Plural Piperidine Rings Patents (Class 546/186)
  • Patent number: 6440996
    Abstract: The invention provides compounds of formula (I): X—L—X1  (I) wherein X and X1 are substituted piperidine, cyclohexane, or tetrahydropyran rings, and L is a linking group between X and X1; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease, depression, or a disease wherein the administration of cocaine is indicated, comprising administering a compound of formula I or a pharmaceutically acceptable salt thereof to a mammal in need of such treatment.
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: August 27, 2002
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Gian Luca Araldi, Amir P. Tamiz
  • Publication number: 20020115754
    Abstract: The invention relates to a process for the preparation of novel Hindered Amine Light Stabilizers having general formula (I): 1
    Type: Application
    Filed: February 22, 2001
    Publication date: August 22, 2002
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Shrojal Mohitkumar Desai, Raj Pal Singh
  • Publication number: 20020111340
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: November 16, 2001
    Publication date: August 15, 2002
    Inventors: Youssef Bennani, Ramin Faghih
  • Patent number: 6414155
    Abstract: Oligomeric compounds and methods of making the compound having the formula: wherein i, j, k, and l are integers from about 0 to 300 and the sum of i, j, k, and l is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcCRd—)n—NH—(Y)m—CO—OD  (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern, and one or more of the hydrogens of the phenylene group may be substituted by a hydrocarbyl group or a functional group; and D is a hydrocarbyl group and the units E, E′ and S are derived from one or more 1-sub
    Type: Grant
    Filed: November 3, 2000
    Date of Patent: July 2, 2002
    Assignee: Cytec Technology Corp.
    Inventors: Thomas Patrick Sassi, Ram Baboo Gupta
  • Publication number: 20020077337
    Abstract: The present invention provides a compound of a formula (I): 1
    Type: Application
    Filed: April 6, 2001
    Publication date: June 20, 2002
    Inventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
  • Publication number: 20020068733
    Abstract: Compounds of formula 1
    Type: Application
    Filed: December 11, 2001
    Publication date: June 6, 2002
    Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
  • Publication number: 20020058654
    Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.
    Type: Application
    Filed: December 21, 2000
    Publication date: May 16, 2002
    Inventors: Steven J. Coats, Louis J. Fitzpatrick, Dennis J. Hlasta, Carolina L. Lanter, Mark J. Macielag, Ke Pan, Ralph A. Rivero, Stephen S. Palmer
  • Patent number: 6388072
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: May 14, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Patent number: 6387930
    Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: May 14, 2002
    Assignee: Schering Corporation
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Publication number: 20020037896
    Abstract: Substituted N-substituted alkoxyphenyl compounds, compositions containing them, and methods of making and using them.
    Type: Application
    Filed: August 6, 2001
    Publication date: March 28, 2002
    Inventors: Michael Bogenstaetter, Wenying Chai, Annette K. Kwok
  • Patent number: 6358980
    Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 19, 2002
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
  • Patent number: 6355695
    Abstract: Compounds of formula I wherein Q1, Q2, Q3, Q4 and Q5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: March 12, 2002
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 6353107
    Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalky group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: March 5, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Andreas Kramer, Peter Nesvadba
  • Patent number: 6342534
    Abstract: Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamines: (i) are capable of uptake by a target cell upon administration thereof to a human or non-human animal; and (ii) upon uptake by the target cell, competitively bind via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell; the polyamines, upon binding to the biological counter-anion
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: January 29, 2002
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 6333338
    Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp IIb/IIIa platelet receptors, and which can be used therepeutically as antithrombotic agents
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: December 25, 2001
    Assignee: Laboratoire L. Lafon
    Inventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
  • Patent number: 6331545
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: December 18, 2001
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Patent number: 6326372
    Abstract: Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: December 4, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Kevin F. Gilbert
  • Publication number: 20010034449
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Application
    Filed: February 21, 2001
    Publication date: October 25, 2001
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Publication number: 20010031872
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Application
    Filed: February 22, 2001
    Publication date: October 18, 2001
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Publication number: 20010025111
    Abstract: Substituted cyanoenamines of the general formula I 1
    Type: Application
    Filed: May 3, 2001
    Publication date: September 27, 2001
    Inventors: John Bondo Hansen, Tina Moller Tagmose, John Patrick Mogensen, Florencio Zaragoza Dorwald, Anker Steen Jorgensen
  • Publication number: 20010020099
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Application
    Filed: February 21, 2001
    Publication date: September 6, 2001
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Publication number: 20010018520
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Application
    Filed: February 21, 2001
    Publication date: August 30, 2001
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Patent number: 6271377
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: August 7, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Publication number: 20010007038
    Abstract: The invention is a catalyst, the use of the catalyst and a method of using the catalyst in the formation of a compound with an amide bond.
