Spiro Patents (Class 548/216)
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Patent number: 7268135Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: December 1, 2004Date of Patent: September 11, 2007Assignee: WyethInventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III
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Patent number: 7202251Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: April 10, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Cory R. Theberge, Xu-Fang Zhang, Craig Stump, C. Blair Zartman
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Patent number: 7199125Abstract: The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(?O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.Type: GrantFiled: October 1, 2004Date of Patent: April 3, 2007Assignees: Bristol-Myers Squibb Company, Cerep SAInventors: T. G. Murali Dhar, Edwin Iwanowicz, Michele Launay, Dominique Potin, Magali Jeannine Blandine Maillet, Eric Nicolai
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Patent number: 7153971Abstract: A compound and method for producing an enantiomerically enriched epoxide from an olefin using a chiral ketone and an oxidizing agent is disclosed.Type: GrantFiled: August 28, 2001Date of Patent: December 26, 2006Assignee: Colorado State University Research FoundationInventor: Yian Shi
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Publication number: 20040259896Abstract: The present invention provides a compound of Formula I or Formula II: 1Type: ApplicationFiled: April 23, 2004Publication date: December 23, 2004Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 6822094Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.Type: GrantFiled: July 26, 2002Date of Patent: November 23, 2004Assignee: Aventis Research & Technologies, GmbH & Co. KGInventors: Josef Salbeck, Donald Lupo
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Publication number: 20040220243Abstract: The present invention relates to novel compounds of the formula (I) 1Type: ApplicationFiled: May 21, 2004Publication date: November 4, 2004Inventors: Reiner Fischer, Thomas Bretschneider, Axel Trautwein, Astrid Ullmann, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20040176588Abstract: A method for production of a sugar oxazoline derivative represented by the following general formula (2), comprising the step of:Type: ApplicationFiled: December 30, 2003Publication date: September 9, 2004Inventors: Shin-ichiro Shoda, Masaya Fujita, Masako Suenaga, Kenji Saito
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Patent number: 6777410Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: April 8, 2003Date of Patent: August 17, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20040147759Abstract: The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).Type: ApplicationFiled: November 13, 2003Publication date: July 29, 2004Inventors: Norbert Hofgen, Hildegard Kuss, Ute Egerland, Chris Rundfeldt, Helge Hartenhauer, Antje Gasparic
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Publication number: 20040142948Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: ApplicationFiled: November 7, 2003Publication date: July 22, 2004Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
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Publication number: 20040106655Abstract: The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products.Type: ApplicationFiled: February 10, 2003Publication date: June 3, 2004Inventors: Hiroshi Kitajima, Hiroshi Sakashita, Fumihiko Akahoshi, Yoshiharu Hayashi
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Publication number: 20040087800Abstract: The present invention relates to certain spirooxindole derivatives of the formula I, and pharmaceutically acceptable salts thereof, which exhibit good analgesic properties and are particularly effective in the treatment of chronic pain.Type: ApplicationFiled: October 27, 2003Publication date: May 6, 2004Applicant: AstraZeneca ABInventors: Alf Claesson, Britt-Marie Swahn, Odd-Geir Berge
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Publication number: 20040063965Abstract: Disclosed are compounds of formula III and a process to prepare a compound of formula III 1Type: ApplicationFiled: June 20, 2003Publication date: April 1, 2004Inventors: Michael R. Reeder, Rick J. Imbordino
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Publication number: 20040044018Abstract: There are provided methods for the treatment of diseases involving dysfunction of the peripheral and central nervous system comprising administering one or more Spiro compounds. Also provided and pharmaceutical compositions useful in such methods, compounds for use in the preparation of such pharmaceutical compositions, processes for preparing compounds useful in the practice of such methods, and some novel such compounds per se.Type: ApplicationFiled: May 2, 2003Publication date: March 4, 2004Applicant: ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCHInventors: Abraham Fisher, Nira Bar-Ner, Yishai Karton
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Publication number: 20040039209Abstract: A compound and method for producing an enantiomerically enriched epoxide from an olefin using a chiral ketone and an oxidizing agent is disclosed. In particular, the compound is of the formula: I wherein R1, R2, R3 and R4 are those defined herein.Type: ApplicationFiled: July 15, 2003Publication date: February 26, 2004Inventor: Yian Shi
