Phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, m, R 1 , R 2 , R 3 , R 4 , and R 5 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms.

BI-FUNCTIONAL QUINOLINE ANALOGS

Provided are compounds of Formula I: 2. The compound of wherein Ris selected from Calkylene claim 1 , Calkenylene claim 1 , Calkynylene claim 1 , R—O—R claim 1 , R—N(R)—R claim 1 , Ccycloalkylene claim 1 , R—Ccycloalkylene claim 1 , R—Ccycloalkylene-Het claim 1 , Ccycloalkylene-R claim 1 , R—Ccycloalkylene-R claim 1 , phenylene claim 1 , R-phenylene claim 1 , phenylene-R claim 1 , R-phenylene-R claim 1 , R-phenylene-O—R claim 1 , R-phenylene-N(R)—R claim 1 , R-phenylene-phenylene claim 1 , Het claim 1 , R—Het claim 1 , Het-R claim 1 , R-Het-R claim 1 , R—O-Het claim 1 , R-phenylene-O-Het claim 1 , R-phenylene-C(O)—Het claim 1 , R-phenylene-N(R)—Het claim 1 , R-Het-phenylene claim 1 , R-phenylene-Het claim 1 , and R—O—R-phenylene; or a pharmaceutically acceptable salt thereof.4. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris CHOH and Ris H.5. The compound according to or a pharmaceutically acceptable salt thereof wherein Rand Rtogether with the phenyl to which they are bound form a bicyclic claim 1 , fused heterocyclic ring having 9 or 10 ring atoms wherein 1 or 2 ring atoms are selected from N claim 1 , O and S claim 1 , and said bicyclic fused heterocyclic ring is optionally substituted with one additional substituent selected from alkyl claim 1 , oxo and OH.7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from Calkylene claim 1 , Calkenylene claim 1 , Calkynylene claim 1 , R—O—R claim 1 , and R—N(R)—R claim 1 , wherein said alkylene claim 1 , alkenylene or alkynylene are each optionally substituted with 1 claim 1 , 2 or 3 substituents selected from halo claim 1 , oxo claim 1 , and OR.8. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from Calkylene claim 1 , Calkenylene claim 1 , Calkynylene claim 1 , R—O—R claim 1 , and R—N(R)—R claim 1 , wherein each Ris Calkylene claim 1 , Calkenylene claim 1 , ...

Phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which n, m, R 1 , R 2 , and R 3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present disclosure provides phosphatidylinositol -kinase (PBK) inhibitors of formula (J), 32. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently methyl claim 1 , chloro claim 1 , fluoro claim 1 , cyano claim 1 , tetrahydropyridinyl claim 1 , —CH2—C(═O)OH claim 1 , —CH—C(═O)OH claim 1 , —CH—C(═O)OH claim 1 , —CH—C(═O)NH claim 1 , —CH—C(═O)N(CH) claim 1 , —CH—C(═O)NH claim 1 , —CH—C(═O)N(CH) claim 1 , —CH—C(═O)NH claim 1 , —CH—C(═O)N(CH) claim 1 , —CH—C(═O)-Het claim 1 , CH—C(═O)-Het claim 1 , —CH—C(═O)-Het claim 1 , O—CH—C(═O)OCH claim 1 , O—CH—C(═O)OCH claim 1 , O—CH—C(═O)OCH claim 1 , —CH-Het claim 1 , —CH-Het claim 1 , —CH-Het claim 1 , —CH-cyclopropyl claim 1 , —CH-cyclopropyl claim 1 , —CH-cyclopropyl claim 1 , —CH-cyclobutyl claim 1 , —CH-cyclobutyl claim 1 , —CH-cyclobutyl claim 1 , —CH-cyclopentyl claim 1 , —CH-cyclopentyl claim 1 , CH-cyclopentyl claim 1 , —CH-cyclohexyl claim 1 , —CH-cyclohexyl claim 1 , —CH-cyclohexyl claim 1 , O—CH—NH claim 1 , O—CH—NH claim 1 , O—CH—NH claim 1 , O—CH—N(CH) claim 1 , O—CH—N(CH) claim 1 , O—CH—N(CH) claim 1 , O—-CH-Het claim 1 , O—CH-Het claim 1 , O—CH-Het claim 1 , O—CH—C(═O)OH claim 1 , O—CH—C(═O)OH claim 1 , O—CH—C(═O)OH claim 1 , O—CH—C(═O)OCH claim 1 , O—CH—C(═O)OCH claim 1 , O—CH—C(═O)OCH claim 1 , O—CH—C(═O)-Het claim 1 , O—CHC(CH)(CHOH) claim 1 , S—CHOH claim 1 , S—CHOH claim 1 , SO-phenyl claim 1 , SO-methylphenyl claim 1 , —SO-ethylphenyl claim 1 , —SO-cyclopropyl claim 1 , —SO-cyclobutyl claim 1 , —SO-cyclopentyl claim 1 , —SOCH-HET claim 1 , —SOCH claim 1 , —SOCH claim 1 , —SOCH claim 1 , —SOCHOH claim 1 , or —SOCHOH; wherein Het is independently selected from piperidinyl claim 1 , morpholinyl claim 1 , piperazinyl claim 1 , azepanyl claim 1 , imidazolyl claim 1 , oxetanyl claim 1 , azetidinyl claim 1 , pyrrolidinyl claim 1 , tetrahydropyridinyl claim 1 , 2-oxa-7-azaspiro[3.5]nonanyl claim 1 , 2-oxa-6-azaspiro[3.4]octanyl claim 1 , and 6-oxa-1-azaspiro[3.3 ...

