The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 549/71)
-
Patent number: 4931458Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--; R.sup.1 is the group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl; and R.sup.4 is hydrogen, hydroxy, amino, lower-alkyl amino, di-(lower alkyl)amino or lower alkyl; with at least one ring of the molecule being heterocyclic, as well as salts of such compounds are useful in rodenticidal compositions containing a bait to eliminate rodents.Type: GrantFiled: October 5, 1988Date of Patent: June 5, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
-
Patent number: 4927947Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above, or --CH.sub.2 OH and its ether and acyl ester derivatives; or a pharmaceutically acceptable salt.Type: GrantFiled: January 30, 1989Date of Patent: May 22, 1990Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
-
Patent number: 4923884Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above, or --CH.sub.2 OH and its ether and acyl ester derivatives; or a pharmaceutically acceptable salt.Type: GrantFiled: April 1, 1988Date of Patent: May 8, 1990Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
-
Patent number: 4910221Abstract: Pesticidal novel .alpha.-methylsulphonyl-benzaldoxime derivatives of the formula ##STR1## in which R represents alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkenyloxy, aryl or aryloxy which is in each case optionally monosubstituted to polysubstituted by identical or different substituents, aralkyloxy which is optionally monosubstituted to polysubstituted in the aryl radical by identical or different substituents, cycloalkyloxy which is optionally monosubstituted to polysubstituted by identical or different substituents, or a heterocyclic ring which is optionally monosubstituted to polysubstituted by identical or different substituents,X represents hydrogen or halogen, andHal represents halogen.Type: GrantFiled: April 8, 1988Date of Patent: March 20, 1990Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Gerd Hanssler, Wilhelm Brandes
-
Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
-
Patent number: 4886832Abstract: Fungicidally active benzaldoxime derivatives of the formula ##STR1## in which R represents alkyl, alkoxy, halgenoalkyl, halogenoalkoxy or alkenyloxy, or aryl or aryloxy, in each case optionally mono- or polysubstituted by identical or different substituents, aralkyloxy which is optionally mono- or polysubstituted in the aryl radical by identical or different substituents, or represents cycloalkoxy which is optionally mono- or polysubstituted by identical or different substituents, or represents a heterocyclic radical which is optionally mono- or polysubstituted by identical or different substituents,R.sup.1 represents hydrogen, halogen, alkyl or alkoxy,R.sup.2 represents hydrogen, alkyl or halogenoalkyl,R.sup.3 represents hydrogen or halogen,R.sup.4 represents halogen andR.sup.5 represents hydrogen or halogen.Type: GrantFiled: March 10, 1988Date of Patent: December 12, 1989Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Kurt Findeisen, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler, Paul Reinecke
-
Patent number: 4882341Abstract: The invention relates to amino substituted propenoates and their use against fungi.Type: GrantFiled: September 9, 1988Date of Patent: November 21, 1989Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Ian T. Kay
-
Patent number: 4863503Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, wherein R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl groups, and Z is either an oxygen or sulphur atom; A is an oxygen or sulphur atom, --NR.sup.3 --, or --CR.sup.4 R.sup.5 --; X, Y and Z.sup.Type: GrantFiled: April 17, 1987Date of Patent: September 5, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul de Fraine, Christopher R. A. Godfrey, Kevin Beautement
-
Novel class of acyl-derivatives of carnitine, process for preparing same and therapeutic use thereof
Patent number: 4859698Abstract: A novel class of acyl-derivatives of carnitine is disclosed wherein the acyl radical is either the radical of unsaturated organic acids (typically, acrylic acid) or the radical of saturated organic acids substituted with tert-alkyl, cycloalkyl, cycloalkenyl, alkoxyl, heterocyclic and carboalkoxylradicals, or with aldehyde or hydroxy groups. These acyl-derivatives of carnitine are useful therapeutical agents in the treatment of cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias.Type: GrantFiled: May 31, 1988Date of Patent: August 22, 1989Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Claudio Cavazza, Paolo De Witt, Maria O. Tinti -
Patent number: 4847288Abstract: The present invention relates to compounds which are allenyl amines, more specifically, .beta.-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a noval reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.Type: GrantFiled: February 8, 1988Date of Patent: July 11, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Thomas M. Bargar, Charlotte L. Barney, Donald P. Matthews, Robert J. Broersma
-
Patent number: 4840953Abstract: 9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.Type: GrantFiled: June 15, 1988Date of Patent: June 20, 1989Assignee: Shionogi & Co., Ltd.Inventors: Shigeru Matsutani, Yukio Mizushima, Masami Doteuchi, Yasunobu Ishihara
-
Patent number: 4818273Abstract: Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonamides, e.g., 5,7-dimethyl-N-(2,6-dichlorophenyl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulf onamide and their agriculturally acceptable salts are prepared. These compounds and compositions containing them are useful for the control of unwanted vegetation. Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonyl chlorides and substituted anilines and their use as intermediates are also described.Type: GrantFiled: December 10, 1986Date of Patent: April 4, 1989Assignee: The Dow Chemical CompanyInventors: William A. Kleschick, Robert J. Ehr, Mark J. Costales, Ben C. Gerwick, III, Richard W. Meikle, deceased, William T. Monte, Pearson, Norman R.
-
Patent number: 4798892Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
-
Patent number: 4797486Abstract: Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates therefor.Type: GrantFiled: October 14, 1987Date of Patent: January 10, 1989Assignee: Pfizer Inc.Inventors: Edward A. Glazer, James W. McFarland
-
Patent number: 4792612Abstract: Novel compounds, 2-(.alpha.-alkoxyimino)ethylthiophenes are susceptible to electrophilic substitution reactions, and the acetylation, nitration, sulfonation and halogenation of the compounds provide 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-nitro-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenesulfonic acid and 5-halo-2-(.alpha.-alkoxyimino)ethylthiophenes, respectively.The hydrolysis of 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes readily provides a known compound, 2,5-diacetylthiophene which is an important intermediate for the production of medicines, whereas the haloform reaction provides novel compounds, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenecarboxylic acids, the hydrolysis of which compounds readily provides a known compound, 5-acetyl-2-thiophenecarboxylic acids, an important intermediate for the production of medicines.The hydrolysis of 5-(.alpha.Type: GrantFiled: March 21, 1988Date of Patent: December 20, 1988Assignee: Seitetsu Kagaku Co., Ltd.Inventors: Hiroshi Goda, Masao Kawamura, Kunioki Kato, Makoto Sato
-
Patent number: 4778803Abstract: The invention relates to new nitrogen-arylmethoxy-thiophene derivatives of the formula I ##STR1## wherein the R--CH.sub.2 --O-group is in position 4 or 5 of the thiophene ring, R denotes a 2-pyridinyl- or 2-quinolinyl group and R.sub.1 denotes a --COO-lower alkyl-, --CO--(CH.sub.2)n--CH.sub.3 or --CH(OH)--(CH.sub.2).sub.n --CH.sub.3 group, wherein n represents an integer from 2 to 6, and their hydrates and/or their pharmaceutically acceptable acid addition salts, a process for their preparation and pharmaceutical products containing these compounds. The new compounds and their salts have useful pharmacological properties. They can be used as active compounds for medicaments for the treatment and prevention of diseases, caused by a disturbance in arachidonic acid metabolism.Type: GrantFiled: December 24, 1986Date of Patent: October 18, 1988Assignee: Chemie Linz AktiengesellschaftInventors: Dieter Binder, Franz Rovenszky, Hubert P. Ferber, Karsten Schror
-
Patent number: 4758369Abstract: There are disclosed novel, highly stable sulfone peroxycarboxylic acids useful in detergent compositions alone or as bleaching agents which are represented by the formula ##STR1## wherein A and B are organic moieties bonded to the sulfur atom by a carbon atom and at least one of A and B containing at least one ##STR2## group bonded to a carbon atom.Type: GrantFiled: September 17, 1987Date of Patent: July 19, 1988Assignee: Monsanto CompanyInventors: David R. Dyroff, Daniel P. Getman, Joan K. Glascock
-
Patent number: 4755527Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
-
Patent number: 4752613Abstract: Compounds represented by the formula ##STR1## wherein X is halogen, lower alkyl, arylalkyl, alkoxy or hydroxy; wherein the phenyl ring is mono or disubstituted, R' is --COOH or ##STR2## wherein R" is lower alkyl or aryl and n and m are independently zero, one, two or three which are potent thromboxane A.sub.2 receptor antagonists.Type: GrantFiled: August 3, 1987Date of Patent: June 21, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: David M. Floyd, Philip D. Stein
-
Patent number: 4743617Abstract: This invention relates to novel heterocyclyl-2-propyn-1-amines which are useful as dopamine beta hydroxylase inhibitors in the treatment of hypertension.Type: GrantFiled: August 31, 1987Date of Patent: May 10, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Thomas M. Bargar, Lawrence C. Creemer, James R. McCarthy
-
Patent number: 4725599Abstract: Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates therefor.Type: GrantFiled: September 8, 1986Date of Patent: February 16, 1988Assignee: Pfizer Inc.Inventors: Edward A. Glazer, James W. McFarland
-
Patent number: 4691050Abstract: The present invention provides a process for the preparation of aromatic dicarboxylic acids by the carbonylation of aromatic diiodides. The aromatic diiodides are reacted with carbon monoxide in the presence of a soluble rhodium catalyst in a hydrocarbon acid reaction medium to prepare the aromatic dicarboxylic acids.Type: GrantFiled: May 23, 1986Date of Patent: September 1, 1987Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
-
Patent number: 4677113Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by a thenoyl group, which thenoyl group is substituted by an acid group are useful as inhibitors of leukotriene synthesis and as antiallergic agents.Type: GrantFiled: April 22, 1986Date of Patent: June 30, 1987Assignee: Riker Laboratories, Inc.Inventors: Randy L. Bell, George G. I. Moore
-
Patent number: 4663429Abstract: A process for producing a lactone polymer which comprises reacting an ester compound synthesized from an alcohol and an acid or acid anhydride thereof with a lactone and a ring-opening polymerization initiator without being accompanied by condensation. The thus produced lactone polymer is effective for preventing shrinkage of thermosetting resins, particularly unsaturated polyester resins.Type: GrantFiled: July 31, 1985Date of Patent: May 5, 1987Assignee: Daicel Chemical Industries, Ltd.Inventors: Takaaki Murai, Shoji Watanabe, Kimio Inoue, Tomohisa Isobe, Naoki Nakashima, Takuya Miho, Yoshiyuki Ikemoto
-
Patent number: 4659735Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O--or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.Type: GrantFiled: April 19, 1985Date of Patent: April 21, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
-
Patent number: 4652303Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from the group consisting of:the groups R.sup.5 --CO-- and R.sup.5 --CS-- wherein: R.sup.5 is selected from alkenyl, alkynyl, benzyl, phenyl, substituted alkyl, substituted alkenyl, substituted alkynyl, substituted benzyl, substituted phenyl and the acetal, hemiacetal, oxime, imine and Schiff base derivatives of the group R.sup.5 --CO--;the groups Y--CO-- and Y--CS-- wherein Y is selected from hydroxy, mercapto, alkylthio and the groups MO-- and MS-- wherein M is an organic or an inorganic cation;the groups R.sup.6 R.sup.7 NCO-- and R.sup.6 R.sup.7 NCS-- wherein R.sup.6 and R.sup.7 are independently selected from hydrogen, alkyl, substituted alkyl, alkanoyl, carboxy, alkoxycarbonyl, alkylsulfonyl, benzoyl, benzenesulfonyl, substituted benzoyl, substituted benzenesulfonyl, or R.sup.6 and R.sup.Type: GrantFiled: July 2, 1984Date of Patent: March 24, 1987Assignee: ICI Australia LimitedInventors: Keith G. Watson, Graham J. Bird, Graeme J. Farquharson
-
Patent number: 4643849Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compounds, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: November 14, 1983Date of Patent: February 17, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanagi, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
-
Patent number: 4637902Abstract: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.Type: GrantFiled: March 14, 1984Date of Patent: January 20, 1987Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroyuki Hirai, Ken Kawata
-
Patent number: 4609739Abstract: The present invention provides novel compositions of matter and processes for their preparation. More particularly, the present invention consists of novel chemical intermediates and associated processes for the preparation of khellin and other furochromone analogues, which have demonstrated antiatherosclerotic activity. These novel intermediates and processes can also be used for the preparation of benzofurans and benzothiophenes which inhibit the synthesis of leukotriene and/or lipoxygenase.Type: GrantFiled: November 6, 1984Date of Patent: September 2, 1986Assignee: The Upjohn CompanyInventor: Ronald B. Gammill
-
Patent number: 4602095Abstract: Novel 3-hydroxy-4-alkyloxphenyl heterocyclic aromatic carboxylate compounds particularly well suited as sweeteners in foodstuff.Type: GrantFiled: December 29, 1983Date of Patent: July 22, 1986Assignee: General Foods CorporationInventors: Paul R. Zanno, Ronald E. Barnett, Jed A. Riemer
-
