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US 2019/0337929 A1Published application
Indolinones compounds and their use in the treatment of fibrotic diseases
AssigneeRespivert Limited
InventorsIain Walters, Louise Birch, Joseph Hill-Cousins, Stephen Paul Collingwood, Christopher Scott Stevenson
Life of this patent
Estimating the term…
Abstract
The present invention relates inter alia to a compound of formula (I) Wherein R1, R2, R3 and Z are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.
Claims36
A compound of formula (I):
- wherein
- R1 represents H, Me, Et, CH═CH2, C≡C—H or C≡C-Me;
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- R3 represents
- Q represents a heteroatom selected from O, N and S and if N may optionally be substituted with C1-4alkyl;
- Z represents CO or SO2;
- Y1 represents (CH2)n and, except when n represents 0, may optionally be substituted by Me;
- X1 represents (CH2)m and, except when m represents 0, may optionally be substituted by Me;
- n and m independently represent 0, 1, 2, 3, 4 or 5;
- Y2 represents (CH2)s and may optionally be substituted by Me;
- s represents 2, 3, 4, 5 or 6;
- Y3 represents (CH2)t and may optionally be substituted by Me;
- X2 represents (CH2)v and may optionally be substituted by Me;
- t and v independently represent 2 or 3 save that t+v=4 or 5;
- R4 represents H, OH, NR6R7 or an aliphatic 4-8 membered heterocycle containing one or more heteroatoms selected from O, N and S, save that when R4 is OH or NR6R7, m is 2, 3, 4 or 5;
- R5 represents H, OH, NR8R9 or aliphatic 4-8 membered heterocycle containing one or more heteroatoms selected from O, N and S save that when R5 is OH or NR8R9, n is 2, 3, 4 or 5;
- in which the aliphatic heterocycle groups that R4 and R5 may represent may optionally contain a carbonyl or sulphone group and may optionally be substituted by one or more groups selected from —C1-C4alkyl, C1-C4hydroxyalkyl-, C1-C4alkoxy(C1-C4)alkyl-, —C1-C4alkyleneCONR10R11, CN, OH and NR12R13;
- R6, R7, R8, R9 independently represent H, or C1-C4 alkyl optionally substituted by OH, oxo, NR14R15 or —C1-C4alkoxy;
- and
- R10, R11, R12, R13, R14 and R15 independently represent H or C1-C4alkyl;
- or a pharmaceutically acceptable salt thereof.
18 more elements
-29. (canceled)
A compound of formula (II):
- wherein
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me, especially Me
- or a protected derivative thereof or a salt thereof.
A compound of formula (VI):
- wherein
- R1 represents Et, CH═CH2, C≡C—H or C≡C-Me,
- or a protected derivative thereof or a salt thereof.
A compound of formula (VII):
- wherein
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me, especially Me
- or a protected derivative thereof or a salt thereof.
A compound of formula (IX):
- wherein
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me, especially Me;
- and
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- or a protected derivative thereof or a salt thereof.
2 more elements
A compound of formula (XI):
- wherein
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me, especially Me;
- and
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- or a protected derivative thereof or a salt thereof.
2 more elements
A compound of formula (XIII):
- wherein
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me, especially Me;
- and
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- or a protected derivative thereof or a salt thereof.
2 more elements
A compound of formula (XVI):
- wherein
- Z represents CO or SO2;
- and
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me;
- and
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- or a protected derivative thereof or a salt thereof.
4 more elements
A compound of formula (XVII):
- wherein
- Z represents CO or SO2;
- and
- R1 represents Me, Et, CH═CH2, C≡C—H or C≡C-Me;
- and
- R2 represents H, C1-C6alkyl, C1-C6alkoxy, C3-C8cycloalkyl, —CH2—(C3-C8cycloalkyl), halogen or cyano;
- or a protected derivative thereof or a salt thereof.
4 more elements
Dependencies are inferred from the claim text.