Patents Represented by Attorney, Agent or Law Firm J. Eric Thies
  • Patent number: 8349872
    Abstract: The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
  • Patent number: 8283360
    Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 9, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
  • Patent number: 8268842
    Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 18, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Patent number: 8263627
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
  • Patent number: 8263586
    Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, David B. Whitman
  • Patent number: 8252799
    Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
  • Patent number: 8242121
    Abstract: The present invention is. directed to pyridyl piperidine compounds of formula (I) which are antagonists of orexin receptors, and which are useful' in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, John D. Schreier
  • Patent number: 8242143
    Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
  • Patent number: 8163770
    Abstract: Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: April 24, 2012
    Assignee: MSD. K. K.
    Inventors: Takashi Mizutani, Nagaaki Sato, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8158791
    Abstract: A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: April 17, 2012
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Nagaaki Sato, Daisuke Tsukahara
  • Patent number: 8158652
    Abstract: Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lower alkyl et al], or pharmaceutical acceptable salts thereof. These have a potency antagonistic to binding to histamine H3 receptor, or have a potency inhibiting the constant activity of histamine H3 receptor, and are useful in the therapy of obesity, diabetes et al.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: April 17, 2012
    Assignee: MSD K.K.
    Inventors: Norikazu Ohtake, Takuya Suga, Shigeru Tokita
  • Patent number: 8138206
    Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
    Type: Grant
    Filed: May 29, 2006
    Date of Patent: March 20, 2012
    Assignee: MSD. K.K.
    Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
  • Patent number: 8101618
    Abstract: A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: January 24, 2012
    Assignee: MSD K.K.
    Inventors: Hiroshi Kawamoto, Toshifumi Kimura, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
  • Patent number: 8044070
    Abstract: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: October 25, 2011
    Assignee: MSD K.K.
    Inventors: Norikazu Ohtake, Akira Naya, Yuji Haga, Makoto Jitsuoka, Takuya Suga, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani
  • Patent number: 8030495
    Abstract: The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: October 4, 2011
    Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
  • Patent number: 8003797
    Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: August 7, 2008
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
  • Patent number: 7960394
    Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
    Type: Grant
    Filed: May 30, 2005
    Date of Patent: June 14, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Patent number: 7960402
    Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: June 14, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Makoto Jitsuoka, Norikazu Ohtake, Nagaaki Sato, Shigeru Tokita, Daisuke Tsukahara
  • Patent number: 7951797
    Abstract: The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: May 31, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox
  • Patent number: 7902369
    Abstract: The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: March 8, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki