The Spiro Includes The Five-membered Hetero Ring Patents (Class 548/408)
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Publication number: 20040009999Abstract: The invention concerns substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives depicted by the formula: 1Type: ApplicationFiled: February 24, 2003Publication date: January 15, 2004Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Publication number: 20030232872Abstract: Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.Type: ApplicationFiled: May 6, 2003Publication date: December 18, 2003Inventors: Richard Glennon, Richard Westkaemper
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Publication number: 20030229072Abstract: Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.Type: ApplicationFiled: March 3, 2003Publication date: December 11, 2003Inventors: William H Bullock, Harold C E Kluender, William L Collibee, Robert Dally, Martha E Rodriguez, Ming Wang
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Publication number: 20030212278Abstract: The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I 1Type: ApplicationFiled: April 8, 2003Publication date: November 13, 2003Inventors: Csaba Gonczi, Eva Csikos, Istvan Hermecz, Gergely Heja, Arpad Illar, Lajos Nagy, Andrea Santane Csutor, Attila Simon, Kalman Simon, Agota Smelkone Esek, Tiborne Szomor, Gyorgyne Szvoboda
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Publication number: 20030158178Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.Type: ApplicationFiled: October 30, 2002Publication date: August 21, 2003Applicant: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6608068Abstract: 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: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: December 11, 2001Date of Patent: August 19, 2003Assignees: Wyeth, Ligand PharmaceuticalsInventors: 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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Publication number: 20030144292Abstract: The compounds have a structure according to the following Formula (I): 1Type: ApplicationFiled: September 18, 2002Publication date: July 31, 2003Inventors: Michael George Natchus, Stanislaw Pikul, Neil Gregory Almstead, Matthew John Laufersweiler, Biswanath De
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Publication number: 20030138791Abstract: The invention concerns sterically shielded, stabilized fluorescent dyes based on symmetrical or unsymmetrical 3-spirocyanines and their utilization as marker-molecules in analytical procedures. The fluorescent dyes according to the invention are characterized by a strongly reduced proneness towards aggregation due to the insertion of bulky spiro-substituents and thus enable to reach a high degree of coupling to the target molecule without a significant loss of fluorescence due to self quenching effects. They therefor exhibit a high quantum yield and are thus excellently suitable as fluorescent dyes, especially as NIR-fluorescent dyes, for the coupling or binding to biological and non-biological target molecules used in analytical methods. The analytical methods comprise all methods in which fluorescence-optical methods are used to detect biological and non-biological molecules.Type: ApplicationFiled: September 19, 2002Publication date: July 24, 2003Inventors: Lutz Haalck, Erk Gedig, Hans-Juergen Hoelpert, Viola Podsadlowski
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Patent number: 6589976Abstract: The invention relates to novel spirocyclic phenylketoenols of the formula in which Het represents one of the groups in which Q represents and X, Y, Z, m, n, R6, R9, R10 and R11 are each as defined in the description, to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2000Date of Patent: July 8, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Markus Dollinger, Andreas Turberg
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Publication number: 20030119858Abstract: Novel substituted amino acids of formula 1Type: ApplicationFiled: October 22, 2002Publication date: June 26, 2003Inventors: Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
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Publication number: 20030099910Abstract: The present invention relates to a photochromic spirobenzopyran compound of the formula (1) and its derivatives, a spirobenzopyran group having unsaturated terminal groups, a polymer prepared therefrom, a method for the production thereof, a composition comprising said spirobenzopyran or said spirobenzopyran group-containing polymer and a photochromic switch film using the same: 1Type: ApplicationFiled: August 24, 1999Publication date: May 29, 2003Inventors: EUN-KYOUNG KIM, YUN-KI CHOI, SAM-ROK KEUM
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Patent number: 6562857Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB, RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoType: GrantFiled: January 9, 2002Date of Patent: May 13, 2003Assignee: WyethInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030013861Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): 1Type: ApplicationFiled: July 24, 2002Publication date: January 16, 2003Inventors: Long Y. Chiang, Vijayaraj Anantharaj
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Publication number: 20030009055Abstract: A process for the preparation of gabapentin of formula (I) 1Type: ApplicationFiled: May 29, 2002Publication date: January 9, 2003Applicant: PROCOS S.P.AInventors: Francesco Velardi, Mirco Fornaroli
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Patent number: 6458965Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketonols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: January 2, 2001Date of Patent: October 1, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretshneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Publication number: 20020132792Abstract: Aryl-substituted indirubin derivatives, their production and their intermediate products for production, as well as their use as medications for treating cancer, such as solid tumors and leukemia; auto-immune diseases, such as psoriasis, alopecia and multiple sclerosis, chemotherapy agent-induced alopecia and mucositis; cardiovascular diseases, such as stenoses, arterioscleroses and restenoses; infectious diseases, such as, e.g., those caused by unicellular parasites, such as trypanosoma, toxoplasma or plasmodium, or those caused by fungi; nephrological diseases, such as, e.g., glomerulonephritis; chronic neurodegenerative diseases, such as Huntington's disease, amyotrophic lateral sclerosis, Parkinson's disease, AIDS dementia and Alzheimer's disease; acute neurodegenerative diseases, such as ischemias of the brain and neurotraumas; viral infections, such as, e.g., cytomegalic infections, herpes, hepatitis B and C, and HIV diseases, are described.Type: ApplicationFiled: November 29, 2001Publication date: September 19, 2002Applicant: Schering AGInventors: Olaf Prien, Andreas Steinmeyer, Gerhard Siemeister, Rolf Jautelat
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Patent number: 6417370Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogeno-alkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenyl-alkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their use as pesticides and herbicides.Type: GrantFiled: October 23, 2000Date of Patent: July 9, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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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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Publication number: 20020068735Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1Type: ApplicationFiled: January 9, 2002Publication date: June 6, 2002Applicant: American Home Products CorporationInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6391907Abstract: 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: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: April 19, 2000Date of Patent: May 21, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: 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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Publication number: 20020058813Abstract: Compounds of general structural formula I such as that shown in structural formula II 1Type: ApplicationFiled: June 29, 2001Publication date: May 16, 2002Inventors: Ying-Duo Gao, Douglas J. Macneil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6384069Abstract: 2-Pyrrolidinone derivatives substituted in position 4 are provided according to the invention for use as therapeutic active ingredient. It has been found, surprisingly, that these compounds are able markedly to reduce the extracellular glutamate level, and the compounds are therefore suitable for the prophylaxis and treatment of a large number of disorders, in particular, stroke.Type: GrantFiled: July 12, 2000Date of Patent: May 7, 2002Assignee: Klinikum der Albert-Ludwigs-UniversitaetInventors: Thomas J. Feuerstein, Rainer Knoerle
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Patent number: 6358887Abstract: The present invention relates to new compounds of the formula (I) in which X, Y and Z have the meanings given in the description and Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: August 5, 1997Date of Patent: March 19, 2002Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
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Publication number: 20020019540Abstract: Novel substituted amino acids of formula 1Type: ApplicationFiled: August 8, 2001Publication date: February 14, 2002Inventors: Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
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Patent number: 6316638Abstract: Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: August 16, 2000Date of Patent: November 13, 2001Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
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Patent number: 6262060Abstract: The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes, obesity or inflammation utilizing them.Type: GrantFiled: November 27, 2000Date of Patent: July 17, 2001Assignee: Sanofi-SynthelaboInventors: Manuel Bedoya-Zurita, Juan Antonio Diaz Martin, Marc Daumas
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Patent number: 6218548Abstract: A compound represented by formula (III): wherein n is an integer of 2 to 5; and R11 represents a substituent group represented by formula: wherein Ra, Rb and Rc each represents a phenyl, phenylmethyl or naphthyl group (which may be substituted with at least one substituent group selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, a halogen atom and a nitro group), a hydrogen atom, or an alkyl group having 1 to 4 carbon atoms, with the proviso that Ra, Rb and Rc are different from one another, and a salt thereof.Type: GrantFiled: November 23, 1999Date of Patent: April 17, 2001Assignee: Daiichi Paharmaceutical Co., Ltd.Inventors: Toshifumi Akiba, Tutomu Ebata, Tatsuru Saito, Sadahiro Shimizu, Keiichi Hirai, Naoki Ohta, Toshiaki Tojo
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Patent number: 6197974Abstract: The invention relates to a process of preparing a chiral compound of the formula: wherein R1 is selected from the group consisting of hydrogen and lower alkyl, and R2 and R2′ are the same, and R2 and R2′ are selected from a group consisting of hydrogen and primary alkyl, or R2 and R2′ taken together form a C3 to C6 cycloalkyl, comprising the steps of chirally reducing a &bgr;-keto ester to afford a &bgr;-hydroxy ester, activating the &bgr;-hydroxy ester by treatment with a sulfonic acid or a derivative thereof to provide an activated compound having sulfonate leaving group, displacing the sulfonate leaving group with an azido moiety, or treating the activated compound with an alkylamine, deprotecting and cyclizing to afford a pyrrolidinone, and reducing the pyrrolidinone to afford a stereoisomerically preferred 3-aminopyrrolidine derivative.Type: GrantFiled: October 25, 1999Date of Patent: March 6, 2001Assignee: Abbott LaboratoriesInventors: Daniel J. Plata, Steven A. King, Frederick A. Plagge, Anne E. Bailey, Louis Seif
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Patent number: 6191160Abstract: Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.Type: GrantFiled: November 8, 1999Date of Patent: February 20, 2001Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6175020Abstract: Azaspirononanes of formula I and their synthesis are disclosed. The compounds are useful as templates for constructing synthetic receptors and as intermediates in the synthesis of enzyme inhibitors. They are prepared by an intramolecular ylide cycloaddition of a 6-hydrazone of 2,10-undecadienoic acid ester.Type: GrantFiled: April 9, 1999Date of Patent: January 16, 2001Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Michael C. Barden
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Patent number: 6166057Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.Type: GrantFiled: November 4, 1998Date of Patent: December 26, 2000Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 6110872Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in whichHet represents one of the groups ##STR1## wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.Type: GrantFiled: December 22, 1997Date of Patent: August 29, 2000Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
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Patent number: 6015912Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: January 18, 2000Assignee: The Procter & Gamble CompanyInventors: Zhe Wang, Neil Gregory Almstead, Rimma Sandler Bradley, Michael George Natchus, Biswanath De, Stanislaw Pikul, Yetunde Olabisi Taiwo
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Patent number: 6013806Abstract: This invention is to provide a compound represented by the following formula (I) and a compound represented by the following formula (II) useful as an antibacterial agent which is obtained by the compound of formula (I), and also to provide a novel synthetic process for the inexpensive, short-step and industrially advantageous production thereof.Type: GrantFiled: July 9, 1998Date of Patent: January 11, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toshifumi Akiba, Tutomu Ebata, Tatsuru Saito, Sadahiro Shimizu, Keiichi Hirai, Naoki Ohta, Toshiaki Tojo
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Patent number: 5994274Abstract: The present invention relates to new compounds of the formula (I) ##STR1## in which X represents alkyl,Y represents halogen or alkyl andZ represents halogen or alkyl,with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl,Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description,a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: December 23, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 5952365Abstract: The present invention is directed to an improved antihyperlipidemic agent, the dimaleate salt of 2-?2-(dimethylamino)ethyl!-8,8-dipropyl-2-azaspiro?4.5!decane.Type: GrantFiled: January 12, 1998Date of Patent: September 14, 1999Assignee: AnorMED Inc.Inventors: Raymond E Dagger, Carolyn W Grady
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Patent number: 5939450Abstract: An improved immunomodulatory agent, the dimaleate salt of N,N-dimethyl-8,8-dipropyl-2-azaspiro?4.5!decane-2-propanamine.Type: GrantFiled: January 12, 1998Date of Patent: August 17, 1999Assignee: AnorMED Inc.Inventors: Raymond E Dagger, Carolyn W Grady
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Patent number: 5830826Abstract: The present invention relates to novel 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, G, X, Y and Z have the meaning given in the description, to processes for their preparation and to intermediates for this purpose. The compounds of the formula (I) are used as pesticides and herbicides.Type: GrantFiled: September 27, 1996Date of Patent: November 3, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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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: 5744495Abstract: An improved immumomodulatory agent, the dimaleate salt of N,N-diethyl-8,8-dipropyl-2-azaspiro?4.5!decane-2-propanamine.Type: GrantFiled: July 12, 1996Date of Patent: April 28, 1998Assignee: SmithKline Beecham CorporationInventors: Raymond E. Dagger, Carolyn W. Grady
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Patent number: 5734061Abstract: The invention is directed to an improved process for the preparation of spirocyclic lactams which utilizes diiodides in the spiro alkylation of lactams N-substituted with a tertiary amine group. The resultant spirocyclic lactams are useful in the production of various substituted azaspiranes which are useful as immunomodulatory agents.Type: GrantFiled: June 13, 1996Date of Patent: March 31, 1998Assignee: SmithKline Beecham CorporationInventor: David Ryckman
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Patent number: 5723625Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.Type: GrantFiled: October 4, 1996Date of Patent: March 3, 1998Assignee: Immodal Pharmaka Gesellschaft m.b.HInventors: Dietmar Keplinger, Klaus Keplinger, Gerhard Laus
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Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
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Patent number: 5686461Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl group;X represents a bond or a C.sub.1-4 alkylene chain;R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.Type: GrantFiled: September 18, 1995Date of Patent: November 11, 1997Assignee: Glaxo Wellcome S.p.A.Inventors: Alfredo Cugola, Giovanni Gaviraghi, Fabrizio Micheli
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Patent number: 5622917Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: January 3, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5616536Abstract: There are provided substituted 3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## The new compounds (I) have highly pronounced insecticidal, acaricidal and herbicidal properties.Type: GrantFiled: June 3, 1996Date of Patent: April 1, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Bernd-Wieland Kruger, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5602078Abstract: Dialkyl-1-H-3-(2,4-dimethylphenyl)-pyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents alkyl which is optionally substituted by halogen andB represents C.sub.2 -C.sub.10 -alkyl orA and B together with the carbon atom to which they are bonded represent an unsubstituted cycle,G represents hydrogen,L and M represent oxygen and/or sulphur. These compounds possess herbicidal and pesticidal activity.Type: GrantFiled: December 4, 1995Date of Patent: February 11, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 5591748Abstract: Invented are substituted azaspirane compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to induce an immunosuppressive effect in a mammal in need thereof.Type: GrantFiled: July 19, 1994Date of Patent: January 7, 1997Assignee: SmithKline Beecham CorporationInventors: Alison M. Badger, Gary J. Bridger, David A. Schwartz
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Patent number: 5589596Abstract: A process is disclosed for producing an amine by carrying out a reductive amination of a cyclic ketone or by carrying out a reduction of an imino derivative of a cyclic ketone to the corresponding amine which process is characterized in using a cobalt catalyst containing a carbonate of an alkaline earth metal and/or lanthanum oxide.Type: GrantFiled: February 8, 1994Date of Patent: December 31, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Atsushi Furutani, Takuo Hibi, Michio Yamamoto, Kazuyuki Tanaka, Kazuhiro Tada, Masami Fukao, Gohfu Suzukamo
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Patent number: 5587479Abstract: Compounds of general formula (I), in which r is 1 or 2, R.sub.1 is selected independently from: unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, the 2(beta)-naphthyl group, and heterocyclic, monocyclic or dicyclic groups; R.sub.2 is selected independently from: heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups, and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group comprising from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group.Type: GrantFiled: October 11, 1994Date of Patent: December 24, 1996Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati