The Aryl Ring Or Ring System Is Bonded Directly To Another Ring Patents (Class 564/337)
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Patent number: 7423181Abstract: The invention provides novel alkoxyaminochalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, bacteriostatic, and bacteriocidal agents.Type: GrantFiled: May 19, 2003Date of Patent: September 9, 2008Assignee: Lica Pharmaceuticals A/SInventors: Simon Feldbæk Nielsen, Thomas Boesen, Mogens Larsen, Mette Bjerg Nielsen, Hasse Kromann
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Patent number: 7417169Abstract: The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is —COR10, -A1-COR10, —O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, —OCH2—, etc, which exhibit potent and selective ?3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: GrantFiled: October 5, 2004Date of Patent: August 26, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Junichi Kobayashi, Tetsuya Nakamura, Hideyuki Muranaka, Takehiro Ishikawa, Tetsuro Tamai, Satoshi Akahane
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Publication number: 20080146845Abstract: The invention provides a process for preparing Cinacalcet base in which a compound VI, having the structure: where X is C1-3 alkylsulfonate, substituted and non-substituted C6-10 aryl sulfonate or halogen, is reacted with (R)-1-Naphthylethylamine and, optionally, a base: 1) under minimal solvent conditions, 2) at a minimum temperature of about 100° C., preferably, greater than 121° C., and, more preferably, at a temperature of greater than 121° C. to about 130° C., and 3) under elevated pressure.Type: ApplicationFiled: November 20, 2007Publication date: June 19, 2008Inventors: Boaz Gome, Leonid Levenfeld
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Publication number: 20080139848Abstract: A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.Type: ApplicationFiled: December 11, 2006Publication date: June 12, 2008Applicant: Apicore, LLCInventors: Satyam S. Nampalli, Brijesh Patel, Peter Xavier Tharial, Ravishanker Kovi
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Patent number: 7368462Abstract: The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provide a means for reducing body mass and controlling obesity.Type: GrantFiled: July 13, 2005Date of Patent: May 6, 2008Assignee: The Procter & Gamble CompanyInventor: Xiufeng Eric Hu
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Patent number: 7368606Abstract: Provided is amorphous cinacalcet hydrochloride, processes for the preparation thereof, and pharmaceutical compositions therewith.Type: GrantFiled: May 23, 2006Date of Patent: May 6, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Revital Lifshitz-Liron, Michael Pinchasov, Shlomit Wizel, Sharon Avhar-Maydan
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Patent number: 7361789Abstract: The present invention relates to novel dihydronaphthalene compounds, compositions, methods for using the same, and processes for preparing the same. The present invention also relates to novel total synthesis approaches for preparing these compounds. In addition, the present invention relates to methods of producing quantities of isomers of these compounds and separating and purifying them using chiral separation techniques. The present invention also relates to methods of producing quantities of a single isometric compound without the need for chiral separation techniques.Type: GrantFiled: July 27, 2005Date of Patent: April 22, 2008Assignee: Amgen Inc.Inventors: Qi Yan, Carlos Orihuela, Bo Shen, Ying Chen, Xin Wang, John Ng, Ruizhi Ji, Pengzu Zhou
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Patent number: 7342133Abstract: The invention relates to substituted amino compounds, to processes for their preparation, to pharmaceutical formulations containing these compounds and to the use of these substances in the preparation of pharmaceutical formulations, especially for the treatment or inhibition of depression, anxiety, pain and urinary incontinence, and to related methods of treating or inhibiting these disorders.Type: GrantFiled: January 16, 2007Date of Patent: March 11, 2008Assignee: Gruenenthal GmbHInventors: Petra Bloms-Funke, Elmar Friderichs, Ivars Graudums, Hagen-Heinrich Hennies, Achim Kless, Klaus Schiene, Oswald Zimmer
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Publication number: 20080045757Abstract: The invention relates to the compounds of formula: (I) which are as defined in the specification. Their use as chiral ligands in catalytic aryl transfer reactions to aromatic aldehydes is also described.Type: ApplicationFiled: March 10, 2005Publication date: February 21, 2008Inventors: Albert Sun-Chi Chan, Jianxin Ji
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Patent number: 7279600Abstract: This invention provides estrogen receptor modulators having the structure: wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 29, 2004Date of Patent: October 9, 2007Assignee: WyethInventors: Richard Eric Mewshaw, Cuijian Yang
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Patent number: 7273952Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.Type: GrantFiled: March 31, 2003Date of Patent: September 25, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Corinna Maul, Helmut Buschmann, Michael Finkam, Babette-Yvonne Koegel
