Ring Nitrogen In The Polycyclo Ring System Patents (Class 544/80)
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Patent number: 6949521Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2?-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: May 4, 2001Date of Patent: September 27, 2005Assignees: The University of Georgia Research Foundation, Inc., Emory UniversityInventors: Chung K. Chu, Lakshmi P. Kotra, Konstantine Manouilov, Jinfa Du, Raymond Schinazi
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Publication number: 20040106596Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: November 25, 2003Publication date: June 3, 2004Inventor: William R. Perrault
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Patent number: 6653307Abstract: The present invention provides compounds of formula I which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 5, 2001Date of Patent: November 25, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Mark E. Schnute
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Patent number: 6613772Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.Type: GrantFiled: June 16, 2000Date of Patent: September 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel, Peter Schindler
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Publication number: 20030130255Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: December 19, 2002Publication date: July 10, 2003Inventors: Joseph Walter Strohbach, Steven P. Tanis, Malcolm Wilson Moon, William R. Perrault
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Patent number: 6583146Abstract: Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.Type: GrantFiled: July 12, 2001Date of Patent: June 24, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Patent number: 6579885Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.Type: GrantFiled: March 6, 2002Date of Patent: June 17, 2003Assignee: Albany Molecular Research, Inc.Inventors: James P. Beck, Matt A. Curry, Mark A. Smith
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Patent number: 6559143Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: GrantFiled: October 16, 2000Date of Patent: May 6, 2003Assignee: AstraZeneca ABInventors: Annika Björe, Magnus Björsne, Kurt-Jürgen Hoffmann, Fritiof Pontén, Gert Strandlund, Peder Svensson, Michael Wilsterman
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Patent number: 6506762Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: September 29, 2000Date of Patent: January 14, 2003Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 6479499Abstract: Two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines, such as epidermoid carcinoma of the nasopharynx (KB), lung carcinoma (A-549), ileocecal carcinoma (HCT-8), breast cancer (MCF-7), melanoma (SKMEL-2), ovarian cancer (1A9), glioblastoma (U-87-MG), bone (HOS), P-gp-expressing epidermoid carcinoma of the nasopharynx (KB-VIN), and prostate cancer (PC3) cell lines, and some of the compounds are found potent. The present invention also synthesizes 2-phenyl-4-alkoxy-quinazoline compounds, wherein some of the compounds exhibit antiplatelet activity.Type: GrantFiled: June 28, 2000Date of Patent: November 12, 2002Assignee: National Science CouncilInventors: Sheng-Chu Kuo, Mann-Jen Hour, Li-Jiau Huang, Kuo-Hsiung Lee
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Patent number: 6407103Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: December 6, 2000Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: David A. Nugiel, David J. Carini, Susan V. Di Meo, Eddy W. Yue
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Patent number: 6271212Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: March 3, 1998Date of Patent: August 7, 2001Assignees: University of Georgia Research Foundation Inc., Emory UniversityInventors: Chung K. Chu, Lakshimi Kotra, Kostantine K. Manouilov, Jinfa Du, Raymond Schinazi
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Patent number: 6124306Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: September 21, 1998Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
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Patent number: 5948784Abstract: Disclosed are quinazoline derivatives represented by formula (I): wherein R.sup.1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R.sup.10 represents hydrogen, lower alkyl, or the like; R.sup.11 and R.sup.12 represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R.sup.11 and R.sup.12 are combined together with N to form a heterocyclic group; and n represents 0, 1 or 2, and pharmaceutically acceptable salts thereof. These compounds have adenosine uptake inhibitory activity and are useful for the protection of myocardium and for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.Type: GrantFiled: June 3, 1998Date of Patent: September 7, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Yuko Okamura, Haruki Takai, Hiromi Nonaka, Takahiro Moriyama, Kozo Yao, Akira Karasawa
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Patent number: 5880125Abstract: The present invention is directed to certain novel compounds identified as 4-spiroindoline piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, R.sup.8, and A 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: March 18, 1997Date of Patent: March 9, 1999Assignee: Merck & Co., Inc.Inventor: Ravi Nargund
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Patent number: 5744602Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and X are variables; andW is phenyl optionally substituted with straight or branched chain lower alkyl having 1-6 carbon atoms or straight or branched chain lower alkoxy having 1-6 carbon atoms.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: May 15, 1995Date of Patent: April 28, 1998Assignee: Neurogen CorporationInventors: Philip Whitcome, Kenneth Shaw
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Patent number: 5616537Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.Type: GrantFiled: March 1, 1994Date of Patent: April 1, 1997Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
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Patent number: 5478825Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.Type: GrantFiled: June 15, 1994Date of Patent: December 26, 1995Assignee: Egis GyogyszergyarInventors: Jozsef Reiter, Gabor Berecz, Gizella Zsila, Lujza Pet cz, Gabor Gigler, Marton Fekete, Maria Szecsey nee Heged s, Enik Szirt nee Kiszelly, Ludmila Rohacs nee Zamkovaja, Frigyes Gorgenyi, Margit Csorg
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Patent number: 5330987Abstract: Novel substituted pyridopyrimidinones of formula (I), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: June 4, 1992Date of Patent: July 19, 1994Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, Prasun K. Chakravarty, Stephen E. de Laszlo, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5326744Abstract: Glycol aldehyde and lactic acid derivatives and their sulfur analogs of the formula I ##STR1## where R.sup.1 to R.sup.3 have the meanings given in the specification, X is oxygen, sulfur or a single bond, and Y is a C.sub.2 -C.sub.4 -alkylene or C.sub.2 -C.sub.4 -alkenylene chain where in each case a methylene group may be substituted by an oxo group (.dbd.O), environmentally compatible salts of the compounds I, methods of preparing the compounds I, and their use as herbicides.Type: GrantFiled: December 21, 1992Date of Patent: July 5, 1994Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Ernst Baumann, Uwe J. Vogelbacher, Thomas Saupe, Matthias Bratz, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Uwe Kardorff
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Patent number: 5250533Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
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Patent number: 5250530Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.Type: GrantFiled: July 9, 1990Date of Patent: October 5, 1993Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke
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Patent number: 5223505Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: April 20, 1990Date of Patent: June 29, 1993Assignee: Imperial Chemical Industries PlcInventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
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Patent number: 5175287Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.Type: GrantFiled: September 18, 1989Date of Patent: December 29, 1992Assignee: S R I InternationalInventors: William W. Lee, J. Martin Brown, Edward W. Grange, Abelardo P. Martinez, Michael Tracy, Daniel J. Pollart
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Patent number: 5166344Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.Type: GrantFiled: September 19, 1991Date of Patent: November 24, 1992Assignee: Berlex Laboratories, Inc.Inventor: David D. Davey
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Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
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Patent number: 5130430Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent organic or inorganic substituents; X represents hydrogen, halogen, hydroxy or amino and W represents phenyl, thienyl or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABA a brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: October 31, 1990Date of Patent: July 14, 1992Assignee: Neurogen CorporationInventor: Kenneth Shaw
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Patent number: 5106847Abstract: The present invention is directed a new group of indole derivatives that are NMDA antagonists.Type: GrantFiled: August 1, 1991Date of Patent: April 21, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Francesco G. Salituro, Bruce M. Baron
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Patent number: 5071996Abstract: Novel hydroxy-benzoheterocyclic-substituted 3-oxopentane derivatives are produced by reaction of a hydroxy-containing ortho-phenylene amine compound and the source of a five-carbon keto-containing moiety selected from 4-oxoheptanedioic acid compounds or 1,6-dioxa[4.4]spirodilactones. The derivatives produced from hydroxy-phenylenediamines are further reacted to produce compounds of higher cyclic functionality.Type: GrantFiled: October 26, 1990Date of Patent: December 10, 1991Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5071888Abstract: Photopolymerizable prepolymer compositions are provided comprising an unsaturated compound having at least one ethylenic double bond that is photopolymerizable to form a polymer, and a photoinitiator having one of the formulae: ##STR1##Type: GrantFiled: July 8, 1985Date of Patent: December 10, 1991Assignee: Asahi Denka Kogyo K.K.Inventor: Naohiro Kubota
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Patent number: 5064833Abstract: 2,4-diaminoquinazoline compounds are inhibitors of the H.sup.+ K.sup.+ ATPase enzyme and useful for the treatment of diseases of the stomach based on excessive gastric acid secretion. A compound of the invention is 2-[2-methyl-4-fluorophenyl)amino]-4-(N-methylphenylamino)quinazoline.Type: GrantFiled: May 8, 1990Date of Patent: November 12, 1991Assignee: Smithkline Beecham Intercredit B.V.Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach, David J. Keeling
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Patent number: 5055465Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.Type: GrantFiled: May 31, 1989Date of Patent: October 8, 1991Assignee: Berlex Laboratories, Inc.Inventor: David D. Davey
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Patent number: 5004813Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: August 24, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4970308Abstract: Chromogenic di-[bis-(indolyl)ethylenyl] tetrahalophthalides are disclosed of the formula ##STR1## wherein each X.sup.1, X.sup.2, X.sup.3, and X.sup.4 is independently selected from chlorine or bromine;wherein each of R.sup.1 and R.sup.7 is independently selected from cycloalkyl, aralkyl, alkoxyalkyl, or aroxyalkyl;wherein each of R.sup.2 and R.sup.8 is independently selected from alkyl (C.sub.1 -C.sub.8) or aryl (substituted or unsubstituted);wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 is independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, aryl (substituted or unsubstituted), halogen, alkoxy (C.sub.1 -C.sub.8), aroxy, cycloalkoxy, dialkylamino including symmetrical and unsymmetrical (C.sub.1 -C.sub.Type: GrantFiled: August 23, 1989Date of Patent: November 13, 1990Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 4968797Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 30, 1987Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
