The Carbonyl Is Bonded Directly To Nitrogen Of Morpholine Ring Patents (Class 544/176)
-
Publication number: 20090281085Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 3, 2009Publication date: November 12, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
-
Publication number: 20090042855Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 3, 2008Publication date: February 12, 2009Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
-
Publication number: 20090023903Abstract: A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N-trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro-phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N-trifluoroacetylmorpholine.Type: ApplicationFiled: July 14, 2008Publication date: January 22, 2009Applicant: WyethInventors: Terrence Joseph Connolly, Anita Wai-Yin Chan, Zhixian Ding, Mousumi Ghosh, Xinxu Shi, Jianxin Ren, Eric Hansen, Roger Farr, Michael MacEwan, Asaf Alimardanov, Antonia Nikitenko, John Potoski
-
Patent number: 7262296Abstract: 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: December 15, 2005Date of Patent: August 28, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
-
Patent number: 7166600Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: January 11, 2006Date of Patent: January 23, 2007Assignee: Genentech, Inc.Inventor: David Y. Jackson
-
Patent number: 7125871Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: May 24, 2001Date of Patent: October 24, 2006Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Jesus Ezquerra-Carrera, Alicia Marcos Liorente, Luisa Maria Martin-Cabrejas, James Allen Monn
-
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: 7015323Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: May 19, 2004Date of Patent: March 21, 2006Assignee: Genentech, Inc.Inventor: David Y. Jackson
-
Patent number: 6790955Abstract: The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H.Type: GrantFiled: November 5, 2002Date of Patent: September 14, 2004Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
-
Patent number: 6774086Abstract: There are described derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R1a, R1b, R1c, R2, R3, R4 and R5 are various radicals, X1 is a bridging atom, X2 a carbon chain and X3 a chalcogen atom.Type: GrantFiled: September 10, 2002Date of Patent: August 10, 2004Assignee: Bayer CropScience GmbHInventors: Thomas Seitz, Lothar Willms, Andreas van Almsick, Hermann Bieringer, Thomas Auler, Hubert Menne
-
Publication number: 20040143115Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists 1Type: ApplicationFiled: November 5, 2003Publication date: July 22, 2004Inventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
-
Patent number: 6700025Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: January 5, 2001Date of Patent: March 2, 2004Assignee: United Therapeutics CorporationInventors: Robert M. Moriarty, Hitesh Batra
-
Publication number: 20040030129Abstract: An NF-&kgr;B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R4 is H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 16, 2002Publication date: February 12, 2004Inventors: Yoichi Nunokawa, Kenji Suzuki, Masayuki Saitoh
-
Patent number: 6649616Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.Type: GrantFiled: August 30, 2001Date of Patent: November 18, 2003Assignee: Bayer AktiengesellschaftInventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Müller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
-
Patent number: 6649612Abstract: Compounds of formula (I): in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.Type: GrantFiled: August 21, 2001Date of Patent: November 18, 2003Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Nedoncelle
-
Publication number: 20030125548Abstract: A method for identifying molecules and designing novel pharmaceuticals is disclosed. The disclosed method of novel pharmaceutical design identifies a novel chemical group that triggers a mechanism of action for an identified reaction, thereby avoiding the various structural complexities associated with the application of the structure-based drug design. Additionally, examples of potential therapeutics identified by the mechanism based drug design method are provided.Type: ApplicationFiled: September 13, 2002Publication date: July 3, 2003Inventors: Dorit Arad, Arthur P Bollon, David c Young, Bradley W Poland, Andrew S Peek
-
Patent number: 6573387Abstract: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.Type: GrantFiled: January 31, 2000Date of Patent: June 3, 2003Assignee: The Scripps Research InstituteInventors: K. Barry Sharpless, A. Erik Rubin
-
Patent number: 6566553Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.Type: GrantFiled: August 10, 2001Date of Patent: May 20, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: François Soucy, Louis Plamondon, Mark Behnke, William Roush
-
Publication number: 20030073832Abstract: Novel heteroaryl aminophenyl ketone derivatives which are inhibitors of MAP kinases, in particular the p38 MAP kinase, are useful as anti-inflammatory agents in the prophylaxis or treatment of inflammatory diseases or conditions.Type: ApplicationFiled: April 10, 2002Publication date: April 17, 2003Inventor: Sophie Elisabeth Havez
-
Patent number: 6534652Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)- enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable saltsType: GrantFiled: July 10, 2001Date of Patent: March 18, 2003Assignee: AstraZeneca ABInventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
-
Patent number: 6531471Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 14, 2001Date of Patent: March 11, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
-
Patent number: 6506939Abstract: A process for the preparation of a mixture comprising a compound of formula (1) and a compound of formula (2) wherein R1 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl, optionally substituted C5-7 cycloalkyl or optionally substituted benzyl, R2 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, A is either S or NR3, R3 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, or R2 and R3 together form a 5-7 membered ring which can contain an oxygen atom, R4 is hydrogen or methyl, R5 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl, optionally substituted C5-7 cycloalkyl or optionally substituted benzyl and, R6 is hydrogen or an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, or R5 and R6 together form a 5-7 membered ring which can contType: GrantFiled: July 13, 2001Date of Patent: January 14, 2003Assignee: Ciba Specialty Chemicals Water Treatments Ltd.Inventors: Peter Stuart Littlewood, Michael Singh
-
Publication number: 20020107390Abstract: Compounds of the formula 1Type: ApplicationFiled: August 16, 2001Publication date: August 8, 2002Inventor: Paivi J. Kukkola
-
Patent number: 6362182Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 30, 2000Date of Patent: March 26, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
-
Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
-
Publication number: 20020028801Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: ApplicationFiled: August 9, 2001Publication date: March 7, 2002Inventors: Michael Francis Rafferty, Yuntao Song
-
Patent number: 6316475Abstract: Compounds of formula (I) are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands.Type: GrantFiled: November 17, 2000Date of Patent: November 13, 2001Assignee: Abbott LaboratoriesInventors: Youssef L. Bennani, Ramin Faghih
-
Patent number: 6218390Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 17, 1998Date of Patent: April 17, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
-
Patent number: 6207716Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: GrantFiled: October 30, 1998Date of Patent: March 27, 2001Assignee: Glaxo Wellcome Inc.Inventor: Timothy Mark Willson
-
Patent number: 6200972Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: February 23, 1998Date of Patent: March 13, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Jia-He Li, Gregory S. Hamilton
-
Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
-
Patent number: 6107494Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.Type: GrantFiled: March 24, 1999Date of Patent: August 22, 2000Assignee: G.D. Searle and CompanyInventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
-
Patent number: 6069247Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: October 5, 1998Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
-
Patent number: 6020332Abstract: Fluorine-containing diphenyl acrylamide of general formula (I) have antimicrobial properties. wherein R.sub.1 and R.sub.2 are independently selected from (C.sub.1 -C.sub.6)alkyl group, alkyl group, (C.sub.1 -C.sub.6)alkoxy group, halo(C.sub.1 -C.sub.6)alkyl group, halo(C.sub.1 -C.sub.6)alkoxy group, (C.sub.1 -C.sub.6)alkoxy(C.sub.1 -C.sub.6)alkyl group, (C.sub.3 -C.sub.6)cycloalkyl group, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl group, (C.sub.2 -C.sub.6)alkenyl group, halo(C.sub.2 -C.sub.6)alkenyl group, (C.sub.3 -C.sub.6)alkynyl group, halo(C.sub.3 -C.sub.6)alkynyl group, aryl group, aryloxy(C.sub.1 -C.sub.12)alkyl group, aralkyl group, heterocyclic group;or R.sub.1 and R.sub.2 when taken together may form a 5 or 6-membered ring such that;when R.sub.1 and R.sub.2 are in a 5 membered ring R.sub.1 and R.sub.2 taken together is C(R.sub.6 R.sub.7); andwhen R.sub.1 and R.sub.2 are in a 6 membered ring R.sub.1 and R.sub.2 taken together is CHR.sub.6 -CHR.sub.7 ;where R.sub.6 and R.sub.Type: GrantFiled: February 9, 1998Date of Patent: February 1, 2000Assignee: Shenyang Research Institute of Chemical IndustryInventors: Zongcheng Li, Changling Liu, Wucheng Liu
-
Patent number: 5917038Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: April 11, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
-
Patent number: 5877219Abstract: Described herein are non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: GrantFiled: June 18, 1997Date of Patent: March 2, 1999Assignee: Glaxo WellcomeInc.Inventor: Timothy Mark Willson
-
Patent number: 5869663Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.Type: GrantFiled: March 18, 1997Date of Patent: February 9, 1999Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
-
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: 5703076Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: December 30, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
-
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: 5686435Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.Type: GrantFiled: December 7, 1995Date of Patent: November 11, 1997Assignee: Research Institute for Medicine and ChemistryInventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
-
Patent number: 5681835Abstract: Prescribed herein are novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: GrantFiled: April 25, 1994Date of Patent: October 28, 1997Assignee: Glaxo Wellcome Inc.Inventor: Timothy Mark Willson
-
Patent number: 5635103Abstract: Improved cleaning and/or bleaching compositions including fabric laundry and bleaching compositions, automatic dishwashing compositions, hard surface cleaners, bleach additives and the like, suitable for domestic use, comprising improved bleach activators having particular alpha-modified lactam leaving groups leading to improved in-use performance of bleaching agents such as perborate even under wash conditions less alkaline than those typically encountered or when hydrogen peroxide source is at low levels in a cleaning operation. A preferred class of activators are N-acyl-3-morpholinone compounds with benzoyl being a preferred acyl group and N-Benzoyl-3-oxomorpholine being a highly preferred activator.Type: GrantFiled: January 20, 1995Date of Patent: June 3, 1997Assignee: The Procter & Gamble CompanyInventors: Alan D. Willey, Kevin L. Kott, Gregory S. Miracle, Eugene P. Gosselink, James C. T. R. B. St. Laurent
-
Patent number: 5554581Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.Type: GrantFiled: May 25, 1995Date of Patent: September 10, 1996Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.Inventors: Kenji Hirai, Tomoko Matsukawa, Tomoyuki Yano, Emiko Ejiri, Kiyomi Aizawa, Koichi Shikakura, Tomoko Yoshii, Sadayuki Ugai, Osamu Yamada, Shigeki Kishi
-
Patent number: 5506190Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.Type: GrantFiled: September 19, 1994Date of Patent: April 9, 1996Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co. Ltd.Inventors: Kenji Hirai, Tomoko Matsukawa, Tomoyuki Yano, Emiko Ejiri, Kiyomi Aizawa, Koichi Shikakura, Tomoko Yoshii, Sadayuki Ugai, Osamu Yamada, Shigeki Kishi
-
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
-
Process for trans-6[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
Patent number: 5489690Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.Type: GrantFiled: May 15, 1995Date of Patent: February 6, 1996Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Tung V. Le, Thomas N. Nanninga -
Patent number: 5481035Abstract: Process for the preparation of asymmetrically substituted ureas, carbamates, thiocarbamates or substituted isocyanates by reaction of an adduct of isocyanic acid and a tertiary amine with a primary and secondary amine, an alcohol, a thiol or a compound having one or two non-cumulated olefinic double bonds, and a process for the preparation of N-mono- or N,N-disubstituted ureas by reaction of ammonium isocyanates with a primary or secondary amine in a diluent.Type: GrantFiled: July 6, 1993Date of Patent: January 2, 1996Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Martin Mullner, Gerhard Stern, Markus Rossler
-
Patent number: 5475027Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: November 8, 1993Date of Patent: December 12, 1995Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
-
Patent number: 5389680Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: October 18, 1993Date of Patent: February 14, 1995Assignee: Monsanto CompanyInventor: Peter G. Ruminski