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Patent number: 7271291Abstract: The invention provides 1,3,5-tris(arylamino)benzenes represented by the general formula (I) wherein A is naphthyl, anthryl or phenanthryl group, and R is hydrogen atom or diarylamino group. These 1,3,5-tris(arylamino)benzenes have oxidation potentials in the range of about 0.5-0.6V, excellent reversibility in oxidation-reduction process, high glass transition temperatures and high heat resistance, so that they can form practicable organic semiconductor film readily by a coating method or a vacuum deposition method. In addition, they are capable of forming stable and durable amorphous film useful as high performance organic semiconductors at normal temperatures or higher with no aid of binder resins, that is, by themselves.Type: GrantFiled: March 15, 2004Date of Patent: September 18, 2007Assignee: Bando Chemical Industries, Ltd.Inventors: Hiroshi Inada, Nobutaka Akashi, Tomoko Hayashi
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Patent number: 7247751Abstract: The invention provides processes for the preparation of cinacalcet hydrochloride crystalline Form I.Type: GrantFiled: May 23, 2006Date of Patent: July 24, 2007Assignee: Teva Pharmaceutical Industries LtdInventors: Revital Lifshitz-Liron, Sharon Avhar-Maydan
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Patent number: 7211695Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: April 10, 2006Date of Patent: May 1, 2007Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 7186864Abstract: A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: May 28, 2003Date of Patent: March 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot, David Thomson
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Patent number: 7169817Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.Type: GrantFiled: May 27, 2003Date of Patent: January 30, 2007Assignee: IRM LLCInventors: Shifeng Pan, Nathanael S. Gray, Wenqui Gao, Klaus Hinterding, Sophie Lefebvre, Yuan Mi, Peter Nussbaumer, Wei Wang, Federic Zecri, Fan Yi, Lawrence Blas Perez, Kenneth Richad la Montagne, Peter Ettmayer
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Patent number: 7105701Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: May 10, 2005Date of Patent: September 12, 2006Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 7030160Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.Type: GrantFiled: May 29, 2001Date of Patent: April 18, 2006Assignee: Sanofi-AventisInventors: Laura Barzaghi, Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Stefano Romagnano
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Patent number: 6984738Abstract: The present invention is to provide a process for producing an optically active amino alcohol which is useful for the synthesis of natural substances and as an intermediate for drugs and agricultural chemicals in a high yield, a high selectivity and an economical manner with a good working efficiency and the present invention relates to a process for producing an optically active amino alcohol represented by the following formula (2) (in the formula, R1 is a hydrocarbon group, a substituted hydrocarbon group, an aromatic heterocyclic group, a substituted aromatic heterocyclic group, an aliphatic heterocyclic group or a substituted aliphatic heterocyclic group; R2 and R3 each independently is hydrogen atom, a hydrocarbon group, a substituted hydrocarbon group, an acyl group, an acyloxy group, an alkyloxycarbonyl group, an aralkyloxycarbonyl group, an aryloxycarbonyl group, an aromatic heterocyclic group, a substituted aromatic heterocyclic group, an aliphatic heterocyclic group or a substituted aliphatic hType: GrantFiled: October 17, 2003Date of Patent: January 10, 2006Inventors: Tohru Yokozawa, Kenji Yagi, Takao Saito
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Patent number: 6924391Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula wherein X, Z, X1, R1, R2, Ra, Rb, R3, R4 and Y are as defined in the specification.Type: GrantFiled: May 3, 2001Date of Patent: August 2, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Neelakantan Balasubramanian, Gilles Bouthillier, Alain Martel
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Publication number: 20040209949Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.Type: ApplicationFiled: May 5, 2004Publication date: October 21, 2004Inventors: Andrew Francis Browning, Eric William Collington, Martin James Procter, Joanna Victoria Geden
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Patent number: 6770786Abstract: The antifungal agent (E)-N-methyl-N-(1-naphthylmethyl)-6,6-dimethyl-hept-2-ene-4-ynyl-1-amine of formula (I) and acid addition salts thereof are prepared by reacting a chloro-compound of formula (IIIb) with a secondary amine of formula (II) in an aliphatic ketone-type solvent in the presence of a base and optionally iodide salt catalyst, and subsequently treating the resulting reaction mixture directly with aqueous hydrochloric acid to precipitate the hydrochloride of the compound of formula (I). The precipitate is separated, and the base of formula (I) can be liberated from the hydrochloride and can be converted into other pharmaceutically acceptable acid addition salts.Type: GrantFiled: February 21, 2003Date of Patent: August 3, 2004Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Peter Bod, Laszlo Terdy, Ferenc Trischler, Eva Fekecs, Maria Demeter, Anna Lauko, Gyorgy Domany, Gyorgyi Szabone Komlosi, Katalin Varga
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Patent number: 6762330Abstract: Phosphine oxide and sulfoxide compounds were used with transition metals, preferably palladium and nickel, to produce biaryls, arylthiols, arylphosphine oxides and arylamines via cross-coupling reactions with aryl halides and arylboronic acids, aryl Grignard reagents, thiols, phosphine oxides or amines.Type: GrantFiled: July 6, 2001Date of Patent: July 13, 2004Assignee: E. I. du Pont de Nemours and CompanyInventor: George Y. Li
