HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 4. The compound of any one of - , wherein ring A is aromatic.13. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis CRand Xis CR.14. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis N and Xis CR.15. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis N , Xis CRand Xis CR.16. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis CRand Xis N.17. The compound of any one of - and - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein R , Rand R , when applicable , are each independently selected from H , Calkyl and halo.18. The compound of or , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein R , Rand R , when applicable , are each independently selected from H , Calkyl and halo.19. The compound of any one of - and - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Ris —CH—R.20. The compound of claim 19 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 19 , wherein Ris —NRR.21. The compound of any of claim 19 , and claim 19 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 19 , wherein Ris —CH—R.22. The compound of claim 21 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 21 , wherein Ris —NRR.23. The compound of any of - claim 21 , and - or a pharmaceutically acceptable salt or a stereoisomer thereof claim 21 , wherein Ris 2-hydroxyethylaminomethyl claim 21 , 2-carboxypiperidin-1-ylmethyl claim 21 , (S)-2- ...

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein U is CR.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is N.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is CR.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is N.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is CR.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y and Z are each CH.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl claim 1 , 5-10 membered heteroaryl claim 1 , or 4-10 membered heterocycloalkyl claim 1 , wherein the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl of ring A each has at least one ring-forming carbon atom and 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 ring-forming heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , wherein N or S is optionally oxidized; and wherein a ring-forming carbon atom of the 4-10 membered heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is 5-10 membered heteroaryl.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is pyridyl claim 1 , 1H-indazolyl claim 1 , 1H-pyrrolo[2 claim 1 ,3-b]pyridinyl claim 1 , or 1H-benzo[d]imidazolyl.16. The compound of claim 1 , or a pharmaceutically ...

Bicyclic heterocycles as FGFR inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES AS A2A / A2B INHIBITORS

This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 239-. (canceled)40. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Cy is phenyl claim 1 , 2 claim 1 ,3-dihydro-1 claim 1 ,4-benzodioxin-6-yl claim 1 , 2-fluorophenyl claim 1 , 2-fluoro-3-methoxyphenyl claim 1 , or 1-methyl-1H-indazol-4-yl.41. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , Rand Rare each independently selected from H claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl- claim 1 , Caryl claim 1 , Caryl-Calkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , (5-10 membered heteroaryl)-Calkyl- claim 1 , (4-10 membered heterocycloalkyl)-Calkyl- claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , halo claim 1 , CN claim 1 , OH claim 1 , Calkoxy claim 1 , Chaloalkyl claim 1 , Chaloalkoxy claim 1 , NH claim 1 , —NH—Calkyl claim 1 , —N(Calkyl) claim 1 , NHOR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , NRC(O)NRR claim 1 , C(═NR) R claim 1 , C(═NR) NRR claim 1 , NRC(═NR) NRR claim 1 , NRS(O)R claim 1 , NRS(O)R claim 1 , NRS(O)NRR claim 1 , S(O)R claim 1 , S(O)NRR claim 1 , S(O)R claim 1 , and S(O)NRR claim 1 , wherein each Ris independently selected from H claim 1 , Calkyl claim 1 , Calkoxy claim 1 , Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl- claim 1 , Caryl claim 1 , Caryl-Calkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , (5-10 membered heteroaryl)-Calkyl- claim 1 , and (4-10 membered heterocycloalkyl)-Calkyl- claim 1 , wherein the Calkyl claim 1 , Calkoxy claim 1 , Ccycloalkyl claim 1 , Ccycloalkyl-Calkyl- claim 1 , Caryl ...

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

TRICYCLIC COMPOUNDS AS INHIBITORS OF KRAS

Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 151.-. (canceled)54. The method of claim 52 , wherein q is 0.55. The method of claim 52 , wherein q is 1.56. The method of claim 52 , wherein s is 1.57. The method of claim 52 , wherein n is 0.58. The method of claim 52 , wherein both Rand Rare H.59. The method of claim 52 , wherein both Rand Rare H.60. The method of claim 52 , wherein Ris CN claim 52 , OR claim 52 , or Cy.61. The method of claim 52 , wherein Ris CN.62. The method of claim 52 , wherein Ris OR.63. The method of claim 52 , wherein Ris ORand Ris selected from Calkyl claim 52 , Caryl claim 52 , Ccycloalkyl claim 52 , 5-10 membered heteroaryl claim 52 , Caryl-Calkyl- claim 52 , and Ccycloalkyl-Calkyl- claim 52 , each of which is optionally substituted with halo or CN.64. The method of claim 52 , wherein Ris methoxy.65. The method of claim 52 , wherein Ris ethoxy.66. The method of claim 52 , wherein Ris phenoxy substituted by 1 or 2 substituents independently selected from halo and CN.67. The method of claim 52 , wherein Ris (Caryl-Calkyl)-O—.68. The method of claim 52 , wherein Ris (pyridinyl)-O— or (pyrimidinyl)-O— claim 52 , of which is substituted by 1 or 2 substituents independently selected from halo.69. The method of claim 52 , wherein Ris (Ccycloalkyl-Calkyl)-O—.70. The method of claim 52 , wherein Ris (Ccycloalkyl)-O—.71. The method of claim 52 , wherein Ris Cy.72. The method of claim 52 , wherein Ris phenyl substituted by 1 or 2 substituents independently selected from Cy claim 52 , halo claim 52 , CN claim 52 , Calkoxy claim 52 , —C(O)NRR claim 52 , —C(O)OR claim 52 , (4-10 membered heterocycloalkyl)-O— claim 52 , and Ccyanoalkyl.73. The method of claim 52 , wherein Ris phenyl substituted by 1 or 2 substituents independently selected from Cy claim 52 , halo claim 52 , and Ccyanoalkyl.74. The method of claim 52 , wherein Ris phenyl substituted by 1 or 2 ...

BICYCLIC HETEROCYCLES AS FGFR INHIBITORS

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. 34-. (canceled)5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , or (4-10 membered heterocycloalkyl)-Calkyl claim 1 , wherein said Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , and (4-10 membered heterocycloalkyl)-Calkyl are each optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5 substituents independently selected from R.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , or (5-10 membered heteroaryl)-Calkyl claim 1 , wherein said Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , and (5-10 membered heteroaryl)-Calkyl are each optionally substituted with 1 or 2 substituents independently selected from halo and Calkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl claim 1 , 2H-tetrazol-5-yl claim 1 , benzyl claim 1 , 1H-pyrazol-4-ylmethyl claim 1 , cyclopentyl claim 1 , or cyclopropylmethyl each ...