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), 2. The compound of claim 1 , whereinn is 1 or 2;{'sup': '1', 'each Ris independently selected from halo, cyano, alkyl, or alkylsulfonyl, wherein the alkyl moiety may be optionally substituted with 1 to 3 halogen;'}m is 0, 1, or 2;{'sup': '2', 'each Ris independently selected from halo, alkoxy, alkyl, or cycloalkyl, wherein the alkyl moiety may be optionally substituted with 1 to 3 halogen;'}{'sup': '3', 'Ris hydrogen, alkyl, or cycloalkyl, wherein the alkyl moiety may be optionally substituted with cycloalkyl; and'}{'sup': '4', 'Ris cyano.'}3. The compound of claim 1 , wherein each Ris independently selected from halo claim 1 , cyano claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , or Calkylsulfonyl.4. The compound of claim 3 , wherein each Ris independently selected from fluoro claim 3 , chloro claim 3 , iodo claim 3 , bromo claim 3 , cyano claim 3 , methyl claim 3 , ethyl claim 3 , propyl claim 3 , butyl claim 3 , fluoromethyl claim 3 , fluoroethyl claim 3 , difluoromethyl claim 3 , difluoroethyl claim 3 , trifluoromethyl claim 3 , trifluoroethyl claim 3 , methylsulfonyl claim 3 , ethylsulfonyl claim 3 , or propylsulfonyl.5. The compound of claim 1 , wherein each Ris independently selected from halo claim 1 , —NH claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , or Ccycloalkyl.6. The compound of claim 5 , wherein each Ris independently selected from —NH claim 5 , fluoro claim 5 , chloro claim 5 , iodo claim 5 , bromo claim 5 , methoxy claim 5 , ethoxy claim 5 , propoxy claim 5 , butoxy claim 5 , pentoxy claim 5 , hexoxy claim 5 , methyl claim 5 , ethyl claim 5 , propyl claim 5 , butyl claim 5 , fluoromethyl claim 5 , fluoroethyl claim 5 , difluoromethyl claim 5 , difluoroethyl claim 5 , trifluoromethyl claim 5 , cyclopropyl claim 5 , cyclobutyl claim 5 , cyclopentyl claim 5 , or cyclohexyl.7. The compound of claim 1 , wherein Ris selected from hydrogen ...

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), 120-. (canceled)22. The method of claim 21 , wherein the disease is selected from the group consisting of acute lymphocytic leukemia (ALL) claim 21 , acute myeloid leukemia (AML) claim 21 , chronic lymphocytic leukemia (CLL) claim 21 , small lymphocytic lymphoma (SLL) claim 21 , myelodysplastic syndrome (MDS) claim 21 , myeloproliferative disease (MPD) claim 21 , chronic myeloid leukemia (CML) claim 21 , juvenile myelomonocytic leukemia (JMML) claim 21 , multiple myeloma (MM) claim 21 , Hodgkin lymphoma claim 21 , indolent non-Hodgkin's lymphoma (iNHL) claim 21 , refractory iNHL claim 21 , non-Hodgkin's lymphoma (NHL) claim 21 , mantle cell lymphoma (MCL) claim 21 , follicular lymphoma claim 21 , Waldestrom's macroglobulinemia (WM) claim 21 , minimal residual disease (MRD) claim 21 , T-cell lymphoma claim 21 , B-cell lymphoma claim 21 , diffuse large B-cell lymphoma (DLBCL) claim 21 , T-cell acute lymphoblastic leukemia (T-ALL) claim 21 , B-cell acute lymphoblastic leukemia (B-ALL) claim 21 , lymphoplasmacytic lymphoma claim 21 , marginal zone lymphoma claim 21 , Burkitt lymphoma claim 21 , pancreatic cancer claim 21 , bladder cancer claim 21 , colorectal cancer claim 21 , breast cancer claim 21 , prostate cancer claim 21 , renal cancer claim 21 , hepatocellular cancer claim 21 , lung cancer claim 21 , ovarian cancer claim 21 , cervical cancer claim 21 , gastric cancer claim 21 , esophageal cancer claim 21 , head and neck cancer claim 21 , melanoma claim 21 , neuroendocrine cancers claim 21 , CNS cancers claim 21 , brain tumors claim 21 , bone cancer claim 21 , soft tissue sarcoma claim 21 , systemic lupus erythematosus (SLE) claim 21 , myestenia gravis claim 21 , rheumatoid arthritis (RA) claim 21 , psoriasis claim 21 , acute disseminated encephalomyelitis claim 21 , idiopathic thrombocytopenic purpura claim 21 , multiple sclerosis (MS) claim 21 , Sjoegren's syndrome ...

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present application provides the compounds of formula I 11. A pharmaceutical composition comprising the compound of and at least one pharmaceutically acceptable vehicle.12. A method of treating a disease or condition in a human in need thereof comprising administering to the human a therapeutically effective amount of the compound of claim 1 , wherein the disease or condition is selected from cancer claim 1 , hematologic malignancies claim 1 , leukemias claim 1 , lymphomas claim 1 , myeloproliferative disorders claim 1 , myelodysplastic syndromes claim 1 , plasma cell neoplasms claim 1 , or solid tumor.13. A method of treating a disease or condition in a human in need thereof comprising administering to the human a therapeutically effective amount of the compound of claim 1 , wherein the disease or condition is selected from inflammation claim 1 , fibrosis claim 1 , autoimmune disorders claim 1 , allergic conditions claim 1 , hypersensitivity claim 1 , cardiovascular diseases claim 1 , neurodegenerative diseases claim 1 , renal disorders claim 1 , viral infections claim 1 , obesity claim 1 , and autoimmune diseases.14. A method of treating prostate cancer in a human in need thereof comprising administering to the human a therapeutically effective amount of the compound of .15. A method of inhibiting the activity of phosphatidylinositol 3-kinase polypeptide by contacting the polypeptide with the compound of .16. A method of inhibiting excessive or destructive immune reactions or growth or a proliferation of cancer cells claim 1 , comprising administering an effective amount of the compound of .17. A method of treating a disease or condition in a human in need thereof comprising administering to the human a therapeutically effective amount of the compound of in combination with therapeutically effective amount of a compound that inhibits or modulates the activity of poly(ADP-ribose) polymerases (PARP) claim 1 , Tankyrases (TANKs) claim 1 , matrix ...

Phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as described herein.

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present application provides the compounds of formula I 13. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , fluoro claim 1 , chloro claim 1 , bromo claim 1 , iodo claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , fluoromethyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , fluoroethyl claim 1 , difluoroethyl and trifluoroethyl; or a pharmaceutically acceptable salt claim 1 , isomer claim 1 , or a mixture thereof.14. The compound of claim 1 , wherein Ris Calkyl claim 1 , Ccycloalkyl claim 1 , 5-6 membered heteroaryl containing 1 to 3 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S claim 1 , and 4-6 membered heterocyclyl containing 1 to 4 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S; wherein each Calkyl claim 1 , Ccycloalkyl claim 1 , 5-6 membered heteroaryl and 4-6 membered heterocyclyl is optionally substituted with one to four R;or a pharmaceutically acceptable salt, isomer, or a mixture thereof.15. The compound of claim 1 , wherein Ris selected from 5-10 membered heteroaryl containing 1 to 4 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S claim 1 , —C(O)OH claim 1 , and —C(O)NH; or a pharmaceutically acceptable salt claim 1 , isomer claim 1 , or a mixture thereof.16. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , trifluoromethyl claim 1 , carboxamide claim 1 , cyano claim 1 , piperazinyl claim 1 , cyclopropyl claim 1 , phenyl and triazolyl; or a pharmaceutically acceptable salt claim 1 , isomer claim 1 , or a mixture thereof.18. A pharmaceutical composition comprising the compound according to and at least one pharmaceutically acceptable vehicle.19. A method of treating a disease or condition in a human in need thereof comprising administering to the human a therapeutically effective amount of the compound or composition according to claim 1 , ...

IMIDAZOPYRIDINE DERIVATIVES

The present disclosure provides a compound of Formula (I):

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris:unsubstituted aryl;unsubstituted heteroaryl;unsubstituted cycloalkyl;{'sup': 1a', '1a', '1a', '1a, 'sub': '2', 'aryl, heteroaryl, or cycloalkyl substituted with 1 or 2 substituents independently selected from the group consisting of halo, —OR, —C(O)OR, —C(O)R, NH, alkyl, and haloalkyl, wherein Ris alkyl or haloalkyl;'}unsubstituted alkyl; oralkyl substituted with OH.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently halo or unsubstituted alkyl claim 1 , alkyl substituted with cyano or haloalkyl.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris:{'sub': '6-12', 'unsubstituted Caryl; or'}{'sub': 6-12', '2', '1-6, 'sup': 3a', '3b', '3a', '3b', '3a', '3b, 'Caryl substituted with 1 or 2 substituents independently selected from the group consisting of halo, alkyl, haloalkyl, cyano, —C(O)NRRand —SONRR, wherein Rand Rare independently hydrogen or Calkyl.'}7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen claim 1 , Calkyl claim 1 , or NH.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rtogether with the carbon to which it is attached and Rtogether with the nitrogen to which it is attached are taken together to form a five- or six-membered heterocycloalkyl.11. The compound of claim 1 , wherein the compound is the (S)-enantiomer.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting ...

QUINOLINE DERIVATIVES

The present disclosure provides a compound of Formula (I): 1. (canceled)339-. (canceled)4157-. (canceled)5961-. (canceled)63. The compound of claim 2 , or a pharmaceutically acceptable salt thereof; wherein Rand Rare H.6465-. (canceled)66. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein each Rand Ris independently selected from F and —CH.6770-. (canceled)7280-. (canceled)81. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from H claim 2 , methyl claim 2 , and ethyl.8286-. (canceled)8899-. (canceled)104. A pharmaceutical composition comprising the compound of claim 100 , or a pharmaceutically acceptable salt thereof claim 100 , and at least one pharmaceutically acceptable carrier.105. The pharmaceutical composition of claim 104 , further comprising at least one or more additional therapeutic agents.106. The pharmaceutical composition of claim 105 , wherein the at least one or more additional therapeutic agents are independently selected from JAK tyrosine kinase inhibitors claim 105 , Tumor Progression Locus 2 (TPL2) inhibitors claim 105 , and IRAK4 inhibitors.107. The pharmaceutical composition of claim 106 , wherein the additional therapeutic agent is a JAK tyrosine kinase inhibitor claim 106 , and wherein the JAK tyrosine kinase inhibitor is Filgotinib.108. A method for treating an inflammatory disease or condition associated with α4β7 integrin comprising administrating to a subject an effective amount of the compound of claim 100 , or a pharmaceutically acceptable salt thereof.109. The method of claim 108 , wherein the inflammatory disease or condition is selected from inflammatory bowel disease (IBD) claim 108 , Ulcerative colitis claim 108 , Crohn's disease claim 108 , graft-versus-host disease (GVHD) claim 108 , and primary sclerosing cholangitis (PSC).110. A pharmaceutical composition comprising the compound of claim 101 , or a pharmaceutically acceptable salt ...

