Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Adrenochrome, Etc.) Patents (Class 548/512)
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Patent number: 7060843Abstract: Electroluminescent device comprising in this order (a) an anode (b) a hole transporting layer (c) a light-emitting layer (d) optionally an electron transporting layer and (e) a cathode and a light-emitting substance, wherein the light-emitting substance is a diketopyrrolopyrrole represented by formula I or formula III processes for the preparation of compounds I, its uses and compositions comprising the compounds I and/or III.Type: GrantFiled: September 8, 2000Date of Patent: June 13, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Junji Otani, Hiroshi Yamamoto, Norihisa Dan, Abul Iqbal, Robert Moretti
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Patent number: 7005439Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: June 14, 2001Date of Patent: February 28, 2006Assignee: AstraZeneca ABInventors: Tomas Eriksson, Krister Henriksson
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Patent number: 6900322Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.Type: GrantFiled: May 10, 1999Date of Patent: May 31, 2005Assignee: Solvay Pharmaceuticals GmbHInventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
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Patent number: 6878738Abstract: The present invention relates to compounds of the formula I in which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8 and R9, together with the carbon atom to which they are bonded, are a carbonyl group and the radicals R1 to R7 have the meanings indicated in the description. The compounds inhibit the release of various mediators of the arachidonic acid cascade and can thus be used for the prevention of allergically induced disorders or for the treatment of disorders of the rheumatic type.Type: GrantFiled: November 23, 1999Date of Patent: April 12, 2005Assignee: Merckle GmbHInventors: Stefan Laufer, Karola Tollmann, Hans-Guenter Striegel
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Publication number: 20040180235Abstract: The present invention relates to fluorescent diketopyrrolopyrroles (“DPPs”) of Formula (I), wherein A1 and A2 independently from each other stand for (II) wherein R1, R2 and R5 to R11 are as defined in claim 1, a process for their preparation and their use for the preparation of inks, colorants, pigmented plastics for coating, non-impact-printing material, color filters, cosmetics, or for the preparation of polymeric ink particles, toners, dye lasers and electroluminescent devices. The fluorescent diketopyrrolopyrroles (“DPPs”) of Formula (I) exhibit a high lightfastness, a high heat stability, especially in plastics. A luminescent device comprising a DPP compound of Formula (I) is high in the efficiency of electrical energy utilisation, high in luminance and high in colour purity.Type: ApplicationFiled: December 22, 2003Publication date: September 16, 2004Inventors: Hiroshi Yamamoto, Norihisa Dan, Olof Wallquist
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Patent number: 6482957Abstract: A cyclopentenecarboxamide derivative represented by the formula (I): and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): and a method for preparing the bicycloamide derivative.Type: GrantFiled: April 25, 2002Date of Patent: November 19, 2002Assignee: Kuraray Co., Ltd.Inventors: Nobuya Katagiri, Chikara Kaneko, Junko Sato, Masahiro Torihara, Koichi Kanehira, Yoshin Tamai
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Patent number: 6395766Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.Type: GrantFiled: November 6, 2000Date of Patent: May 28, 2002Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
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Patent number: 6355668Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects A bicyclolactam derivative represented by the following formula (1) is also disclosed, and is useful as an effective component of an anxiolytic agentType: GrantFiled: August 28, 2000Date of Patent: March 12, 2002Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
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Patent number: 6353109Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 1, 1998Date of Patent: March 5, 2002Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Publication number: 20020015938Abstract: The invention relates to a method of simultaneous high-throughput preformulation quantification of potential drug candidates, where an aliquot of a mixture of solutions containing different compounds is injected into a high pressure liquid chromatograph. The concentration of each compound can be determined by high pressure liquid chromatographic analysis, and correlated to a physico-chemical property of the compound.Type: ApplicationFiled: October 29, 1998Publication date: February 7, 2002Inventor: NARMADA SHENOY
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Publication number: 20020010085Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1Type: ApplicationFiled: March 6, 2001Publication date: January 24, 2002Inventor: Peter Herold
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Patent number: 6316486Abstract: The present invention relates to new compounds of the formula (I) in which X represents halogen, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that always one of the radicals Y and Z represents halogen while the other represents alkyl, and Het represents one of the groups in which A, B, D and G have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: October 31, 1997Date of Patent: November 13, 2001Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans-Joachim Santel, Alan Graff, Wolfram Andersch, Norbert Mencke, Andreas Turberg
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Patent number: 6291507Abstract: A pharmaceutical composition which comprises a compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1, and wherein A and B form an optionally substituted alkylene chain so as to form a ring with the carbon atoms to which they are attached; X is CH2 or SO2, R1 is an optionally substituted aryl or heteroaryl ring; R2 is a specified organic group such as carboxy, and R3 is hydrogen or a specified organic group; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and are claimed as such.Type: GrantFiled: July 26, 2000Date of Patent: September 18, 2001Assignee: Astrazeneca UK LimitedInventors: Alan W Faull, Andrew J Barker, Jason G Kettle
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Patent number: 6288104Abstract: There is disclosed the use of mesembrine and related compounds (e.g. mesembranol, mesembranone) as scrotonin-uptake inhibitors, pharmaceutical compositions comprising such compounds or dry material or an extract of plants from the Mesembryanthemaceae family (e.g. Sceletium (Aizoaceae) tortuosum) containing a standardized content of said compounds, for use in the treatment of depressive states, psychological or psychiatric disorders with an anxiety component, alcohol and drug dependence, bulimia nervosa and obsessive-compulsive disorders. Also disclosed are new derivatives of mesembrine.Type: GrantFiled: March 22, 1999Date of Patent: September 11, 2001Assignee: African Natural Health CCInventors: Nigel Peter Gericke, Ben-Erik Van Wyk
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Publication number: 20010020035Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: June 1, 1998Publication date: September 6, 2001Inventors: PAMELA ALBAUGH, GANG LIU, ALAN HUTCHISON
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Patent number: 6245919Abstract: A cyclopropylglycine derivative having the following formula: and an intermediate compound for the synthesis of the cyclopropylglycine derivative are novel compounds. The cyclopropylglycine derivative shows a selectivity higher than that of the known agonists to metabotropic L-glutamate receptors, and therefore is a metabotropic type agonist to L-glutamate which has excellent characteristics.Type: GrantFiled: December 28, 1998Date of Patent: June 12, 2001Assignees: Nippon Chemiphar Co., Ltd.Inventors: Haruhiko Shinozaki, Takeo Taguchi, Michiko Ishida
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Patent number: 6232473Abstract: 2-Azabicyclo[2.2.1]hept-5-en-3-one is prepared by a process comprising: continuously mixing a substituted sulfonyl cyanide represented by formula (I): R—SO2CN (I), wherein R represents an alkyl group or a phenyl group or a substituted phenyl group, with cyclopentadiene; and then continuously adding the resultant reaction solution to water or to a mixed solvent comprising water and a hydrocarbon solvent under the condition that the pH of the present reaction mixture ranges from 4 to 7.Type: GrantFiled: May 1, 2000Date of Patent: May 15, 2001Assignee: Kuraray Co., Ltd.Inventors: Takashi Fukumoto, Rensuke Ikarashi
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6211377Abstract: A process for the purification of (±)-2-azabicyclo[2.2.1]hept-5-en-3-one wherein the purification is obtained exclusively by means of extraction procedures.Type: GrantFiled: March 1, 1999Date of Patent: April 3, 2001Assignee: Degussa-Huls AGInventors: Johny de Schrijver, Philippe Otten
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Patent number: 6153765Abstract: A process for producing 2-azabicyclo[2.2.1]hept-5-en-3-one is provided by reacting a sulfonyl cyanide represented by the general formula R--SO.sub.2 CN (in which R represents an alkyl group or a phenyl group which may have a substituent), in the presence of water and in a hydrocarbon solvent at a pH of 4 to 7 inclusive. 2-Azabicyclo[2.2.1]hept-5-en-3-one can be produced in a high yield and a high purity in one step process, with a reduced amount of solvent used, safely and with good productivity. A method of crystallizing 2-azabicyclo[2.2.1]hept-5-en-3-one is also provided, which includes dissolving 2-azabicyclo[2.2.1]hept-5-en-3-one into an organic solvent mainly including at least one of diisopropyl ether and methyl tertiary butyl ether, cooling the solution to deposit crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one. Finely divided particulate crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one excellent in fluidity and handleability can be obtained with a simple procedure and in a high recovery rate.Type: GrantFiled: February 24, 2000Date of Patent: November 28, 2000Assignee: Kuraray Co., Ltd.Inventors: Takashi Fukumoto, Rensuke Ikarashi
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Patent number: 6133305Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: September 25, 1998Date of Patent: October 17, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6121306Abstract: Racemic (.+-.)-1-azobicyclo[2.2.1]heptan-3-one may be efficiently resolved into its (1S,4R)- and (1R,4S)-1-azabicyclo[2.2.1]heptan-3-one isomers by formation of di-p-toluoyl hemitartrate salts by combination with di-p-toluoyl-L-tartaric acid and di-p-toluoyl-D-tartaric acid, respectively. Selective crystallization using one of the di-p-toluoyltartaric acids in less than stoichiometric amount in a suitable solvent mixture allows isolation of the desired isomer as its respective di-p-toluoyl hemitartrate in high isomeric purity. The isolated hemitartrates are storage stable and may be used as such in the preparation of pharmaceuticals and other biologically active compounds, or may be used to provide the free base of the respective 1-azabicyclo[2.2.1]heptan-3-one isomer.Type: GrantFiled: September 29, 1999Date of Patent: September 19, 2000Assignee: Warner-Lambert CompanyInventor: Denis Martin Sobieray
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Patent number: 6107491Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group,Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--,--C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: January 26, 1999Date of Patent: August 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 6096887Abstract: The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## W represents substituted or unsubstituted heteroaryl; X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1,2,3, or 4,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: February 25, 1998Date of Patent: August 1, 2000Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Patent number: 6071908Abstract: A method of treating neoplastic disease wherein a patient in need of such treatment is administered an effective amount of a radiation-activated cytotoxin prodrug (RACP) which has low toxicity, which is reducible by reducing agents generated by the radiolysis of water and which, upon reduction, releases a sufficient amount of a cytotoxic effector of sufficient cytotoxic potency to kill tumor cells. The tumor cells are irradiated with ionizing radiation to reduce the prodrug which is present at the locus of the tumor cells to release the cytotoxic effector.Type: GrantFiled: May 7, 1998Date of Patent: June 6, 2000Assignee: Auckland Uniservices LimitedInventors: William A. Denny, Moena Tercel, William R. Wilson
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Patent number: 6060609Abstract: A process for producing 2-azabicyclo[2.2.1]hept-5-en-3-one is provided by reacting a sulfonyl cyanide represented by the general formula R-SO.sub.2 CN (in which R represents an alkyl group or a phenyl group which may have a substituent), in the presence of water and in a hydrocarbon solvent at a pH of 4 to 7 inclusive. 2-Azabicyclo[2.2.1]hept-5-en-3-one can be produced in a high yield and a high purity in one step process, with a reduced amount of solvent used, safely and with good productivity. A method of crystallizing 2-azabicyclo[2.2.1]hept-5-en-3-one is also provided, which includes dissolving 2-azabicyclo[2.2.1]hept-5-en-3-one into an organic solvent mainly including at least one of diisopropyl ether and methyl tertiary butyl ether, cooling the solution to deposit crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one. Finely divided particulate crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one excellent in fluidity and handleability can be obtained with a simple procedure and in a high recovery rate.Type: GrantFiled: December 28, 1998Date of Patent: May 9, 2000Assignee: Kuraray Co., Ltd.Inventors: Takashi Fukumoto, Rensuke Ikarashi
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Patent number: 6054464Abstract: A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R.sub.4 ; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or fluoro; R.sub.3 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR .sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; R.sub.4 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR.sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ;or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.Type: GrantFiled: March 26, 1999Date of Patent: April 25, 2000Assignee: Astra AktiebolagInventors: John Macor, Edwin Wu
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Patent number: 6037361Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 9, 1998Date of Patent: March 14, 2000Assignee: Warner-Lambert CompanyInventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 5998429Abstract: A compound of formula ##STR1## wherein: A is ##STR2## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C-R.sub.4 ; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or fluoro;R.sub.3 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR.sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; R.sub.4 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR.sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ;or R.sub.2 and R.sub.3 or R.sub.4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.Type: GrantFiled: June 13, 1997Date of Patent: December 7, 1999Assignee: Astra ABInventors: John Macor, Edwin Wu
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Patent number: 5972248Abstract: The present invention relates to novel stabilizers of the formula (I) ##STR1## in which the substituents have the meaning defined in the description. These novel stabilizers are particularly suitable for stabilizing organic material, such as plastics, oils, paints and coatings, against degradation by light, radiation, heat and oxygen.Type: GrantFiled: October 7, 1997Date of Patent: October 26, 1999Assignee: Clariant GmbHInventors: Thomas Stahrfeldt, Josef Wiedemann, Matthias Zah
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Patent number: 5969154Abstract: A liquid crystalline compound of formula ##STR1## wherein B and D are each independently of the other C.sub.6 -C.sub.24 alkyl, ##STR2## L is ##STR3## methyl or C.sub.10 -C.sub.18 alkyl, wherein R.sub.1 is C.sub.4 -C.sub.18 alkyl, with the proviso that when L is methyl, at least one of B and D is C.sub.6 -C.sub.24 alkyl;R2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, cyano or nitro,R3, R4 and R5 are each independently of one another hydrogen, OR6, SR6, SeR6, --NHR6, --NR6R7, ##STR4## with the proviso that at least one of R3, R4 and R5 is not hydrogen, R6 is C.sub.7 -C.sub.37 alkyl, C.sub.7 -C.sub.37 alkylene or C.sub.5 -C.sub.18 alkyl which is interrupted by 1 to 6 hetero atoms selected from the group consisting of O, S and N,R7 is hydrogen or R9,R8 is hydrogen or C.sub.1 -C.sub.4 alkyl, andR9 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkylene or C.sub.3 -C.sub.12 alkyl which is interrupted by 1 to 6 hetero atoms selected from the group consisting of O, S and N.Type: GrantFiled: December 10, 1997Date of Patent: October 19, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, Abul Iqbal, Nancy Tebaldi, Klaus Praefcke
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Patent number: 5958943Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid variety and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1996Date of Patent: September 28, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5919944Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: July 20, 1998Date of Patent: July 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 5919790Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignees: Warner-Lambert Company, BASF AktiengesellsschaftInventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
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Patent number: 5902814Abstract: There are provided new compounds of formula I: ##STR1## wherein R represents hydrogen or methyl; andn represents 1 or 2;or a pharmaceutically acceptable acid addition salt thereof, together with processes for preparing them, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful in the treatment of psychotic disorders, intellectual impairment disorders and anxiety.Type: GrantFiled: September 18, 1995Date of Patent: May 11, 1999Assignee: Astra ABInventors: John Charles Gordon, Ronald Conrad Griffith, Robert John Murray, Michael Balestra
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Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5886192Abstract: A method for the preparation of a lactam compound of formula ##STR1## wherein R'.sub.1 and R".sub.1 independently are acyl or aroyl, or taken together form an optionally substituted methylene, and G.sub.1 is hydrogen or an amino protecting group, comprising oxidizing a bis O-protected 1R-2-azadihydroxybicyclo-?2.2.1!heptane compound of formula ##STR2## with about 0.1 mol % to about 1 mol % of RuO.sub.2 or hydrate thereof in the presence of about 3 equivalents of an oxidant to form the lactam compound with an enantiomeric excess of greater than or equal to about 95%.Type: GrantFiled: June 10, 1997Date of Patent: March 23, 1999Assignee: Rhone-Poulenc Rorer S.A.Inventors: Patrick Leon, Denis Largeau, Thierry Durand, Michael O'Brien, Matthew Powers
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Patent number: 5847157Abstract: The present invention relates to a simplified method of producing .+-.2-azabicyclo?2.2.1!hept-5-en-3-one from cyclopentadiene and sulfocyanides by reacting cyclopentadiene with sulfonylcyanides without the use of organic solvents.Type: GrantFiled: June 25, 1997Date of Patent: December 8, 1998Assignee: Degussa AktiengesellschaftInventors: Frank Romanowski, Kurt Vroman, Rudolf Vanheertum
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Patent number: 5811374Abstract: New 3-arylpyrrolidine-2,4-dione derivatives of the formula (I): ##STR1## in which the variables A, B, E, R, X, Y, Z and n are set forth in the specification, are useful as insecticides, acaricides, and herbicides.Type: GrantFiled: June 7, 1995Date of Patent: September 22, 1998Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Bertram, Reiner Fischer, Bernd-Wieland Kruger, Christoph Erdelen, Klaus Lurssen, Robert R. Schmidt, Hans-Joachim Santel
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Patent number: 5773458Abstract: The compound of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are centrally active muscarinic agents.Type: GrantFiled: October 17, 1997Date of Patent: June 30, 1998Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Reinhardt P. Stein
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Patent number: 5756764Abstract: Described herein are compounds related to lactacystin and lactacystin .beta.-lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: June 6, 1995Date of Patent: May 26, 1998Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Patent number: 5731441Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: March 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5698579Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.Type: GrantFiled: August 27, 1996Date of Patent: December 16, 1997Assignee: Celgene CorporationInventor: George W. Muller
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Patent number: 5693824Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN, G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --, R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.Type: GrantFiled: September 12, 1996Date of Patent: December 2, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
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Patent number: 5670649Abstract: Novel derivatives of 1R- or 1S-2-azabicyclo?2.2.1!heptane with the general formula (I) or (I'), their preparation and their application. ##STR1## In the general formulas (I) and (I'), R represents a hydrogen atom or a group with the formula ##STR2## respectively, in which R.sub.1 represents an alkyl group containing 1-4 carbon atoms and Ar represents an optionally substituted phenyl or .alpha.- or .beta.-naphthyl group.The novel products with the general formula (I) are particularly useful for the preparation of adenosine agonists.Type: GrantFiled: May 30, 1996Date of Patent: September 23, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Denis Largeau, Patrick Leon
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Patent number: 5659075Abstract: A process is claimed for preparing [1S(1(.alpha., 2.beta., 4.beta.)]-4-amino-2-hydroxymethyl -1-cyclopentanol from cis-4-((R)-benzoylamino)-2-cyclopentenecarboxylic acid, methyl ester in five steps. The invention also describes a number of novel intermediates useful in the synthesis of [1S(1.alpha., 2.beta.,4.beta.)]-4-amino-2-hydroxymethyl-1-cyclopentanol.Type: GrantFiled: April 6, 1995Date of Patent: August 19, 1997Assignee: Glaxo Group LimitedInventors: Bernard Charles Halter, Clive Alwin Meerholz, Mark Brian Schilling, David Joszef Tapolczay, John Peter Turnbull
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Patent number: 5654314Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.Type: GrantFiled: March 28, 1995Date of Patent: August 5, 1997Assignee: Boehringer Ingelheim KGInventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
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Patent number: 5631383Abstract: Novel derivatives of 1R- or 1S-2-azabicyclo[2.2.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Denis Largeau, Patrick Leon
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Patent number: 5616604Abstract: New pharmaceutical compounds, which are novel aminopyrrolizinone analogues, having anti-inflammatory and analgesic function and method of making the same.Type: GrantFiled: February 15, 1996Date of Patent: April 1, 1997Inventors: Shoufang Zhang, Xinxian Zhao, Wenfang Kao, Jinrui Wang