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Patent number: 6683709Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.Type: GrantFiled: February 7, 2002Date of Patent: January 27, 2004Assignee: Rodenstock GmbHInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Publication number: 20040009976Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: ApplicationFiled: April 30, 2002Publication date: January 15, 2004Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
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Patent number: 6670507Abstract: Compounds of formula I wherein R1 is for example 3-methoxyprop-3-yloxy, R2 is for example methoxy, R3 and R4 are in each case for example isopropyl, and R5 is H2NC(O)—[C(CH3)2]—CH2—, are obtainable by reaction of compounds of formula IV with a metal organic derivative of 1-(3-R1-4-R2-phen-1-yl)-2-R3-3-halogen propanes to form a compound of formula VI, followed by removal of the pseudoephedrine protecting group and the OH group, reaction of the resulting lactone with an amine R5—NH2 and removal of protecting group Z.Type: GrantFiled: January 15, 2003Date of Patent: December 30, 2003Assignee: Speedel Pharma AGInventors: Daniel Bellus, Alessandro Dondoni
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Patent number: 6528534Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: GrantFiled: July 6, 2001Date of Patent: March 4, 2003Assignees: Millennium Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffrey T. Mullaney, Kenneth J. Ruterbories, Michael Paal, Gerd Ruhter, Theo Schotten, Wolfgang Stenzel, Robert M. Scarborough
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Patent number: 6512112Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: June 28, 2001Date of Patent: January 28, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Publication number: 20020193578Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: ApplicationFiled: December 5, 2001Publication date: December 19, 2002Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6444825Abstract: A method for preparing an oxazolidinecarboxylic acid of general formula (I), which is useful for preparing therapeutically active taxoids of general formula (III), from an oxazolidinecarboxylic acid of general formula (II). In formulae (I), (II) and (III), R is a hydrogen atom or an acetyl radical; R1 is a benzyl radical or a radical of the general formula R2—O—CO—, wherein R2 is an optionally substituted alkyl radical, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl; each of R3 and R4, which are the same or different, is hydrogen, alkyl, alkoxy, optionally substituted aryl or optionally substituted aralkyl, or together they form a 4-7 membered ring; R5 is alkenyl, alkynyl, phenyl, formyl, alkanoyl, aroyl, hydroxymethyl, carboxy or alkyloxycarbonyl; and R′ is a hydrogen atom or an alkali or alkaline-earth metal atom or an alkyl radical with 1-4 carbon atoms optionally substituted by phenyl radical.Type: GrantFiled: December 14, 1995Date of Patent: September 3, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Dominique Bourzat, Alain Commerçon
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Patent number: 6444819Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: October 11, 2001Date of Patent: September 3, 2002Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6437145Abstract: The invention concerns a method of producing oxazolidinones of formula (I), wherein R1-R5 have the meanings given in the description, by reacting cyclical anhydrides of formula (II) with carbonyl compounds of general formula (III) at temperatures between ambient temperature and approximately 150° C. The invention also concerns the production of the cyclical anhydrides of formula (II) by reacting N-protected aminodicarboxylic acids of formula (IV) with a dehydrating agent in situ. The invention further concerns the use of oxazolidinones of formula (I) for the &agr;-selective production of esters of formula (V) and amides of general formula (VII).Type: GrantFiled: April 4, 2000Date of Patent: August 20, 2002Assignee: Degussa-Huls AGInventors: Karlheinz Drauz, Günter Knaup, Stefan Retzow
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Publication number: 20020086874Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1Type: ApplicationFiled: December 14, 2001Publication date: July 4, 2002Applicant: American Home Products CorporationInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6387892Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.Type: GrantFiled: June 7, 2001Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6369271Abstract: The invention relates to a process for large-scale industrial production of biphenyl-2-carboxylic acid derivatives (I) wherein R1 and R2 may have the meanings given in the specification and claims.Type: GrantFiled: February 22, 2000Date of Patent: April 9, 2002Assignee: Boehringer Ingelheim Pharma KGInventor: Heinrich Schneider
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Patent number: 6365747Abstract: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.Type: GrantFiled: June 1, 2001Date of Patent: April 2, 2002Assignee: H. Lundbeck A/SInventors: Leone Dall'Asta, Umberto Casazza, Hans Petersen
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Publication number: 20020013325Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: ApplicationFiled: July 6, 2001Publication date: January 31, 2002Inventors: Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffrey T. Mullaney, Kenneth J. Ruterbories, Michael Paal, Gerd Ruhter, Theo Schotten, Wolfgang Stenzel, Robert M. Scarborough
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Patent number: 6340751Abstract: Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): and (IV): represented by the following formula (III): MgR5R6 (III) wherein R5 represents a C1-12 alkyl group, a C2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C1-4 alkyl group, a phenyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom, and R6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR7 group (R7 representingType: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takasago International CorporationInventors: Takao Saito, Toshiyuki Murayama, Takaji Matsumoto, Takashi Miura
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Publication number: 20010041710Abstract: The present invention relates to a compound of the formula 1Type: ApplicationFiled: December 5, 2000Publication date: November 15, 2001Inventors: Ralph P. Robinson, Ellen R. Laird
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Patent number: 6277985Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.Type: GrantFiled: September 9, 1996Date of Patent: August 21, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Robert C. Gadwood, Bharat V. Kamdar
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Patent number: 6271387Abstract: A process produces 1,3-oxazolidine derivatives by reacting an imine derivative of the following formula (1): with an epoxy compound of the following formula (2): to yield an oxazolidine derivative of the following formula (3):Type: GrantFiled: January 27, 2000Date of Patent: August 7, 2001Assignee: Daicel Chemical Industries, Ltd.Inventors: Yasutaka Ishii, Tatsuya Nakano
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Patent number: 6194582Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.Type: GrantFiled: July 31, 1998Date of Patent: February 27, 2001Assignee: Rhone-Poulenc Rorer S.A.Inventors: Hervé Bouchard, Jean-Dominique Bourzat, Alain Commercon
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Patent number: 6107036Abstract: Compounds of the general formula Ia and Ib are described ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, straight-chain or branched C.sub.1 to C.sub.6 lower alkyl or an aryl group optionally substituted by electron-withdrawing groups, R.sup.3 denotes a cleavable group, W is hydrogen, halogen or a pseudohalogen and at least one of the groups R.sup.4 or R.sup.5 is a group stabilizing the dioxetane structure and at most one of the groups R.sup.4 or R.sup.5 represents hydrogen and X or Y represents oxygen, N-R or C(R).sub.2 in which R has the meanings stated for R.sup.1 and R.sup.2 or represents a mesomeric double bond or a carbonyl group and n denotes the number 0 or 1 and m denotes the number 1 or 2, as well as a process for their production. These compounds are new and can be used as substrates in immunological assays and in DNA diagnostics using activating agents for colour formation.Type: GrantFiled: April 20, 1998Date of Patent: August 22, 2000Assignee: Roche Diagnostics GmbHInventors: Dieter Heindl, Hans-Peter Josel, Herbert Von Der Eltz, Rupert Herrmann, Hans-Joachim Holtke, Rainer Beckert, Dieter Weiss, Waldemar Adam
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Patent number: 6020491Abstract: Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Representative monomers have the structure: ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen and from C.sub.1 to C.sub.4 alkyl; R.sup.10 is a bond or parasubstituted phenyl; and R.sup.11 is cyclic amine unit of a 5- to 6-membered heterocyclic ring selected from the group consisting of: (a) 1,3,5-triazine-2,4-dione; (b) 3,4,5,6-tetrahydro(1H)pyrimidin-2-one; and (c) 2-oxazolidinone; R.sup.10 is attached to a linkage carbon of R.sup.11, wherein said linkage carbon of R.sup.11 is a carbon located on the ring of R.sup.11 and is substituted with a substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl, benzyl, and alkyl-substituted benzyl; from 0 to 2 non-linkage carbon members are a carbonyl group; and from 0 to 1 non-linkage carbon member is substituted with a moiety selected from the group consisting of C.sub.1 -C.sub.Type: GrantFiled: July 7, 1998Date of Patent: February 1, 2000Assignee: Auburn UniversityInventors: Shelby D. Wonley, Gang Sun, Wanying Sun, Tay-Yuan Chen
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Patent number: 6015823Abstract: The present invention relates to novel 4-cyclohexylphenyl-oxazolines of the formula (I) ##STR1## in which X.sup.1, X.sup.2, X.sup.3, R.sup.1 and R.sup.2 are each as defined in the description,to processes for their preparation and to their use for controlling animal pests.Type: GrantFiled: May 19, 1999Date of Patent: January 18, 2000Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Patent number: 5962683Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.Type: GrantFiled: June 17, 1997Date of Patent: October 5, 1999Assignee: Ciba Specialty Chemicals Corp.Inventors: Alfred Steinmann, Rolf Mulhaupt
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Patent number: 5902814Abstract: There are provided new compounds of formula I: ##STR1## wherein R represents hydrogen or methyl; andn represents 1 or 2;or a pharmaceutically acceptable acid addition salt thereof, together with processes for preparing them, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful in the treatment of psychotic disorders, intellectual impairment disorders and anxiety.Type: GrantFiled: September 18, 1995Date of Patent: May 11, 1999Assignee: Astra ABInventors: John Charles Gordon, Ronald Conrad Griffith, Robert John Murray, Michael Balestra
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Patent number: 5869680Abstract: This invention relates to a method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 -CO--O- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 and R.sub.4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R.sub.5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, 2-trichloromethylisopropyl).Type: GrantFiled: August 8, 1997Date of Patent: February 9, 1999Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Jean-Manuel Mas, Viviane Massonneau
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Patent number: 5864041Abstract: Racemic or optically active threo-3-(3,4-dihydroxyphenyl)serine can be readily produced via a few short steps by a process involving the steps of reacting a racemic or optically active N-acyl DOPA derivative represented by the formula ?I!: ##STR1## wherein X is a halogen atom; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 independently represent a protecting group for a hydroxyl group; R.sup.3 is a protecting group for carboxyl group; R.sup.4 is an alkyl group which may have a substituent or a phenyl group which may have a substituent; and a carbon marked with the symbol * is an asymmetric carbon, with a halogen radical generator, a cerium (IV) salt, or a persulfate salt in the presence of a copper catalyst to produce racemic or optically active oxazolines represented by the formula ?IV!: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, n and * are as defined above; and thereafter conducting an oxazoline ring opening and removing R.sup.1, R.sup.2 and R.sup.3 and, optionally, removing X when n is 1, 2 or 3.Type: GrantFiled: July 24, 1997Date of Patent: January 26, 1999Assignee: Sumitomo Chemical Company, Ltd.Inventors: Yoshiaki Oda, Kazunori Iwakura
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Patent number: 5840217Abstract: Use of spiro compounds of the formula (I) ##STR1## where K.sup.1 and K.sup.2 are, independently of one another, conjugated systems, in electroluminescence devices.Preferred compounds of the formula (I) are 9,9'-spirobifluorene derivatives of the formula (II) ##STR2## where the benzo groups can be substituted independently of one another. Compounds of the formula (I) have a good solubility in customary organic solvents, improved film-forming properties and a significantly reduced tendency to crystallize. The production of electroluminescence devices is thereby made easier and their service life is increased.Type: GrantFiled: April 5, 1995Date of Patent: November 24, 1998Assignee: Hoechst AktiengesellschaftInventors: Donald Lupo, Josef Salbeck, Hermann Schenk, Thomas Stehlin, Roland Stern, Arno Wolf
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Patent number: 5798376Abstract: The invention relates to new azatrioxaspiroalkenes of the formula (I) ##STR1## in which Ar.sup.1 and Ar.sup.2 are identical or different and independently of one another in each case represent optionally substituted aryl, to processes for their preparation, to new intermediates, and to the use of the azatrioxaspiroalkenes of the formula (I) as pesticides.Type: GrantFiled: July 11, 1996Date of Patent: August 25, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Ulrike Wachendorff-Neumann, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Patent number: 5760029Abstract: This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: March 13, 1997Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joanne Marie Smallheer
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Patent number: 5716989Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.Type: GrantFiled: November 27, 1991Date of Patent: February 10, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl Heinz Thierauch, Peter Verhallen
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Patent number: 5696137Abstract: Azaheterocyclylmethyl-chromans of the formula: ##STR1## in which E represents an azaheterocyclyl group selected from the group consisting of: ##STR2## wherein R.sup.6 represents hydrogen, hydroxyl, halogen or phenyl; andn represents an integer 0-8;and the other substituents are as defined herein;or an optically isomeric form thereof or a salt thereof;are useful to treat anxiety, depression and psychoses.Type: GrantFiled: June 2, 1995Date of Patent: December 9, 1997Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean Marie Viktor De Vry, Wolfgang Dompert, Henning Sommermeyer
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Patent number: 5677462Abstract: Disclosed is a compound of formula VII: ##STR1## where Ar represents an optionally substituted phenyl or .alpha.- or .beta.-naphthyl radical; R.sub.3 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; and R.sub.4 represents hydrogen, a C.sub.1-4 alkyl radical, a C.sub.2-4 alkenyl radical, an aralkyl radical, or an aryl radical; or alternatively R.sub.3 and R.sub.4, together with the carbon atom to which they are linked, form a 4- to 7-membered ring; and R.sub.5 represents an C.sub.1-4 alkyl radical substituted with at least one chlorine atom. The compound of formula VI may be used to manufacture a compound of formula VIII: ##STR2## where Ar, R.sub.3, R.sub.4 and R.sub.5 are defined above; G.sub.1 represents a group protecting the hydroxyl function; and where appropriate, G.sub.2 represents a group protecting the hydroxyl function.Type: GrantFiled: October 31, 1996Date of Patent: October 14, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Jean-Manuel Mas, Viviane Massonneau
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Patent number: 5529998Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 27, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling