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    • 2. 发明专利
    • New applications of amino acid antispasmodics
    • JP4307068B2
    • 2009-08-05
    • JP2002520843
    • 2001-08-24
    • リサーチ コーポレイション テクノロジーズ,インコーポレイテッドResearch Corporation Technologies, Inc.
    • ロバート エイチ. ハリス、
    • A61K31/16A61K38/00A61K31/165A61K31/195A61P25/04A61P25/06A61P29/00C07K5/10
    • A61K38/05A61K31/16A61K31/165A61K31/195A61K31/40A61K31/44A61K38/04
    • The present invention describes the use of a compound of the following formula (I) for the manufacture of a medicament effective in the treatment or prevention of bipolar disease of a mammal: wherein R is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl lower alkyl, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with at least one electron withdrawing or electron donating group; R1  is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocyclic lower alkyl, heterocyclic, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with an electron donating or an electron withdrawing group; R2 and R3   are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, halogen, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, or Z-Y; R2 and R3 are optionally substituted with at least one electron withdrawing or electron donating group; Z is O, S, S(O)a, NR4 or PR4; Y is hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, heterocyclic, heterocyclic lower alkyl, and Y is optionally substituted with an electron donating or electron withdrawing group, or ZY  taken together is NR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6, PR4NR5R7, NR4C(=O)R5, S(C=O)R5, NR4C(=O)OR5, or S(C=O)OR5, R4, R5 and R6   are independently hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl, or lower alkynyl, each optionally substituted with an electron withdrawing or an electron donating group; R7  is COOR8, COR8, hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl or lower alkynyl, each optionally substituted with an electron withdrawing or electron donating group; R8  is hydrogen, lower alkyl or aryl lower alkyl, the aryl or alkyl group is optionally substituted with an electron withdrawing or an electron donating group; n is 1-4; and a is 1-3.
    • 4. 发明专利
    • New applications of amino acid antispasmodics
    • JP2004506692A
    • 2004-03-04
    • JP2002520843
    • 2001-08-24
    • リサーチ コーポレイション テクノロジーズ,インコーポレイテッドResearch Corporation Technologies, Inc.
    • ハリス、 ロバート エイチ.
    • A61K38/00A61K31/16A61K31/165A61K31/195A61P25/04A61P25/06A61P29/00C07K5/10
    • A61K38/05A61K31/16A61K31/165A61K31/195A61K31/40A61K31/44A61K38/04
    • The present invention describes the use of a compound of the following formula (I) for the manufacture of a medicament effective in the treatment or prevention of bipolar disease of a mammal: wherein R is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl lower alkyl, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with at least one electron withdrawing or electron donating group; R1  is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocyclic lower alkyl, heterocyclic, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with an electron donating or an electron withdrawing group; R2 and R3   are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, halogen, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, or Z-Y; R2 and R3 are optionally substituted with at least one electron withdrawing or electron donating group; Z is O, S, S(O)a, NR4 or PR4; Y is hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, heterocyclic, heterocyclic lower alkyl, and Y is optionally substituted with an electron donating or electron withdrawing group, or ZY  taken together is NR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6, PR4NR5R7, NR4C(=O)R5, S(C=O)R5, NR4C(=O)OR5, or S(C=O)OR5, R4, R5 and R6   are independently hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl, or lower alkynyl, each optionally substituted with an electron withdrawing or an electron donating group; R7  is COOR8, COR8, hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl or lower alkynyl, each optionally substituted with an electron withdrawing or electron donating group; R8  is hydrogen, lower alkyl or aryl lower alkyl, the aryl or alkyl group is optionally substituted with an electron withdrawing or an electron donating group; n is 1-4; and a is 1-3.
    • 8. 发明专利
    • New applications of amino acid antispasmodics
    • JP5190334B2
    • 2013-04-24
    • JP2008304255
    • 2008-11-28
    • リサーチ コーポレイション テクノロジーズ,インコーポレイテッドResearch Corporation Technologies, Inc.
    • ロバート エイチ. ハリス、
    • A61K31/165A61K38/00A61K31/16A61K31/195A61P25/04A61P25/06A61P29/00C07K5/10
    • A61K38/05A61K31/16A61K31/165A61K31/195A61K31/40A61K31/44A61K38/04
    • The present invention describes the use of a compound of the following formula (I) for the manufacture of a medicament effective in the treatment or prevention of bipolar disease of a mammal: wherein R is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl lower alkyl, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with at least one electron withdrawing or electron donating group; R1  is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocyclic lower alkyl, heterocyclic, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each optionally substituted with an electron donating or an electron withdrawing group; R2 and R3   are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, halogen, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, or Z-Y; R2 and R3 are optionally substituted with at least one electron withdrawing or electron donating group; Z is O, S, S(O)a, NR4 or PR4; Y is hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, heterocyclic, heterocyclic lower alkyl, and Y is optionally substituted with an electron donating or electron withdrawing group, or ZY  taken together is NR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6, PR4NR5R7, NR4C(=O)R5, S(C=O)R5, NR4C(=O)OR5, or S(C=O)OR5, R4, R5 and R6   are independently hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl, or lower alkynyl, each optionally substituted with an electron withdrawing or an electron donating group; R7  is COOR8, COR8, hydrogen or lower alkyl, aryl, aryl lower alkyl, lower alkenyl or lower alkynyl, each optionally substituted with an electron withdrawing or electron donating group; R8  is hydrogen, lower alkyl or aryl lower alkyl, the aryl or alkyl group is optionally substituted with an electron withdrawing or an electron donating group; n is 1-4; and a is 1-3.