    Type: Application
    Filed: February 22, 2001
    Publication date: July 5, 2001
    Inventor: William Leonard Scott
  • Patent number: 6225324
    Abstract: Compounds of formula I are useful antidepressant agents demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: May 1, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Poss, David R. Tortolani, Ronald J. Mattson, Joseph P. Yevich
  • Patent number: 6222046
    Abstract: The invention has disclosed a trifluoroacetoxylation agent and a preparation process of the agent, which is safe and ease to handle, very useful in industry, and represented by the formula (1); wherein R1 to R4 are a substituted or unsubstituted, saturated or unsaturated alkyl group or a substituted or unsubstituted aryl group and can be the same or different, R1 and R2 or R3 and R4 can bond to form a ring containing a nitrogen atom or a nitrogen atom and other hetero atoms, and R1 and R3 can bond to form a ring containing a nitrogen atom or a nitrogen atom and other hetero atoms.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: April 24, 2001
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hidetoshi Hayashi, Hiroshi Sonoda, Kenichi Goto, Kouki Fukumura, Junko Naruse, Teruyuki Nagata
  • Patent number: 6204391
    Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: March 20, 2001
    Assignee: The Regents of the University of California
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
  • Patent number: 6194435
    Abstract: Novel lactams, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of Formula I below: are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: February 27, 2001
    Assignee: Cor Therapeutics, Inc.
    Inventors: Bing-Yan Zhu, Robert M. Scarborough
  • Patent number: 6184232
    Abstract: Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamines: (i) are capable of uptake by a target cell upon administration thereof to a human or non-human animal; and (ii) upon uptake by the target cell, competitively bind via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell; the polyamines, upon binding to the biological counter-anion
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: February 6, 2001
    Assignee: University of Florida
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 6169097
    Abstract: The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy;
    Type: Grant
    Filed: June 22, 1998
    Date of Patent: January 2, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans Eduard Janssens, Fran├žois Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Yves Emiel Maria Van Roosbroeck
  • Patent number: 6166037
    Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: December 26, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
  • Patent number: 6166033
    Abstract: This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents a phenyl group or a substituted phenyl group; R.sup.1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group; Y.sup.1 --Y.sup.2 represents CH--CO or C.dbd.CR.sup.2, wherein R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; and n is an integer of from 1 to 4, or a pharmaceutically acceptable salt thereof. The disclosed compounds are useful as drugs for preventing and treating dopamine D receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia and do not induce extrapyramidal disorders as side effects.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: December 26, 2000
    Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.
    Inventors: Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
  • Patent number: 6127583
    Abstract: A preparation process of an acetylene derivative comprising reacting a compound having a skeleton represented by the formula (1): ##STR1## in the molecular formula with a compound represented by the formula (2): ##STR2## wherein R.sup.1, R.sup.2 R.sup.3 and R.sup.4 are individually an alkyl group having 1 to 6 carbon atoms and can be the same or different, R.sup.1 and R.sup.3 can bond each other to form a ring, and R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 can be bond each other to form one or two heterocyclic rings: or with a compound represented by the formula (3): wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as in the formula (2), and X.sub.1 is a ##STR3## chlorine, bromine or iodine atom.
    Type: Grant
    Filed: March 31, 1999
    Date of Patent: October 3, 2000
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hiroshi Sonoda, Kazunari Okada, Kenichi Goto, Kouki Fukumura, Junko Naruse, Hidetoshi Hayashi, Teruyuki Nagata, Akira Takahashi
  • Patent number: 6126736
    Abstract: The invention relates to a process of using certain piperidine compounds of formula I ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkyl, lower alkoxy or acyl,R.sub.2 is a substituted or unsubstituted mono- or bicyclic radical which is aromatic in type,R.sub.3 is oxygen, --NH-- or --N(C.sub.1-4 -alkyl)-- andR.sub.8 independently at each occurrence is hydrogen or methylfor stabilizing natural or synthetic, organic or inorganic pigments or pigment mixtures in natural or synthetic, polymeric or prepolymeric substrates against the adverse effects of heat and/or light on the light fastness and color stability, respectively, especially against alterations in shade or light-induced bleaching. The invention also relates to a masterbatch composition.
