Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Nitrogen Of The Hetero Ring Patents (Class 540/607)
-
Publication number: 20020082255Abstract: The invention is directed to physiologically active compounds of general formula (I): 1Type: ApplicationFiled: November 2, 2001Publication date: June 27, 2002Inventor: Paul Robert Eastwood
-
Publication number: 20020049199Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked ureas and carbamates of heterocyclic thioesters 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: ApplicationFiled: June 21, 2001Publication date: April 25, 2002Inventors: Gregory S. Hamilton, Jia-He Li, Wei Huang
-
Publication number: 20020045751Abstract: Compounds of the present invention of the formula 1Type: ApplicationFiled: September 28, 2001Publication date: April 18, 2002Inventor: Paivi Jaana Kukkola
-
Publication number: 20020045613Abstract: This invention relates to compounds of formula 1Type: ApplicationFiled: April 24, 2001Publication date: April 18, 2002Inventors: Heinz Pauls, Yong Gong, Julian Levell, Peter Astles, Paul R. Eastwood
-
Patent number: 6362174Abstract: 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: GrantFiled: August 9, 2001Date of Patent: March 26, 2002Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
-
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: 6344466Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: February 28, 2001Date of Patent: February 5, 2002Assignee: 3-Dimensional Pharmaceuticals Inc.Inventors: Richard M. Soll, Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
-
Patent number: 6337394Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: December 29, 1998Date of Patent: January 8, 2002Assignee: AstraZeneca ABInventors: Olle Karlsson, Marcel Linschoten, Jan-Erik Nyström
-
Publication number: 20010056185Abstract: Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.Type: ApplicationFiled: March 12, 2001Publication date: December 27, 2001Inventor: Dennis Lee
-
Patent number: 6316440Abstract: 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: GrantFiled: December 27, 1999Date of Patent: November 13, 2001Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
-
Publication number: 20010036942Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones 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: ApplicationFiled: April 26, 2001Publication date: November 1, 2001Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
-
Patent number: 6310246Abstract: Herbicidal fluorovinyloxyacetamide compounds of formula (I) are useful for protecting crops from weeds: wherein: R1 is a phenyl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy and halogen; R2 is a C1-6 alkyl; or R1 and R2 together with the nitrogen atom to which they are bound form a 5-, 6- or 7-membered nitrogen heterocycle optionally having one or more ring oxygen atoms, double bonds and C1-6 alkyl substituents; R3 is a phenyl or thiophen-2-yl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, methylenedioxy and halogen; and R4is a perfluoro C1-6 alkyl group.Type: GrantFiled: August 14, 2000Date of Patent: October 30, 2001Assignee: Korea Research Institute of Chemical TechnologyInventors: Bum-Tae Kim, No-Kyun Park, Kyung-Sik Hong, Jae-Eup Park, Yong-Woong Kwon
-
Publication number: 20010031890Abstract: The present invention relates to a process for the racemization of N-acylamino acids of the formula (I)Type: ApplicationFiled: March 12, 2001Publication date: October 18, 2001Inventors: Thomas Riermeier, Matthias Beller, Daniel Schichl, Martin Hateley
-
Patent number: 6294551Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters 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: March 1, 2000Date of Patent: September 25, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
-
Publication number: 20010020092Abstract: The present invention relates to a compound of the formula (I) 1Type: ApplicationFiled: December 7, 2000Publication date: September 6, 2001Inventors: Mark James Ford, Jan Vermehren
-
Patent number: 6251949Abstract: Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydrogeType: GrantFiled: December 9, 1999Date of Patent: June 26, 2001Assignee: Shionogi & Co., Ltd.Inventors: Moriyasu Masui, Norihiko Tanimoto, Kuniyoshi Nishida
-
Patent number: 6201126Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.Type: GrantFiled: June 2, 1997Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventor: Manfred Lorenz
-
Patent number: 5939437Abstract: Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R.sup.1 is halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, substituted phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, m is 0, 1, 2, 3, or 4, provided that m is not more than 2 unless R.sup.1 is exclusively halo, x+y=0 or 1, R.sup.2 and R.sup.4 independently are II, or C.sub.1 to C.sub.3 alkyl, R.sup.3 is H or C.sub.1 to C.sub.15 hydrocarbyl, where one or more hydrogen atoms of die hydrocarbyl group may be replaced by a halogen atom, and where up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R.sup.3 does not contain a --O--O-- group, R.sup.5 is H or C.sub.1 to C.sub.Type: GrantFiled: December 20, 1996Date of Patent: August 17, 1999Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Katherine Isobel Mary Steel, David John Dunstone, Ildiko Maria Buck
-
Patent number: 5917034Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein A is optionally monosaturated C.sub.1 -C.sub.4 alkylene optionaly monounsaturatred with C.sub.1 -C.sub.4 alkyl; B is C.sub.1 -C.sub.3 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl; R.sup.1 is N-amidino-4-piperidyl or 4-amidinophenyl; R.sup.2 is C.sub.4 -C.sub.12 alkyl; (C.sub.3 -C.sub.8 cycalkyl)C.sub.1 -C.sub.4 alkylene; optionally methylene-bridged C.sub.5 -C.sub.8 cycloalkyl optionally substituted with one to three C.sub.1 -C.sub.4 alkyl groups or with hydroxy; C.sub.5 -C.sub.8 alkenyl; C.sub.5 -C.sub.8 cycloalkenyl optionally subsituted with C.sub.1 -C.sub.4 alkyl; piperidyl N-substituted with C.sub.1 -C.sub.4 alkyl; tetrahydrothiopyranyl or tetrahydropyranyl; and R.sup.3 is H or C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy or with hydroxy; or R.sup.2 and R.sup.Type: GrantFiled: March 9, 1998Date of Patent: June 29, 1999Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, John Christopher Danilewicz, Paul Vincent Fish
-
Patent number: 5891876Abstract: Compounds useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof, and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also he used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: June 5, 1995Date of Patent: April 6, 1999Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
-
Patent number: 5859002Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: January 12, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried H. Reich, John H. Tatlock, Michael J. Rodriguez
-
Patent number: 5856318Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 11, 1997Date of Patent: January 5, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
-
Patent number: 5852008Abstract: Compounds having the following structural formula, ##STR1## are useful for enhancing synaptic response mediated by AMPA receptors are disclosed, the invention compounds can also be used for the treatment of non-impaired subject for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptor and for improving memory encoding.Type: GrantFiled: June 5, 1995Date of Patent: December 22, 1998Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
-
Patent number: 5846979Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones 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 28, 1997Date of Patent: December 8, 1998Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
-
Patent number: 5847159Abstract: 1-?.omega.-(3,4-Dihydro-2-naphthalenyl)alkyl!cyclic amine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are H, halogen, OH, alkyl, alkoxy, hydroxymethyl, etc., or R.sup.1 and R.sup.2 combine to form methylenedioxy, trimethylene, etc., R.sup.3 is H, etc., R.sup.4 is H, OH, alkyl, etc., R.sup.5 is H, alkyl, etc., p is integer of from 2 to 6, and q is integer of from 3 to 7, provided that when p is 2, and q is 5, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are not simultaneously H, or salts thereof, or N-oxide derivatives thereof, or a process for preparing the same, or pharmaceutical composition containing the same. The compounds of the present invention show potent inhibitory effect on the micturition reflex, and are useful as agents for treatment of frequent urination and urinary incontinence.Type: GrantFiled: October 14, 1997Date of Patent: December 8, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Naoki Kai, Aki Kanehira, Toshiya Morie, Katsuhiko Hino, Katsuyoshi Kawashima, Isao Shimizu, Kazuhisa Akiyama
-
Patent number: 5741799Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: November 8, 1995Date of Patent: April 21, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau, Steven E. Hall, Wen-Ching Han
