Publication number: 20030050309
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Type:
Application
Filed:
September 12, 2001
Publication date:
March 13, 2003
Inventors:
Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
Patent number: 6514996
Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I):
wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C
Type:
Grant
Filed:
November 19, 1997
Date of Patent:
February 4, 2003
Assignee:
Kyowa Hakko Kogyo Co., Ltd.
Inventors:
Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
Patent number: 6380197
Abstract: Provided herein are novel polyhydroxyalkylpyrazine derivatives useful in treating and preventing a plethora of diseases including diabetes, having a general formula of
wherein Rc1 represents the chain (II) —CH(OR4)CH(OR3)CH(OR2)CH2OR1 and either Rc2 represents a hydrogen atom and either Rc3 represents the chain (III)—CH2CH(OR6)CH(OR7)CH2OR8 or Rc2 represents the chain (IV)—CH(OR5)CH(OR6)CH(OR7)CH2OR8 or chain (III) —CH2CH(OR6)CH(OR7)CH2OR8 and Rc3 represents a hydrogen atom, and 1 to 8 substituents R1, R2, R3, R4, R5, R6, R7, R8, identical or different, represent a radical independently selected among the radicals a) —COR9, b) —COOR10, c) —CR11R12OCOR13, d) —CR11R12OR13, e) —CONR14R15, and f) one or more pairs of the substituents R1, R2, R3, R4, R6, R7, R8, consecutive or separated by one of the other substituents R2, R3, R6, R7 can also form a group: —C(O)—; the other substituents R1, R2, R3, R4, R6, R7, R8 are hydrogen atoms
Type:
Grant
Filed:
January 18, 2000
Date of Patent:
April 30, 2002
Assignee:
Aventis Pharma S. A.
Inventors:
Hervé Bouchard, Alain Commercon, Jean-François Peyronel, Corinne Terrier