Patents Represented by Attorney, Agent or Law Firm Norbert Gruenfeld
  • Patent number: 6878707
    Abstract: Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enanti
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: April 12, 2005
    Assignee: Novartis AG
    Inventor: Gary Michael Ksander
  • Patent number: 6790978
    Abstract: Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 14, 2004
    Assignee: Novartis AG
    Inventor: Paivi Jaana Kukkola
  • Patent number: 6777443
    Abstract: Compounds of the formula wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: August 17, 2004
    Assignee: Novartis AG
    Inventor: Cynthia Anne Fink
  • Patent number: 6727281
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: July 23, 2002
    Date of Patent: April 27, 2004
    Assignee: Novartis AG
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
  • Patent number: 6689896
    Abstract: Compounds of the formula in which W is O, S, S(O) or S(O)2; X is —SR4, —S(O)R4, or —S(O)2R4, —S(O)2NR5R6; or X is —C(O)NR5R6 provided that —C(O)NR5R6 is located at the 3′, 4′ or 5′ position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or —NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring;
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: February 10, 2004
    Assignee: Novartis AG
    Inventor: Paivi Janna Kukkola
  • Patent number: 6689801
    Abstract: Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: February 10, 2004
    Assignee: Novartis AG
    Inventors: Cynthia A. Fink, Faribroz Firooznia
  • Patent number: 6645970
    Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
    Type: Grant
    Filed: November 5, 2001
    Date of Patent: November 11, 2003
    Assignee: Novartis AG
    Inventors: Rainer Albert, Nigel Graham Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jürgen Wagner, Gerhard Zenke
  • Patent number: 6642225
    Abstract: Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: November 4, 2003
    Assignee: Novartis AG
    Inventors: Rainer Albert, Janet Dawson, Claus Ehrhardt, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach
  • Patent number: 6642239
    Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof: In which R1 and R2 are independently H or C1-C7lower alkyl, or R1 and R2 together with the carbon atom to which they are attached form a C3-C8cycloalkyl ring, and Het is an optionally substituted nitrogen-containing heterocyclic substituent, are provided, useful e.g. for therapeutic or prophylactic treatment of a disease or medical condition in which cathepsin K is implicated.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: November 4, 2003
    Assignee: Novartis AG
    Inventor: Martin Missbach
  • Patent number: 6613782
    Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: September 2, 2003
    Assignee: Novartis AG
    Inventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
  • Patent number: 6599942
    Abstract: Compounds of the formula in which W is O, S, S(O) or S(O)2; X is —SR4, —S(O)R4, or —S(O)2R4, —S(O)2NR5R6; or X is —C(O)NR5R6 provided that —C(O)NR5R6 is located at the 3′, 4′ or 5′ position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or —NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring;
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: July 29, 2003
    Assignee: Novartis AG
    Inventor: Paivi Janna Kukkola
  • Patent number: 6451858
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: September 13, 2001
    Date of Patent: September 17, 2002
    Assignee: Novartis AG
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
  • Patent number: 6432923
    Abstract: Compounds of the formula I as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, particularly inflammatory airways diseases. They are particularly useful in reducing post-surgical inflammation, especially that resulting from transplant surgery.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 13, 2002
    Assignee: Novartis AG
    Inventors: Sompong Wattanasin, Peter Josef Von Matt
  • Patent number: 6426354
    Abstract: Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: July 30, 2002
    Assignee: Novartis AG
    Inventors: Cynthia Anne Fink, Fariborz Firooznia
  • Patent number: 6423727
    Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: July 23, 2002
    Assignee: Novartis AG
    Inventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
  • Patent number: 6407065
    Abstract: Compounds of the formula I as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, particularly inflammatory airways diseases. They are particularly useful in reducing post-surgical inflammation, especially that resulting from transplant surgery.
    Type: Grant
    Filed: January 19, 1999
    Date of Patent: June 18, 2002
    Assignee: Novartis AG
    Inventors: Sompong Wattanasin, Peter Josef Von Matt
  • Patent number: 6399599
    Abstract: Compounds of formula I wherein n is 1, 2 or 3; R1 is H, C1-4alkyl, aryl, or aryl-C1-4alkyl; Y is C1-4alkylene, —CO—C1-4alkylene, —CO—C2-5alkenylene, —CO—NH—, —CO—C1-3alkylene-NH—, or —CO—O—; R2 is an aromatic or heteroaromatic residue, each being optionally substituted by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; R3is the side chain present on the C&agr; of an &agr;-amino acid; R4 is biphenylyl, benzyl, hydroxy-benzyl, &agr;- or &bgr;-naphthyl-methyl, 5,6,7,8-tetrahydro-&bgr;-naphthyl-methyl or indolyl-methyl, each being optionally substituted on the ring by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; and X is —CN, —NR5R6 or —O—R8 wherein R5 is H, C1-6alkyl, aryl or aryl-C1-4alkyl; R6 is H or C1-6alkyl;
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: June 4, 2002
    Assignee: Novartis AG
    Inventors: Rainer Albert, Josef G. Meingassner, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach, Ulrich Hommel, Claus Ehrhardt, Didier Roche, Joerg Kallen
  • Patent number: 6353017
    Abstract: N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: March 5, 2002
    Assignee: Novartis AG
    Inventors: Eva Altmann, Claudia Betschart, Keigo Gohda, Miyuki Horiuchi, Rene Lattmann, Martin Missbach, Junichi Sakaki, Michihiro Takai, Naoki Teno, Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry van Duzer
  • Patent number: 6310099
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: November 27, 2000
    Date of Patent: October 30, 2001
    Assignee: Novartis Ag
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
  • Patent number: 6291530
    Abstract: Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di cabocyclic or heterocyclic aryl)-lower alkyl; R1 is hydrogen or lower alkyl; R2 and R3 are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R2 and R3 joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, S2 or a direct bond; X1 is O, S, SO, SO2 or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl,, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester, and pharmaceutically acceptable salts thereof; which arm useful as LTB-4 antagonists.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: September 18, 2001
    Assignee: Novartis AG
    Inventors: Paul David Greenspan, Roger Aki Fujimoto