CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE SULFONAMIDE DERIVATIVES

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. 2. The compound of claim 1 , wherein said compound exhibits an ICof less than 30 μM in the T84 assay.3. The compound of claim 1 , wherein said compound exhibits a greater than 30% inhibition at 20 μM in the FRT assay.4. The compound of claim 1 , wherein said compound exhibits a greater than 35% inhibition at 50 μM in a T84 assay claim 1 , provided that the compound does not have an ICgreater than 30 μM.5. The compound of claim 1 , wherein R is hydrogen claim 1 , hydroxyl claim 1 , bromo claim 1 , chloro claim 1 , methoxy claim 1 , amino claim 1 , —NH—S(O)—R claim 1 , or —C(O)NH—S(O)—Rwhere Ris selected from the group consisting of alkyl claim 1 , substituted alkyl claim 1 , aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , amino claim 1 , and substituted amino.6. The compound of claim 1 , wherein R is —NH—S(O)—R claim 1 , where Ris selected from the group consisting of alkyl claim 1 , substituted alkyl claim 1 , aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , amino claim 1 , and substituted amino.7. The compound of claim 6 , wherein substituted aryl is substituted with a substituent selected from the group consisting of halo claim 6 , alkyl claim 6 , alkoxy claim 6 , halo claim 6 , cyano claim 6 , amino claim 6 , substituted amino claim 6 , heterocycle claim 6 , and substituted heterocycle.8. The compound of claim 6 , ...

NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 2. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Me or Et.5. A compound or pharmaceutically acceptable salt according to claim 4 , wherein Ris Calkyl.6. A compound or pharmaceutically acceptable salt according to claim 4 ,{'sup': '2', 'sub': '1-4', 'wherein Ris Calkyl.'}7. A compound or pharmaceutically acceptable salt according to claim 4 , wherein the compound is according to Formula VId claim 4 , VIe claim 4 , or VIf claim 4 , and Ris H claim 4 , Me or Et.8. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris 4-7 membered heterocycloalkenyl comprising 1 double bond claim 1 , and comprising 1 or 2 heteroatoms independently selected from N claim 1 , O claim 1 , and S claim 1 , substituted with one or more groups independently selected from R.11. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Lis —C(═O)— claim 9 , —C(═O)O— claim 9 , —O— claim 9 , or SO—.12. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Ris Me claim 9 , Et claim 9 , n-Pr claim 9 , i-Pr claim 9 , or t-Bu.13. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Ris —CH—CN claim 9 , —CH—CH—CN claim 9 , —CH—CH—OH—C(OH)H—CH claim 9 , —C(OH)H—CF claim 9 , —CHF claim 9 , —CH—CF claim 9 , —CH—CMe-OH claim 9 , —CMeH—OMe claim 9 , —CH—OH claim 9 , CMe-OH claim 9 , —CH—OMe claim 9 , —CH—C(═O)t-Bu claim 9 , ...

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound according to .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment or prophylaxis of allergic or inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of the compound according to claim 1 , sufficient to effect said treatment or prophylaxis.9. The method according to claim 1 , wherein the compound according to claim 1 , is administered in combination with a further therapeutic agent.10. The pharmaceutical composition according to claim 3 , wherein the further therapeutic agent is an agent for the treatment or prophylaxis of allergic or inflammatory conditions claim 3 , autoimmune diseases claim 3 , proliferative diseases claim 3 , transplantation rejection claim 3 , diseases involving impairment of cartilage turnover claim 3 , congenital cartilage malformations claim 3 , and/or diseases associated with hypersecretion of IL6 or interferons.11. The method according to claim 9 ...

CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 412.-. (canceled)14. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.15. A pharmaceutical composition comprising a compound of claim 3 , and a pharmaceutically acceptable adjuvant claim 3 , diluent or carrier.16. A pharmaceutical composition comprising a compound of claim 3 , and a pharmaceutically acceptable adjuvant claim 3 , diluent or carrier.17. A pharmaceutical composition comprising a compound of claim 13 , and a pharmaceutically acceptable adjuvant claim 13 , diluent or carrier.18. A method of treating an obstructive disease of the airway in a patient in need thereof claim 1 , comprising administering to the patient a therapeutically effective amount of the compound of .19. A method of treating an obstructive disease of the airway in a patient in need thereof claim 2 , comprising administering to the patient a therapeutically effective amount of the compound of .20. A method of treating an obstructive disease of the airway in a patient in need thereof claim 3 , comprising administering to the patient a therapeutically effective amount of the compound of .21. A method of treating an obstructive disease of the airway in a patient in need thereof claim 13 , comprising administering to the patient a therapeutically effective amount of the compound of .22. The method of claim 18 , wherein the administering comprises oral administration.23. The method of claim 19 , wherein the administering comprises oral administration.24. The method of claim 20 , wherein the administering comprises oral administration.25. The method of claim 21 , wherein the administering comprises oral administration. This application is a continuation of U.S. application Ser. No. 15/708,634, filed on Sep. 19, 2017, which is a continuation ...

