Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

The invention relates to compounds of formula (I) wherein X 1 to X 5 , Y, Z 1 to Z 3 , and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS

The present invention relates to compounds of formula (I) 2. (canceled)3. A compound of claim 1 , wherein Ris T claim 1 , C(O)T claim 1 , Calkyl substituted with one or more T claim 1 , or N(R)T.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. A compound of claim 1 , wherein R is H.10. A compound of claim 1 , wherein ring A is a pyrazole claim 1 , an oxazole or an isoxazole.11. (canceled)12. (canceled)13. A compound of claim 1 , wherein Ris ORor Calkyl claim 1 , which is optionally substituted with 1 or 2 R claim 1 , which are the same or different.14. (canceled)15. (canceled)16. A compound of claim 1 , wherein Ris halogen; CN; OR; C(O)N(RR); C(O)T claim 1 , wherein Tis an unsubstituted 4 to 7 membered heterocycle containing at least one ring nitrogen atom which is attached to C(O).17. (canceled)18. (canceled)19. (canceled)20. (canceled)22. (canceled)23. (canceled)24. A compound of claim 1 , wherein none or one of X claim 1 , X claim 1 , X claim 1 , X claim 1 , Xis N.25. (canceled)26. A compound of claim 1 , wherein one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , Ris Rand the others are independently selected from the group consisting of H; unsubstituted Calkyl; and halogen.27. (canceled)28. (canceled)29. A compound of claim 1 , wherein Tis a 4 to 7 membered heterocyclyl; or 7 to 11 membered heterobicyclyl.30. A compound of claim 29 , wherein Tis morpholinyl claim 29 , piperazinyl claim 29 , piperidinyl claim 29 , thiomorpholinyl-1 claim 29 ,1-dioxide claim 29 , tetrahydro-2H-pyranyl claim 29 , azetidinyl claim 29 , oxetane claim 29 , or pyrrolidine claim 29 , and wherein Tis optionally substituted with one or more R claim 29 , which are the same or different.31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. (canceled)42. (canceled)43. (canceled)45. A compound of selected from the group consisting of(R)—N-(1-methyl-1H-pyrazol-4-yl)-1-((6-(3- ...

Substituted biphenyl carboxylic acids and derivatives thereof

Substituted biphenyl carboxylic acids and derivatives thereof

The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4 R9, and R10, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of .gamma.-secretase activity, wherein A is O, NH, S; X is a bond or a group -CR5R6 .UPSILON. is a carboxy group -C(O)OH or a substituted or unsubstituted tetrazole group..

Substituted biphenyl carboxylic acids and their derivatives

Substituted bisphenyl carboxylic acids and derivatives thereof

Η παρούσα εφεύρεση αφορά ενώσεις που έχουν τον γενικό τύπο (I) με τους ορισμούς των Χ,Υ και Α που δίδονται παρακάτω και άλας ή εστέρα αυτών. Περαιτέρω η εφεύρεση αφορά την χρήση των εν λόγω ενώσεων για την θεραπεία ασθένειας Alzheimer και χρήση αυτών για την ρύθμιση δραστικότητας της γ-εκκριτάσης όπου το Α είναι Ο, NH,S,το Χ είναι δεσμός ή μία ομάδα -CR5R6,το Υ είναι καρβόξυ ομάδα -C(O)OH ή υποκατεστημένη ή μη υποκατεστημένη ομάδα τετραζολίου ή/και άλας ή εστέρας αυτής. The present invention relates to compounds having the general formula (I) with the definitions of X, Y and A given below and a salt or ester thereof. Further the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use to modulate γ-secretase activity where A is O, NH, S, X is a bond or a group -CR5R6, Y is carboxy a -C (O) OH group or a substituted or unsubstituted tetrazolium group and / or a salt or ester thereof.

Terphenyl derivatives for treatment of alzheimer' s disease

The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of .gamma.-secretase activity.

(Biphenyl) carboxylic acids and derivatives thereof

The present invention relates to compounds having the general formula (I) with the definitions of A, X, R 1 -R 6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.

Terphenyl derivatives for treatment of alzheimer' s disease

The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.

SUBSTITUTED BIFENYLOCARBOYCLIC ACIDS AND THEIR DERIVATIVES

l o ester del mismo; mas aun, la invencion se relaciona con el uso de dichos compuestos para el tratamiento de la enfermedad de Alzheimer y con su uso para la modulacion de la actividad y-secretasa, en donde A es O, NH, S; X es un enlace o grupo -CR5R6 Y es un grupo carboxi-C(O)OH o un grupo tetrazol sustituido o no sustituido.

Substituted biphenylcarboxylic acids and derivatives thereof

(Biphenyl) carboxylic acids and derivatives thereof

Substituted biphenyl carboxylic acids and derivatives thereof

The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4 R9, and Rl0, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity, wherein A is O, NH, S; X is a bond or a group -CR5R6 Υ is a carboxy group -C(O)OH or a substituted or unsubstituted tetrazole group..

(DIFFINYL) CARBOXYLIC ACIDS AND THEIR DERIVATIVES

Η παρούσα εφεύρεση αφορά ενώσεις που έχουν τον γενικό τύπο (I) με τους ορισμούς των A, Χ, R1-R6 που δίνονται στη συνέχεια, και/ή ένα άλας ή εστέρα αυτών. Επιπλέον, η εφεύρεση αφορά τη χρήση των αναφερθέντων ενώσεων για την αντιμετώπιση της νόσου Αλτσχάιμερ και τη χρήση τους για την τροποποίηση της δράσης της γ-σεκρετάσης. The present invention relates to compounds having the general formula (I) with the definitions of A, X, R 1 -R 6 hereinafter provided, and / or a salt or ester thereof. In addition, the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use to modify the activity of gamma-secretase.

TERFENIL DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE

La presente invencion se relaciona con compuestos que tienen la formula general (I) con las definiciones de X, Y, R1, R2, R3, R4, R9, R10, que se detallan a continuacion y solvatos, hidratos, esteres y sales farmaceuticamente aceptables de los mismos. Ademas, la invencion se refiere al uso de dichos compuestos para el tratamiento de la enfermedad de Alzheimer y su uso para la modulacion de la actividad de la y-secretasa.

(biphenyl) carboxylic acids and derivatives thereof ()

Acids (biphenyl) carboxylic and their derivatives

Terphenylderivate zur alzheimerbehandlung

(biphenyl)carbonsauren und derivate davon