公开(公告)号：WO2019134984A1

公开(公告)日：2019-07-11

申请号：PCT/EP2019/050194

申请日：2019-01-07

Applicant: CELON PHARMA S.A.

Inventor： MACH, Mateusz ,  DZIDA, Radoslaw ,  SMUGA, Damian ,  STELMACH, Filip ,  MATLOKA, Mikolaj ,  BAZYDLO, Katarzyna ,  DUBIEL, Krzysztof ,  WIECZOREK, Maciej ,  PIECZYKOLAN, Jerzy

IPC: A61P3/10 ,  C07C57/42 ,  C07C57/60 ,  A61K31/192

CPC classification number: A61P3/10 ,  C07B2200/07 ,  C07C59/64

Abstract: A compound of the formula (I)wherein R represents a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated, or a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated and wherein one or more of hydrogen atoms is replaced with fluorine atom; X represents hydrogen atom or halogen atom,and* denotes chiral center, and salts thereof. The compound is useful for the treatment of diseases mediated by GPR40, in particular type II diabetes. (I)

公开(公告)号：WO2019097282A1

公开(公告)日：2019-05-23

申请号：PCT/IB2017/057247

申请日：2017-11-20

Applicant: CELON PHARMA S.A. ,  UNIWERSYTET JAGIELLONSKI ,  INSTYTUT FARMAKOLOGII POLSKIEJ AKADEMII NAUK

Inventor： KAMINSKI, Krzysztof ,  GRYCHOWSKA, Katarzyna ,  CANALE, Vittorio ,  BOJARSKI, Andrzej J. ,  SATALA, Grzegorz ,  LENDA, Tomasz ,  POPIK, Piotr ,  MATLOKA, Mikolaj ,  DUBIEL, Krzysztof ,  MOSZCZYNSKI-PETKOWSKI, Rafal ,  PIECZYKOLAN, Jerzy ,  WIECZOREK, Maciej ,  ZAJDEL, Pawel

IPC: C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/12 ,  C07D413/04 ,  C07D487/08 ,  C07D209/44 ,  A61P25/28 ,  A61K31/4035

CPC classification number: C07D209/44 ,  A61K31/4035 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5513 ,  A61K31/554 ,  A61P25/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/04 ,  C07D487/08

Abstract: A compound of the formula (I) wherein R 1 represents hydrogen atom and R 2 represents moiety of the formula G1, or R 1 and R 2 are connected with each other to form with nitrogen atom to which they are attached a moiety of the formula G2; A is selected from the group consisting of phenyl substituted with one or two substituents selected from the group consisting of halogen atom, straight or branched C1- C4 alkyl, C1-C2 alkoxyl, CF 3 , CN, and -OCF 3 , naphthyl, quinolinyl, thienyl, thienyl substituted with halogen atom, and pyridyl; X is selected from the group consisting of -NR 4 , -0-, and -CHN(R 5 ) 2 ; R 3 is selected from the group consisting of hydrogen atom, methyl, ethyl, and cyclopropyl; R 4 is selected from the group consisting of hydrogen atom, straight or branched C1-C4 alkyl, straight or branched C1-C4 alkyl substituted with one or two halogen atoms, cyclopropyl and methylcyclopropyl; R 5 represents C1-C2 alkyl; k is an integer equal 1 or 2; I is an integer equal 1 or 2; m is an integer equal 0, 1 or 2; n is an integer 0 or 1 when X represents -NR4"or -CHN(R5) 2, wherein n is 1 only when m is 1; and n is 0 when X represents -0-; and acid addition salts thereof, can be useful as selective inhibitors of 5HT6 in the treatment of CNS diseases.

公开(公告)号：WO2018206739A1

公开(公告)日：2018-11-15

申请号：PCT/EP2018/062164

申请日：2018-05-10

Applicant: CELON PHARMA S.A.

Inventor： MROCZKIEWICZ, Michal ,  STYPIK, Bartosz ,  BUJAK, Anna ,  SZYMCZAK, Krzysztof ,  GUNERKA, Pawel ,  DUBIEL, Krzysztof ,  WIECZOREK, Maciej ,  PIECZYKOLAN, Jerzy

IPC: C07D487/04 ,  A61P29/00 ,  A61P37/00 ,  A61K31/519

Abstract: A compound or its acid addition salt of the general formula (I), wherein R 1 represents phenyl substituted with one or two substituents selected from the group consisting of halogen and C1-C3 alkoxyl, or 6-membered heteroaryl with 1 or 2 nitrogen atoms, which is unsubstituted or substituted with a substituent selected from the group consisting of -NH 2 , halogen, alkyl C1-C4, alkoxyl C1-C3, and 6-membered heterocyclyl comprising 1 or 2 heteroatoms selected from the group consisting of N and O. The compound has the activity of kinase JAK1/JAK3 inhibitor and can find use in the treatment of chronic inflammatory and autoimmunological diseases.