Chemical compounds

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Chemical compounds

and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 3. A compound according to either or whereinX is O;{'sup': '6', 'sub': '1-3', 'Ris Calkyl; and'}{'sup': '7', 'Ris hydrogen; or a pharmaceutically acceptable salt thereof.'}4. A compound of the formula (I) according to selected from:(2S)-N-[(1S)-1-Cyano-2-(4′-cyanobiphenyl-4-yl)ethyl]-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(3,7-dimethyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;4′-[(2S)-2-Cyano-2-{[(2S)-1,4-oxazepan-2-ylcarbonyl]amino}ethyl]biphenyl-3-yl methanesulfonate;(2S)-N-{(1S)-1-Cyano-2-[4-(3-methyl-1,2-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4′-(trifluoromethyl)biphenyl-4-yl]ethyl1-1,4-oxazepane-2-carboxamide;(2S)-N-[(1S)-1-Cyano-2-(3′,4′-difluorobiphenyl-4-yl)ethyl]-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(6-cyanopyridin-3-yl)phenyl]ethyl1-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(3-ethyl-7-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;(2S)-N-[(1S)-1-Cyano-2-{4-[3-(2-hydroxy-2-methylpropyl)-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl]phenyl}ethyl]-1,4-oxazepane-2-carboxamide;(2S)-N-[(1S)-1-Cyano-2-{4-[3-(2,2-difluoroethyl)-7-fluoro-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl]phenyl}ethyl]-1,4-oxazepane-2-carboxamide;(2S)-N-[(1S)-1-Cyano-2-(4-{3-[2-(dimethylamino)ethyl]-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl}phenyl)ethyl]-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(3,3-difluoro-1-methyl-2-oxo-2,3-dihydro-1H-indol-6-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide;(2S)-N-{(1S)-1-Cyano-2-[4-(7-fluoro-3- ...

CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 112.-. (canceled)21. The method of claim 13 , wherein the compound is present in a sterile solution claim 13 , suspension or emulsion.22. The method of claim 19 , wherein the compound is present in a sterile solution claim 19 , suspension or emulsion.23. The method of claim 22 , wherein administering comprises parenteral administration.24. The method of claim 23 , wherein the parenteral administration is intravenous claim 23 , subcutaneous claim 23 , intramuscular claim 23 , intravascular or infusion administration.25. The method of claim 24 , wherein the parenteral administration is intravenous administration.26. The method of claim 13 , wherein administering comprises oral administration.27. The method of claim 19 , wherein administering comprises oral administration. This application is a continuation of U.S. application Ser. No. 16/855,522, filed Apr. 22, 2020, which is a continuation of U.S. application Ser. No. 16/358,091, filed Mar. 19, 2019, now U.S. Pat. No. 10,669,245, which is a continuation of U.S. application Ser. No. 15/708,634, filed Sep. 19, 2017, now U.S. Pat. No. 10,287,258, which is a continuation of U.S. application Ser. No. 15/346,411, filed Nov. 8, 2016, now U.S. Pat. No. 9,815,805, which is a continuation of U.S. application Ser. No. 14/601,371, filed Jan. 21, 2015, now U.S. Pat. No. 9,522,894, which claims the benefit of priority under 35 U.S.C. § 119(e) of U.S. Provisional Patent Application No. 61/931,090, filed Jan. 24, 2014. The contents of the foregoing application are hereby incorporated by reference in their entirety.The technical field relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof) that inhibit dipeptidyl peptidase 1 (DPP1; EC 3.4.14.1) activity, to their utility in ...

CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 112-. (canceled)14. A pharmaceutical composition comprising a compound of formula (I) as claimed in and a pharmaceutically acceptable adjuvant claim 13 , diluent or carrier.15. A method of treating an obstructive disease of the airway claim 13 , which comprises administering to the patient a therapeutically effective amount of a compound of formula (I) as claimed in .16. A method of treating asthma or chronic obstructive pulmonary disease in a patient suffering from said disease claim 13 , which comprises administering to the patient a therapeutically effective amount of a compound of formula (I) as claimed in .17. The method of claim 15 , wherein administering comprises oral administration.18. The method of claim 16 , wherein administering comprises oral administration. This application is a continuation of U.S. application Ser. No. 15/346,411, now U.S. Pat. No. 9,815,805, filed on Nov. 8, 2016, which is a continuation of U.S. application Ser. No. 14/601,371, now U.S. Pat. No. 9,522,894, filed on Jan. 21, 2015, which claims the benefit of priority under 35 U.S.C. § 119(e) of U.S. Provisional Patent Application No. 61/931,090, filed Jan. 24, 2014. The contents of the foregoing applications are hereby incorporated by reference in their entirety.The technical field relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof) that inhibit dipeptidyl peptidase 1 (DPP1; EC 3.4.14.1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.Dipeptidyl peptidase 1 (DPP1; EC 3.4.14.1), also ...

CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 112.-. (canceled)21. The method of claim 13 , wherein the obstructive disease of the airway is due to a coronavirus infection.22. The method of claim 13 , wherein the obstructive disease of the airway is due to an influenza infection.23. The method of claim 14 , wherein the obstructive disease of the airway is due to a coronavirus infection.24. The method of claim 14 , wherein the obstructive disease of the airway is due to an influenza infection.25. The method of claim 15 , wherein the obstructive disease of the airway is due to a coronavirus infection.26. The method of claim 15 , wherein the obstructive disease of the airway is due to an influenza infection.27. The method of claim 16 , wherein the obstructive disease of the airway is due to a coronavirus infection.28. The method of claim 16 , wherein the obstructive disease of the airway is due to an influenza infection.29. The method of claim 17 , wherein the obstructive disease of the airway is due to a coronavirus infection.30. The method of claim 17 , wherein the obstructive disease of the airway is due to an influenza infection.31. The method of claim 18 , wherein the obstructive disease of the airway is due to a coronavirus infection.32. The method of claim 18 , wherein the obstructive disease of the airway is due to an influenza infection.33. The method of claim 19 , wherein the obstructive disease of the airway is due to a coronavirus infection.34. The method of claim 19 , wherein the obstructive disease of the airway is due to an influenza infection.35. The method of claim 20 , wherein the obstructive disease of the airway is due to a coronavirus infection.36. The method of claim 20 , wherein the obstructive disease of the airway is due to an influenza infection.37. The method of claim 21 , wherein the coronavirus is a SARS coronavirus. ...

Compounds, Compositions and Methods Comprising Triazole Derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Compounds, Compositions and Methods Comprising Triazine Derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

The present disclosure relates to certain (2 S )- N -[(1 S )-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

(2S) -N - [(1S) -1-CYANO-2-PHENYLETHYL] -1,4-OXAZEPAN-2-CARBOXAMIDES AS DIPEPTIDYLPEPTIDASE I INHIBITORS

Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

The present disclosure relates to certain (2S)-N- [(IS)-1 -cyano-2-phenylethyl] -1,4 oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 5 (Formula (I)) that inhibit dipeptidyl peptidase 1(DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4- oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), (Formula (I)) that inhibit dipeptidyl peptidase 1(DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Pyridine-3-sulfonamide compounds as pi3-kinase inhibitors

The invention is directed to compounds of formula (I) and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.

Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors.

La presente descripción se refiere a determinados compuestos de (2S)-N-[(1S)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamida (incluidas sales farmacéuticamente aceptable de estos), (Fórmula (I)) que inhiben la actividad de dipeptidil peptidasa 1 (DPP1), para su uso en el tratamiento y/o prevención de afecciones clínicas que incluyen enfermedades respiratorias, tales como asma y enfermedad pulmonar obstructiva crónica (COPD), a su uso en terapia, a composiciones farmacéuticas que los contienen y a procesos para la preparación de los compuestos.

Compounds, Compositions and Methods Comprising Pyridazine Derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

(2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase I inhibitors

The present disclosure relates to certain (2

Chemical compounds as inhibitors of kinase activity

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3- kinase activity.

Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Compounds, compositions and methods comprising triazole derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

The present disclosure relates to certain (2S)-N- [(IS)-1 -cyano-2-phenylethyl] -1,4 oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), 5 (Formula (I)) that inhibit dipeptidyl peptidase 1(DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Compounds, compositions and methods comprising isoxazole derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

ジペプチジルペプチダーゼ１阻害剤としての（２ｓ）－ｎ－［（１ｓ）－１－シアノ－２－フェニルエチル］－１，４－オキサゼパン－２－カルボキサミド

【課題】ジペプチジルペプチダーゼ１（ＤＰＰ１）の阻害剤である化合物、喘息および慢性閉塞性肺疾患（ＣＯＰＤ）のような呼吸器疾患を包含する臨床状態の処置および／または予防におけるそれらの有用性、治療におけるそれらの使用、それらを含有する医薬組成物、ならびに該化合物の製造方法を提供する。【解決手段】ジペプチジルペプチダーゼ１（ＤＰＰ１）活性を阻害する、下記式で表される(２Ｓ)－Ｎ－[(１Ｓ)－１－シアノ－２－フェニルエチル]－１,４－オキサゼパン－２－カルボキサミド化合物（その医薬上許容される塩を含む）を提供する。TIFF2023156479000111.tif4164【選択図】なし

Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Compounds, compositions and methods comprising imidazole and triazole derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formulas (I), (IA), (IB), (II), and (III)) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2,S)-N-[(1,S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Composto, composição farmacêutica, e, uso de um composto

A invenção está direcionada a certos novos compostos. Especificamente, a invenção está direcionada a compostos da fórmula (I): (I) e sais dos mesmos. Os compostos da invenção são inibidores da atividade da cinase, em particular da atividade da PI3 cinase.

Compounds, compositions and methods comprising thiazole derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Compounds, compositions and methods comprising oxadiazole derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I, II, or III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Compounds, compositions and methods comprising imidazole and triazole derivatives

Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

(2s)-n-[(1s)-1-kyano-2-φainyλaιθyλ]-1,4-oξazeπan-2-καρβοξαμιδια ως αναστολεις της διπεπτιδυλικης πεπτιδασης ι

Η παρούσα δημοσίευση σχετίζεται με ορισμένες ενώσεις του (2S)-N-[(1S)-1-κυανο-2-φαινυλαιθυλ] -1,4-οξαζεπαν-2-καρβοξαμιδίου (συμπεριλαμβανομένων των φαρμακευτικώς αποδεκτών αλάτων αυτών), που αναστέλλουν τη δράση της διπεπτιδυλικής πεπτιδάσης 1 (DPP1), στη χρησιμότητα τους στη θεραπεία και / ή την πρόληψη των κλινικών παθήσεων συμπεριλαμβανομένων των αναπνευστικών νόσων, όπως το άσθμα και η χρόνια αποφρακτική πνευμονοπάθεια (ΧΑΠ), στη χρήση τους στη θεραπεία, σε φαρμακευτικές συνθέσεις που τις περιέχουν και διεργασίες για την παρασκευή τέτοιων ενώσεων.

Compounds, compositions and methods comprising pyridazine derivatives

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-a]pyrimidines as antidepressant agents

The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia, head injuries and haemorrhage.

Chemical compounds as inhibitors of kinase activity

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3- kinase activity.

Compuestos químicos como inhibidores de la actividad cinasa

Un compuesto de fórmula (I): **(Ver fórmula)** en la que R1 es alcoxi C1-6 o -N(alquil-C1-6)2; R2 es hidrógeno o alquilo C1-6 opcionalmente sustituido con -C(O)Oalquilo C1-6 o -OC(O)alquilo C1-6; R3, R4, R5 y R6 se seleccionan cada uno independientemente de hidrógeno y halógeno; R7 y R8 son cada uno independientemente alquilo C1-6, o R7 y R8, junto con el átomo de nitrógeno al que están unidos, se unen para formar un heterociclilo de 5 o 6 miembros, en el que el heterociclilo de 5 o 6 miembros opcionalmente contiene un átomo de nitrógeno adicional y está opcionalmente sustituido con cicloalquilo C3-6, un heterociclilo de 4 a 6 miembros que contiene uno o dos heteroátomos seleccionados independientemente de oxígeno y nitrógeno o alquilo C1-6, en el que el alquilo C1-6 está opcionalmente sustituido con hidroxi o alcoxi C1-6, o R7 y R8, junto con el átomo de nitrógeno al que están unidos, se unen para formar un heterociclilo de 5 o 6 miembros, en el que el heterociclilo de 5 o 6 miembros contiene un átomo de oxígeno y está opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados de alquilo C1-6; o una sal del mismo.

composto, composição farmacêutica, uso de um composto, e, método para tratar um distúrbio

a invenção está direcionada a certos novos compostos. especificamente, a invenção está direcionada a compostos da fórmula (i): (i) e sais dos mesmos. os compostos da invenção são inibidores da atividade da cinase, em particular da atividade da pi3 cinase.

Chemical compounds as inhibitors of kinase activity

Chemical compounds

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-a]pyrimidines as antidepressant agents

The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia, head injuries and haemorrhage.

Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.