Ether Containing Patents (Class 544/174)
-
Patent number: 7595315Abstract: Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.Type: GrantFiled: December 10, 2004Date of Patent: September 29, 2009Assignee: Eli Lilly and CompanyInventors: Peter Thaddeus Gallagher, Carlos Lamas-Peteira, Francisco Javier Agejas-Chicharro
-
Publication number: 20080161309Abstract: The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: ApplicationFiled: February 21, 2008Publication date: July 3, 2008Inventors: Paul Vincent Fish, Malcolm Christian MacKenny, Alan Stobie, Florian Wakenhut, Gavin Alistair Whitlock
-
Patent number: 7375236Abstract: In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon.Type: GrantFiled: August 18, 2005Date of Patent: May 20, 2008Assignee: Eisai Co., Ltd.Inventors: Naoyuki Shimomura, Manabu Sasho, Akio Kayano, Kazuhiro Yoshizawa, Masahiko Tsujii, Hiroshi Kuroda, Ken Furukawa
-
Patent number: 7297794Abstract: Phenoxy amine compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: November 13, 2002Date of Patent: November 20, 2007Assignee: Emisphere Technologies, Inc.Inventors: David Gschneidner, Kelly Kraft, Chen Zhu, Yi Chen
-
Patent number: 7271264Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 18, 2003Date of Patent: September 18, 2007Assignee: Eli Lilly and CompanyInventors: Ronald Jay Hinklin, Owen Brendan Wallace
-
Patent number: 7057040Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: GrantFiled: February 7, 2002Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
-
Patent number: 6900243Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: February 20, 2001Date of Patent: May 31, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
-
Patent number: 6894191Abstract: The present invention provides a process for the preparation of arylamines comprises reacting aryl halide and aryl amine/heterocyclic amine. The said process is carried out in the presence of a solvent, catalyst and a base.Type: GrantFiled: December 10, 2003Date of Patent: May 17, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Ashutosh Anant Kelkar, Nandkumar Manikrao Patil, Raghunath Vitthal Chaudhari
-
Patent number: 6749988Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: GrantFiled: November 28, 2001Date of Patent: June 15, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
-
Patent number: 6727244Abstract: This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.Type: GrantFiled: April 24, 2003Date of Patent: April 27, 2004Assignee: Merck & Co., Inc.Inventors: Su-er Wu Huskey, Shuet-Hing Lee Chiu
-
Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
-
Patent number: 6600040Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.Type: GrantFiled: June 8, 2001Date of Patent: July 29, 2003Assignee: Merck & Co., Inc.Inventors: Karel M. Jos Brands, Fuh-Rong Tsay, Karen M. Conrad, Matthew M. Zhao
-
Publication number: 20030100754Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.Type: ApplicationFiled: August 26, 1997Publication date: May 29, 2003Inventors: HENRY UHLMAN BRYANT, THOMAS ALAN CROWELL, CHARLES DAVID JONES
-
Publication number: 20030009029Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1Type: ApplicationFiled: June 5, 2002Publication date: January 9, 2003Applicant: Merck Patent GmbHInventors: Herwig Buchholz, Urs Welz-Biermann
-
Patent number: 6503905Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: August 6, 1999Date of Patent: January 7, 2003Assignee: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
-
Patent number: 6482860Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: July 18, 1997Date of Patent: November 19, 2002Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
-
Patent number: 6479491Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.Type: GrantFiled: November 13, 2000Date of Patent: November 12, 2002Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
-
Patent number: 6469164Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-1,4-oxazin-3-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.Type: GrantFiled: June 8, 2001Date of Patent: October 22, 2002Assignee: Merck & Co., Inc.Inventors: Karel M. Jos Brands, Joseph F. Payack, Philip J. Pye
-
Patent number: 6395898Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.Type: GrantFiled: June 8, 2001Date of Patent: May 28, 2002Assignee: Merck & Co. Inc.Inventors: James M. McNamara, Matthew M. Zhao
-
Patent number: 6376711Abstract: The invention relates to a method for preparing aryl ethers that are useful as antidepressants. The invention also relates to intermediates useful in the method and to methods for preparing such intermediates.Type: GrantFiled: December 23, 1999Date of Patent: April 23, 2002Assignee: Pharmacia and Upjohn CompanyInventors: Kevin E. Henegar, Sarah E. Mancini, Keith D. Maisto
-
Publication number: 20020022725Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.Type: ApplicationFiled: June 8, 2001Publication date: February 21, 2002Inventors: James M. McNamara, Matthew M. Zhao
-
Patent number: 6265402Abstract: A 2-phenylmorpholin-5-one derivative having the formula (I): wherein R1 represents a C1 to C8 alkyl group, a C3 to C7 cycloalkyl group or an indanyl group, R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C1 to C5 alkyl group, etc., R4 represents a hydrogen atom, a C1 to C6 alkyl group, etc., R5, R6 represent a hydrogen atom, a C1 to C5 alkyl group, etc., an optical isomer thereof or a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof and a pharmaceutical composition containing the same. The above compound has a strong type IV phosphodiesterase (PDE) inhibitory activity and has bronchodilater and antiinflammatory effects.Type: GrantFiled: February 25, 1999Date of Patent: July 24, 2001Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda
-
Patent number: 6156750Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 13, 1999Date of Patent: December 5, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
-
Preparation of a mannich base intermediate for 2-[(4-heterocyclic-phenoxymethyl)-phenoxy]-alkanoates
Patent number: 6136972Abstract: A Mannich base intermediate for 2-[(4-heterocyclic-phenoxymethyl)-phenoxyl]-alkanoates and methods for its preparation are provided. A method for preparation of an alkyl 2-[2-(secondary amino methyl)-5-alkylphenoxy]-alkanoate comprises the steps of: reacting a mixture of m-alkyl phenol, a secondary amine, and an aldehyde, with or without a catalyst, in a first solvent at reflux temperatures to form a 2-[(secondary amino)methyl]-5-alkylphenol. That product is then reacted with an alkyl 2-haloalkanoate, and an alkali metal carbonate, with or without a second catalyst in a second solvent at reflux temperatures to form the 2-[2-(secondary amino methyl)-5-alkylphenoxy]-alkanoate. The aldehyde may be paraformaldehyde, aqueous formaldehyde, formaldehyde, or polymerized acetal derivatives thereof. The first solvent may be acetonitrile or toluene. The catalyst may be an acid catalyst or a base catalyst.Type: GrantFiled: February 22, 2000Date of Patent: October 24, 2000Assignee: FMC CorporationInventors: Gerard A. Crispino, Mark R. Diener -
Patent number: 6037367Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.Type: GrantFiled: September 14, 1998Date of Patent: March 14, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, James S. Frazee
-
Patent number: 5958916Abstract: The instant invention provides dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods for use in the treatment of bone loss or bone resorption.Type: GrantFiled: August 26, 1997Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
-
Patent number: 5889000Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: September 22, 1997Date of Patent: March 30, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
-
Patent number: 5856323Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
-
Patent number: 5811421Abstract: The present invention provides compounds of formula ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.7 cycloalkyl which is optionally substituted with 1 to 3 substitutents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, amino, nitro, and halo;X is --CH(OH)-- or --CH.sub.2 --;M is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Also provided are methods of using the compounds of the present invention for the treatment of various medical indications associated with post-menopausal syndrome, uterine fibroid disease, endometriosis, and aortal smooth muscle cell proliferation.Type: GrantFiled: July 16, 1996Date of Patent: September 22, 1998Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Kennan Joseph Fahey, Charles David Jones, Charles Willis Lugar, III
-
Patent number: 5811459Abstract: The invention relates to compounds of the formula (I): ##STR1## wherein A, B and D are various ring systems such as phenyl, R.sup.1 includes carboxy, R.sup.3 is hydrogen or C.sub.1-4 alkyl and Z is a linking group such as --(CH(R.sup.5)).sub.m -- wherein m is 2, 3 or 4, and R.sub.5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.Type: GrantFiled: June 4, 1996Date of Patent: September 22, 1998Assignee: Zeneca LimitedInventors: Gloria Ann Breault, John Oldfield, Howard Tucker, Peter Warner
-
Patent number: 5780625Abstract: A description is given of novel O-phenol-substituted aminophenol derivatives of the formula ##STR1## in which the symbols are as defined in claim 1, which can be used in particular as stabilizers for magenta couplers in color-photographic recording materials.Type: GrantFiled: November 25, 1996Date of Patent: July 14, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Suruliappa Gowper Jeganathan, Christophe Bulliard
-
Patent number: 5756733Abstract: The invention relates to novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues, comprising compounds of general formula (I) ##STR1## where R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group; R.sup.3 represents a methyl group having .alpha.- or .beta.-configuration; X represents a valence bond or a C.sub.1-2 alkylene group; Y represents --O--, --S--, --CH.sub.2 -- or --NR-- where R is a hydrogen atom or an organic group; Z represents a valence bond or a C.sub.1-3 alkylene group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A.dbd. does not carry an exocyclic methylene group at the 10-position.Type: GrantFiled: January 5, 1996Date of Patent: May 26, 1998Assignee: Research Institute for Medicine and ChemistryInventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal
-
Patent number: 5686586Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.Type: GrantFiled: October 4, 1996Date of Patent: November 11, 1997Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
-
Patent number: 5677303Abstract: Enolethers and thioenolethers of formula I ##STR1## are disclosed. The compounds are useful for combatting phytopathogenic fungi.Type: GrantFiled: June 20, 1996Date of Patent: October 14, 1997Assignee: American Cyanamid CompanyInventors: Juergen Curtze, Guido Albert
-
Patent number: 5637699Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: May 22, 1995Date of Patent: June 10, 1997Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Paul E. Finke, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark S. Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian J. Williams
-
Patent number: 5565611Abstract: The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.Type: GrantFiled: June 6, 1995Date of Patent: October 15, 1996Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shinozaki Fumihiko, Nagasawa Hiroshi, Maruhashi Kazuo
-
Patent number: 5525633Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.Type: GrantFiled: June 15, 1994Date of Patent: June 11, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
-
Patent number: 5521180Abstract: A morpholine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group; R.sup.2 represents a halogen atom; and the dotted line indicates an optional double bond. These compounds exhibit a selective 5-HT reuptake inhibitory activity and a selective 5-HT.sub.2 receptor antagonistic activity and useful as a therapeutic agent for depression, anxiety, etc. with reduced side effects.Type: GrantFiled: August 3, 1995Date of Patent: May 28, 1996Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuo Fujii, Takayuki Suzuki, Satoshi Hayashibe, Shin-ichi Tsukamoto, Shin-ichi Yatsugi, Tokio Yamaguchi
-
Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
-
Patent number: 5495019Abstract: The invention provides a process for the preparation of 3,3-diaryl acrylic acid amides of the general formula ##STR1## in which A, B and Q are as defined in the specification, by condensing a compound of formula ##STR2## with a compound of formulaCH.sub.3 --CO--Q (III)in which Q has the meaning given above, in a solvent in the presence of an alkali metal hydroxide, characterised in that the solvent is selected from alkanes, cycloalkanes or mixtures thereof.Type: GrantFiled: March 16, 1995Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Jurgen Curtze, Bodo Haertel
-
Patent number: 5491233Abstract: A catalytic asymmetric reduction process, which, by hydrogenating trisubstituted olefins, yields a corresponding organic compound having a high level of enantiomeric purity is disclosed. The process is also effective for the catalytic asymmetric reduction of certain enamines and related compounds to yield a corresponding amine or related compound, respectively, having a high level of enantiomeric purity. The reduction process utilizes a chiral metal catalyst that includes a metal or metal complex that is selected from groups 3, 4, 5, or 6, lanthanides and actinides. Moreover, the process uses hydrogen as the stoichiometric reducing agent and may be carried out at pressures ranging from about 0.5 to 200 atmospheres. The reaction can also be carried out using an acidic compound as a rate enhancing additive.Type: GrantFiled: July 12, 1994Date of Patent: February 13, 1996Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Richard D. Broene, Nancy E. Lee
-
Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
-
Patent number: 5464836Abstract: A description follows of benzophenones having an antifungal activity and responding to the general formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, the same or different, represent C.sub.1 -C.sub.6 alkyl groups, C.sub.7 -C.sub.10 arylalkyl groups; or R.sub.1 and R.sub.2, considered jointly with N, represent a C.sub.3 -C.sub.8 heterocyclic group or a C.sub.2 -C.sub.7 heterocyclic group containing a second hetero-atom selected from O and S, said heterocyclic groups being optionally subsituted with one or more C.sub.1 -C.sub.4 alkyl groups;R.sub.3 and R.sub.4, the same or different, represent H atoms, C.sub.1 -C.sub.3 alkyl groups;K represents an oxygen atom or methylene;A represents a benzene group, optionally sustituted with one or more halogen atoms, C.sub.1 -C.sub.4 alkyl or haloalkyl groups, C.sub.1 -C.sub.4 alkoxylics, C.sub.1 -C.sub.4 haloalkoxylics;Y represents a C.sub.6 -C.sub.10 aryl group; said group may be optionally substituted with one or more halogen atomos, C.sub.1 -C.sub.Type: GrantFiled: October 5, 1993Date of Patent: November 7, 1995Assignee: Ministero dell'Universita` e della Ricerca Scientifica e TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5459262Abstract: A new process for the preparation of a phenylbenzamide derivative of the formula ##STR1## wherein R is C.sub.1 -C.sub.2 alkyl, substituted with 2 to 5 F, and each of R.sub.1 and R.sub.2, which can be identical or different, is methyl or ethyl, or --NR.sub.1 R.sub.2 is morpholino, comprising condensing a haloenone (I) with an acetoamide (II), according to scheme ##STR2## in the presence of an organic solvent and 1 to 2 equivalents of base, followed by converting the resulting product in two steps, one of which is a reduction, to the corresponding compound of formula (A). Phenylbenzamides of formula (A) are agricultural fungicides. The new process is suited to large-scale production of these compounds.Type: GrantFiled: February 8, 1994Date of Patent: October 17, 1995Assignee: Rhone-Poulenc AgrochimieInventor: Christian Schmitz
-
Patent number: 5447930Abstract: An improved, clear and non-greasy topical anesthetic for the relief of various skin irritations such as minor burns, insect bites, rashes and allergic reactions is prepared using pramoxine hydrochloride and zinc acetate as the active ingredients.Type: GrantFiled: May 6, 1993Date of Patent: September 5, 1995Assignee: Warner-Lambert CompanyInventor: Ammunje S. Nayak
-
Patent number: 5391735Abstract: The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2-hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.Type: GrantFiled: April 12, 1994Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Piero Melloni, Arturo D. Torre, Ettore Lazzari, Giuseppe Mazzini
-
Patent number: 5385892Abstract: The ethylamino phenyl ethers of the invention and compositions thereof are endowed with high activities as inhibitors of the growth of several species of pathogen fungi and are applied to plants or to plant parts and are effective in preventing the diseases caused by pathogen fungi, such as, e.g., those belonging to Erysiphe and Helminthosporium genera.Type: GrantFiled: January 4, 1993Date of Patent: January 31, 1995Assignee: Ministero Dell "Universita" E Dell Ricerca Scientifica E TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5378707Abstract: Aryl-propyl-aminic compounds having the following formula ##STR1## have high activity and are useful in the agricultural field as fungicides.Type: GrantFiled: November 22, 1993Date of Patent: January 3, 1995Assignee: Minestero Dell' Universita 'e Della Ricerca Scientifica e TechnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5314879Abstract: The invention relates to the manufacture and use of aryl-propyl-aminic compounds having the following formula ##STR1## that have a high antifungal activity and are useful in the agricultural field as fungicides.Type: GrantFiled: February 28, 1991Date of Patent: May 24, 1994Assignee: Ministero Delli `Universita` E Della Ricerca Scientifica E TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5310909Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.Type: GrantFiled: November 21, 1990Date of Patent: May 10, 1994Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer, Walter Fischer, Jurgen Finter, Kurt Meier, Martin Roth