COMPOUNDS FOR INHIBITION OF ALPHA 4 BETA 7 INTEGRIN

The present disclosure provides a compound of Formula (I): 57-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from phenyl claim 1 , naphthyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , pyrimidinyl claim 1 , quinolinyl claim 1 , isoquinolinyl claim 1 , isoxazolyl claim 1 , triazolyl claim 1 , pyrazolyl claim 1 , benzothiazolyl claim 1 , pyridinonyl claim 1 , quinolinonyl claim 1 , isoquinolinonyl claim 1 , quinazolindionyl claim 1 , pyrazinonyl claim 1 , pyrimidinonyl claim 1 , pyrimidinedionyl claim 1 , pyridazinonyl claim 1 , quinazolinonyl claim 1 , benzofuranyl claim 1 , tetrahydrocyclopenta[b]pyridinonyl claim 1 , naphthyridinonyl claim 1 , chromanyl claim 1 , isochromanyl claim 1 , and chromenonyl claim 1 , and wherein each Ris independently optionally substituted with one to four R.1016-. (canceled)17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from —CH claim 1 , —CD claim 1 , F claim 1 , and Cl.1825-. (canceled)27. (canceled)2931-. (canceled)3334-. (canceled)36. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from H claim 1 , methyl claim 1 , and ethyl.37. (canceled)39. (canceled)44. (canceled)45. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable carrier.46. The pharmaceutical composition of claim 45 , further comprising at least one or more additional therapeutic agents.47. A method for treating an inflammatory disease or condition mediated by α4β7 integrin comprising administrating to a subject an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.4854-. (canceled)55. The pharmaceutical composition of claim 46 , wherein the at least one or more additional therapeutic ...

Compounds for Inhibition of Alpha 4 Beta 7 Integrin

The present disclosure provides a compound of Formula (I): 2. (canceled)67-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , where A claim 1 , A claim 1 , or Ais selected from phenyl claim 1 , naphthyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , pyrimidinyl claim 1 , quinolinyl claim 1 , isoquinolinyl claim 1 , isoxazolyl claim 1 , triazolyl claim 1 , pyrazolyl claim 1 , benzothiazolyl claim 1 , pyridinonyl claim 1 , quinolinonyl claim 1 , isoquinolinonyl claim 1 , quinazolindionyl claim 1 , pyrazinonyl claim 1 , pyrimidinonyl claim 1 , pyrimidinedionyl claim 1 , pyridazinonyl claim 1 , quinazolinonyl claim 1 , benzofuranyl claim 1 , tetrahydrocyclopenta[b]pyridinonyl claim 1 , naphthyridinonyl claim 1 , chromanyl claim 1 , isochromanyl claim 1 , and chromenonyl claim 1 , and wherein each Rwhich is independently optionally substituted with one to four R.1011-. (canceled)1415-. (canceled)16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from F claim 1 , Cl claim 1 , cyano claim 1 , hydroxyl claim 1 , —CH claim 1 , -CD claim 1 , —CHCH claim 1 , —CH(CH) claim 1 , —C(CH) claim 1 , cyclopropyl claim 1 , —OCH claim 1 , —OCHCH claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —CHCHF claim 1 , —CHCHF claim 1 , —CHCF claim 1 , —OCF claim 1 , —NH claim 1 , and —N(CH).17. (canceled)18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Rand Ris independently selected from H claim 1 , Calkyl claim 1 , Calkoxyl claim 1 , Chaloalkyl claim 1 , and Chaloalkoxyl.1922-. (canceled)2434-. (canceled)36. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from H claim 1 , methyl claim 1 , and ethyl.3738-. (canceled)4042-. (canceled)43. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt ...

IMIDAZOPYRIDINE DERIVATIVES

The present disclosure provides a compound of Formula (I): 35-. (canceled)7. (canceled)10. (canceled)13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is a bond.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from phenyl claim 1 , naphthyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , quinolinyl claim 1 , isoxazolyl claim 1 , pyridinonyl claim 1 , quinolinonyl claim 1 , pyrazinonyl claim 1 , pyrimidinonyl claim 1 , pyridazinonyl claim 1 , quinazolinonyl claim 1 , quinazolindionyl claim 1 , pyridopyrimidine-dionyl claim 1 , and imidazopyridinonyl; and wherein each Ris independently optionally substituted with one to four R.1518-. (canceled)2022-. (canceled)2433-. (canceled)35. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.36. (canceled)3839-. (canceled)40. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable carrier.41. A method for treating an inflammatory disease or condition associated with α4β7 integrin comprising administrating to a subject an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.42. (canceled)43. The method of claim 41 , wherein the inflammatory disease or condition is selected from inflammatory bowel disease (IBD) claim 41 , Ulcerative colitis claim 41 , Crohn's disease claim 41 , graft-versus-host disease (GVHD) claim 41 , and primary sclerosing cholangitis (PSC).4447-. (canceled)48. The pharmaceutical composition of claim 40 , further comprising at least one or more additional therapeutic agents.49. The pharmaceutical composition of claim 48 , wherein the at least one or more additional therapeutic agents are independently selected from JAK tyrosine kinase inhibitors claim 48 , Tumor Progression Locus 2 (TPL2) inhibitors claim 48 , and IRAK4 inhibitors.50. The pharmaceutical composition of claim 49 , ...

Phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R 1 , R 2 , n, R 3 , R 4 , R 5 and R 6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

Phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts or isomers thereof, in which n, m, R 1 , R 2 , R 4 , and R 3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts or isomers thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present application provides the compounds of formula (J), 2. The compound of claim 1 , whereinA is a single bond or C(O);{'sub': 1-4', '1-4', '3-6', '1-4, 'each R′ is independently selected from hydrogen, halo, Calkyl, Chaloalkyl, and Ccycloalkyl, wherein the alkyl moiety is optionally substituted with Calkoxy;'}{'sup': '1', 'sub': 1-4', '1-4', '2', '1-4, 'each Ris independently selected from halo, cyano, Calkyl, Chaloalkyl, and —SOCalkyl;'}{'sup': '2', 'sub': 1-4', '1-4', '3-6', '1-4, 'each Ris independently selected from halo, Calkyl, Chaloalkyl, and Ccycloalkyl, wherein the alkyl moiety is optionally substituted with Calkoxy;'}{'sup': '3', 'sub': 1-4', '3-6', '6-10', '1-4', '1-4', '6-10, 'Ris hydrogen, Calkyl, Ccycloalkyl, or Caryl; wherein the alkyl moiety is optionally substituted with hydroxyl or Calkoxy, wherein Calkoxy is optionally substituted with Caryl;'}{'sup': '4', 'sub': 2', '2-4', '1-4', '1-4', '2-4', '6-10', '3-8', '6-10', '3-8', '1-6, 'Ris a six- to twelve-membered heteroaryl having at least one aromatic ring and at least two nitrogen atoms, wherein the heteroaryl is optionally substituted with one, two, or three members independently selected from halo, cyano, —NH, Calkynyl, Chaloalkyl, and Calkyl, wherein the Calkynyl moiety is optionally substituted with Caryl or Cheteroaryl, wherein each of the Caryl and Cheteroaryl moieties is optionally substituted with one or two members independently selected from halo and Chaloalkyl; and'}{'sup': 5', '5', '3, 'sub': '1-4', 'Ris hydrogen or Calkyl; Rand Rtogether with the nitrogen to which they are attached optionally form a five-membered heterocyclic ring;'}or a pharmaceutically acceptable salt, isomer, or a mixture thereof.3. The compound of claim 1 , wherein each Ris independently selected from fluoro claim 1 , chloro claim 1 , bromo claim 1 , iodo claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , fluoromethyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , ...

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present application provides the compounds of formula (J), 2. The compound of claim 1 , whereinn is 1 or 2;m is 0 or 1;{'sup': '1', 'sub': 1-6', '1-6, 'each Ris independently selected from halo, Calkyl, and Chaloalkyl;'}{'sup': '2', 'sub': '1-6', 'each Ris independently selected from Calkyl;'}{'sup': '3', 'sub': 1-6', '3-8, 'Ris hydrogen, Calkyl, or Ccycloalkyl;'}{'sup': '4', 'sub': 2', '1-6', '1-6, 'Ris a six- to twelve-membered heteroaryl having at least one aromatic ring and at least two nitrogen atoms, wherein the heteroaryl is optionally substituted with one, two, or three members independently selected from halo, cyano, —NH, Chaloalkyl, and Calkyl; and'}{'sup': 5', '5', '3, 'Ris hydrogen, methyl, ethyl, or propyl, or Rand Rtogether with the atoms to which they are attached optionally form a five-membered heterocyclic ring;'}or a pharmaceutically acceptable salt, isomer, or a mixture thereof.3. The compound of claim 1 , wherein each Ris independently selected from chloro claim 1 , bromo claim 1 , fluoro claim 1 , methyl claim 1 , ethyl claim 1 , and propyl.4. The compound of claim 1 , wherein each Ris independently selected from methyl claim 1 , ethyl claim 1 , and propyl.5. The compound of claim 1 , wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , cyclopropyl claim 1 , or cyclobutyl.6. The compound of claim 1 , wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , or propyl.7. The compound of claim 1 , Rand Rtogether with the atoms to which they are attached optionally form pyrrolidinyl.8. The compound of claim 1 , wherein Ris a monocyclic heteroaryl having at least two nitrogen atoms claim 1 , wherein Ris substituted with two or three members independently selected from bromo claim 1 , chloro claim 1 , fluoro claim 1 , cyano claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , and —NH.9. The compound of claim 8 , wherein Ris pyrimidinyl substituted with two or three members selected from the ...

PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS

The present application provides the compounds of formula (J), 3. The compound of claim 1 , whereinn is 0, 1, 2, or 3;m is 0, 1, or 2;{'sup': 2', 'w, 'Wis C(R) or N;'}{'sup': 'w', 'sub': '1-6', 'Ris hydrogen, halo, or Calkyl;'}{'sup': '1', 'sub': 1-6', '1-6', '1-6, 'each Ris independently halo, cyano, optionally substituted Calkyl, Chaloalkyl, or Calkylsulfonyl;'}{'sup': '2', 'sub': 1-6', '1-6', '3-8, 'each Ris independently halo, optionally substituted Calkyl, optionally substituted Calkoxy, or optionally substituted Ccycloalkyl;'}{'sup': '3', 'sub': 1-6', '3-8', '3-8, 'Ris hydrogen, optionally substituted Calkyl, optionally substituted Ccycloalkyl, or optionally substituted Caryl;'}{'sup': '4', 'sub': 2', '1-6', '2-4', '1-6, 'Ris a six to twelve-membered heteroaryl having at least one aromatic ring and at least two heteroatoms selected from N, O, and S, and the heteroaryl is optionally substituted with one, two, or three members which are independently halo, cyano, —NH, Chaloalkyl, Calkynyl which is substituted with heteroaryl, or optionally substituted Calkyl; and'}{'sup': 5', '5', '3, 'sub': '1-6', 'Ris hydrogen or optionally substituted Calkyl; or Rand Rtogether with the atoms to which they are attached form a four- to eight-membered heterocyclic ring;'}or a pharmaceutically acceptable salt, isomer, or a mixture thereof.4. The compound of claim 1 , wherein each Ris chloro claim 1 , bromo claim 1 , fluoro claim 1 , methyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , ethyl claim 1 , propyl claim 1 , or cyano.5. The compound of claim 1 , wherein each Ris chloro claim 1 , bromo claim 1 , fluoro claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , cyclopropyl claim 1 , methoxyproproyl claim 1 , methoxyethyl claim 1 , ethoxypropyl claim 1 , or ethoxyethyl.6. The compound of claim 1 , wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , or phenyl.7. The ...

Bifunctional quinoline derivatives

Provided are compounds of Formula (I): Wherein X is:(Formula (II)) or (Formula (III)) R 1 and R 2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

Compounds for inhibition of .alpha.4.beta.7 integrin

The present disclosure provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Compounds for inhibition of alpha 4 beta 7 integrin

The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors

The present application provides fee compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m', A', R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidyiinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R

Phosphatidylinositol 3-kinase inhibitors

The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R1, R2, R3 R4, R5, R6 and R7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more ?I3? isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms.

3-QUINASA PHOSFATIDYLINOSITOL INHIBITORS

Los compuestos son inhibidores de las actividades de la fosfatidilinositol 3-quinasa (Pl3K) y son útiles para el tratamiento de condiciones mediadas por una o más isoformas de Pl3K. La presente solicitud provee adicionalmente composiciones farmacéuticas que incluyen un compuesto de fórmula (1), o sales, isómeros, tautómeros o mezclas de los mismos farmacéuticamente aceptables, y métodos para utilizar estos compuestos y composiciones para el tratamiento de condiciones mediadas por una o más isoformas de Pl3K. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), en donde: X, Y, Z son seleccionados independientemente de C(R) o N, en donde al menos uno de X, Y, y Z es C(R); n es 0, 1, 2, 3, o 4; m es 0 ó 1; A es un enlace sencillo o C(O); cada R es seleccionado independientemente de hidrógeno, halo, alquilo opcionalmente sustituido, haloalquilo opcionalmente sustituido, y cicloalquilo opcionalmente sustituido; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono opcionalmente sustituido, alcoxi de uno a seis átomos de carbono opcionalmente sustituido, hidroxi, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, y sulfonilo opcionalmente sustituido; cada R² es seleccionado independientemente de halo, alquilo de uno a seis átomos de carbono opcionalmente sustituido, haloalquilo de uno a seis átomos de carbono opcionalmente sustituido, y cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido; R³ es hidrógeno, alquilo de uno a seis átomos de carbono opcionalmente sustituido, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, o arilo de seis a diez átomos de carbono opcionalmente sustituido; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos dos heteroátomos, en donde cada heteroátomo es seleccionado independientemente de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionado ...

Compounds for inhibition of alpha 4 beta 7 integrin

The present disclosure provides a compound of Formula (I):or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof wherein n, m, R1, R2, R3, R4, and R5 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (?I3?) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more ?I3? isoforms.

Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors

Compounds for inhibition of alpha 4 beta 7 integrin

The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors

The present application provides fee compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m', A', R 1 , R 2 , and R 3 are described herein. The compounds are inhibitors to the activities of phosphatidyiinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Quinoline derivatives

The present disclosure provides a compound of Formula (I):or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Macrocyclic inhibitors of peptidylarginine deiminases

The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

Compounds for inhibition of alpha 4 beta 7 integrin

【課題】 疾患を処置するための方法を提供すること【解決手段】 本開示は、本明細書中に記載される、式（Ｉ）：TIFF2022140725000340.tif4741の化合物、またはその薬学的に受容可能な塩を提供するものである。本開示はまた、式（Ｉ）の化合物を含有する薬学的組成物、式（Ｉ）の化合物を調製するためのプロセス、および炎症性疾患を処置するための治療法を提供するものである。本開示は、一般的に、α４β７インテグリン阻害作用を有する新規の化合物、α４β７インテグリン阻害作用を有する化合物のプロドラッグ、ならびにその使用および製造の方法に関するものである。【選択図】なし

Quinoline derivatives as alpha4beta7 integrin inhibitors

The present disclosure provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein X, Y, Z, n, m′, A′, R 1 , R 2 , and R 3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Quinoline derivatives as alpha4beta7 integrin inhibitors

The present disclosure provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Phosphatidylinositol 3-kinase inhibitors

Phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A', W1, W2, W3, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors

Un compuesto que tiene la estructura de Fórmula (I):**Fórmula** en donde: X, Y y Z se seleccionan independientemente de C(R') y N, en donde al menos uno de X, Y y Z es C(R'); n es 0, 1, 2, 3 o 4; m' es 0 o 1; A es un enlace simple o C(O); cada R' se selecciona independientemente de hidrógeno, halo, alquilo opcionalmente sustituido, haloalquilo opcionalmente sustituido y cicloalquilo opcionalmente sustituido; cada R1 se selecciona independientemente de halo, ciano, C1-6 alquilo opcionalmente sustituido, C1-6 alcoxi opcionalmente sustituido, hidroxi, C3-8 cicloalquilo opcionalmente sustituido y sulfonilo opcionalmente sustituido; cada R2 se selecciona independientemente de halo, C1-6 alquilo opcionalmente sustituido, haloC1-6 alquilo opcionalmente sustituido y C3-8 cicloalquilo opcionalmente sustituido; R3 es hidrógeno, C1-6 alquilo opcionalmente sustituido, C3-8 cicloalquilo opcionalmente sustituido, o C6-10 arilo opcionalmente sustituido; R4 es un heteroarilo de seis a doce miembros que tiene al menos dos heteroátomos, en donde cada heteroátomo se selecciona independientemente de N, O y S, en donde el heteroarilo está opcionalmente sustituido con uno, dos o tres miembros seleccionados independientemente de halo, ciano, -NH2, C1-6 alquilo opcionalmente sustituido, y C2-6 alquinilo opcionalmente sustituido; y R5 es hidrógeno o C1-6 alquilo opcionalmente sustituido; o R5 y R3 junto con los átomos a los que están unidos forman opcionalmente un anillo heterocíclico de cuatro a ocho miembros; o una sal farmacéuticamente aceptable, isómero de doble enlace, racemato, estereoisómero, enantiómero, diastereómero, atropisómero o una mezcla de los mismos.

compound, pharmaceutical composition, and method for treating a human

1 / 1 resumo “composto, composiã‡ãƒo farmacãšutica, e, mã‰todo para o tratamento de um humanoâ€� a presente descriã§ã£o fornece inibidores de fosfatidilinositol 3-quinase (pi3k) da fã³rmula (i), (i), ou um sal farmaceuticamente aceitã¡vel do mesmo, na qual n, 3 m, râ¹, râ², e r sã£o definido aqui. estes compostos sã£o ãºteis no tratamento de condiã§ãµes mediadas por um ou mais isoformas de pi3k, tais como pi3kî´. a presente descriã§ã£o fornece adicionalmente composiã§ãµes farmacãªuticas que incluem um composto da fã³rmula (i), ou sais farmaceuticamente aceitã¡veis do mesmo, e mã©todos para usar estes compostos e composiã§ãµes para tratar condiã§ãµes medidas por uma ou mais isoformas de pi3k, tais como pi3kî´. 1/1 summary "compound, pharmaceutical composition, and method for the treatment of a human" This description provides phosphatidylinositol 3-kinase (pi3k) inhibitors of the formula (i), ( i), or a pharmaceutically acceptable salt thereof, wherein n, 3 m, râ, râ², and r are defined herein. These compounds are useful in treating conditions mediated by one or more pi3k isoforms, such as pi3k ''. The present disclosure additionally provides pharmaceutical compositions comprising a compound of formula (i), or pharmaceutically acceptable salts thereof, and methods for using these compounds and compositions to treat metered conditions. by one or more pi3k isoforms, such as pi3k ''.

Quinoline derivatives as alpha4beta7 integrin inhibitors

The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as described herein. The compounds of formula I or IA selectively inhibit the activities of PI3K isoforms and are therefore useful in therapeutic treatments, in particular in the treatment of cancer and inflammatory conditions.

COMPOUND, A PHARMACEUTICALLY ACCEPTABLE SALT, ISOMER OR MIXTURE OF THE SAME, PHARMACEUTICAL COMPOSITION, METHOD FOR TREATMENT OF A DISEASE OR CONDITION, INHIBITION OF THE ACTIVITY OF A FOSPHTIDILINOS OR CRISPID EIBASE OR EXIFIED CRISIS OR EFFECTS CANCER CELLS, KIT, AND, USE OF A COMPOUND, A PHARMACEUTICALLY ACCEPTABLE SALT, ISOMER OR A MIXTURE OF THE SAME

“composto, um sal farmaceuticamente aceitável, isômero ou uma mistura dos mesmos, composição farmacêutica, método para tratamento de uma doença ou condição, inibição da atividade de um polipeptídeo fosfatidilinositol 3-quinase e inibição de reações imunes excessivas ou destrutivas ou crescimento ou uma proliferação de células de câncer, kit, e, uso de um composto, um sal farmaceuticamente aceitável, isômero ou uma mistura dos mesmos” o presente pedido fornece os compostos da fórmula i fórmula i ou sais farmaceuticamente aceitáveis, isômeros, tautômero, ou uma mistura dos mesmos, em que s, t, n, r1 , r2 , r3 , r4 , r5 , e r6 são da maneira aqui descrita. "Compound, a pharmaceutically acceptable salt, isomer or a mixture thereof, pharmaceutical composition, method for treating a disease or condition, inhibiting the activity of a phosphatidylinositol 3-kinase polypeptide and inhibiting excessive or destructive immune reactions or growth or proliferation" cancer cells, kit, and, use of a compound, a pharmaceutically acceptable salt, isomer or a mixture thereof ”The present application provides the compounds of formula I or pharmaceutically acceptable salts, isomers, tautomer, or a mixture of the same, wherein s, t, n, r1, r2, r3, r4, r5, and r6 are as described herein.

Derivados de quinolina como inhibidores de la integrina alfa4beta7

La presente descripción proporciona un compuesto de Fórmula (I): (I); una sal farmacéuticamente aceptable del mismo como se describe en el presente documento. La presente descripción también proporciona composiciones farmacéuticas que comprenden un compuesto de Fórmula (I), procesos para preparar compuestos de Fórmula (I) y métodos terapéuticos para tratar enfermedades inflamatorias.

Inhibidores macrociclicos de las peptidilarginina deiminasas

Referido a un compuesto de Formula I, o una sal, estereoisomero, mezcla de estereoisomeros, o tautomero farmaceuticamente aceptable del mismo, en donde: X1 y X2 son C o N; X3 es N-R3 o C-R3; siempre que dos de X1, X2, y X3 son C; X4 es N o C-R2; X5 es N o CR6; X7 es N o CR7; R1 es H, halo, -CN, -OR12, entre otros; L1, L2, L3, L4, L5, y L6 son cada uno independientemente: alquileno C1-10, opcionalmente sustituido con 1 a 3 Z8; alquenileno C2-10, opcionalmente sustituido con 1 a 3 Z8; entre otros; m1, m2, m3, m4, m5, y m6 son cada uno independientemente 0 o 1; R10 es H, -alquilo C1-8 opcionalmente sustituido con 1 a 3 Z10, o cicloalquilo C3-6 opcionalmente sustituido con 1 a 3 Z10; R11 es H, -alquilo C1-8 opcionalmente sustituido con 1 a 4 Z11, -cicloalquilo C3-8 opcionalmente sustituido con 1 a 4 Z11, entre otros; cada Z10 y Z11 se selecciona independientemente de oxo, halo, -CN, alquilo C1-8 opcionalmente sustituido, entre otros. Estos compuestos son inhibidores macrociclicos de las peptidilarginina deiminasas (PAD). Tambien se refiere a procesos e intermediarios para la preparacion de tales compuestos, composicion farmaceutica que comprende dicho compuesto, un metodo para inhibir PAD tipo 4 y su uso en el tratamiento de artritis reumatoide o una enfermedad o afeccion mediada por PAD4.

Inhibidores macrocíclicos de las peptidilarginina deiminasas

La presente divulgación se refiere a compuestos novedosos para su uso en el tratamiento terapéutico de una enfermedad asociada con peptidilarginina deiminasas (PAD), tales como peptidilarginina deiminasa tipo 4 (PAD4). La presente divulgación también se refiere a procesos e intermediarios para la preparación de tales compuestos, métodos para usar tales compuestos y composiciones farmacéuticas que comprenden los compuestos descritos en este documento.

Inhibitors of peptidylarginine deiminases

The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

Inhibidores de macrociclo de peptidilarginina deiminasas.

La presente descripción se relaciona con compuestos novedosos para usarse en el tratamiento terapéutico de una enfermedad asociada con las peptidilarginina deiminasas (PAD), tal como peptidilarginina deiminasa tipo 4 (PAD4). La presente descripción también se relaciona con procesos e intermedios para la preparación de tales compuestos, métodos de uso de tales compuestos y composiciones farmacéuticas que comprenden los compuestos descritos en la presente descripción.

Compounds for inhibition of .alpha.4.beta.7 integrin

The present disclosure provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Derivados de piridazin-3(2h)-ona

En la presente descripción se proporciona un compuesto de la fórmula (1) en donde los diversos sustituyentes se describen en la presente descripción. Reivindicación 42: Un método para tratar el cáncer, que comprende administrar a un paciente que lo necesita un compuesto, de la reivindicación 1 - 39, o una sal estereoisómero, mezcla de estereoisómeros, o análogo deuterado farmacéuticamente aceptable de este, o una composición de la reivindicación 40.

Pyridizin-3(2h)-one derivatives

Provided herein is a compound of Formula (I) wherein the various substituents are described herein.

Parp7 inhibitors

Provided herein is a compound of Formula I: or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof, a pharmaceutical composition comprising a compound of the present invention, together with a pharmaceutically acceptable excipient thereof, and a method of treating cancer with the same.

Inhibidores de parp7

Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors

The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as described herein. The compounds of formula I or IA selectively inhibit the activities of PI3K isoforms and are therefore useful in therapeutic treatments, in particular in the treatment of cancer and inflammatory conditions.

Derivados de quinolina como inhibidores de la integrina alfa4beta7

La presente descripción proporciona un compuesto de Fórmula (I): (I); una sal farmacéuticamente aceptable del mismo como se describe en el presente documento. La presente descripción también proporciona composiciones farmacéuticas que comprenden un compuesto de Fórmula (I), procesos para preparar compuestos de Fórmula (I) y métodos terapéuticos para tratar enfermedades inflamatorias.

Quinoline derivatives as alpha4beta7 integrin inhibitors

The present disclosure provides a compound of Formula (I): R4 R 5 R3 R6 R 2 R 13 0 R7 R8 'N OR 14 R1-L 0 - R12 N R9 R" R10 or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease. 1004599188

Inhibitors of peptidylarginine deiminases

The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

Pyridizin-3(2h)-one derivatives

Provided herein is a compound of Formula (I) wherein the various substituents are described herein.

Quinoline derivatives as alpha4beta7 integrin inhibitors

The present disclosure provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Inhibitors of peptidylarginine deiminases

The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

Parp7 inhibitors

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof, a pharmaceutical composition comprising a compound of the present invention, together with a pharmaceutically acceptable excipient thereof, and a method of treating cancer with the same.

Pyridizin-3(2h)-one derivatives

Provided herein is a compound of Formula (I) wherein the various substituents are described herein.

Quinoline derivatives

The present disclosure provides a compound of Formula (I):or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

Parp7 inhibitors

N-benzoyl-phenylalanine derivatives as alpha4beta7 integrin inhibitors for treating inflammatory diseases

Inhibidores de parp7

En la presente descripción se proporciona un compuesto de la Fórmula I: o una sal, estereoisómero, mezcla de estereoisómeros, o análogo deuterado de este farmacéuticamente aceptable de este, una composición farmacéutica que comprende un compuesto de la presente invención, junto con un excipiente farmacéuticamente aceptable de este, y un método para tratar el cáncer con el mismo. Por la presente certifico que el documento adjunto es traducción fiel al idioma español de las partes pertinentes del documento adjunto redactado en idioma inglés al cual me remito en la Ciudad de Buenos Aires a los seis días del mes de febrero de 2023.

Derivados de quinolina como inhibidores de integrina alfa4beta7.

La presente invención se refiere a un compuesto de fórmula (I): (ver Fórmula) (I); o una sal farmacéuticamente aceptable del mismo como se describe en el presente documento. La presente divulgación también proporciona composiciones farmacéuticas que comprenden un compuesto de Fórmula (I), procesos para preparar compuestos de Fórmula (I) y métodos terapéuticos para tratar enfermedades inflamatorias.

Inhibidores de parp7.

(ver Fórmula) En la presente descripción se proporcionan un compuesto de la Fórmula (I) o una sal, estereoisómero, mezcla de estereoisómeros, o análogo deuterado de este, una composición farmacéutica que comprende un compuesto de la presente invención, junto con un excipiente farmacéuticamente aceptable de este, y un método para tratar el cáncer con el mismo.

Compounds for inhibition of alpha4beta7 integrin

N-benzoyl-phenylalanine derivatives as alpha4beta7 integrin inhibitors for treating inflammatory diseases