Heterocyclic compounds as LSD1 inhibitors

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': 1', '2', '1', '2, 'one of Yand Yis N and the other of Yand Yis C;'}{'sup': 1', '1, 'Xis N or CR;'}{'sup': 2', '2, 'Xis N or CR;'}{'sup': 3', '3, 'Xis N or CR;'}{'sup': 4', '4, 'Xis N or CR;'}{'sup': 5', '5, 'Xis N or CR;'}{'sup': 6', '6, 'Xis N or CR;'}{'sub': 6-10', '3-10, 'sup': '7', 'Cy is Caryl, Ccycloalkyl, 5- to 14-membered heteroaryl, or 4- to 10-membered heterocycloalkyl, each of which is optionally substituted with 1 to 4 independently selected Rsubstituents;'}{'sup': 1', '8a, 'Zis N or CR;'}{'sup': 2', '8b, 'Zis N or CR;'}{'sup': 3', '8c, 'Zis N or CR;'}{'sup': 1', '2', '8a', '8b', '8c', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '1', '2', '8a', '8b', '8c, 'sub': 3-4', '2-4', '2-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '1-4', '1-4', '1-4', '3-4', '2-4', '2-4', '1-4, 'R, R, R, Rand Rare each independently selected from H, C, alkyl, Ccycloalkyl, Calkenyl, Calkynyl, halo, CN, OH, Calkoxy, Chaloalkyl, Chaloalkoxy, NH, —NH—Calkyl, —N(Calkyl), NHOR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRS(O)R, NRS(O)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, and S(O)NRR, wherein each Ris independently selected from H and Calkyl optionally substituted with 1 or 2 groups independently selected from halo, OH, CN and Calkoxy; and wherein the Calkyl, Ccycloalkyl, Calkenyl and Calkynyl of R, R, R, Rand Rare each optionally ...

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': 1', '6', '2', '7', '7, '(i) Gis NRand Gis CRR; or'}{'sup': 1', '6', '6', '2', '7, '(ii) Gis CRRand Gis NR;'}{'sup': 1', '1, 'Xis N or CR;'}{'sup': 2', '2, 'Xis N or CR;'}{'sup': 3', '3, 'Xis N or CR;'}{'sup': 4', '4, 'Z is O, S, N, NRor CR;'}{'sup': 1', '2', '1', '2, 'Yand Yare each independently N or C, provided Yand Yare not simultaneously N;'}{'sub': 6-10', '3-10, 'sup': '8', 'Cy is Caryl, Ccycloalkyl, 5- to 14-membered heteroaryl, or 4- to 10-membered heterocycloalkyl, each of which is optionally substituted with 1 to 5 independently selected Rsubstituents;'}{'sup': 1', '2', '3', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '1', '2', '3, 'sub': 1-4', '3-6', '2-4', '2-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '1-4', '1-4', '1-4', '3-6', '2-4', '2-4', '1-4', '1-4, 'R, Rand Rare each independently selected from H, Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, halo, CN, OH, Calkoxy, Chaloalkyl, Chaloalkoxy, NH, —NH—Calkyl, —N(Calkyl), NHOR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRS(O)R, NRS(O)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, and S(O)NRR, wherein each Ris independently selected from H and Calkyl optionally substituted with 1 or 2 groups independently selected from halo, OH, CN and Calkoxy; and wherein the Calkyl, Ccycloalkyl, Calkenyl, Calkynyl and Calkoxy of R, Rand Rare each optionally substituted with 1 or 2 ...

AZA spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

BICYCLIC HETEROCYCLES AS FGFR INHIBITORS

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is NRor CRR.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is NR.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , or (4-10 membered heterocycloalkyl)-Calkyl claim 1 , wherein said Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , and (4-10 membered heterocycloalkyl)-Calkyl are each optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5 substituents independently selected from R.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , or (5-10 membered heteroaryl)-Calkyl claim 1 , wherein said Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , and (5-10 membered heteroaryl)-Calkyl are each optionally substituted with 1 or 2 substituents independently selected from halo and Calkyl.9. The compound of claim 1 , or a pharmaceutically ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 29.-. (canceled)10. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.11. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.12. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 2.13. (canceled)14. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently selected from F and methoxy.1519.-. (canceled)20. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CH—.2124.-. (canceled)25. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopentyl.26. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclobutyl.27. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopropyl.2847.-. (canceled)48. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris cyanomethyl.49. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methoxymethyl.5052.-. (canceled)53. The method of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , having a trans configuration with respect to the di-substituted cyclopropyl group depicted in Formula I.5467.-. (canceled)68. The method of claim 1 , wherein the compound is 1-{[4-(methoxymethyl)-4-({[(1R claim 1 ,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclopentanecarboxylic acid claim 1 , or a pharmaceutically acceptable salt thereof.69. The method of claim 1 , wherein the compound is 1-{[4-(methoxymethyl)-4-({[(1R claim 1 ,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid claim 1 , or a pharmaceutically ...

HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein U is CR.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is N.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is CR.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is N.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is CR.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y and Z are each CH.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl claim 1 , 5-10 membered heteroaryl claim 1 , or 4-10 membered heterocycloalkyl claim 1 , wherein the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl of ring A each has at least one ring-forming carbon atom and 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 ring-forming heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , wherein N or S is optionally oxidized; and wherein a ring-forming carbon atom of the 4-10 membered heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is 5-10 membered heteroaryl.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is pyridyl claim 1 , 1H-indazolyl claim 1 , 1H-pyrrolo[2 claim 1 ,3-b]pyridinyl claim 1 , or 1H-benzo[d]imidazolyl.16. The compound of claim 1 , or a pharmaceutically ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': 1', '6', '2', '7', '7, '(i) Gis NRand Gis CRR; or'}{'sup': 1', '6', '6', '2', '7, '(ii) Gis CRRand Gis NR;'}{'sup': 1', '1, 'Xis N or CR;'}{'sup': 2', '2, 'Xis N or CR;'}{'sup': 3', '3, 'Xis N or CR;'}{'sup': 4', '4, 'Z is O, S, N, NRor CR;'}{'sup': 1', '2', '1', '2, 'Yand Yare each independently N or C, provided Yand Yare not simultaneously N;'}{'sub': 6-10', '3-10, 'sup': '8', 'Cy is Caryl, Ccycloalkyl, 5- to 14-membered heteroaryl, or 4- to 10-membered heterocycloalkyl, each of which is optionally substituted with 1 to 5 independently selected Rsubstituents;'}{'sup': 1', '2', '3', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '1', '2', '3, 'sub': 1-4', '3-6', '2-4', '2-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '1-4', '1-4', '1-4', '3-6', '2-4', '2-4', '1-4', '1-4, 'R, Rand Rare each independently selected from H, Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, halo, CN, OH, Calkoxy, Chaloalkyl, Chaloalkoxy, NH, —NH—Calkyl, —N(Calkyl), NHOR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRS(O)R, NRS(O)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, and S(O)NRR, wherein each Ris independently selected from H and Calkyl optionally substituted with 1 or 2 groups independently selected from halo, OH, CN and Calkoxy; and wherein the Calkyl, Ccycloalkyl, Calkenyl, Calkynyl and Calkoxy of R, Rand Rare each optionally substituted with 1 or 2 ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 167.-. (canceled)68. A method of treating a disease , wherein said disease is selected from hematological cancer , sarcoma , liver cancer , lung cancer , nervous system cancer , breast cancer , ovarian cancer , head and neck cancer , myelofibrosis , gastrointestinal cancer , genitourinary tract cancer , skin cancer and thyroid cancer , comprising administering to a patient a therapeutically effective amount of a compound selected from:1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl)cyclopentanecarboxylic acid,1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid,1-{[4-({[(1R,2S)-2-(4-fluorophenyl)cyclopropyl]amino}methyl)-4-(methoxymethyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, or1-{[4-(ethoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl)cyclobutanecarboxylic acid,or a pharmaceutically acceptable salt thereof.69. The method of claim 68 , wherein the hematological cancer is selected from acute lymphoblastic leukemia (ALL) claim 68 , acute myelogenous leukemia (AML) claim 68 , acute promyelocytic leukemia (APL) claim 68 , chronic lymphocytic leukemia (CLL) claim 68 , chronic myelogenous leukemia (CML) claim 68 , diffuse large B-cell lymphoma (DLBCL) claim 68 , mantle cell lymphoma claim 68 , Non-Hodgkin lymphoma claim 68 , Hodgkin lymphoma claim 68 , primary myelofibrosis (PMF) claim 68 , polycythemia vera (PV) claim 68 , essential thrombocytosis (ET) claim 68 , myelodysplasia syndrome (MDS) claim 68 , or multiple myeloma.70. The method of claim 68 , wherein the hematological cancer is acute myelogenous leukemia (AML).71. The method of claim 68 , wherein the sarcoma is selected from chondrosarcoma claim 68 , Ewing's sarcoma claim 68 , osteosarcoma claim 68 , rhabdomyosarcoma claim 68 ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 4. The compound of any one of - , wherein ring A is aromatic.13. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis CRand Xis CR.14. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis N and Xis CR.15. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis N , Xis CRand Xis CR.16. The compound of any one of - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Xis CR , Xis CRand Xis N.17. The compound of any one of - and - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein R , Rand R , when applicable , are each independently selected from H , Calkyl and halo.18. The compound of or , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein R , Rand R , when applicable , are each independently selected from H , Calkyl and halo.19. The compound of any one of - and - , or a pharmaceutically acceptable salt or a stereoisomer thereof , wherein Ris —CH—R.20. The compound of claim 19 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 19 , wherein Ris —NRR.21. The compound of any of claim 19 , and claim 19 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 19 , wherein Ris —CH—R.22. The compound of claim 21 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 21 , wherein Ris —NRR.23. The compound of any of - claim 21 , and - or a pharmaceutically acceptable salt or a stereoisomer thereof claim 21 , wherein Ris 2-hydroxyethylaminomethyl claim 21 , 2-carboxypiperidin-1-ylmethyl claim 21 , (S)-2- ...

Bicyclic heterocycles as FGFR inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 3. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 ,{'sub': '3-14', 'when ring C is 4- to 14-membered heterocycloalkyl or Ccycloalkyl,'}{'sup': 4', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8, 'sub': 1-6', '1-6', '2-6', '2-6', '1-6', '1-6', '3-6', '1-6', '1-6', '2-6', '2-6', '3-6', '1-6', '1-6', '1-6', '3-6', '2', '2', '2', '2', '2, 'Ris H, halo, oxo, CN, Calkyl, Calkoxy, Calkenyl, Calkynyl, Chaloalkyl, Chaloalkoxy, 4 to 6-membered heterocycloalkyl, 5- to 6-membered heteroaryl, phenyl, or Ccycloalkyl, wherein the Calkyl, Calkoxy, Calkenyl, Calkynyl, 4- to 6-membered heterocycloalkyl, 5- to 6-membered heteroaryl, phenyl and Ccycloalkyl are each optionally substituted with 1, 2 or 3 substituents independently selected from halo, CN, Calkoxy, Chaloalkyl, Chaloalkoxy, 4 to 6-membered heterocycloalkyl, Ccycloalkyl, 5- to 6-membered heteroaryl, phenyl, NH, —NHR, —NRR, C(O)R, C(O)NRR, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, NRS(O)R, NRS(O)NRR, S(O)R, S(O)R, and S(O)NRR,'}{'sup': '8', 'sub': '1-6', 'wherein each Ris independently H or Calkyl.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 ,{'sup': 4', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8', '8, 'sub': 1-6', '1-6', '2-6', '2-6', '1-6', '1-6', '3-6', '1-6', '1-6', '2-6', '2-6', '3-6', '1-6', '1-6', '1-6', '3-6', '2', '2', '2', '2', '2, 'wherein Ris halo, oxo, CN, Calkyl, Calkoxy, Calkenyl, Calkynyl, Chaloalkyl, Chaloalkoxy, 4 to 6-membered heterocycloalkyl, 5- to 6-membered ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

