SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
申请人:BlinkBio, Inc.
公开号:US20170202970A1
公开(公告)日:2017-07-20
Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.
2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS
申请人:Schadt Oliver
公开号:US20100280030A1
公开(公告)日:2010-11-04
Compounds of the formula (I), in which R
1
, R
2
, R
3
, R
3′
, R
4
, R
4′
, E, E′, E″ and E′″ have the meanings indicated in Claim
1
, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
A series of 3-(aminoalkyl)- and 3-[(4-aryl-1-piperazinyl)alkyl]oxazolo[4,5-b]pyridin-2(3H)-ones were prepared from their respective oxazolo[4,5-b]pyridin-2(3H)-ones. Several members of this group were found to possess potent analgesic activity in the mouse during a p-phenylquinone writhing induced test. Among them, phenylpiperazine compounds with two-carbon length alkyl chains, 2a and 2b, appeared
Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure:
where the definitions of the variables are provided herein.
Formula I的Chroman化合物和衍生物是TRPM8的有用抑制剂。这些化合物在治疗多种由TRPM8介导的疾病和症状方面具有用途,并可用于制备治疗这些疾病和症状的药物和药物组合物。这些疾病的例子包括,但不限于,偏头痛和神经病性疼痛。Formula I的化合物具有以下结构:变量的定义在此提供。
BICYCLIC (THIO)CARBONYLAMIDINES
申请人:BAYER INTELLECTUAL PROPERTY GMBH
公开号:US20140113824A1
公开(公告)日:2014-04-24
Bicyclic (thio)carbonylamidines of the formula (I)
in which Q, B, Y, R
1
and A are as defined in the description
their preparation and their use for controlling plant pests and pests encountered in veterinary medicine.