Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.
Compounds are provided having a piperazine or homopiperazine ring which are useful in the treatment of thrombosis.
提供了具有哌嗪或同源哌嗪环的化合物,这些化合物在治疗血栓症方面很有用。
Methods and compounds for inhibiting mrp1
申请人:——
公开号:US20030100576A1
公开(公告)日:2003-05-29
The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
本发明还涉及一种抑制哺乳动物中MRP1的方法,包括向需要的哺乳动物施用化合物(I)的有效量。
[EN] HEPATITIS C VIRUS INHIBITORS<br/>[FR] INHIBITEURS DU VIRUS DE L'HÉPATITE C
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2010138488A1
公开(公告)日:2010-12-02
This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
[EN] CELL PROLIFERATION INHIBITORS AND CONJUGATES THEREOF<br/>[FR] INHIBITEURS DE LA PROLIFÉRATION CELLULAIRE ET LEURS CONJUGUÉS
申请人:NOVARTIS AG
公开号:WO2014151030A1
公开(公告)日:2014-09-25
Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: [insert last structure from page 68 here] The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, optionally including a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.