Plural Hetero Atoms In The Additional Hetero Ring Patents (Class 540/603)
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Patent number: 6562964Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.Type: GrantFiled: January 23, 2002Date of Patent: May 13, 2003Assignee: Pfizer IncInventors: Mark Ian Kemp, Michael John Palmer, Mark Allen Sanner, Martin James Wythes
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Publication number: 20030078252Abstract: The invention provides compounds of formula 1 1Type: ApplicationFiled: May 13, 2002Publication date: April 24, 2003Applicant: Pfizer Inc.Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
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Patent number: 6512112Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: January 28, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Publication number: 20030018022Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.Type: ApplicationFiled: May 22, 2002Publication date: January 23, 2003Applicant: Tularik Inc.Inventors: Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
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Patent number: 6500817Abstract: The present invention relates to thiazolylurea derivatives, a process for their preparation, and their use as pharmaceuticals, in particular as antiviral pharmaceuticals.Type: GrantFiled: August 31, 2001Date of Patent: December 31, 2002Assignee: Bayer AktiengesellschaftInventors: Rüdiger Fischer, Gerald Kleymann, Judith Baumeister, Wolfgang Bender, Ulrich Betz, Peter Eckenberg, Gabriele Handke, Martin Hendrix, Udo Schneider, Olaf Weber, Kerstin Henninger, Axel Jensen, Jörg Keldenich
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Patent number: 6495568Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: December 17, 2002Assignee: Warner-Lambert CompanyInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6472416Abstract: The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.Type: GrantFiled: August 25, 2000Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Teodozyj Kolasa, Meena V. Patel
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Patent number: 6465395Abstract: The present invention provides thiochroman- and dihydrobenzothiophene-substituted methylene compounds of formula I. Further provided are compositions and methods utilizing said formula I compounds for the control of undesirable plant species.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignees: BASF Aktiengesellschaft, Idemitsu Kosan Company, Ltd.Inventors: Stephen S. Szucs, Kun-Jian Gu
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Publication number: 20020137740Abstract: The subject of the invention is the compounds of formula: 1Type: ApplicationFiled: November 15, 2001Publication date: September 26, 2002Inventors: Evelyne Fontaine, Danielle Gully, Pierre Roger, Camille Georges Wermuth
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Publication number: 20020119963Abstract: The invention provides compounds of formula 1 1Type: ApplicationFiled: July 31, 2001Publication date: August 29, 2002Inventors: Mark A. Sanner, Chris J. Helal, Christoper B. Cooper, Frank S. Menniti, Michael K. Ahlijanian, Anabella Villalobos, Lit-Fui Lau, Patricia A. Seymour
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Publication number: 20020103185Abstract: The invention provides compounds of formula 1 1Type: ApplicationFiled: August 28, 2001Publication date: August 1, 2002Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper, Travis T. Wager
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Publication number: 20020099217Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I 1Type: ApplicationFiled: March 18, 2002Publication date: July 25, 2002Inventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Mark E. Salvati, Joseph E. Sundeen, Hai-Yun Xiao, Rulin Zhao
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Patent number: 6420395Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.Type: GrantFiled: November 29, 1999Date of Patent: July 16, 2002Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
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Publication number: 20020082253Abstract: Fibrinogen receptor antagonists of the formula: 1Type: ApplicationFiled: July 13, 2001Publication date: June 27, 2002Inventors: John Wityak, Prabhakar K. Jadhav
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Publication number: 20020077483Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) 1Type: ApplicationFiled: May 22, 2001Publication date: June 20, 2002Inventors: Yijun Deng, Dennis Hlasta
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6384219Abstract: There is disclosed a 1H-pyrrolo-[1,2-b][1,2,4]triazole compound represented by formula (I): wherein R is an alkyl group; R1, R2, R3, R1′, R2′, and R3′ each are a hydrogen atom or an alkyl group; R1 and R2, and R1′ and R2′ may bond together to form a ring, respectively; R4 is a hydrogen atom or an alkyl group, and X is heterocyclic group, a substituted amino group, or an aryl group. The compound is useful as a photographic cyan coupler. There is also disclosed synthetic intermediates of the compound and a production method of the intermediates.Type: GrantFiled: January 7, 1998Date of Patent: May 7, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Yasuhiro Shimada, Hideki Maeta, Yoshio Shimura
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Publication number: 20020049316Abstract: The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.Type: ApplicationFiled: December 17, 2001Publication date: April 25, 2002Inventors: Stacie Marie Halbert, Evelyne Michaud, Scott Kevin Thompson, Daniel Frank Veber
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Patent number: 6372736Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.Type: GrantFiled: July 21, 1999Date of Patent: April 16, 2002Assignee: Pfizer INCInventors: Mark Ian Kemp, Michael John Palmer, Mark Allen Sanner, Martin James Wythes
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Patent number: 6365584Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.Type: GrantFiled: September 21, 2000Date of Patent: April 2, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
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Patent number: 6358978Abstract: Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NF&kgr;B is involved.Type: GrantFiled: June 22, 2000Date of Patent: March 19, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Olaf Ritzeler, Hans Ulrich Stilz, Bernhard Neises, William Jerome Bock, Jr., Armin Walser, Gary A. Flynn, Jörg Habermann, Gerhard Jähne
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Patent number: 6358942Abstract: A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR1; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are independently H or halo; R5 is H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.Type: GrantFiled: November 15, 2000Date of Patent: March 19, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel
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Patent number: 6352981Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2 (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: October 27, 2000Date of Patent: March 5, 2002Assignee: BASF AktiengesellschaftInventors: Hans-Jörg Treiber, Stefan Blank, Dorothea Starck, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 6329528Abstract: New synthetic procedures for preparing insecticidal 3-(substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazoles utilizing thioimidate intermediate.Type: GrantFiled: October 22, 1999Date of Patent: December 11, 2001Assignee: Dow AgroSciences LLCInventors: Mary L. Ash, Mark W. Zettler, Norman R. Pearson, Duane R. Romer, John W. Hull, Jr., David E. Podhorez
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Patent number: 6306880Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted; Ar2 represents a phenyl group which may be substituted; R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represnet a hydrogen atom or an unsubstituted or halo substituted alkyl; n represnets 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic, not including 1,3-dioxan-5-yl. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 23, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Patent number: 6291450Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 7, 2000Date of Patent: September 18, 2001Assignee: Amgen Inc.Inventors: Kevin Koch, Andreas Termin, John A. Josey
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Publication number: 20010020100Abstract: A class of N-substituted-1,2,4-triazolone compounds is described for use in treatment of cardiovascular disorders.Type: ApplicationFiled: December 20, 2000Publication date: September 6, 2001Applicant: G.D. Searle & Co.Inventors: Robert E. Manning, David B. Reitz, Horn-Chih Huang
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Patent number: 6211214Abstract: The present invention relates to novel biphenyl ether-oxazolines of the formula (I) in which X, Y, Z, R1, R2, A, m and n have the meaning given in the description, to processes for their preparation and to their use for controlling animal pests, and two novel intermediate products.Type: GrantFiled: May 12, 1998Date of Patent: April 3, 2001Assignee: Bayer AktiengesellschaftInventors: Wolfgang Krämer, Udo Kraatz, Christoph Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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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
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6133291Abstract: The present invention discloses novel N(imidazolylalkyl)-substituted cyclic amine compounds which have excellent histamine-H.sub.3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat allergy, inflammatory and CNS-related diseases.Type: GrantFiled: October 16, 1998Date of Patent: October 17, 2000Assignee: Schering CorporationInventors: Ronald Wolin, Stuart B. Rosenblum, Adriano Afonso
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Patent number: 6124330Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: April 29, 1999Date of Patent: September 26, 2000Assignee: Janssen-Cilag S.A.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 6121300Abstract: The present invention relates to compositions and methods for reversing advanced glycosylation end product-mediated cross-linking and protein aging. Accordingly, compositions are described which comprise thiazolium compounds substituted with heterocyclic groups which are capable of reversing the formation of advanced glycosylation end product cross-links. Both industrial and therapeutic applications for the invention are disclosed, as food spoilage and animal protein aging can be treated. Such compounds have particular application in the treatment of protein aging such as is responsible for the complications of aging and diabetes.Type: GrantFiled: November 10, 1998Date of Patent: September 19, 2000Inventors: Dilip R. Wagle, Sheng-Ding Fang, Taikyun Rho, John J. Egan, Sara Vasan, Peter Ulrich, Anthony Cerami
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Patent number: 6114329Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of a linear, cyclic or bicyclic, aromatic or aliphatic moiety containing a nitrogen atom;and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: January 26, 1998Date of Patent: September 5, 2000Assignee: SmithKline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 6110939Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --; .dbd.Q is .dbd.O or .dbd.NR.sup.3 ; R.sup.1 is Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl wherein the C.sub.1-6 alkyl group is optionally substituted; R.sup.2 is Ar.sup.2, Ar.sup.2 C.sub.1-6 alkyl, Het or HetC.sub.1-6 alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B) Ar.sup.1 is optionally substituted phenyl Ar.sup.2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 19, 1998Date of Patent: August 29, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Fran.cedilla.ois Maria Sommen, Dominique Louis Nester Ghislaine Surleraux, Joseph Elisabeth Leenaerts
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Patent number: 6100279Abstract: Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.Type: GrantFiled: November 5, 1998Date of Patent: August 8, 2000Assignee: Schering CorporationInventors: Wayne D. Vaccaro, Ronald L. Wolin, Daniel M. Solomon, Robert G. Aslanian, John J. Piwinski, Stuart B. Rosenblum
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Patent number: 6096746Abstract: An indazole compound having a piperazinyl moiety in the structure thereof, which is a 5-HT.sub.4 receptor agonist which is useful in the treatment of digestive tract disorders.Type: GrantFiled: March 23, 1999Date of Patent: August 1, 2000Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Masashi Suzuki, Masahiro Ueno, Ryuta Fukutomi, Hiroaki Satoh, Haruhiko Kikuchi, Koichiro Hagihara, Takeo Arai, Sugure Taniguchi, Setsuko Mino, Yumiko Noguchi
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Patent number: 6090804Abstract: Thiophene derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof. Said compounds act as an anti-PCP agonist and therefore are useful as psychotropic or antischizophrenic agents and so on. ##STR1## (In the above formula, R.sub.1 is a formula --A.sub.1 --X.sub.1 --R.sub.3 ; R.sub.2 is a formula --A.sub.2 --X.sub.2 --R.sub.4 or does not exist; B ring is a 7- to 10-membered nitrogen-containing cycloalkyl ring; Ar ring is an aryl or heteroaryl ring; A.sub.1, A.sub.2 and A.sub.3 may be the same or different from one another and each represents a bond or a lower alkylene group; X.sub.1 and X.sub.2 may be the same or different from each other and each represents a bond or a formula --O--, --S--or the like; R.sub.3 and R.sub.Type: GrantFiled: December 30, 1998Date of Patent: July 18, 2000Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Takenori Kimura, Takeshi Murakami, Junya Ohmori, Takuma Morita, Shin-ichi Tsukamoto
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Patent number: 6037342Abstract: This invention provides a serotonin 5-HT.sub.3 receptor partial activator which has a serotonin 5-HT.sub.3 receptor activating action, in addition to its serotonin 5-HT.sub.3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT.sub.3 receptor antagonism and serotonin 5-HT.sub.3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT.sub.3 receptor partial activators. ##STR1## In the above formula, R.sub.1 to R.sub.4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R.sub.1 and R.sub.2 may be linked together to form a ring structure, namely benzene ring; R.sub.Type: GrantFiled: May 6, 1997Date of Patent: March 14, 2000Assignees: Meiji Seika Kaisha, Ltd, Koichi ShudoInventors: Yasuo Sato, Megumi Yamada, Kazuko Kobayashi, Katsuyoshi Iwamatsu, Fukio Konno, Koichi Shudo
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6015813Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 8, 1998Date of Patent: January 18, 2000Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Per Sauerberg
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Patent number: 5968962Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.Type: GrantFiled: August 13, 1996Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
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Patent number: 5942532Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5925661Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.Type: GrantFiled: November 24, 1997Date of Patent: July 20, 1999Assignee: SANOFIInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5874586Abstract: Herbicidally active 1-aryl-4-carbamoyl-tetrazolinones of the formula (I) ##STR1## in which Ar represents optionally substituted aryl,R.sup.1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or alkoxy, andR.sup.2 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or, together with R.sup.1, represents alkanediyl,are obtained in good yields and at high purity by reacting 1-aryl-tetrazolinones of the formula (II) with phosgene in the presence of a diluent at temperatures of between 0.degree. C. and 150.degree. C. ("first process step"), and reacting the resulting (novel) 1-aryl-4-chlorocarbonyl-tetrazolinones of the formula (III) with amines of the formula (IV) in the presence of a diluent, and, where appropriate, in the presence of a further basic compound, at temperatures of between -20.degree. C. and +100.degree. C.Type: GrantFiled: February 4, 1998Date of Patent: February 23, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Uwe Stelzer, Carl Casser
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Patent number: 5869481Abstract: Compounds having anticonsulive activity, of the formula 1 ##STR1## in which X is hydrogen, a C.sub.1-4 -alkyl, C.sub.1-4 alkoxy, trifluoromethyl, or halogen residue, R.sup.1 and R.sup.2 are independently of each other C.sub.1-4 -alkyl, C.sub.2-4 hydroxyalkyl, cycloalkyl or heteroalkyl, or R.sup.1 and R.sup.2 are together a C.sub.2-6 alkylene reside in which a--CH.sub.2 --group is optionally replaced by oxygen, nitrogen or sulfur, m is 0 or 1, and n is 0 or a cardinal number from 1 to 5, and their pharmaceutically acceptable salts. The application also relates to a process for making the compound of formula (I).Type: GrantFiled: June 9, 1998Date of Patent: February 9, 1999Assignee: Arzneitmittelwerk Dresden G.m.b.H.Inventors: Hans-Joachim Lankau, Manfred Menzer, Klaus Unverferth, Karl Gewald, Harry Schafer, deceased
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Patent number: 5854234Abstract: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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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