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US 9,067,938 B2Granted
Pyrazolopyridinone derivatives as LPA receptor antagonists
AssigneeMerck Patent GmbH
InventorsKai Schiemann, Wolfgang Staehle, Sr., Dirk Wienke
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases.
Claims17
A method for modulating an LPA receptor 2, said method comprising modulating said receptor with a compound according to formula (I):
- wherein:
- R1 denotes aryl, heteroaryl, cycloalkyl, heterocyclyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocyclylalkyl, which in each case is unsubstituted or substituted with one or more substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, halogen, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ1, —NZ2Z3, —NO2, —OH, —OCF3, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z4, —C(O)O—Z5, —C(O)NH—Z6, —C(O)NZ7Z8, —O—Z9, —O(—Z10—O)a—H, —O(—Z11—O)b—Z12, —OC(O)—Z13, —OC(O)—O—Z14, —OC(O)—NHZ15, —O—C(O)—NZ16Z17, —OP(O)(OZ18)(OZ19), —OSi(Z20)(Z21)(Z22), —OS(O2)—Z23, —NHC(O)—NH2, —NHC(O)—Z24, —NZ25C(O)—Z26, —NH—C(O)—O—Z27, —NH—C(O)—NH—Z28, —NH—C(O)—NZ29Z30, —NZ31—C(O)—O—Z32, —NZ33—C(O)—NH—Z34, —NZ35—C(O)—NZ36Z37, —NHS(O2)—Z38, —NZ39S(O2)—Z40, —S—Z41, —S(O)—Z42, —S(O2)—Z43, —S(O2)NH—Z44, —S(O2)NZ45Z46, —S(O2)O—Z47, —P(O)(OZ48)(OZ49), —Si(Z50)(Z51)(Z52), —C(NH)—NH2, —C(NZ53)—NH2, —C(NH)—NHZ54, —C(NH)—NZ55Z56, —C(NZ57)—NHZ58, —C(NZ59)—NZ60Z61, —NH—C(O)—NH—O—Z62, —NH—C(O)—NZ63—O—Z64, —NZ65—C(O)—NZ66—O—Z67, —N(—C(O)—NH—O—Z68)2, —N(—C(O)—NZ69—O—Z70)2, —N(—C(O)—NH—O—Z71)(—C(O)—NZ72—O—Z73), —C(S)—Z74, —C(S)—O—Z75, —C(S)—NH—Z76, —C(S)—NZ77Z78, —C(O)—NH—O—Z79, —C(O)—NZ80—O—Z81, —C(S)—NH—O—Z82, —C(S)—NZ83—O—Z84, —C(O)—NH—NH—Z85, —C(O)—NH—NZ86Z87, —C(O)—NZ88—NZ89Z90, —C(S)—NH—NH—Z91, —C(S)—NH—NZ92Z93, —C(S)—NZ94—NZ95Z96, —C(O)—C(O)—O—Z97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ98, —C(O)—C(O)—NZ99Z100, —C(S)—C(O)—O—Z101, —C(O)—C(S)—O—Z102, —C(S)—C(S)—O—Z103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ104, —C(S)—C(O)—NZ105Z106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ107, —C(S)—C(S)—NZ108Z109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ110, —C(O)—C(S)—NZ111Z112;
- Z1, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9, Z10, Z11, Z12, Z13, Z14, Z15, Z16, Z17, Z18, Z19, Z20, Z21, Z22, Z23, Z24, Z25, Z26, Z27, Z28, Z29, Z30, Z31, Z32, Z33, Z34, Z35, Z36, Z37, Z38, Z39, Z40, Z41, Z42, Z43, Z44, Z45, Z46, Z47, Z48, Z49, Z50, Z51, Z52, Z53, Z54, Z55, Z56, Z57, Z58, Z59, Z60, Z61, Z62, Z63, Z64, Z65, Z66, Z67, Z68, Z69, Z70, Z71, Z72, Z73, Z74, Z75, Z76, Z77, Z78, Z79, Z80, Z81, Z82, Z83, Z84, Z85, Z86, Z87, Z88, Z89, Z90, Z91, Z92, Z93, Z94, Z95, Z96, Z97, Z98, Z99, Z100, Z101, Z102, Z103, Z104, Z105, Z106, Z107, Z108, Z109, Z110, Z111, Z112 are each, independently from each other, selected from alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, and wherein alternatively Z7, Z8 and/or Z16, Z17 and/or Z29, Z30 and/or Z36, Z37 and/or Z45, Z46 and/or Z55, Z56 and/or Z60, Z61 and/or Z77, Z78 and/or Z86, Z87 and/or Z89, Z90 and/or Z92, Z93 and/or Z95, Z96 and/or Z99, Z100 and/or Z105, Z106 and/or Z108, Z109 and/or Z111, Z112 can each, respectively, together form a heterocyclyl;
- a is 1, 2, 3, 4, or 5;
- b is 1, 2, 3, 4, or 5;
- R2 denotes H or alkyl;
- R3 denotes H or alkyl;
- R4, R5 independently from each other denote H, alkyl, OH-alkyl, alkoxy, halogen, F, Cl, Br, I, CN, NHR, NH2, NR2, S-alkyl or NH-alkyl-OH;
- R independently from each other denotes alkyl, aryl, heteroaryl, cycloalkyl or heterocyclyl;
- R4 and R5 together can also form cycloalkyl or heterocyclyl;
- R6 denotes H;
- X denotes O;
- and the physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios,
- with the proviso that the following compound is excluded from formula (I):
11 more elements
Dependencies are inferred from the claim text.