Patents by Inventor Lihu Yang

Lihu Yang 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: 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: 20070155731
    Abstract: Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, 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: January 26, 2005
    Publication date: July 5, 2007
    Inventors: Gabor Butora, Deodialsingh Guiadeen, Shankaran Kothandaraman, Malcolm MacCoss, Sander Mills, Lihu Yang
  • 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
  • Publication number: 20070135475
    Abstract: The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine.
    Type: Application
    Filed: October 25, 2004
    Publication date: June 14, 2007
    Inventors: Dongwei Cai, Fred Fleitz, Min Ge, Scott Hoerner, Gary Javadi, Mark Jensen, Robert Larsen, Wenjie Lie, Dorian Nelson, Elizabeth Szumigala, Lihu Yang, Changyou Zhou
  • 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
  • Publication number: 20070117797
    Abstract: Compounds of the formula (I) which are modulators of chemokine receptor activity 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, and 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: December 29, 2004
    Publication date: May 24, 2007
    Inventors: Stephen Goble, Lihu Yang, Changyou Zhou, Shankaran Kothandaraman, Deodialsingh Guiadeen, Gabor Butora, Alexander Pastemak, Sander Mills
  • Publication number: 20070021453
    Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
    Type: Application
    Filed: July 14, 2006
    Publication date: January 25, 2007
    Inventors: Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
  • 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: 20060211722
    Abstract: The present invention is directed to compounds of the formulas I and II: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R25, R26, Y, Z, l, m, 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: Application
    Filed: March 15, 2004
    Publication date: September 21, 2006
    Inventors: Richard Jiao, Lihu Yang
  • Publication number: 20060205783
    Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 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: August 6, 2004
    Publication date: September 14, 2006
    Inventors: Gabor Butora, Lihu Yang, Stephen Goble
  • 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
  • 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: 20060173013
    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: Application
    Filed: October 24, 2003
    Publication date: August 3, 2006
    Inventors: Changyou Zhou, Alexander Pastemak, 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: 20060030582
    Abstract: The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of a disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of 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 8, 2005
    Publication date: February 9, 2006
    Inventors: Julie DeMartino, Taro Akiyama, Mary Struthers, Lihu Yang, Joel Berger, Gregori Morriello, Alexander Pastemak, Changyou Zhou, Sander Mills, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Cheng Tang, Richard Jiao, Stephen Goble, Christopher Moyes