Patent number: 4594445Abstract: The present invention provides a process for the preparation of aryl carboxylic acids and derivatives thereof by the carbonylation of diaryliodonium salts. The diaryliodonium salts are reacted with carbon monoxide and water or an alcohol or amine in a base reaction medium having a pK.sub.b greater than about 8.Type: GrantFiled: January 7, 1985Date of Patent: June 10, 1986Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
-
Patent number: 4564701Abstract: The present invention provides a process for the preparation of aryl carboxylic acids by the carbonylation of diaryliodonium salts. The diaryliodonium salts are reacted with carbon monoxide in the presence of a zero-valent palladium in a hydrocarbon acid reaction medium to prepare the aromatic carboxylic acids.Type: GrantFiled: January 22, 1985Date of Patent: January 14, 1986Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
-
Patent number: 4563527Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.Type: GrantFiled: July 19, 1984Date of Patent: January 7, 1986Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shin-ichi Watanabe, Toshiyuki Okutome, Yojiro Sakurai, Masateru Kurumi, Takuo Aoyama
-
Patent number: 4560701Abstract: The invention relates to oxothienobenzoxepin compounds of the formula ##STR1## where X together with the carbon atoms to which it is attached is a thiophene ring;R.sub.1 is hydrogen, a straight or branched chain alkyl group having 1 to 5 carbon atoms or a halogen atom;R.sub.2 is hydrogen or a straight chain alkyl group having 1 to 5 carbon atoms; andR.sub.3 is hydroxyl or ##STR2## where R.sub.4 is a straight chain or branched chain alkyl group having 1 to 10 carbon atoms, a phenyl group or a trifluoromethyl group. Methods for preparing the compounds and their use as antiinflammatory and analgesic agents are provided.Type: GrantFiled: June 13, 1983Date of Patent: December 24, 1985Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak
-
Patent number: 4549025Abstract: Carboxylic acids having the general formula:R--COOHwherein R is selected from the group consisting of aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, alkyl, alkenyl and alkynyl, optionally substituted by inert or non-reactive substituents under the reaction conditions, are obtained by oxidation of the corresponding aldehydes with an alkali metal or alkaline-earth metal chlorite in the presence of hydrogen peroxide and in an aqueous-organic solvent. The resulting carboxylic acids are utilizable as intermediates for preparing fine chemicals in known ways.Type: GrantFiled: December 12, 1984Date of Patent: October 22, 1985Assignee: Montedison S.p.A.Inventors: Enrico Dalcanale, Giorgio Bottaccio, Stefano Campolmi, Fernando Montanari
-
Patent number: 4537970Abstract: This invention relates to the preparation of esters or salts of aromatic or etheroaromatic acids having formula Y--Ar--CO--OR (I), where:Ar represents an aromatic group constituted by one or more benzene rings, optionally condensed, or an etheroaromatic nucleus optionally condensed with one or more benzene rings;Y represents from zero to more substituents, equal or different, chosen among a halogen; an alkyl group having up to 6 carbon atoms; an alkoxy group having up to 5 carbon atoms; an ester group --COOR', where R' contains up to 5 carbon atoms; a hydroxyl group; a phenyloxy group, optionally substituted with groups inert under reaction conditions; a trifluoromethyl group; a nitrile group; an amidic group (--CONH.sub.2); an acetamidic group (--NH--CO--CH.sub.3); or an acyl group --CO--R", where R" represents a hydrocarbon group having up to 8 carbon atoms;R represents an alkyl group R.sub.1 having up to 5 carbon atoms or an alkali metal or alkaline earth metal M.Type: GrantFiled: December 12, 1983Date of Patent: August 27, 1985Assignee: Montedison S.p.A.Inventors: Marco Foa, Franco Francalanci, Andrea Gardano, Elena Bencini
-
Patent number: 4535086Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group--CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.Type: GrantFiled: June 27, 1983Date of Patent: August 13, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
-
Patent number: 4518609Abstract: Naphthenic and heterocyclic retinoic acid analogues such as (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthaldehyde, methyl 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoate, 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoic acid, (E)-1-(5-carbethoxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, (E)-1-(5-carboxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene, (E)-1-(5-carbethoxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, and (E)-1-(5-carboxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene. These retinoids are useful as chemopreventive agents for inhibiting tumor promotion in epithelial cells and for treating nonmalignant skin disorders.Type: GrantFiled: April 12, 1984Date of Patent: May 21, 1985Assignee: SRI InternationalInventors: Marcia I. Dawson, Rebecca L. S. Chan
-
Patent number: 4511577Abstract: A novel derivative of benzoic acid, 2-(2-thenoyloxy)-benzoic acid of formula (I) ##STR1## and pharmaceutically acceptable salts thereof with alkali and alkali-earth metals and with basic amino acids such as lysine, arginine and histidine are valuable antiinflammatory and analgesic agents.They may be prepared by reacting acetylsalicylic acid with a reactive derivative of 2-thiophenecarboxylic acid.The compounds of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents, to provide a pharmaceutical composition.Type: GrantFiled: March 13, 1984Date of Patent: April 16, 1985Assignee: Media Research s.r.l.Inventor: Graziella Bruno
-
Patent number: 4507493Abstract: The present invention provides a process for the preparation of aryl carboxylic acids and derivatives thereof by the carbonylation of aryl sulfonyl chlorides. The aryl sulfonyl chlorides are reacted with carbon monoxide and water or an alcohol or amine in the presence of a zero-valent metal catalyst consisting essentially of palladium.Type: GrantFiled: July 6, 1984Date of Patent: March 26, 1985Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
-
Patent number: 4507316Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclic, ##STR2## wherein R is hydrogen, alkyl, or aryl, and where Y is hydroxy, their pharmaceutically acceptable, nontoxic alkali metal, alkaline earth metal, and amine salts.Type: GrantFiled: June 1, 1981Date of Patent: March 26, 1985Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
-
Patent number: 4506092Abstract: The present invention provides a process for the preparation of aryl carboxylic acids and derivatives thereof by the carbonylation of triaryl sulfonium salts. The triaryl sulfonium salts are reacted with carbon monoxide and water or an alcohol or amine in the presence of a triaryl phosphine and a zero-valent metal catalyst selected from palladium or rhodium.Type: GrantFiled: July 6, 1984Date of Patent: March 19, 1985Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
-
Patent number: 4496580Abstract: The invention relates to oxothienobenzoxepin compounds of the formula ##STR1## where X together with the carbon atoms to which it is attached is a thiophene ring;R.sub.1 is hydrogen, a straight or branched chain alkyl group having 1 to 5 carbon atoms or a halogen atom;R.sub.2 is hydrogen or a straight chain alkyl group having 1 to 5 carbon atoms; andR.sub.3 is hydroxyl or ##STR2## where R.sub.4 is a straight chain or branched chain alkyl group having 1 to 10 carbon atoms, a phenyl group or a trifluoromethyl group.Methods for preparing the compounds and their use as antiinflammatory and analgesic agents are provided.Type: GrantFiled: July 23, 1981Date of Patent: January 29, 1985Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak
-
Patent number: 4487931Abstract: The present invention provides a multistep process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine intermediates of the general formula:- ##STR1## in which R.sub.1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, amino, cyano or carboxyl group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, R.sub.2 is a hydrogen atom, a linear or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, when the aminoethyl radical is in the two position and the radical R.sub.1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580.Type: GrantFiled: June 29, 1982Date of Patent: December 11, 1984Assignee: SanofiInventors: Isaac Chekroun, Alain Heym/e/ s
-
