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    Sulfonamide carboxamide compounds
    4.
    发明授权
    Sulfonamide carboxamide compounds 有权

    公开(公告)号：US11773058B2

    公开(公告)日：2023-10-03

    申请号：US16638646

    申请日：2018-08-15

    申请人： Inflazome Limited

    发明人： David Miller ,  Angus MacLeod ,  Jimmy Van Wiltenburg ,  Stephen Thom ,  Stephen St-Gallay ,  Jonathan Shannon

    IPC分类号： C07C311/55 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D211/24 ,  C07D211/58 ,  C07D213/34 ,  C07D213/40 ,  C07D231/12 ,  C07D295/088

    CPC分类号： C07C311/55 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D211/24 ,  C07D211/58 ,  C07D213/34 ,  C07D213/40 ,  C07D231/12 ,  C07D295/088

    摘要： The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C1-C12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R1 is —NR3R4, —OR5, —(C═NR6)R7, —(CO)R8, —CN, —N3, a quaternary ammonium group or an optionally substituted heterocycle; R3, R4, R5, R6, R7 and R8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C1-C10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R3, or L and R4, or R3 and R4, or L and R5, or L and R6, or L and R7, or R6 and R7, or L and R8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

    Antitumor 2-aminocarbonyl-1, 2-bis(methylsulfonyl)-1-(substituted)hydrazines
    6.
    发明授权
    Antitumor 2-aminocarbonyl-1, 2-bis(methylsulfonyl)-1-(substituted)hydrazines 失效
    抗肿瘤剂2-氨基羰基-1,2-双（甲基磺酰基）-1-（取代）肼

    公开(公告)号：US5637619A

    公开(公告)日：1997-06-10

    申请号：US497931

    申请日：1995-07-05

    申请人： Alan C. Sartorelli ,  Krishnamurthy Shyam ,  Philip G. Penketh

    发明人： Alan C. Sartorelli ,  Krishnamurthy Shyam ,  Philip G. Penketh

    IPC分类号： A61K31/18 ,  A61K31/22 ,  A61P35/00 ,  C07C311/55 ,  C07C317/50 ,  A61K31/175

    CPC分类号： C07C311/55

    摘要： The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhydrazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.

    摘要翻译： 本发明涉及新的2-氨基羰基-1,2-双（甲基磺酰基）-1-（2-氯乙基）肼和2-氨基羰基-1,2-双（甲基磺酰基）-1-甲基肼，及其用于治疗 恶性肿瘤。 这些药剂在治疗动物和人类癌症中尤其有用。 该类中特别用于治疗肿瘤的两种优选的药剂是1,2-双（甲基磺酰基）-1-（2-氯乙基）-2-（2-氯乙基）氨基羰基肼和1,2-双（甲基磺酰基） -1-（2-氯乙基）-2-甲基氨基羰基肼。 这些试剂的特征如下：它们不能通过为灭活CNU而提出的脱硝机制灭活; 它们不能通过为CNU提出的机制产生羟乙基化物种; 它们能够进行氯乙基化或甲基化和氨基甲酰化。