-
Patent number: 5741792Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: November 8, 1995Date of Patent: April 21, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau, Steven E. Hall, Wen-Ching Han
-
Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
-
Patent number: 5637701Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.Type: GrantFiled: April 11, 1995Date of Patent: June 10, 1997Assignee: John Wyeth & Brother, LimitedInventor: Mark A. Ashwell
-
Patent number: 5627283Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.Type: GrantFiled: June 7, 1995Date of Patent: May 6, 1997Assignee: Behringwerke AktiengesellschaftInventors: Werner St uber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
-
Patent number: 5622984Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)--(in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which R.sup.7 and R.sup.8 are (1) H,(2) phenyl, (3) C7-10 phenylalkyl, (4) phenyl or C7-10 phenylalkyl substituted by 1 or 2 C1-4 alkyl, halogen or R.sup.11 --COOR.sup.12 (in which R.sup.11 is bond, C1-8 alkylene, C2-8 alkenylene, C2-8 alkynylene; R.sup.12 is H, C1-4 alkyl, C7-10 phenylalkyl, phenyl, allyl, propargyl), (5) C1-10 alkyl, (6) C2-10 alkenyl having 1 to 3 double bonds, (7) C2-10 alkynyl having 1 or 2 triple bonds, (8) R.sup.11a --COXR.sup.12 (in which R.sup.Type: GrantFiled: March 1, 1995Date of Patent: April 22, 1997Assignee: Ono Pharmaceutical Company, LimitedInventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
-
Patent number: 5610295Abstract: Amide Derivatives of formula (I): R.sup.5 NR.sup.4 (CR.sub.2).sub.2 CHR.sup.3 CONR.sup.1 R.sup.2 and their pharmaceutically acceptable salts are 5-HT1A binding agents and may be used, for example, as anxiolytics. The radicals, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have specified meanings.Type: GrantFiled: May 24, 1995Date of Patent: March 11, 1997Assignee: John Wyeth & Brother, Ltd.Inventors: Ian A. Cliffe, Anderson D. Ifill
-
Patent number: 5571835Abstract: The present invention comprises analogs of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. These CA.sub.1 A.sub.2 X analogs inhibit the farnesylation of Ras. Furthermore, these CA.sub.1 A.sub.2 X analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they have a prolyl like moiety in the A.sub.1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: November 5, 1996Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Samuel L. Graham
-
Patent number: 5559128Abstract: The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: April 18, 1995Date of Patent: September 24, 1996Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Ravi Nargund, Robert W. Marquis, Arthur A. Patchett, Lihu Yang
-
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: 5492916Abstract: The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
-
Patent number: 5457114Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.Type: GrantFiled: January 25, 1994Date of Patent: October 10, 1995Assignee: Behringwerke AktiengesellschaftInventors: Werner Stuber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
-
Patent number: 5385902Abstract: Antimicrobial compounds of the formula ##STR1## wherein A is selected from the group consisting of alkyl; phenyl; alkoxy; phenoxy; benzyloxy; monoalkylamino; dialkylamino; cyclic amino, anilino; heterocyclic; amino substituted with heterocyclic ring, methods of making and using said compounds, and compositions comprising said compounds are disclosed.Type: GrantFiled: September 1, 1993Date of Patent: January 31, 1995Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
-
Patent number: 5382590Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.Type: GrantFiled: July 8, 1992Date of Patent: January 17, 1995Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
-
Patent number: 5364924Abstract: Diamino ureas having the formula ##STR1## wherein each ring is saturated and includes 3-5 carbon atoms and n alkyl substituents R of 1-4 carbon atoms each and n for each ring is 1-4, a method of using these materials as chain extending agents in the manufacture of poly(urethane/urea)s or polyureas, and polymers having at least one constituent unit derived from such diamino ureas are claimed.Type: GrantFiled: March 31, 1993Date of Patent: November 15, 1994Assignee: OSi Specialties Inc.Inventors: Richard M. Gerkin, Forest A. Richey, Jr.
