发明名称 Carbazole and Carboline Compounds for Use in the Diagnosis, Treatment, Alleviation or Prevention of Disorders Associated with Amyloid or Amyloid-Like Proteins
摘要 The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
申请公布号 US2017002005(A1) 申请公布日期 2017.01.05
申请号 US201515112672 申请日期 2015.01.21
申请人 AC IMMUNE SA ;PIRAMAL IMAGING SA 发明人 KROTH Heiko;NAMPALLY Sreenivasachary;MOLETTE Jérôme;GABELLIERI Emanuele;BENDERITTER Pascal André René;FROESTL Wolfgang;SCHIEFERSTEIN Hanno;MUELLER Andre;SCHMITT-WILLICH Heribert;BERNDT Mathias
分类号 C07D471/14;A61K49/00;A61K51/04;C07D519/00 主分类号 C07D471/14
代理机构 代理人
主权项 1. A compound of formula (I): and all detectably labeled derivatives, stereoisomers, racemic mixtures, pharmaceutically acceptable salts, hydrates, solvates and polymorphs thereof; whereinis selected from the group consisting of a pyridine ring, a phenyl ring, an azole ring and a thiazole ring, wherein the pyridine ring, the phenyl ring, the azole ring and the thiazole ring can be attached at any available position of the respective ring to the moiety Z, and whereincan be optionally substituted by one or more substituents R3; V is selected from the group consisting of NRb, O and S; W is selected from the group consisting of CRc and N; X is selected from the group consisting of CRc and N; Z is selected from the group consisting of —N(Ra)— and —O—; Ra is selected from the group consisting of hydrogen, and alkyl, wherein alkyl can be optionally substituted; Rb is selected from the group consisting of hydrogen, alkyl, —(CH2CH2—O)n—H and —(CH2CH2—O)n-alkyl, wherein alkyl can be optionally substituted; Rc is selected from the group consisting of hydrogen, alkyl, and halogen, wherein alkyl can be optionally substituted; Rd is selected from the group consisting of halogen, H, OH and O-alkyl, wherein alkyl can be optionally substituted; Rf is selected from the group consisting of H and alkyl; R1 and R2 together form a 6-membered aromatic ring containing carbon atoms and optionally one or more N atoms or R1 and R2 together form a 6-membered ring containing an amide moiety —C(O)—N(R13)—, wherein the 6-membered aromatic ring or the 6-membered ring containing an amide moiety formed by R1 and R2 can be optionally substituted by R12; for each occurrence, R3 is independently selected from the group consisting of halogen, —CN, —O—R10, —S—R10, —NO2, —NR10R11, —CONR10R11, —N(R10)—C(O)—R11, —C(O)O—R10, —(O—CH2CH2)n—Rd, —(CH2CH2—O)n—Rf, —(CH2CH2—O)n—(CH2CH2)—Rd, alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, and alkynyl, wherein alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, and alkynyl can be optionally substituted, or if more than one group R3 is present and two of the groups R3 are adjacent, they can optionally be taken together and can form a 5- to 8-membered ring containing carbon atoms and optionally one or more heteroatoms selected from O, S, or N or optionally one or more heteroatom (e.g., N, O and/or S)-containing moieties and wherein the 5- to 8-membered ring may be substituted; for each occurrence, R10 and R11 are each independently selected from the group consisting of: hydrogen, alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl, wherein alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl can be optionally substituted; for each occurrence, R12 is independently selected from the group consisting of halogen, —CN, —O—R10, —NR10R11, —CONR10R11, —N(R10)—C(O)—R11, —C(O)O—R10, —(CH2CH2—O)n—Rf, —(CH2CH2—O)n—(CH2CH2)—Rd, alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl, wherein alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl can be optionally substituted; for each occurrence, R13 is independently selected from the group consisting of hydrogen, —CONR10R11, —C(O)O—R10, —(CH2CH2—O)n—Rf, —(CH2CH2—O)n—(CH2CH2)—Rd, alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl, wherein alkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl can be optionally substituted; and for each occurrence, n is 1 to 5.
地址 Lausenne CH