    Type: Grant
    Filed: February 17, 1998
    Date of Patent: October 3, 2000
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Klaus Stoll, Andreas Thuermer, Gilbert Ligner, Joseph Reni Webster
  • Patent number: 6124316
    Abstract: A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: September 26, 2000
    Assignee: Sanofi
    Inventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
  • Patent number: 6096826
    Abstract: A family of piperidone functionalized polymers based on polymers containing a plurality of hydroxyl groups. Piperidone or piperidone derivatives form a cyclic ketal linkage with hydroxyl groups contained on adjacent or alternating carbon atoms of the base polymer. Preferred compositions are piperidone functionalized poly(vinyl alcohol) having the following general formulae: ##STR1## wherein R.sub.1 through R.sub.6 are each independently hydrogen, methyl, or a C.sub.2 to C.sub.4 saturated or unsaturated alkyl groups, R.sub.7 is O.cndot. or OR.sub.8, wherein R.sub.8 is hydrogen or a C.sub.1 to C.sub.4 alkyl or C(.dbd.O)alkyl group; X.sup.- is a salt; x ranges from 50 to 99 mol %; y ranges from 0 to 30 mol %; and z ranges from 1 to 20 mol %. The compounds are useful in ink jet paper coating applications.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: August 1, 2000
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Joseph Rabasco, Eric Howard Klingenberg, Gregory Paul Dado, Robert Krantz Pinschmidt, Jr., John Richard Boylan
  • Patent number: 6043255
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: March 28, 2000
    Assignee: Schering Corporation
    Inventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
  • Patent number: 6040422
    Abstract: The present invention is directed to a process for forming a peptide bond between a first amino acid having a free amino group and a protected carboxy group and a second amino acid or between a peptide having a free amino group and a blocking carboxy group with a second amino acid which comprises (a) reacting the second amino acid of the formula: ##STR1## with a fluoroformamidinium salt of the formula: ##STR2## and (b) reacting the product of (a) with the first amino acid or peptide.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: March 21, 2000
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Louis A. Carpino, Ayman Ahmed El-Faham
  • Patent number: 6037352
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: November 19, 1998
    Date of Patent: March 14, 2000
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 6028082
    Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK.sub.3 receptor antagonists.
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: February 22, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Daniel Bichon, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5998399
    Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: December 7, 1999
    Assignee: Astra Aktiebolag
    Inventors: James E. Macdonald, Robert Gentile, Robert J. Murray
  • Patent number: 5990124
    Abstract: Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.
    Type: Grant
    Filed: October 24, 1997
    Date of Patent: November 23, 1999
    Inventors: Laszlo Gyermek, Chingmuh Lee, Young-Moon Cho
  • Patent number: 5958949
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked ureas and carbamates of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: September 28, 1999
    Assignee: GPI NIL Holdings Inc.
    Inventors: Gregory S. Hamilton, Jia-He Li, Wei Huang
  • Patent number: 5952354
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: September 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
  • Patent number: 5948781
    Abstract: This invention relates to a method of treating cancer by administering a compound of the formula wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E.sup.1, E.sup.2, p, Het' and Het" are defined as indicated in the specification.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: September 7, 1999
    Assignee: Pfizer Inc
    Inventors: Joseph P. Lyssikatos, Robert A. Volkmann
  • Patent number: 5942523
    Abstract: A compound of formula: in which:Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.
    Type: Grant
    Filed: February 29, 1996
    Date of Patent: August 24, 1999
    Assignee: Sanofi
    Inventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
  • Patent number: 5922244
    Abstract: 4-Acylaminopiperidine N-oxides IaA.sup.1 B.sup.1 (Ia)where A.sup.1 is hydrogen or an organic radical and B.sup.1 is a radical IIa ##STR1## where R.sup.1 -R.sup.4 are each C.sub.1 -C.sub.4 -alkyl and R.sup.1 and R.sup.2, on the one hand, and R.sup.3 and R.sup.4, on the other hand, may furthermore be bonded to form a 5-membered or 6-membered ring,R.sup.5 is H or C.sub.1 14 C.sub.4 -alkyl andR.sup.6 is H or C.sub.1 -C.sub.18 -alkyl,are used for stabilizing organic materials against the harmful effect of free radicals, particularly in the distillation of monomers which undergo free radical polymerization, especially styrene.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: July 13, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Koch, Alexander Aumuller, Konrad Mitulla, Gregor Tremmel, Holger Herbst
  • Patent number: 5908934
    Abstract: A process for the preparation of compounds of formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, m, n and q are as defined herein; which comprises the steps of (a)reacting a compound of formula III ##STR2## with a chiral acid in an organic solvent to form a salt of a compound of formula I and (b) treating the salt of a compound of formula I with an aqueous base to obtain the compounds of formula I. Compounds of formula I are intermediates useful in the preparation of protein kinase inhibitors.
    Type: Grant
    Filed: September 12, 1997
    Date of Patent: June 1, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventor: Kyoung Soon Kim
  • Patent number: 5889006
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: March 30, 1999
    Assignee: Schering Corporation
    Inventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle