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: 20100286123
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: April 27, 2010
    Publication date: November 11, 2010
    Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
  • Publication number: 20100256106
    Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.
    Type: Application
    Filed: November 25, 2008
    Publication date: October 7, 2010
    Applicant: MERCK & CO., INC.
    Inventors: Alexander Pasternak, Michael J. Szymonifka
  • Publication number: 20100184758
    Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
    Type: Application
    Filed: July 15, 2008
    Publication date: July 22, 2010
    Inventors: Peter H. Dobbelaar, Wu Du, Liangqin Guo, William K. Hagmann, Shuwen He, Tianying Jian, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Shrenik K. Shah, Quang T. Truong, Zhixiong Ye, James Deliureficio, Raman Bakshi
  • Patent number: 7700772
    Abstract: Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain 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. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Grant
    Filed: February 8, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lihu Yang, Alexander Pasternak, Sander G. Mills
  • Patent number: 7700591
    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: Grant
    Filed: May 13, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Sander G. Mills, Lihu Yang, Alexander Pasternak, Celine Bonnefous, Theodore M Kamenecka, Jean-Michel Vernier, John H. Hutchinson, Essa Hu, Steven Govek
  • Patent number: 7598243
    Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines 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: Grant
    Filed: October 15, 2004
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Stephen D. Goble, Alexander Pasternak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
  • Patent number: 7557120
    Abstract: The present invention is directed to compounds of formulae (I and II)(wherein A, D, E, X, l, m, n and R1 through R18 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: February 23, 2004
    Date of Patent: July 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Cheng Tang, Changyou Zhou, Lihu Yang
  • Patent number: 7514431
    Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z 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: Grant
    Filed: October 24, 2003
    Date of Patent: April 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Changyou Zhou, Alexander Pasternak, Lihu Yang
  • Patent number: 7491737
    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: Grant
    Filed: October 24, 2003
    Date of Patent: February 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Lihu Yang
  • Patent number: 7410961
    Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain 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. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: August 12, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Sander G. Mills, Changyou Zhou, Stephen D. Goble, Alexander Pasternak
  • Patent number: 7393844
    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.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: July 1, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Sander G. Mills, Changyou Zhou, Lihu Yang
  • Patent number: 7390803
    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.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: June 24, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
  • Publication number: 20070238723
    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: October 15, 2004
    Publication date: October 11, 2007
    Inventors: Stephen Goble, Sander Mills, Lihu Yang, Alexander Pasternak
  • Publication number: 20070179158
    Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain 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. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Application
    Filed: January 14, 2005
    Publication date: August 2, 2007
    Inventors: Lihu Yang, Sander Mills, Changyou Zhou, Stephen Goble, Alexander Pasternak
  • Patent number: 7247725
    Abstract: The present invention is directed to compounds of the formula (I), 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: Grant
    Filed: October 24, 2003
    Date of Patent: July 24, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Alexander Pasternak, Lihu Yang, Changyou Zhou
  • Publication number: 20070149529
    Abstract: Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain 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. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Application
    Filed: February 8, 2005
    Publication date: June 28, 2007
    Inventors: Lihu Yang, Alexander Pasternak, Sander Mills
  • Patent number: 7230008
    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: Grant
    Filed: August 20, 2004
    Date of Patent: June 12, 2007
    Assignee: Merck & Co, Inc.
    Inventors: Richard Jiao, Gabor Butora, Stephen D. Goble, Deodialsingh Guiadeen, Sander G. Mills, Gregori Morriello, Alexander Pasternak, Cheng Tang, Lihu Yang, Changyou Zhou, Shankaran Kothandaraman, Christopher Moyes
  • Patent number: 7166614
    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.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: January 23, 2007
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Richard Jiao, Stephen D. Goble, Sander G. Mills, Gregori Morriello, Alexander Pasternak, Lihu Yang, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes
  • Publication number: 20070004714
    Abstract: The present invention is directed to compounds of formulae (I and II) (wherein A, D, E, X, l, m, n and R1 through R18 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: February 23, 2004
    Publication date: January 4, 2007
    Applicant: MERCK & CO., INC.
    Inventors: Stephen Goble, Alexander Pasternak, Cheng Tang, Changyou Zhou, Lihu Yang
  • Publication number: 20060183731
    Abstract: The present invention is directed to compounds of the formula: wherein R1, R1, R3, R4, R5, R6, R7, R8, R9, R10 and R16 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: July 9, 2004
    Publication date: August 17, 2006
    Inventors: Min Ge, Stephen Goble, Alexander Pasternak, Lihu Yang