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Patent number: 6710080Abstract: Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.Type: GrantFiled: February 11, 2002Date of Patent: March 23, 2004Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Babette-Yvonne Koegel, Helmut Buschmann
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Patent number: 6689913Abstract: Provided is a process for preparing terbinafine or its HCl salt comprising: reacting a furan derivative with a base to form a second compound; performing a reductive alkylation of the second compound obtained in the step with N-methyl-1-naphthalenemethylamine or its HCl salt to form a third compound; and purifying the third compound.Type: GrantFiled: December 27, 2002Date of Patent: February 10, 2004Assignee: Yuhan CorporationInventors: Tai-Au Lee, Kyu-Jung Wang, Hong-Bae Kim, Kyoung-Chan Kwon, Chang-Hoe Ku
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Patent number: 6573399Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative which comprises reacting an &agr;-amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an alkyllithium in succession, and treating the reaction product with an acid in an alcohol.Type: GrantFiled: February 21, 2001Date of Patent: June 3, 2003Assignee: Kaneka CorporationInventors: Akira Nishiyama, Kenji Inoue
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Publication number: 20030069288Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, 1Type: ApplicationFiled: July 5, 2002Publication date: April 10, 2003Inventors: Claudia Puetz, Wolfgang Strassburger, Babette-Yvonne Koegel
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Publication number: 20020198251Abstract: Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.Type: ApplicationFiled: February 11, 2002Publication date: December 26, 2002Inventors: Bernd Sundermann, Babette-Yvonne Koegel, Helmut Buschmann
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Patent number: 6482986Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.Type: GrantFiled: February 27, 2002Date of Patent: November 19, 2002Assignee: Sanofi-SynthelaboInventors: Robert Boigegrain, Bernard Bourrie, Martine Bourrie, Pierre Casellas, Jean Marc Herbert, Pierre Lair, Dino Nisato, Raymond Paul, Jean Claude Vernieres
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Publication number: 20020165284Abstract: The present invention provides enantiomers of N-Desmethyl venlafaxine, as well as their use in pharmaceutical compositions and medically useful treatments, particularly including central nervous system uses.Type: ApplicationFiled: July 3, 2002Publication date: November 7, 2002Applicant: WyethInventors: John P. Yardley, Andre A. Asselin
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Publication number: 20020137974Abstract: Phosphine oxide and sulfoxide compounds were used with transition metals, preferably palladium and nickel, to produce biaryls, arylthiols, arylphosphine oxides and arylamines via cross-coupling reactions with aryl halides and arylboronic acids, aryl Grignard reagents, thiols, phosphine oxides or amines.Type: ApplicationFiled: July 6, 2001Publication date: September 26, 2002Inventor: George Y. Li
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Publication number: 20020115576Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.Type: ApplicationFiled: December 22, 2000Publication date: August 22, 2002Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist
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Patent number: 6417357Abstract: This invention relates to a novel, inventive process for the preparation of biphenyls or aromatic olefins by coupling reactions of the Suzuki coupling and Heck coupling type, using allylpalladium catalysts of the &mgr;-halo(triisopropylphosphine)(&eegr;3-allyl)palladium(II) type.Type: GrantFiled: September 14, 2000Date of Patent: July 9, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Michael Tinkl, Andreas Hafner
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Patent number: 6410736Abstract: The present invention relates to compounds of formula I, and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.Type: GrantFiled: October 19, 2000Date of Patent: June 25, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Mavis D. Adam
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Patent number: 6365775Abstract: Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R1, R2, R3, R4, R5, R6 and R7 are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.Type: GrantFiled: July 27, 2000Date of Patent: April 2, 2002Assignee: Aventis Pharma S.A.Inventor: Dominique Lesuisse
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Patent number: 6335366Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)—(CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.Type: GrantFiled: January 22, 2001Date of Patent: January 1, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Patent number: 6323369Abstract: This invention provides substituted cycloheptenes of the general formula I in which R1 represents OH, O-(C1-C6)-alkyl, O-(C3-C7)-cycloalkyl, O-aryl, C1-C6-alkyl-COO-, aryl-COO-, R2 represents C1-C6-alkyl, (CH2)(1-2)-aryl, C2-C6-alkenyl-aryl and R3 represents (CH2)(0-1)-C5-C7-cycloalkyl, (CH2)(0-2)-aryl, heterocyclyl, C1-C6-alkyl-heterocyclyl either as a racemate or in the form of the pure enantiomers, each as a base or as a salt with a pharmaceutically acceptable acid, a process for their preparation and their use as medicaments.Type: GrantFiled: December 14, 1999Date of Patent: November 27, 2001Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Wolfgang Werner Alfred Strassburger, Werner Guenter Englberger, Babette-Yvonne Koegel
