Patents by Inventor Alexander Pasternak

Alexander Pasternak has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20060178363
    Abstract: The present invention is directed to compounds of the formula (1) Wherein A, B, D, X, Y, n, R1, R3, R4, R5, R15, R16, R17, R18 and the dashed line are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: March 12, 2004
    Publication date: August 10, 2006
    Inventors: Stephen Goble, Alexander Pasternak, Sander Mills, Changyou Zhou, Lihu Yang
  • Publication number: 20060116421
    Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: October 24, 2003
    Publication date: June 1, 2006
    Inventors: Gabor Butora, Sander Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen Goble
  • Publication number: 20060089379
    Abstract: The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: April 25, 2003
    Publication date: April 27, 2006
    Inventors: Richard Jiao, Stephen Goble, Sander Mills, Gregori Morriello, Alexander Pasternak, Lihu Yang, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes
  • Publication number: 20060069088
    Abstract: Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
    Type: Application
    Filed: May 13, 2005
    Publication date: March 30, 2006
    Inventors: Stephen Goble, Sander Mills, Lihu Yang, Alexander Pasternak, Celine Bonnefous, Theodore Kamenecka, Jean-Michel Vernier, John Hutchinson, Essa Hu, Steven Govek
  • Publication number: 20050261325
    Abstract: The present invention is directed to compounds of the formula (1), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: October 24, 2003
    Publication date: November 24, 2005
    Inventors: Gabor Butora, Alexander Pasternak, Lihu Yang, Changyou Zhou
  • Publication number: 20050250781
    Abstract: The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: October 24, 2003
    Publication date: November 10, 2005
    Inventors: Stephen Goble, Alexander Pasternak, Lihu Yang
  • Publication number: 20050107422
    Abstract: The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of an inflammatory or immunoregulatory disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Application
    Filed: August 20, 2004
    Publication date: May 19, 2005
    Inventors: Richard Jiao, Gabor Butora, Stephen Goble, Deodialsingh Guiadeen, Sander Mills, Gregori Morriello, Alexander Pasternak, Cheng Tang, Lihu Yang, Changyou Zhou, Shankaran Kothandaraman, Christopher Moyes
  • Patent number: 6812234
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: November 2, 2004
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.
    Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
  • Publication number: 20040167156
    Abstract: The present invention is directed to compounds of the formula I: 1
    Type: Application
    Filed: April 29, 2003
    Publication date: August 26, 2004
    Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
  • Patent number: 6545023
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and X are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: April 8, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Gabor Butora, William H. Parsons, Alexander Pasternak
  • Patent number: 6387932
    Abstract: This invention relates to non-peptide somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are orally active.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Changyou Zhou, Alexander Pasternak, Gregori Morriello, Liangqin Guo, Yanping Pan, Lihu Yang, Arthur Patchett
  • Publication number: 20020049222
    Abstract: The present invention is directed to compounds of the formula I: 1
    Type: Application
    Filed: August 16, 2001
    Publication date: April 25, 2002
    Inventors: Lihu Yang, Gabor Butora, William H. Parsons, Alexander Pasternak
  • Patent number: 6117880
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: September 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Liangquin Guo, Ralph T. Mosley, Alexander Pasternak, Arthur A. Patchett, Lihu Yang
  • Patent number: 6063796
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Scott Berk, Meng Hsin Chen, David Johnston, Kevin Chapman, Ravi Nargund, James R. Tata, Liangqin Guo
  • Patent number: 6057338
    Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: May 2, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Scott Berk
  • Patent number: 6025372
    Abstract: Somatostatin agonist compounds of formula I are disclosed: ##STR1## including pharmaceutically acceptable salts and hydrates thereof These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome and pain. The compounds are potent with high selectivity toward the receptor subtype 2.Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: February 15, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Kevin Chapman, James R. Tata, Liangqin Guo
  • Patent number: 5770732
    Abstract: Novel pyrrolinone-based compounds mimic or inhibit the biological and/or chemical activity of peptides, including peptide .beta.-strand conformations. Certain compounds contain functionalized pyrrolinone units in place of one or more amino acids of a target peptide.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: June 23, 1998
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Ryan C. Holcomb, Terence Keenan, John L. Wood, Mark Guzman, Alexander Pasternak