The Hetero Ring Contains Plural Nitrogens Patents (Class 540/470)
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Patent number: 6444808Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.Type: GrantFiled: April 11, 2001Date of Patent: September 3, 2002Assignee: The Procter & Gamble CompanyInventors: George Douglas Hiler, II, Christopher Mark Perkins
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Patent number: 6444824Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.Type: GrantFiled: August 9, 2000Date of Patent: September 3, 2002Assignee: Albany Molecular Research, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6420354Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.Type: GrantFiled: December 8, 1999Date of Patent: July 16, 2002Assignee: Advanced Medicine, Inc.Inventors: Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins
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Patent number: 6417353Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.Type: GrantFiled: March 7, 2000Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Frank Funke, Joachim Wulff-Döring, Gerhard Schulz, Wolfgang Siegel, Andreas Kramer, Johann-Peter Melder, Arthur Höhn, Philipp Buskens, Wolfgang Reif, Jan Nouwen
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Patent number: 6417355Abstract: This invention involves a new class of compounds, certain geminal-dinitro-substituted heterocycles, including geminal-bis(difluoramino)-substituted heterocyclic nitramines and the production thereof. More specifically, this invention involves the production of 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine (TNFX), which may be formulated into explosives and propellant oxidizers. The method of making a 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine comprises reacting a hexahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocin-3(2H)-one with a difluoramine source to produce a 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine and reacting said 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine with a highly reactive nitrating reagent in the presence of a strong Lewis acid, such as antimony pentafluoride, boron triflate or boron fluorosulfonate.Type: GrantFiled: April 11, 2001Date of Patent: July 9, 2002Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert Dale Chapman, Theodore Axenrod, Jianguang Sun, Xiao-Pei Guan, Lida Qi
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Patent number: 6362174Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: GrantFiled: August 9, 2001Date of Patent: March 26, 2002Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
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Publication number: 20020028801Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: ApplicationFiled: August 9, 2001Publication date: March 7, 2002Inventors: Michael Francis Rafferty, Yuntao Song
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Patent number: 6352981Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2 (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: October 27, 2000Date of Patent: March 5, 2002Assignee: BASF AktiengesellschaftInventors: Hans-Jörg Treiber, Stefan Blank, Dorothea Starck, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke
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Publication number: 20020019393Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: December 21, 2000Publication date: February 14, 2002Inventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Patent number: 6316440Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: GrantFiled: December 27, 1999Date of Patent: November 13, 2001Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
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Patent number: 6294542Abstract: The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.Type: GrantFiled: December 20, 1999Date of Patent: September 25, 2001Assignee: Boryung Pharmaceutical Co. Ltd.Inventors: Jae-hyoung Lee, Kyung-jin Jang, Byoung-wug Yoo, Ji-han Kim, Jae-seog Kang, Sang-lin Kim
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Patent number: 6281206Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: February 11, 2000Date of Patent: August 28, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6277840Abstract: The invention relates to new compounds of general formula I or the pharmaceutically acceptable salts thereof, wherein X=N—R3 or CH—R4, Y=CH2 or (CH2)2, Z=O or H2; and R1, R2, R3, R4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: May 9, 2000Date of Patent: August 21, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
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Patent number: 6245767Abstract: A monohydrate of an aminobenzenesulfonic acid derivative represented by the following formula (I), for example, 2-(1-piperazinyl)-5-methylbenzenesulfonic acid, is substantially free from weight change due to moisture absorption and can be weighed accurately in manufacturing a pharmaceutical composition for the treatment of heart diseases comprising said monohydrate.Type: GrantFiled: September 24, 1999Date of Patent: June 12, 2001Assignee: Mitsubishi Chemical CorporationInventors: Chika Yamazaki, Tadao Sato, Tatsuo Nagano
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Patent number: 6245758Abstract: The present invention provides a method for the treatment of diseases by the decomposition of peroxynitrite, preferably decomposition to benign products, comprising the use of a complex which is a selected ligand structure providing a complexed metal such as Mn, Fe, Ni and V transition metals. The method of use, as well as novel pharmaceutical compositions therefor, are for the treatment of diseases advantageously affected by decomposition of peroxynitrite ed at a rate over the natural background rate of decay of peroxynitrite in humans suffering from the disease which comprises administration of an amount of a complex, in dosage unit form, which is effective for such acceleration of the decomposition of peroxynitrite .Type: GrantFiled: September 9, 1996Date of Patent: June 12, 2001Inventors: Michael K. Stern, Daniela Salvemini
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Patent number: 6229029Abstract: This invention describes 11&bgr;-aryl-substituted 14,17-ethanoestratrienes of general formula (I). The new compounds are selective estrogens whose action occurs in a tissue-selective manner. The estrogenic action occurs in particular on bone, in the cardiovascular system and in the CNS (central nervous system). Only a slight estrogenic action or no estrogenic action occurs in the uterus and in the liver, however. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example for hormone replacement therapy, prevention and treatment of osteoporosis).Type: GrantFiled: June 9, 2000Date of Patent: May 8, 2001Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Karl Heinrich Fritzemeier, Christa Hegele-Hartung, Rudolf Knauthe, Karsten Parzcyk
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Patent number: 6225464Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.Type: GrantFiled: September 7, 1999Date of Patent: May 1, 2001Assignee: The Procter & Gamble CompanyInventors: George Douglas Hiler, II, Christopher Mark Perkins
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Patent number: 6225309Abstract: The invention concerns compounds of formula (I), wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and 1-C)alkyl; M1 is a group of formula: NR2—L1—T1R3, in which R2 and R3 together form a (1-4C)alylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)rL2—T3R5 in which R is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.Type: GrantFiled: August 9, 1999Date of Patent: May 1, 2001Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
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Patent number: 6214988Abstract: A process for preparing an HMX product comprises the steps of: (a) providing a granule that comprises a plurality of alpha-HMX particles and which has internal void spaces; and (b) sorbing at least one second material into the void spaces in the granule. The second material can be sorbed into the granules by using a vacuum to draw a gas phase comprising the second material into the granule. Alternatively, the second material can be sorbed into the granules by dissolving or dispersing the second material in a liquid solvent, contacting the solvent with the granules, and evaporating the solvent, whereby the second material is sorbed into the granules. Various second materials can be used, such as energetic materials and fuels.Type: GrantFiled: January 3, 1999Date of Patent: April 10, 2001Assignee: Schlumberger Technology CorporationInventors: William J. Lukasavage, Lawrence A. Behrmann, Wallace E. Voreck
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Patent number: 6211187Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono- , di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists or human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: October 22, 1999Date of Patent: April 3, 2001Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 6207825Abstract: A compound represented by the following formula (12) useful as an intermediate for production of drug or agricultural chemical: (wherein R21 to R25 are each independently a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxy group of 1 to 4 carbon atoms, a perfluoroalkyl group of 1 to 4 carbon atoms, a cyano group, a nitro group, an amino group, a carboxyl group, a thiol group, an alkylthio group of 1 to 4 carbon atoms or a carbamoyl group) can be produced by reacting a compound represented by the formula (13): (wherein R21 to R25 have the same definitions as given above) with 1,1-cyclopropanedicarboxylic acid. The compound of the formula (12) is useful as a raw material for production of a pyrrolidinone compound useful as an active ingredient of drug.Type: GrantFiled: November 13, 1998Date of Patent: March 27, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hajime Iizuka, Hiroshi Nagase, Naruyoshi Mita
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Patent number: 6166201Abstract: A process for the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid and the salts thereof of formula (I) ##STR1## which comprises the following steps: a) carboxymethylation reaction of a suitable precursor in water, with a haloacetic acid,b) hydrolysis reaction in basic conditions by addition of the base added at the previous step.Type: GrantFiled: March 14, 2000Date of Patent: December 26, 2000Assignee: Dibra S.p.A.Inventors: Giorgio Ripa, Alessandro Scala, Marcella Murru, Emanuela Panetta, Carlo Felice Viscardi, Marina Ausonio
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Patent number: 6162912Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles .Type: GrantFiled: July 28, 1999Date of Patent: December 19, 2000Assignee: Dibra S.p.A.Inventors: Maria Argese, Giorgio Ripa
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Patent number: 6153608Abstract: The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.Type: GrantFiled: July 29, 1998Date of Patent: November 28, 2000Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiroyoshi Hidaka, Akira Matsuura, Takushi Matsuzaki
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Patent number: 6107437Abstract: Curing agents for epoxy resins are provided in which an imidazole is substituted on the nitrogen atom by a long chain group. This provides greater latexing (stability) at ambient temperatures without adversely affecting curing properties at temperatures of 50.degree. C. upwards. Those components in which the chain is substituted by a hydroxy group on the 2 position are particularly preferred and are novel compounds.Type: GrantFiled: September 28, 1998Date of Patent: August 22, 2000Assignee: Hexcel CorporatioinInventors: John Leslie Cawse, Mark Whiter
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Patent number: 6103719Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: May 27, 1999Date of Patent: August 15, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
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Patent number: 6080758Abstract: The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH.sub.2 --, --CH(OH)--, --CH(NH--COCH.sub.3)-- or S, R is H, CO.sub.2 H, CO.sub.2 --B--R.sub.1 or CO--N(R.sub.2)--B--R.sub.1, B is linear, branched or cyclic C.sub.1 -C.sub.10 -alkylene, R.sub.1 is H, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 --NR.sub.3 R.sub.4 or phenyl, R.sub.2 is H or C.sub.1 -C.sub.4 -alkyl, R.sub.3 is H or linear, branched or cyclic C.sub.1 -C.sub.10 -alkyl, R.sub.4 is H or linear or branched C.sub.1 -C.sub.10 -alkyl, it being possible for NR.sub.3 R.sub.4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon carrying the substituent R, when Q is saturated, can be of indeterminate (R,S) configuration or of determinate (R) or (S) configuration; and their addition salts.Type: GrantFiled: April 7, 1997Date of Patent: June 27, 2000Assignee: Fournier Industrie et SanteInventors: Pierre Dodey, Michel Bondoux, Patrick Houziaux, Martine Barth, Khan Ou
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Patent number: 6054581Abstract: A process for the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid and the salts thereof of formula (I) ##STR1## which comprises the following steps: a) carboxymethylation reaction of a suitable precursor in water, with a haloacetic acid,b) hydrolysis reaction in basic conditions by addition of the base added at the previous step.Type: GrantFiled: June 25, 1999Date of Patent: April 25, 2000Assignee: Dibra S.p.A.Inventors: Giorgio Ripa, Alessandro Scala, Marcella Murru, Emanuela Panetta, Carlo Felice Viscardi, Marina Ausonio
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Patent number: 6048980Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.Type: GrantFiled: July 28, 1999Date of Patent: April 11, 2000Assignee: Dibra S.p.AInventors: Maria Argese, Giorgio Ripa
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Patent number: 6022873Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.Type: GrantFiled: July 23, 1998Date of Patent: February 8, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
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Patent number: 6019959Abstract: Oligomeric compounds that contain perfluoroalkyl of general formula IA--R.sup.F (I)in whichA is a molecule portion that contains 2-6 metal complexes that are connected directly or via a linker to a nitrogen atom of an annular skeleton chain, andR.sup.F is a perfluorinated, straight-chain or branched carbon chain with formula --C.sub.n F.sub.2n E, in which E represents a terminal fluorine, chlorine, bromine, iodine, or hydrogen atom and n stands for numbers 4-30,are valuable compounds for diagnosis, especially as in-vivo contrast media.Type: GrantFiled: June 29, 1998Date of Patent: February 1, 2000Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Ulrich Niedballa, Bernd Raduchel, Wolfgang Schlecker, Hanns-Joachim Weinmann, Thomas Frenzel, Bernd Misselwitz, Wolfgang Ebert
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Patent number: 6011152Abstract: New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an .alpha. or .beta. amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the .alpha. or .beta.Type: GrantFiled: September 22, 1998Date of Patent: January 4, 2000Assignee: Carnegie Mellon UniversityInventors: Scott W. Gordon-Wylie, Terrence J. Collins
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Patent number: 6011028Abstract: The current invention discloses useful amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 27, 1998Date of Patent: January 4, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., E. Ann. Hallinan, Timothy J. Hagen, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Dale P. Spangler, Mihaly V. Toth, Kam F. Fok, Arija A. Bergmanis, R. Keith Webber, Mahima Trivedi, Foe S. Tjoeng, Barnett S. Pitzele
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Patent number: 5985878Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.Type: GrantFiled: July 9, 1998Date of Patent: November 16, 1999Assignee: Janssen Pharmaceuticals, N.V.Inventors: Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa, Marc Willems, Lieven Meerpoel, Marcel Gerebernus Maria Luyckx, Robert Tuman
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Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5962455Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.Type: GrantFiled: July 18, 1997Date of Patent: October 5, 1999Assignee: Neurogen CorporationInventors: Charles A. Blum, Alan Hutchison, John M. Peterson
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Patent number: 5962679Abstract: A process for the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid and the salts thereof of formula (I) ##STR1## which comprises the following steps: a) carboxymethylation reaction of a suitable precursor in water, with a haloacetic acid,b) hydrolysis reaction in basic conditions by addition of the base added at the previous step.Type: GrantFiled: June 10, 1998Date of Patent: October 5, 1999Assignee: Dibra S.p.A.Inventors: Giorgio Ripa, Alessandro Scala, Marcella Murru, Emanuela Panetta, Carlo Felice Viscardi, Marina Ausonio
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5866562Abstract: The present invention relates to ring-bridged bis-quinolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides a process for the preparation of compounds of the formula (I), their use for the preparation of drugs, and drugs containing said compounds.Type: GrantFiled: October 25, 1996Date of Patent: February 2, 1999Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe-Loop, Peter-Rudolf Seidel, William Bullock, Achim Feurer, Georg Terstappen, Joachim Schuhmacher, Franz-Josef van der Staay, Bernard Schmidt, Richard J. Fanelli, Jane C. Chisholm, Richard T. McCarthy
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Patent number: 5854234Abstract: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 5847135Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: May 25, 1995Date of Patent: December 8, 1998Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5817489Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as antibacterial and as other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.Type: GrantFiled: August 1, 1996Date of Patent: October 6, 1998Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Pei Pei Kung, Andrew M. Kawasaki
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Patent number: 5811544Abstract: An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the bisacylation of an acyclic diamine to obtain a dichlorodiamide compound in a first step, the cyclization of said diamide compound to obtain dioxocyclam in a second step, and the reduction of dioxocyclam in a third step to obtain the desired 1,4,8,11-tetraazacyclotetradecane.Type: GrantFiled: July 30, 1996Date of Patent: September 22, 1998Assignee: Johnson Matthey PLCInventors: Orin Tempkin, Prasad Kapa
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Patent number: 5723456Abstract: A method for treating endothelial cell dysfunction, such as associated with cardiovascular disease are disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-?N,N'-1,1'-((27"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bi s-(3,3'-indolyl)!-1(H)-pyrrole-2,5-dione hydrochloride salt.Type: GrantFiled: June 13, 1996Date of Patent: March 3, 1998Assignee: Eli Lilly & CompanyInventors: Michael R. Jirousek, William Francis Heath, Jr., Douglas Kirk Ways, Lawrence E. Stramm
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Patent number: 5723608Abstract: This invention encompasses compounds of the formula ##STR1## wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; andR.sub.1 represents lower alkyl;R.sub.2 is hydrogen or lower alkyl; andR.sub.3 and R.sub.4 independently represent organic and inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF.sub.1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: December 31, 1996Date of Patent: March 3, 1998Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 5700799Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive.Type: GrantFiled: March 4, 1996Date of Patent: December 23, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Douglas K. Hutchinson, Michael R. Barbachyn, Steven J. Brickner, Ronald B. Gammill, Mahesh V. Patel
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Patent number: 5656632Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: August 12, 1997Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5650417Abstract: Substituted pyridines, their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## and to salts thereof in which 1, 2, 3 or 4 of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an aliphatic, alicyclic or araliphatic radical bonded by a --O--CH.sub.2 -- or --O--CO--, and the remaining ones of these radicals are H, halogen or an aliphatic or aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent radical and Z is an aromatic radical or optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and to their use as pesticides, in particular as insecticides, acaricides and fungicides.Type: GrantFiled: September 12, 1994Date of Patent: July 22, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
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Patent number: 5643848Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.Type: GrantFiled: May 3, 1995Date of Patent: July 1, 1997Assignee: Bridgestone CorporationInventors: David F. Lawson, James E. Hall, Yoichi Ozawa
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Patent number: 5631275Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, and uses of the pharmaceutical products based on these compounds. The substituted benzenesulfonylureas and -thioureas are of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 E, and y are as defined in the specification. The compounds of formula I have antiarrhythmic activity.Type: GrantFiled: June 5, 1995Date of Patent: May 20, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz G ogelein, Joachim Kaiser, Uwe Gerlach