Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Adrenochrome, Etc.) Patents (Class 548/512)
  • Patent number: 7005439
    Abstract: 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: Grant
    Filed: June 14, 2001
    Date of Patent: February 28, 2006
    Assignee: AstraZeneca AB
    Inventors: Tomas Eriksson, Krister Henriksson
  • Patent number: 6900322
    Abstract: 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: Grant
    Filed: May 10, 1999
    Date of Patent: May 31, 2005
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
  • Patent number: 6878738
    Abstract: 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: Grant
    Filed: November 23, 1999
    Date of Patent: April 12, 2005
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Karola Tollmann, Hans-Guenter Striegel
  • Publication number: 20040180235
    Abstract: 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: Application
    Filed: December 22, 2003
    Publication date: September 16, 2004
    Inventors: Hiroshi Yamamoto, Norihisa Dan, Olof Wallquist
  • Patent number: 6482957
    Abstract: 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: Grant
    Filed: April 25, 2002
    Date of Patent: November 19, 2002
    Assignee: Kuraray Co., Ltd.
    Inventors: Nobuya Katagiri, Chikara Kaneko, Junko Sato, Masahiro Torihara, Koichi Kanehira, Yoshin Tamai
  • Patent number: 6395766
    Abstract: 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: Grant
    Filed: November 6, 2000
    Date of Patent: May 28, 2002
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
  • Patent number: 6355668
    Abstract: 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 agent
    Type: Grant
    Filed: August 28, 2000
    Date of Patent: March 12, 2002
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
  • Patent number: 6353109
    Abstract: 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: Grant
    Filed: June 1, 1998
    Date of Patent: March 5, 2002
    Assignee: Neurogen Corporation
    Inventors: Pamela Albaugh, Gang Liu, Alan Hutchison
  • Publication number: 20020015938
    Abstract: 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: Application
    Filed: October 29, 1998
    Publication date: February 7, 2002
    Inventor: NARMADA SHENOY
  • Publication number: 20020010085
    Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1
    Type: Application
    Filed: March 6, 2001
    Publication date: January 24, 2002
    Inventor: Peter Herold
  • Patent number: 6316486
    Abstract: 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: Grant
    Filed: October 31, 1997
    Date of Patent: November 13, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: 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
  • Patent number: 6291507
    Abstract: 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: Grant
    Filed: July 26, 2000
    Date of Patent: September 18, 2001
    Assignee: Astrazeneca UK Limited
    Inventors: Alan W Faull, Andrew J Barker, Jason G Kettle
  • Patent number: 6288104
    Abstract: 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: Grant
    Filed: March 22, 1999
    Date of Patent: September 11, 2001
    Assignee: African Natural Health CC
    Inventors: Nigel Peter Gericke, Ben-Erik Van Wyk
  • Publication number: 20010020035
    Abstract: Disclosed are compounds of the formula 1
    Type: Application
    Filed: June 1, 1998
    Publication date: September 6, 2001
    Inventors: PAMELA ALBAUGH, GANG LIU, ALAN HUTCHISON
  • Patent number: 6245919
    Abstract: 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: Grant
    Filed: December 28, 1998
    Date of Patent: June 12, 2001
    Assignees: Nippon Chemiphar Co., Ltd.
    Inventors: Haruhiko Shinozaki, Takeo Taguchi, Michiko Ishida
  • Patent number: 6232473
    Abstract: 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: Grant
    Filed: May 1, 2000
    Date of Patent: May 15, 2001
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Rensuke Ikarashi
  • Patent number: 6229011
    Abstract: 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: Grant
    Filed: August 21, 1998
    Date of Patent: May 8, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
  • Patent number: 6211377
    Abstract: 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: Grant
    Filed: March 1, 1999
    Date of Patent: April 3, 2001
    Assignee: Degussa-Huls AG
    Inventors: Johny de Schrijver, Philippe Otten
  • Patent number: 6153765
    Abstract: 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: Grant
    Filed: February 24, 2000
    Date of Patent: November 28, 2000
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Rensuke Ikarashi
  • Patent number: 6133305
    Abstract: 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: Grant
    Filed: September 25, 1998
    Date of Patent: October 17, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6121306
    Abstract: 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: Grant
    Filed: September 29, 1999
    Date of Patent: September 19, 2000
    Assignee: Warner-Lambert Company
    Inventor: Denis Martin Sobieray
  • Patent number: 6107491
    Abstract: 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: Grant
    Filed: January 26, 1999
    Date of Patent: August 22, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 6096887
    Abstract: 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: Grant
    Filed: February 25, 1998
    Date of Patent: August 1, 2000
    Assignee: Neurogen Corporation
    Inventors: Pamela Albaugh, Gang Liu, Alan Hutchison
  • Patent number: 6071908
    Abstract: 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: Grant
    Filed: May 7, 1998
    Date of Patent: June 6, 2000
    Assignee: Auckland Uniservices Limited
    Inventors: William A. Denny, Moena Tercel, William R. Wilson
  • Patent number: 6060609
    Abstract: 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: Grant
    Filed: December 28, 1998
    Date of Patent: May 9, 2000
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Rensuke Ikarashi
  • Patent number: 6054464
    Abstract: 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: Grant
    Filed: March 26, 1999
    Date of Patent: April 25, 2000
    Assignee: Astra Aktiebolag
    Inventors: John Macor, Edwin Wu
  • Patent number: 6037361
    Abstract: 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: Grant
    Filed: March 9, 1998
    Date of Patent: March 14, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
  • Patent number: 5998429
    Abstract: 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: Grant
    Filed: June 13, 1997
    Date of Patent: December 7, 1999
    Assignee: Astra AB
    Inventors: John Macor, Edwin Wu
  • Patent number: 5972248
    Abstract: 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: Grant
    Filed: October 7, 1997
    Date of Patent: October 26, 1999
    Assignee: Clariant GmbH
    Inventors: Thomas Stahrfeldt, Josef Wiedemann, Matthias Zah
  • Patent number: 5969154
    Abstract: 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: Grant
    Filed: December 10, 1997
    Date of Patent: October 19, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Zhimin Hao, Abul Iqbal, Nancy Tebaldi, Klaus Praefcke
  • Patent number: 5958943
    Abstract: 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: Grant
    Filed: March 28, 1996
    Date of Patent: September 28, 1999
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
  • Patent number: 5942535
    Abstract: 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: Grant
    Filed: March 28, 1997
    Date of Patent: August 24, 1999
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
  • Patent number: 5919790
    Abstract: 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: Grant
    Filed: October 2, 1997
    Date of Patent: July 6, 1999
    Assignees: Warner-Lambert Company, BASF Aktiengesellsschaft
    Inventors: 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
  • Patent number: 5919944
    Abstract: 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: Grant
    Filed: July 20, 1998
    Date of Patent: July 6, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 5902814
    Abstract: 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: Grant
    Filed: September 18, 1995
    Date of Patent: May 11, 1999
    Assignee: Astra AB
    Inventors: John Charles Gordon, Ronald Conrad Griffith, Robert John Murray, Michael Balestra
  • Patent number: 5886192
    Abstract: 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: Grant
    Filed: June 10, 1997
    Date of Patent: March 23, 1999
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Patrick Leon, Denis Largeau, Thierry Durand, Michael O'Brien, Matthew Powers
  • Patent number: 5886191
    Abstract: 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: Grant
    Filed: August 18, 1997
    Date of Patent: March 23, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
  • Patent number: 5847157
    Abstract: 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: Grant
    Filed: June 25, 1997
    Date of Patent: December 8, 1998
    Assignee: Degussa Aktiengesellschaft
    Inventors: Frank Romanowski, Kurt Vroman, Rudolf Vanheertum
  • Patent number: 5811374
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: September 22, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Jurgen Bertram, Reiner Fischer, Bernd-Wieland Kruger, Christoph Erdelen, Klaus Lurssen, Robert R. Schmidt, Hans-Joachim Santel
  • Patent number: 5773458
    Abstract: 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: Grant
    Filed: October 17, 1997
    Date of Patent: June 30, 1998
    Assignee: American Home Products Corporation
    Inventors: Annmarie L. Sabb, Reinhardt P. Stein
  • Patent number: 5756764
    Abstract: Described herein are compounds related to lactacystin and lactacystin .beta.-lactone, pharmaceutical compositions containing the compounds, and methods of use.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 26, 1998
    Assignee: President and Fellows of Harvard College
    Inventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
  • Patent number: 5731441
    Abstract: 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: Grant
    Filed: October 29, 1996
    Date of Patent: March 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
  • Patent number: 5698579
    Abstract: 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: Grant
    Filed: August 27, 1996
    Date of Patent: December 16, 1997
    Assignee: Celgene Corporation
    Inventor: George W. Muller
  • Patent number: 5693824
    Abstract: 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: Grant
    Filed: September 12, 1996
    Date of Patent: December 2, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
  • Patent number: 5670649
    Abstract: 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: Grant
    Filed: May 30, 1996
    Date of Patent: September 23, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Denis Largeau, Patrick Leon
  • Patent number: 5659075
    Abstract: 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: Grant
    Filed: April 6, 1995
    Date of Patent: August 19, 1997
    Assignee: Glaxo Group Limited
    Inventors: Bernard Charles Halter, Clive Alwin Meerholz, Mark Brian Schilling, David Joszef Tapolczay, John Peter Turnbull
  • Patent number: 5654314
    Abstract: 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: Grant
    Filed: March 28, 1995
    Date of Patent: August 5, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
  • Patent number: 5631383
    Abstract: Novel derivatives of 1R- or 1S-2-azabicyclo[2.2.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 20, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Denis Largeau, Patrick Leon
  • Patent number: 5616604
    Abstract: New pharmaceutical compounds, which are novel aminopyrrolizinone analogues, having anti-inflammatory and analgesic function and method of making the same.
    Type: Grant
    Filed: February 15, 1996
    Date of Patent: April 1, 1997
    Inventors: Shoufang Zhang, Xinxian Zhao, Wenfang Kao, Jinrui Wang
  • Patent number: RE39128
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: June 13, 2006
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt