or a substituted phenyl-C.sub.3 -C.sub.2 alkyl group (the substituent of said phenyl represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen); R.sup.2 represents a C.sub.1 -C.sub.6 alkyl group; and n represents 1 or 2!.EffectThe optically active thiazolidinone derivative of the present invention has excellent anti-angina pectoris action and is useful as a preventive agent or a therapeutic agent for angina pectoris.Type: GrantFiled: September 2, 1997Date of Patent: July 20, 1999Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Yasuo Ohhata, Shigeki Miyake, Ryosuke Yorikane, Norio Fukuda
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Patent number: 5869679Abstract: Method for synthesizing L-2-oxothiazolidine-4-carboxylate and its acid, L-2-oxothiazolidine-4-carboxylic acid. The present invention involves the separation of phenol from a reaction mixture containing L-2-oxothiazolidine-4-carboxylate and phenol. In the present method a reaction mixture containing phenol, L-2-oxothiazolidine-4-carboxylate, and chloride salt, is contacted with a phenol adsorbing adsorption resin, the adsorption resin comprising a polymer having a polyethylene backbone. The adsorption resin is capable of adsorbing substantially all of the phenol while not adsorbing substantial amounts of the L-2-oxothiazolidine-4-carboxylate from the reaction mixture.Type: GrantFiled: November 10, 1997Date of Patent: February 9, 1999Assignee: Transcend Therapeutics, Inc.Inventors: Francis H. Verhoff, L. Reade Baxley, Xiaofeng Lin, Gordon J. Rossiter
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Patent number: 5861380Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.Type: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5846988Abstract: Compounds useful as cytoprotective agents are disclosed. The compounds possess dual activity, containing a phenolic portion selected to have antioxidant or free radical scavenging properties and a thiazolidine-4-carboxylate portion selected for its potential to act as a cysteine prodrug.Type: GrantFiled: October 20, 1997Date of Patent: December 8, 1998Assignee: Alcon Laboratories, Inc.Inventor: Mark R. Hellberg
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Patent number: 5843973Abstract: A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, ##STR1## wherein W represents sulfur or oxygen and X represents --N(R.sup.1)--, or alternatively X represents sulfur or oxygen and W represents --N(R.sup.1)--, and R.sup.1 represents hydrogen, alkyl or substituted alkyl; R.sup.2 and R.sup.3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R.sup.4 represents hydrogen, alkyl or substituted C.sub.1 -C.sub.4 alkyl; R.sup.5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO.sub.2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.Type: GrantFiled: June 10, 1997Date of Patent: December 1, 1998Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Yasuo Ohhata, Shigeki Miyake, Ryosuke Yorikane, Norio Fukuda
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5795890Abstract: A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.Type: GrantFiled: September 24, 1996Date of Patent: August 18, 1998Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Takahiko Nakae, Masashi Kato, Takehito Fujita, Kazuhito Kawabata, Hiroyuki Ohno
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Patent number: 5773491Abstract: The object of the present invention is polycarbonate molding compositions containing polycarbonates, stabilizers of the general formula (I)R.sub.1 --X--CZ--Y--R.sub.2and optionally polypropylene glycols. The object of the present invention is also use of these molding compositions to produce items for medical applications.Type: GrantFiled: March 7, 1996Date of Patent: June 30, 1998Assignee: Bayer AGInventors: Wolfgang Ebert, Ralf Hufen, Ru digerart, Gerhard Fennhoff
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Patent number: 5693594Abstract: A compound of general formula (I) wherein: A represents a group of general formula (1) or (2) in which each X independently represents a halogen atom or an optionally substituted alkyl, cycloalkyl, alkoxy, aryl or aryloxy group, or an alkenyloxy, alkynyloxy, alkylthio, haloalkylthio, alkenylthio, alkynylthio, alkylsulphinyl, alkylsulphonyl or cyano group; and n is 0, an integer from 1 to 4, or, for the phenyl group, 5; or A represents a group of general formula (3) in which each of R.sup.4, R.sup.5 and R.sup.6 independently represents a hydrogen or halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl alkoxy, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, dialkylcarbamoyl, acyl or acylamido group or a cyano group, with the proviso that R.sup.5 and R.sup.6 do not represent an acyl, acylamido or cyano group; Z represents an oxygen or sulphur atom; R.sup.1 and R.sup.Type: GrantFiled: April 25, 1996Date of Patent: December 2, 1997Assignee: American Cyanamid CompanyInventors: Hans-Peter Niedermann, Dieter Gutheil
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Patent number: 5693310Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.Type: GrantFiled: November 19, 1990Date of Patent: December 2, 1997Assignee: Schering AktiengesellschaftInventors: Heinz Gries, Bernd Raduechel, Hans-Joachim Weinmann, Wolfgang Muetzel, Ulrich Speck
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Patent number: 5672710Type: GrantFiled: November 3, 1995Date of Patent: September 30, 1997Assignee: AllerganInventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
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Patent number: 5618835Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: April 8, 1997Assignee: The Procter & Gamble CompanyInventors: Laurence I. Wu, John M. Janusz
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Patent number: 5614520Abstract: Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): ##STR1## wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group;X is a hydrogen atom, alkyl group or carboxyl group which may be protected, andY is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected.Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.Type: GrantFiled: January 30, 1995Date of Patent: March 25, 1997Assignee: Teijin LimitedInventors: Shiro Kondo, Hisashi Fukushima, Masaichi Hasegawa, Masahiro Tsuchimoto, Ikuo Nagata, Yoshio Osada, Keiji Komoriya, Hisao Yamaguchi