Patent number: 4482718Abstract: The present invention provides a process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives of the general formula: ##STR1## in which R.sub.1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, carboxyl, cyano or amino group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, the aminoethyl chain is in the 2- or 3-position, R.sub.2, R.sub.3 and R.sub.4, which are the same or different, are hydrogen atoms or heterocyclic or non-heterocyclic aromatic radicals, which are optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted.Type: GrantFiled: June 29, 1982Date of Patent: November 13, 1984Assignee: SanofiInventors: Isaac Chekroun, Alain Heymes
-
Patent number: 4480118Abstract: This invention relates to a novel carboxylic acid ester represented by the following general formula (I) and an insecticidal and/or acaricidal composition containing the same as an active ingredient: ##STR1## wherein X is represented by the formula, ##STR2## and further also relates to a carboxylic acid or a reactive derivative thereof represented by the general formula, ##STR3## wherein R.sub.16 is hydroxy group, chlorine or bromine atom, or a C.sub.1-2 alkoxy group, W is oxygen atom or --CH.sub.2 -- group, k is an integer of 0 or 1, E is hydrogen, chlorine, fluorine or bromine atom, and n is an integer of 1 to 4.Type: GrantFiled: December 30, 1981Date of Patent: October 30, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Kazunori Tsushima, Noritada Matsuo, Makoto Hatakoshi, Toshihiko Yano, Nobushige Itaya
-
Patent number: 4480104Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or alkyl, X represents the atoms to complete an aromatic heterocyclic ring system and Y is hydrogen or has the meaning assigned to X, are readily cleaved in alkaline solutions to release a hydroquinone derivative.The compounds can be incorporated into photographic materials used for activation processing.Type: GrantFiled: May 15, 1983Date of Patent: October 30, 1984Assignee: Ciba-Geigy AGInventors: Stephen R. Postle, Patrick D. P. Thomas
-
Patent number: 4472424Abstract: Esters of 2-thenoylmercaptopropionylglycine with substituted hydroxybenzenes, having general formula ##STR1## wherein R is p-acetamidophenyl, p-propyloxy carbophenyl or o-alkyloxycarbophenyl wherein the oxyalkyl radical contains 1-4 carbon atoms, are prepared by reacting 2-thenoylmercaptopropionylglycine with an alkylchloroformate thus obtaining a mixed anhydride which is reacted with the proper substituted hydroxybenzene selected among p-hydroxybenzeneacetamide, propyl p-hydroxybenzoate and alkyl o-hydroxybenzoate. These esters are useful therapeutical agents as mucolytic and antiinflammatory agents.Type: GrantFiled: June 24, 1982Date of Patent: September 18, 1984Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventor: Claudio Cavazza
-
Patent number: 4460601Abstract: Dipeptides are claimed which consist of a mercaptoalkanoic acid and a derivative of said acid, namely an S-alkyl-, aralkyl-, aryl-, acyl- or aroyl derivative with methionine, a methionine ester or a methionine amide, as well as their salts with metallic cations and organic bases. These compounds have the property of protecting the liver against intoxications and have sedative and hypnotic properties.Type: GrantFiled: December 21, 1982Date of Patent: July 17, 1984Assignee: Maggioni Farmaceutici, S.p.A.Inventors: Giampaolo Picciola, Franco Ravenna, Mario Riva
-
Patent number: 4456618Abstract: Naphthenic and heterocyclic retinoic acid analogues such as (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthaldehyde, methyl 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoate, 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoic acid, (E)-1-(5-carbethoxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, (E)-1-(5-carboxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene, (E)-1-(5-carbethoxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1- yl)-1,3-butadiene, and (E)-1-(5-carboxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl) -1,3-butadiene. These retinoids are useful as chemopreventive agents for inhibiting tumor promotion in epithelial cells and for treating nonmalignant skin disorders.Type: GrantFiled: October 15, 1982Date of Patent: June 26, 1984Assignee: SRI InternationalInventors: Marcia I. Dawson, Rebecca L. S. Chan