-
Patent number: 5340801Abstract: This invention relates to N-arylcarbamoyl proline analogues which are useful as cholecystokinin and gastrin antagonists, to pharmaceutical compositions including such proline analogues, and to their use in preventing or treating cholecystokinin or gastrin related disorders.Type: GrantFiled: May 8, 1991Date of Patent: August 23, 1994Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: William R. Ewing, Bruce F. Molino
-
Patent number: 5274098Abstract: Amidinophenylalanine derivatives, a process for their preparation, their use and pharmaceutical compositions which contain these compounds are described.Type: GrantFiled: April 7, 1992Date of Patent: December 28, 1993Assignee: Behringwerke AktiengesellschaftInventors: StuWerner, Gerhard Dickneite
-
Patent number: 5248673Abstract: The present invention provides new thrombin inhibiting bisamidines derivatives, their pharmaceutically acceptable salts and hydrates, methods for their preparation, pharmaceutical composition, a process for their preparation, and use of the compounds in treatment of thrombosis, ischemia and stroke.Type: GrantFiled: December 23, 1992Date of Patent: September 28, 1993Assignee: Bristol-Myers Squibb Co.Inventors: Neelakantan Balasubramanian, William T. Han
-
Patent number: 5232920Abstract: Novel N-(mercaptoalkyl)amides of the formula ##STR1## wherein R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 is (COR.sub.3)-aryl, heteroaryl, substituted (COR.sub.3)-aryl or substituted heteroaryl, wherein the substituents are 1-3 substituents selected from the group consisting of carboxy, alkoxycarbonyl, lower alkyl, hydroxy, halo, lower alkoxy, cyclolower alkyl, cyano, trifluoromethyl, phenyl, phenoxy and phenylthio;R.sub.3 is --OR.sub.4 or --NR.sub.4 R.sub.5 ;R.sub.4 and R.sub.5 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;Q is hydrogen or R.sub.6 CO--;R.sub.Type: GrantFiled: December 21, 1990Date of Patent: August 3, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
-
Patent number: 5196439Abstract: A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.Type: GrantFiled: January 24, 1992Date of Patent: March 23, 1993Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizo Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu, Kohshi Ueno, Masuhiro Ikeda
-
Patent number: 5192766Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur; A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.Type: GrantFiled: August 28, 1991Date of Patent: March 9, 1993Assignee: Sankyo Company, LimitedInventors: Norio Nakamura, Nobuyuki Ohkawa, Takeshi Oshima, Masaaki Miyamoto, Yasuteru Iijima
-
Patent number: 5166153Abstract: Novel N-acylated 2-[4-(halophenoxy)-phenoxy]-ethylcarbamic acid esters of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.5 alkenyl,R.sub.2 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, --CO--R.sub.7 or --NR.sub.8 R.sub.9,R.sub.3 and R.sub.4 independently of one another are hydrogen or methyl,R.sub.5 is chlorine or fluorine,R.sub.6 is either the same substituent as R.sub.5 or is hydrogen,R.sub.7 is C.sub.1 -C.sub.8 alkoxy or --NR.sub.10 R.sub.11,R.sub.8 is C.sub.1 -C.sub.4 alkyl,R.sub.9 is C.sub.1 -C.sub.4 alkyl orR.sub.8 and R.sub.9 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --,R.sub.10 is hydrogen or C.sub.1 -C.sub.4 alkyl andR.sub.11 is hydrogen or C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or phenyl substituted by halogen or by methyl, orR.sub.10 and R.sub.11 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.Type: GrantFiled: April 24, 1990Date of Patent: November 24, 1992Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
-
Patent number: 5142044Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structure formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## or ##STR3## wherein R" is H or halogen.Type: GrantFiled: January 22, 1990Date of Patent: August 25, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
-
Patent number: 5135926Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p - or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p - (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: April 26, 1991Date of Patent: August 4, 1992Inventor: Nicholas S. Bodor