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Publication number: 20010023257Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising themType: ApplicationFiled: December 12, 2000Publication date: September 20, 2001Inventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
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Patent number: 6268520Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.Type: GrantFiled: April 5, 1999Date of Patent: July 31, 2001Assignee: Hoechst Marion RousselInventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
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Patent number: 6235791Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.Type: GrantFiled: April 12, 1999Date of Patent: May 22, 2001Assignee: Sanofi-SynthelaboInventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
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Patent number: 6221871Abstract: Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: June 11, 1999Date of Patent: April 24, 2001Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 6147119Abstract: Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.Type: GrantFiled: September 28, 1998Date of Patent: November 14, 2000Assignee: Hoechst Marion RousselInventor: Dominique Lesuisse
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Patent number: 6121489Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.Type: GrantFiled: March 5, 1997Date of Patent: September 19, 2000Assignee: Trega Biosciences, Inc.Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
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Patent number: 6080768Abstract: Compounds of the formula: ##STR1## wherein the variables are as defined in the specification. These compounds are useful in the treatment of arterial hypertension and heart failure, of renal insufficiency, of peripheral arteriopathies and of cerebrovascular insufficiencies.Type: GrantFiled: October 17, 1997Date of Patent: June 27, 2000Assignee: Zambon Group S.p.A.Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
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Patent number: 6066672Abstract: The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.Type: GrantFiled: July 16, 1998Date of Patent: May 23, 2000Assignees: Taisho Pharmaceutical Co., Ltd., Sagami Chemical Research CenterInventors: Takeo Kobori, Kenichi Goda, Kikuo Sugimoto, Tomomi Ota, Kazuyuki Tomisawa
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Patent number: 6063932Abstract: Arthropodicidal oxazoline derivatives and processes and intermediates for the preparation thereof are disclosed. The intermediates are racemic or enantiomerically enriched compounds having formula (I), wherein R and n are disclosed in the specification.Type: GrantFiled: May 13, 1999Date of Patent: May 16, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, Rafael Shapiro
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Patent number: 6031134Abstract: The invention relates to a novel process for the preparation of 2-amino-2-arylehanols of the formula (I) ##STR1## in which Ar represents aryl or hetaryl each unsubstituted or identically or differently monosubstituted to pentasubstituted, where as substituents there may be mentioned:halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, unsubstituted or substituted cycloalkyloxy or unsubstituted or substituted phenyl,which comprises catalytically hydrogenating .alpha.-hydroxyketoximes of the formula (II) ##STR2## in which Ar has the meaning given above,using Raney nickel or Raney cobalt in the presence of a diluent and in the presence of a base andnovel 2-amino-2-arylethanols and novel .alpha.-hydroxyketoximes.Type: GrantFiled: November 4, 1998Date of Patent: February 29, 2000Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Ernst Kysela, Albrecht Marhold
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Patent number: 6022995Abstract: The invention relates to a novel process for the preparation of 2-amino-2-arylethanols of the formula (I) ##STR1## in which Ar represents aryl or hetaryl each unsubstituted or identically or differently monosubstituted to pentasubstituted, where as substituents there may be mentioned:halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, unsubstituted or substituted cycloalkyloxy or unsubstituted or substituted phenyl,which comprises catalytically hydrogenating .alpha.-hydroxyketoximes of the formula (II) ##STR2## in which Ar has the meaning given above,using Raney nickel or Raney cobalt in the presence of a diluent and in the presence of a base andnovel 2-amino-2-arylethanols and novel .alpha.-hydroxyketoximes.Type: GrantFiled: September 27, 1996Date of Patent: February 8, 2000Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Ernst Kysela, Albrecht Marhold
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Patent number: 6011068Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca.sup.2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.Type: GrantFiled: December 8, 1994Date of Patent: January 4, 2000Assignees: NPS Pharmaceuticals, Inc., The Brigham and Women's HospitalInventors: Edward F. Nemeth, Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. DelMar, Scott T. Moe
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Patent number: 5998667Abstract: The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R.sup.1 represents C.sub.1 -C.sub.6 -halogenoalkylthio andR.sup.2 represents hydrogen, orR.sup.1 and R.sup.2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring,X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: June 4, 1998Date of Patent: December 7, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Albrecht Marhold, Christoph Erdelen