摘要:
The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x) or (z): and wherein R3 is optionally substituted C3-8cycloalkyl, optionally substituted C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R4 is H, C1-3alkyl, C1-2fluoroalkyl, cyclopropyl, —CH2OR4a, —CH(Me)OR4a, or —CH2CH2OR4a; and R5 is inter alia H, C1-8alkyl, C1-3fluoroalkyl, C3-8cycloalkyl, certain substituted alkyl groups, —(CH2)n13-Het, or optionally substituted phenyl or —CH2-Ph; or R4 and R5 taken together are —(CH2)p1— or —(CH2)p3—X5—(CH2)p4—; provided that at least one of R4 and R5 is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.
摘要:
The invention provides a compound of formula (I) or a salt thereof: wherein: R1 is C1-3alkyl, C1-3fluoroalkyl, or —CH2CH2OH; R2 is hydrogen, methyl or C1fluoroalkyl; R3 is of sub-formula (aa) or (bb): wherein Y is NCONH2 and n1 is 0 or 1; R4 is H; and R5 is a group of the sub-formula (x), (y), (y1) or (z): These compounds are PDE4 inhibitors.
摘要翻译:本发明提供式(I)化合物或其盐:其中:R 1是C 1-3烷基,C 1-3 氟代烷基或-CH 2 CH 2 OH; R 2是氢,甲基或C 1氟代烷基; R 3是亚式(aa)或(bb):其中Y是NCONH 2和n 1是0或1; R 4是H; 和R 5是子式(x),(y),(y1)或(z)的一组:这些化合物是PDE4抑制剂。
摘要:
The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxamide, which is the compound of formula (I): or a salt thereof.
摘要:
The invention provides a compound of formula (I) or a salt thereof: wherein R2 is H, C1-3alkyl, n-butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl-, —CN, or —CH2OH; R3 is inter alia optionally substituted C4-7cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); Ra is H, methyl or ethyl; Rb is H or methyl; R4 is H, methyl, ethyl, n-propyl, —C(O)-Me, or —C(O)—C1fluoroalkyl; and R5 is: —C(O)—(CH2)n—Ar, —C(O)-Het, —C(O)—C1-6alkyl, —C(O)—C1 fluoroalkyl, —C(O)—(CH2)2—C(O)—NR15bNR15b, —C(O)—CH2—C(O)—NR15bNR15b, —C(O)—NR15b—(CH2)m1—Ar, —C(O)—NR15b—Het, —C(O)—NR15b—C1-6alkyl, —C(O)—NR5aR5b, —S(O)2—(CH2)m2—Ar, —S(O)2-Het, —S(O)2—C1-6alkyl, or —CH2—Ar; or R4 and R5 taken together are —(CH2)p1—, —(CH2)2—X5—(CH2)2—, —C(O)—(CH2)p2—, —C(O)—N(R15)—(CH2)p3—; or NR4R5 is of sub-formula (y), (y1), (y2) or (y3). The invention provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as COPD and the like.
摘要翻译:本发明提供式(I)化合物或其盐:其中R2是H,C1-3烷基,正丁基,C1-2氟烷基,环丙基,环丁基,(环丙基)甲基,-CN或-CH2OH; R3特别是任选取代的C 4-7环烷基或任选取代的杂环基团(aa),(bb)或(cc); Ra是H,甲基或乙基; Rb是H或甲基; R 4是H,甲基,乙基,正丙基,-C(O)-Me或-C(O)-C 1-6氟烷基; 并且R 5是:-C(O) - (CH 2)n -Ar,-C(O)-Het,-C(O)-C 1-6烷基,-C(O)-C 1氟代烷基,-C(O) (CH 2)2 -C(O)-NR 15 b N R 15 b,-C(O)-CH 2 -C(O)-NR 15 b NR 15 b,-C(O)-NR 15 b - (CH 2)m -Ar,-C(O) C(O)-NR 15 b -C 1-6烷基,-C(O)-NR 5 R 5a,-S(O)2 - (CH 2)m -Ar,-S(O)2 -Het,-S(O) 2-C 1-6烷基或-CH 2 -Ar; 或(R 4)和R 5和R 5一起为 - (CH 2)p1 - , - (CH 2)2 -X 5 - (CH 2)2 - , - - (CH 2)p3-; 或NR4R5为子式(y),(y1),(y2)或(y3)。 本发明提供了化合物作为IV型磷酸二酯酶抑制剂(PDE4)和/或用于治疗和/或预防炎性和/或过敏性疾病如COPD等的用途。
摘要:
The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH2)n— moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要:
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要:
The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要:
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要:
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要:
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.