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Patent number: 4960784Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.Type: GrantFiled: October 2, 1989Date of Patent: October 2, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: George P. Lahm
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Patent number: 4950668Abstract: A novel pyrazole derivative and an insecticidal or miticidal composition containing the derivative as the effective ingredient are disclosed.The pyrazole derivative of the present invention has an excellent controlling effect also against harmful insects and mites exhibiting resistance to conventional insecticides and does not disturb the ecosystem since it is less toxic and less residual.Type: GrantFiled: April 14, 1988Date of Patent: August 21, 1990Assignee: Mitsubishi Kasei CorporationInventors: Itaru Okada, Shuko Okui, Yoji Takahashi, Toshiki Fukuchi
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Patent number: 4939140Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.Type: GrantFiled: October 27, 1988Date of Patent: July 3, 1990Assignee: Pfizer Inc.Inventors: Eric R. Larson, Banavara L. Mylari
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Patent number: 4933447Abstract: A quinoline derivative represented by the following formula is disclosed. ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group which may contain a substituent and R.sub.2 represents an alkyl group which may contain a substituent, or R.sub.1 and R.sub.2 in combination with each other and with the adjacent nitrogen atom from a ring which may contain a nitrogen atom other than said adjacent nitrogen atom, an oxygen atom, or a substituent, and R.sub.3 represents a cyano group, a carbamoyl group, or a lower alkoxycarbonyl group. The compound exhibits superior cardiotonic activity and vasodilative activity, and thus is effective as a medicine.Type: GrantFiled: September 16, 1988Date of Patent: June 12, 1990Assignee: SS Pharmaceutical Co., Ltd.Inventors: Fujiko Koono, Norimitsu Umehara, Hideaki Matsuda, Tatsuhiko Katori
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Patent number: 4933338Abstract: Benzimidazole-2-sulfonamide and imidazopyridine-2-sulfonamide derivatives corresponding to the general formula I: ##STR1## and their pharmaceutically acceptable salts, especially those of the formula in which:Z.sup.1 to Z.sup.4 represent a nitrogen atom or a substituted or unsubstituted carbon atom;R.sup.1 and R.sup.2 represent a hydrogen atom or an alkyl, alkylaryl, alkylcarbonylalkyl, alkylcarbonylaryl, alkylcarbonylheteroaryl, cycloalkyl, carboxyalkyl, acyl or nitro radical, or alternativelyR.sup.1 and R.sup.2 can together form a linkage represented by a group X;R.sup.Type: GrantFiled: April 15, 1987Date of Patent: June 12, 1990Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Jordi F. Constansa, Juan P. Corominas, Agusto C. Pinol
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Patent number: 4912107Abstract: The invention concerns new pyrrolocarbazole derivatives of formula ##STR1## processes for their preparation, as well as medicaments containing these for the inhibition of protein kinases, such as protein kinase C, and thus for the prevention and/or treatment of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertension, of inflammatory processes, allergies, cancers, and certain degenerative damages of the central nervous system as well as for the treatment of viral diseases.Type: GrantFiled: September 26, 1989Date of Patent: March 27, 1990Assignee: Goedecke AktiengesellschaftInventors: Jurgen Kleinschroth, Johannes Hartenstein, Christoph Schachtele, Claus Rudolph, David J. Dooley, Gunther Weinheimer
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Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4897105Abstract: A compound of the general formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted, R.sub.2 and R.sub.3 respectively are a lower alkyl or lower alkoxy group, Z is CH or N and n is 0 or 1, or a salt thereof which is useful as a herbicide.Type: GrantFiled: March 20, 1987Date of Patent: January 30, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshiyuki Okada, Isao Aoki, Nobuyuki Okajima, Takashi Kuragano
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Patent number: 4876357Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: October 26, 1987Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4874759Abstract: Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.Type: GrantFiled: September 23, 1988Date of Patent: October 17, 1989Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Tsuguo Ikebe, Ichiro Hakamada, Osamu Yaoka
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Patent number: 4871734Abstract: Thienoimidazole-toluidines of the formula I ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, and R.sup.1 to R.sup.9 have the meanings stated in the description, and a process for their preparation, pharmaceutical compositions containing them, and their use as inhibitors of gastric acid secretion, are described.Type: GrantFiled: November 20, 1987Date of Patent: October 3, 1989Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Manfred Rosner, Weidmann, Klaus, Robert Rippel, Andreas W. Herling
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Patent number: 4870072Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is ##STR2## or ##STR3## and R.sub.2, R.sub.3 and R.sub.4 are as defined herein.Type: GrantFiled: January 19, 1988Date of Patent: September 26, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4861777Abstract: A novel pyrazole derivative and an insecticidal or miticidal composition containing the derivative as the effective ingredient are disclosed.The pyrazole derivative of the present invention has an excellent controlling effect also against harmful insects and mites exhibiting resistance to conventional insecticides and does not disturb the ecosystem since it is less toxic and less residual.Type: GrantFiled: September 7, 1988Date of Patent: August 29, 1989Assignee: Mitsubishi Kasei CorporationInventors: Itaru Okada, Shuko Okui, Mana Nishimata, Yoji Takahashi, Toshiki Fukuchi
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Patent number: 4851409Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: February 5, 1987Date of Patent: July 25, 1989Assignee: Merck Frosst Canada Inc.Inventors: Robert N. Young, Robert Zamboni, Serge Leger