BICYCLIC HETEROCYCLES AS FGFR INHIBITORS

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. 193-. (canceled)94. A method of treating cancer in a patient , comprising administering to said patient a therapeutically effective amount of 2′-(2 ,6-difluoro-3 ,5-dimethoxyphenyl)-6′-[(2-morpholin-4-ylethyl)amino]-1′ ,2′-dihydro-3′H-spiro[cyclopropane-1 ,4′-[2 ,7]naphthyridin]-3′-one , or a pharmaceutically acceptable salt thereof , and an additional therapeutic agent.95. The method of claim 94 , wherein said cancer is selected from kidney cancer claim 94 , gastric cancer claim 94 , esophageal cancer claim 94 , multiple myeloma claim 94 , pancreatic cancer claim 94 , lung cancer claim 94 , prostate cancer claim 94 , breast cancer claim 94 , bladder cancer claim 94 , liver cancer claim 94 , polycythemia vera claim 94 , essential thrombocythemia claim 94 , primary myelofibrosis claim 94 , head and neck cancer claim 94 , ovarian cancer claim 94 , and glioblastoma.96. The method of claim 94 , wherein said cancer is kidney cancer.97. The method of claim 94 , wherein said cancer is gastric cancer.98. The method of claim 94 , wherein said cancer is esophageal cancer.99. The method of claim 94 , wherein said cancer is multiple myeloma cancer.100. The method of claim 94 , wherein said cancer is pancreatic cancer.101. The method of claim 94 , wherein said cancer is lung cancer.102. The method of claim 94 , wherein said cancer is prostate cancer.103. The method of claim 94 , wherein said cancer is breast cancer.104. The method of claim 94 , wherein said cancer is bladder cancer.105. The method of claim 94 , wherein said cancer is liver cancer.106. The method of claim 94 , wherein said cancer is polycythemia vera.107. The method of claim 94 , wherein said cancer is essential thrombocythemia.108. The method of claim 94 , wherein said cancer is primary ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 23-. (canceled)59-. (canceled)10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 2.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently selected from halo and —O—(Calkyl).14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently selected from F and methoxy.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H.16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each independently selected from H and Calkyl.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H and Ris methyl.18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —(CH)— claim 1 , —C(═O)— claim 1 , —C(═O)NR— claim 1 , or —S(O)— claim 1 , wherein r is 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4.19. (canceled)20. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CH—.2125-. (canceled)26. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclobutyl.2738-. (canceled)39. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , Calkyl claim 1 , or Caryl-Calkyl- claim 1 , or (5-10 membered heteroaryl)-Calkyl- claim 1 , wherein said Calkyl claim 1 , Caryl-Calkyl- and (5-10 membered heteroaryl)-Calkyl- are each optionally substituted by CN claim 1 , halo claim 1 , OR ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

AZA Spiro Alkane Derivatives as Inhibitors of Metalloproteases

The present invention provides a compound of Formula I or Formula II: 195-. (canceled)97. The method of claim 96 , wherein Y is CH.98. The method of claim 96 , wherein V′ is phenyl.99. The method of claim 96 , wherein Ris H.100. The method of claim 96 , wherein Ris C(O)(CR′R′)-T.101. The method of claim 96 , wherein Ris C(O)O(CR′R′)-T.102. The method of claim 96 , wherein the compound is selected from:N-hydroxy-6-{[4-(3-methylphenyl)piperazin-1-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;Methyl 7-[(hydroxyamino)carbonyl]-6-[(4-phenyl-3, 6-dihydropyridin-1(2H)-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate;Benzyl 7-[(hydroxyamino)carbonyl]-6-[(4-phenyl-3,6-dihydropyridin-1(2H)-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate;6-{[4-[3-(aminocarbonyl)phenyl]-3,6-dihydropyridin-1(2H)-yl]carbonyl}-N-hydroxy-5-azaspiro[2.5]octane-7-carboxamide;6-{[4-(3-fluoro-2-methylphenyl)piperazin-1-yl]carbonyl}-N-hydroxy-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-{[4-(2-methyl-3-nitrophenyl)piperazin-1-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-{[3-methyl-4-(3-methylphenyl)piperazin-1-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-{[4-(3-methoxyphenyl)piperidin-1-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;6-{[4-(4-cyano-2-methylphenyl)-3,6-dihydropyridin-1(2H)-yl]carbonyl}-N-hydroxy-5-azaspiro[2.5]octane-7-carboxamide;6-{[4-(4-cyanophenyl)piperazin-1-yl]carbonyl}-N-hydroxy-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-[(4-phenylpiperidin-1-yl)carbonyl]-5-azaspiro[2.5]octane-7-carboxamide;N-Hydroxy-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-7-carboxamide;Methyl 3-[1-({7-[(hydroxyamino)carbonyl]-5-azaspiro[2.5]oct-6-yl}carbonyl)piperidin-4-yl]benzoate;N-Hydroxy-6-{[4-(3-isopropylphenyl)-3, 6-dihydropyridin-1(2H)-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-{[4-(3-isopropylphenyl)piperidin-1-yl]carbonyl}-5-azaspiro[2.5]octane-7-carboxamide;N-hydroxy-6-{[4-(4-propylphenyl)-3,6-dihydropyridin-1(2H)-yl] ...

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. 179-. (canceled)81. The method of claim 80 , wherein the immune disorder is an autoimmune disease.8283-. (canceled)84. The method of claim 80 , wherein the compound is N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 80 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 80 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 80 , or a pharmaceutically acceptable salt thereof.85. The method of claim 80 , wherein the compound is N-{4-[(3R claim 80 ,4R claim 80 ,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 80 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-62 claim 80 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 80 , or a pharmaceutically acceptable salt thereof.86. The method of claim 80 , wherein the compound is N-{4-[(3R claim 80 ,4R claim 80 ,5S claim 80 ,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 80 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 80 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 80 , or a pharmaceutically acceptable salt thereof.87. The method of claim 80 , wherein the compound is N-{4-[(3R claim 80 ,4R claim 80 ,5S claim 80 ,7S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 80 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 80 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 80 , or a pharmaceutically acceptable salt thereof.89. The method of claim 80 , wherein the immune disorder is selected from multiple sclerosis claim 80 , rheumatoid arthritis claim 80 , allergy claim 80 , food allergy claim 80 , asthma claim 80 , lupus claim 80 , inflammatory bowel disease claim 80 , and ulcerative colitis.90. The method of claim 80 , wherein the immune disorder ...

Heterocyclic compounds as LSD1 inhibitors

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. 183.-. (canceled)84. A method of treating a proliferative disorder comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound , wherein the compound is N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide , a stereoisomer thereof , or a pharmaceutically acceptable salt thereof , and a therapeutically effective amount of an anti-cancer agent , wherein the anti-cancer agent is selected from abarelix , aldesleukin , alemtuzumab , alitretinoin , allopurinol , altretamine , anastrozole , arsenic trioxide , asparaginase , azacitidine , bevacizumab , bexarotene , bleomycin , bortezombi , bortezomib , busulfan intravenous , busulfan oral , calusterone , capecitabine , carboplatin , carmustine , cetuximab , chlorambucil , cisplatin , cladribine , clofarabine , cyclophosphamide , cytarabine , dacarbazine , dactinomycin , dalteparin sodium , dasatinib , daunorubicin , decitabine , denileukin , denileukin diftitox , dexrazoxane , docetaxel , doxorubicin , dromostanolone propionate , eculizumab , epirubicin , erlotinib , estramustine , etoposide phosphate , etoposide , exemestane , fentanyl citrate , filgrastim , floxuridine , fludarabine , fluorouracil , fulvestrant , gefitinib , gemcitabine , gemtuzumab ozogamicin , goserelin acetate , histrelin acetate , ibritumomab tiuxetan , idarubicin , ifosfamide , imatinib mesylate , interferon alfa 2a , irinotecan , lapatinib ditosylate , lenalidomide , letrozole , leucovorin , leuprolide acetate , levamisole , lomustine , meclorethamine , megestrol acetate , melphalan , mercaptopurine , ...

AZA spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': 1', '2', '1', '2, 'one of Yand Yis N and the other of Yand Yis C;'}{'sup': 1', 'i, 'Xis N or CR;'}{'sup': 2', '2, 'Xis N or CR;'}{'sup': 3', '3, 'Xis N or CR;'}{'sup': 4', '4, 'Xis N or CR;'}{'sup': 5', '5, 'Xis N or CR;'}{'sup': 6', '6, 'Xis N or CR;'}{'sub': 6-10', '3-10, 'sup': '7', 'Cy is Caryl, Ccycloalkyl, 5- to 14-membered heteroaryl, or 4- to 10-membered heterocycloalkyl, each of which is optionally substituted with 1 to 4 independently selected Rsubstituents;'}{'sup': 1', '8a, 'Zis N or CR;'}{'sup': 2', '8b, 'Zis N or CR;'}{'sup': 3', '8c, 'Zis N or CR;'}{'sup': 1', '2', '8a', '8b', '8c', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '1', '2', '8a', '8b', '8c, 'sub': 1-4', '3-4', '2-4', '2-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '1-4', '1-4', '1-4', '3-4', '2-4', '2-4', '1-4, 'R, R, R, Rand Rare each independently selected from H, Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, halo, CN, OH, Calkoxy, Chaloalkyl, Chaloalkoxy, NH, —NH—Calkyl, —N(Calkyl), NHOR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRS(O)R, NRS(O)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, and S(O)NRR, wherein each Ris independently selected from H and Calkyl optionally substituted with 1 or 2 groups independently selected from halo, OH, CN and Calkoxy; and wherein the Calkyl, Ccycloalkyl, Calkenyl and Calkynyl of R, R, R, Rand Rare each optionally ...

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is C.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is N.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is a fused 3-7 membered carbocycle optionally substituted by 1 claim 1 , 2 or 3 substituents independently selected from R.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein n is 0 or 1.7. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein ring B is a fused 3-7 membered cycloalkyl ring optionally substituted by 1 claim 4 , 2 or 3 substituents independently selected from R.10. The compound of claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein n is 0 or 1.11. The compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein m is 0 or 1.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is a fused 4-7 membered heterocycle optionally substituted by 1 claim 1 , 2 or 3 substituents independently selected from R.13. The compound of claim 12 , or a pharmaceutically acceptable salt thereof claim 12 , wherein ring B is a fused 4-7 membered heterocycloalkyl ring optionally substituted by 1 claim 12 , 2 or 3 substituents independently selected from R.14. The compound of claim 12 , or a pharmaceutically acceptable salt thereof claim 12 , wherein ring B is a fused 5-membered heteroaryl optionally substituted by 1 claim 12 , 2 or 3 substituents independently selected from R.15. The compound of claim 12 , or a ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is monocyclic 4-7 membered heterocycloalkyl having carbon and 1 claim 1 , 2 claim 1 , or 3 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 0.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 1.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris halo.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is monocyclic Ccycloalkyl.16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is monocyclic 4-7 membered heterocycloalkyl having carbon and 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms selected from N claim 1 , O claim 1 , and S.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopropyl claim 1 , cyclobutyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , or piperidinyl.18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopropyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , or piperidinyl.19. The compound of ...

Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES AS A2A / A2B INHIBITORS

This application relates to compounds of Formula (I): 1. (canceled)3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof; wherein:{'sup': J', 'a7', 'a7', 'a7', 'b7', 'c7', 'd7', 'c7', 'a7', 'a7', 'b7', 'c7', 'd7', 'c7', 'd7', 'c7', 'c7', 'd7', 'c7', 'b7', 'c7', 'a7', 'c7', 'c7', 'd7', 'e7', 'b7', 'e7', 'c7', 'd7', 'c7', 'e7', 'c7', 'd7', 'c7', 'e7', 'b7', 'c7', 'b7', 'c7', 'c7', 'd7', 'c7', 'b7', 'c7', 'e7', 'b7', 'c7', 'c7', 'd7', 'b7', 'c7', 'd7', 'b7', 'c7', 'd7', 'e7', 'b7', 'b7', 'f7', 'g7', 'h7', 'i7', 'h7', 'i7', 'j7', 'k7, 'sub': 1-6', '1-6', '2-6', '2-6', '6-14', '3-14', '6-14', '1-6', '3-14', '1-6', '1-6', '1-6', '2', '2', '2', '2', '2', '2', '5, 'each Ris independently selected from D, halo, oxo, Calkyl, Chaloalkyl, Calkenyl, Calkynyl, Caryl, Ccycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, Caryl-Calkyl-, Ccycloalkyl-Calkyl-, (5-14 membered heteroaryl)-Calkyl-, and (4-14 membered heterocycloalkyl)-Calkyl-, CN, NO, OR, SR, NHOR, C(O)R, C(O)NRR, C(O)NR(OR), C(O)OR, OC(O)R, OC(O)NRR, NRR, NRNRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRC(═NR)R, NRS(O)R, NRS(O)NRR, NRS(O)R, NRS(O)(═NR)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, S(O)NRR, OS(O)(═NR)R, OS(O)R, SF, P(O)RR, OP(O)(OR)(OR), P(O)(OR)(OR), and BRR;'}{'sup': a7', 'c7', 'd7, 'sub': 1-6', '1-6', '2-6', '2-6', '6-14', '3-14', '6-14', '1-6', '3-14', '1-6', '1-6', '1-6, 'each R, R, and Ris independently selected from H, Calkyl, Chaloalkyl, Calkenyl, Calkynyl, Caryl, Ccycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, Caryl-Calkyl-, Ccycloalkyl-Calkyl-, (5-14 membered heteroaryl)-Calkyl-, and (4-14 membered heterocycloalkyl)-Calkyl-;'}{'sup': c7', 'd7, 'or any Rand Rattached to the same N atom, together with the N atom to which they are attached, form a 5- or 6-membered heteroaryl or a 4-14-membered heterocycloalkyl group; and'}{'sup': 'b7', 'sub': 1-6', '2-6', '2-6', '6-14', '3-14', '6-14', '1-6', '3-14', '1-6', '1-6', '1-6, ' ...

AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. 183-. (canceled)84. A method of treating a solid tumor comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound , wherein the compound is selected from:N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;N-{4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide; andN-{4-[(3R,4R,5S,7S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;or a pharmaceutically acceptable salt thereof.85. The method of claim 84 , wherein the compound is N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 84 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 84 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 84 , or a pharmaceutically acceptable salt thereof.86. The method of claim 84 , wherein the compound is N-{4-[(3R claim 84 ,4R claim 84 ,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 84 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 84 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 84 , or a pharmaceutically acceptable salt thereof.87. The method of claim 84 , wherein the compound is N-{4-[(3R claim 84 ,4R claim 84 ,5S claim 84 ,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 84 ,7-dihydro-5H- ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 119-. (canceled)2134-. (canceled)35. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein Ris H.3639-. (canceled)40. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein Ris (3-hydroxypyrrolidin-1-yl)methyl claim 20 , (R)-(3-hydroxypyrrolidin-1-yl)methyl claim 20 , or (S)-(3-hydroxypyrrolidin-1-yl)methyl.4143-. (canceled)44. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein Ris halo or Calkyl.45. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein Ris halo claim 20 , methyl or CN.46. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein Ris methyl or Cl.4756-. (canceled)57. The compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , wherein —NRRis carboxypyrrolidin-1-yl claim 20 , (R)-3-carboxypyrrolidin-1-yl claim 20 , or (S)-3-carboxypyrrolidin-1-yl.5867-. (canceled)68. A pharmaceutical composition comprising a compound of claim 20 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 20 , and one or more pharmaceutically acceptable excipient or carrier.6971-. (canceled)72. The compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , wherein each Ris independently selected from Calkyl claim 20 , which is optionally substituted with 1 or 2 Rsubstituents.73. The compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , wherein the subscript r is an integer of 1.74. The compound of claim 20 , or a pharmaceutically ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. 183-. (canceled)84. A method of treating a myeloproliferative disorder comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound , wherein the compound is selected from:N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;N-{4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide; andN-{4-[(3R,4R,5S,7S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;or a pharmaceutically acceptable salt thereof;wherein the myeloproliferative disorder is polycythemia vera (PV), essential thrombocythemia (ET), primary myelofibrosis (PMF), myelofibrosis with myeloid metaplasia (MMM), post-polycythemia vera/essential thrombocythemia myelofibrosis (Post-PV/ET MF), post-essential thrombocythemia myelofibrosis (Post-ET MF) or post-polycythemia vera myelofibrosis (Post-PV MF).85. The method of claim 84 , wherein the compound is N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6 claim 84 ,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2 claim 84 ,6-difluorophenyl)-5-fluoropyridine-2-carboxamide claim 84 , or a pharmaceutically acceptable salt thereof.86. The method of claim 84 , wherein the compound is N-{4-[(3R claim 84 ,4R claim 84 ,5S)-3-amino-4-hydroxy-5- ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': 1', '6', '2', '7', '7, '(i) Gis NRand Gis CRR; or'}{'sup': 1', '6', '6', '2', '7, '(ii) Gis CRRand Gis NR;'}{'sup': 1', '1, 'Xis N or CR;'}{'sup': 2', '2, 'Xis N or CR;'}{'sup': 3', '3, 'Xis N or CR;'}{'sup': 4', '4, 'Z is O, S, N, NRor CR;'}{'sup': 1', '2', '1', '2, 'Yand Yare each independently N or C, provided Yand Yare not simultaneously N;'}{'sub': 6-10', '3-10, 'sup': '8', 'Cy is Caryl, Ccycloalkyl, 5- to 14-membered heteroaryl, or 4- to 10-membered heterocycloalkyl, each of which is optionally substituted with 1 to 5 independently selected Rsubstituents;'}{'sup': 1', '2', '3', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '10', '1', '2', '3, 'sub': 1-4', '3-6', '2-4', '2-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '1-4', '1-4', '1-4', '3-6', '2-4', '2-4', '1-4', '1-4, 'R, Rand Rare each independently selected from H, Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, halo, CN, OH, Calkoxy, Chaloalkyl, Chaloalkoxy, NH, —NH—Calkyl, —N(Calkyl), NHOR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRC(O)R, NRC(O)OR, NRC(O)NRR, C(═NR)R, C(═NR)NRR, NRC(═NR)NRR, NRS(O)R, NRS(O)R, NRS(O)NRR, S(O)R, S(O)NRR, S(O)R, and S(O)NRR, wherein each Ris independently selected from H and Calkyl optionally substituted with 1 or 2 groups independently selected from halo, OH, CN and Calkoxy; and wherein the Calkyl, Ccycloalkyl, Calkenyl, Calkynyl and Calkoxy of R, Rand Rare each optionally substituted with 1 or 2 ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is monocyclic 4-7 membered heterocycloalkyl having carbon and 1 claim 1 , 2 claim 1 , or 3 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 0.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 1.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris halo.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris F.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is monocyclic Ccycloalkyl.16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is monocyclic 4-7 membered heterocycloalkyl having carbon and 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms selected from N claim 1 , O claim 1 , and S.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopropyl claim 1 , cyclobutyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , or piperidinyl.18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring C is cyclopropyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , or piperidinyl.19. The compound of ...

AZA Spiro Alkane Derivatives as Inhibitors of Metalloproteases

The present invention provides a compound of Formula I or Formula II: 194-. (canceled)95. A method for treating a disease associated with unwanted ADAM10 , ADAM15 , or ADAM17 activity in a mammalian subject , the method comprising administering to said mammal in need thereof a therapeutically effective amount of a compound which is methyl (6S ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate , or a pharmaceutically acceptable salt thereof.96. The method of claim 95 , wherein the disease is associated with unwanted ADAM10 activity.97. The method of claim 95 , wherein the disease is associated with unwanted ADAM15 activity.98. The method of claim 95 , wherein the disease is associated with unwanted ADAM17 activity.99. The method of claim 95 , wherein the disease is selected from breast cancer claim 95 , ovarian cancer claim 95 , prostate cancer claim 95 , non-small cell lung cancer claim 95 , colon cancer claim 95 , gastric cancer claim 95 , pancreatic cancer claim 95 , and glioma.100. The method of claim 95 , wherein the disease is glioma.101. The method of claim 95 , wherein the compound methyl (6S claim 95 ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.102. The method of claim 96 , wherein the compound methyl (6S claim 96 ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.103. The method of claim 97 , wherein the compound methyl (6S claim 97 ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.104. The method of claim 98 , wherein the compound methyl (6S claim 98 ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.105. The method of claim 99 , wherein the compound methyl (6S claim 99 ,7S)-7-[(hydroxyamino)carbonyl]-6-[(4- ...

Bicyclic heterocycles as FGFR inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein U is CR.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is N.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is CR.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is N.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is CR.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y and Z are each CH.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl claim 1 , 5-10 membered heteroaryl claim 1 , or 4-10 membered heterocycloalkyl claim 1 , wherein the 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl of ring A each has at least one ring-forming carbon atom and 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 ring-forming heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , wherein N or S is optionally oxidized; and wherein a ring-forming carbon atom of the 4-10 membered heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is Caryl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is 5-10 membered heteroaryl.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is pyridyl claim 1 , 1H-indazolyl claim 1 , 1H-pyrrolo[2 claim 1 ,3-b]pyridinyl claim 1 , or 1H-benzo[d]imidazolyl.16. The compound of claim 1 , or a pharmaceutically ...

BICYCLIC HETEROCYCLES AS FGFR INHIBITORS

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 6. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': i', 'q, 'any two Rsubstituents together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7-, 8-, 9- or 10-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 independently selected Rsubstituents;'}{'sup': k', 'q, 'or any two Rsubstituents together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7-, 8-, 9- or 10-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 independently selected Rsubstituents.'}7. The compound of any of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein (1) when L is C(O)NH— claim 1 , ring A is not 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-1H-imidazo[4 claim 1 ,5-c]pyridin-2-yl; (2) when L is a bond claim 1 , ring A is not [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ,5-a]pyridin-2-yl; (3) when L is —NH— claim 1 , ring A is not 1 claim 1 ,7-naphthyridin-8-yl or pyrido[3 claim 1 ,2-d]pyrimidin-4-yl; or (4) when L is C(O)NH— claim 1 , ring A is not 2-pyridyl.22. The compound of claim 16 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 16 , wherein Ris H.34. The compound of claim 8 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 8 , wherein L is —C(O)NH—.35. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein L is —NH—.40. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein Ris H claim 1 , Calkyl claim 1 , 2-hydroxyethyl claim 1 , 1-(2-hydroxyethyl)azetidin-3-yl claim 1 , pyrrolidin-2-yl ...

AZA spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 430.-. (canceled)31. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , and one or more pharmaceutically acceptable excipient or carrier.32. A method of inhibiting PD-1/PD-L1 interaction claim 1 , said method comprising administering to a patient a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof.33. A method of treating a disease or disorder associated with inhibition of PD-1/PD-L1 interaction claim 1 , said method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof.34. A method of enhancing claim 1 , stimulating and/or increasing the immune response in a patient claim 1 , said method comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof. The present application is concerned with pharmaceutically active compounds. The disclosure provides compounds as well as their compositions and methods of use. The compounds modulate PD-1/PD-L1 protein/protein interaction and are useful in the treatment of various diseases including infectious diseases and cancer.The immune system plays an important role in controlling and eradicating diseases such as cancer. However, cancer cells often develop strategies to evade or to suppress the immune system in order to favor their growth. One such mechanism is altering the expression of co-stimulatory and co-inhibitory molecules expressed on immune cells (Postow et al, J. Clinical Oncology 2015, 1-9). ...

PYRAZOLYL PYRIMIDINYLAMINE COMPOUNDS AS CDK2 INHIBITORS

The present application provides pyrazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same. 4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from H claim 2 , halo claim 2 , CN claim 2 , and Chaloalkyl; and Ris selected from Calkyl and Chaloalkyl; or Ris selected from halo claim 2 , CN claim 2 , and Chaloalkyl; and Ris selected from H claim 2 , Calkyl claim 2 , and Chaloalkyl.5. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from H claim 2 , F claim 2 , Cl claim 2 , CN claim 2 , and CF; and Ris selected from CHand CF; or Ris selected from F claim 2 , Cl claim 2 , CN claim 2 , and CF; and Ris selected from CHand CF.6. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from H and Chaloalkyl.7. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from H and CF.8. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from Chaloalkyl claim 2 , Calkenyl claim 2 , Calkynyl claim 2 , Ccycloalkyl claim 2 , 4-7 membered heterocycloalkyl claim 2 , 5-6 membered heteroaryl claim 2 , Ccycloalkyl-Calkyl claim 2 , phenyl-Calkyl claim 2 , 4-7 membered heterocycloalkyl-Calkyl claim 2 , 5-6 membered heteroaryl-Calkyl claim 2 , (R)-phenyl- claim 2 , and (R)—Calkyl-; wherein said Calkenyl claim 2 , Calkynyl claim 2 , Chaloalkyl claim 2 , Ccycloalkyl claim 2 , 4-7 membered heterocycloalkyl claim 2 , 5-6 membered heteroaryl claim 2 , Ccycloalkyl-Calkyl claim 2 , phenyl-Calkyl claim 2 , 4-7 membered heterocycloalkyl-Calkyl claim 2 , and 5-6 membered heteroaryl-Calkyl are each optionally substituted by 1 claim 2 , 2 claim 2 , 3 claim 2 , or 4 independently selected Rsubstituents.9. (canceled)10. The compound of claim 2 , or ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. 3. The compound of or , or a pharmaceutically acceptable salt thereof , wherein ring B is monocyclic 4-7 membered heterocycloalkyl having carbon and 1 , 2 , or 3 heteroatoms selected from N , O , and S.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 0.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein q is 1.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein s is 1.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both Rand Rare H.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CN claim 1 , ORB claim 1 , or Cy.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CN.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris ORB.16. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris ORand Ris selected from Calkyl claim 1 , Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , Caryl-Calkyl- claim 1 , and Ccycloalkyl-Calkyl- claim 1 , each of which is optionally substituted with halo or CN.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methoxy.18. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris ethoxy.19. The compound of claim 1 , or a ...

Bicyclic heterocycles as FGFR inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 4. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein:{'sup': i', 'q, 'any two Rsubstituents together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7-, 8-, 9- or 10-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 independently selected Rsubstituents;'}{'sup': k', 'q, 'or any two Rsubstituents together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7-, 8-, 9- or 10-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 independently selected Rsubstituents.'}5. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein (1) when L is —C(O)NH— claim 1 , ring A is not 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-1H-imidazo[4 claim 1 ,5-c]pyridin-2-yl; (2) when L is a bond claim 1 , ring A is not 2-benzoxazolyl; (3) when L is —NH— claim 1 , ring A is not 1 claim 1 ,7-naphthyridin-8-yl or pyrido[3 claim 1 ,2-d]pyrimidin-4-yl; or (4) when L is a bond claim 1 , ring A is not [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ,5-a]pyridin-2-yl.14. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein L is a bond claim 1 , —NH— claim 1 , —CH═CH— or —C(O)NH— claim 1 , wherein the carbonyl group in the —C(O)NH— linkage is attached to ring A.15. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein the subscript m is 0.16. The compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , wherein the subscript n is 1 and Ris halo or Calkyl.17. The compound of claim 1 , or a pharmaceutically ...

AZA Spiro Alkane Derivatives as Inhibitors of Metalloproteases

The present invention provides a compound of Formula I or Formula II: 2. The compound of wherein A is CWNHOH claim 1 , CWNHOR claim 1 , N(OH)CHO or N(OH)CWR.3. The compound of wherein A is CWNHOH or CWNHOR.4. The compound of wherein A is C(O)NHOH.5. The compound of wherein B is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , (CRR)O(CRR) claim 1 , (CRR)S(CRR) claim 1 , O(C═W)NR claim 1 , O claim 1 , NR claim 1 , S(O) claim 1 , S claim 1 , C(O)NR(CRR)or C(O)(CRR).6. The compound of wherein B is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , O(C═W)NR claim 1 , O claim 1 , NR claim 1 , S(O) claim 1 , S claim 1 , C(O)NR(CRR)or C(O)(CRR).7. The compound of wherein B is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , O(C═W)NR claim 1 , C(O)NR(CRR)or C(O)(CRR).8. The compound of wherein B is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NRor NR(CRR).9. The compound of wherein B is (CH).10. The compound of wherein B is CH.11. The compound of wherein G is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , (CRR)O(CRR) claim 1 , (CRR)S(CRR) claim 1 , O(C═W)NR claim 1 , O claim 1 , NR claim 1 , S(O) claim 1 , S claim 1 , C(O)NR(CRR)or C(O)(CRR).12. The compound of wherein G is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , O(C═W)NR claim 1 , O claim 1 , NR claim 1 , S(O) claim 1 , S claim 1 , C(O)NR(CRR)or C(O)(CRR).13. The compound of wherein G is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR) claim 1 , O(C═W)NR claim 1 , C(O)NR(CRR)or C(O)(CRR).14. The compound of wherein G is (CH) claim 1 , (CH)C═W claim 1 , (CRR)NR claim 1 , NR(CRR).15. The compound of wherein G is (CH).16. The compound of wherein G is CH.17. The compound of wherein B and G are both CH.18. The compound of wherein D is oxygen.19. The compound of wherein X is (CH) claim 1 , Calkylene substituted with 0 to 3 R claim 1 , NR claim 1 , S(O) claim 1 , C═O claim 1 , NRC(O) claim 1 , NRC(O)O claim 1 , NRC(O)NR ...

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. 335.-. (canceled)36. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof claim 1 , and at least one pharmaceutically acceptable carrier or excipient.37. A method of inhibiting PD-1/PD-L1 interaction claim 1 , said method comprising administering to a patient a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof.38. A method of treating a disease or disorder associated with inhibition of PD-1/PD-L1 interaction claim 1 , said method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof.39. A method of enhancing claim 1 , stimulating and/or increasing the immune response in a patient claim 1 , said method comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or a stereoisomer thereof. The present application is concerned with pharmaceutically active compounds. The disclosure provides compounds as well as their compositions and methods of use. The compounds modulate PD-1/PD-L1 protein/protein interaction and are useful in the treatment of various diseases including infectious diseases and cancer.The immune system plays an important role in controlling and eradicating diseases such as cancer. However, cancer cells often develop strategies to evade or to suppress the immune system in order to favor their growth. One such mechanism is altering the expression of co-stimulatory and co-inhibitory molecules expressed on immune cells (Postow et al, J. Clinical Oncology 2015, 1-9). ...

BICYCLIC HETEROCYCLES AS FGFR INHIBITORS

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. 310-. (canceled)11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each Calkyl.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each methyl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim 1 , 5- claim 1 , 6- claim 1 , or 7-membered cycloalkyl group or a 4- claim 1 , 5- claim 1 , 6- claim 1 , or 7-membered heterocycloalkyl group claim 1 , each optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from Cy claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , halo claim 1 , CN claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)NRR claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , S(O)R claim 1 , S(O)NRR claim 1 , S(O)R claim 1 , NRS(O)R claim 1 , NRS(O)NRR claim 1 , and S(O)NRR claim 1 , wherein said Calkyl is optionally substituted by 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from Cy claim 1 , halo claim 1 , CN claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)NRR claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , S(O)R claim 1 , S(O)NRR claim 1 , S(O)R claim 1 , NRS(O)R claim 1 , NRS(O)NRR claim 1 , and S(O)NRR.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim ...

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

HETEROCYCLIC COMPOUNDS USED AS IMMUNOMODULATORS

Pyridine derivatives as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Bicyclic heterocycles as fgfr inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Cyclopropylamines as lsd1 inhibitors

The present invention is directed to compounds of Formula II: (see formula II) and pharmaceutically acceptable salts thereof, which are LSD1 inhibitors and therefore may be useful in the treatment of diseases such as cancer.

Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors

The present disclosure describes thiazole and pyridine carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is C or N; A, B and D are rings; the bond— represents a normalized bond within the aromatic ring containing both an N and X, which formally is represented by a C=C bond when X is C and a single bond when X is N; ring A is of the formula (A-l) or (A-2): wherein El and E2 are rings; their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

The present disclosure describes thiazole and pyridine carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is C or N; A, B and D are rings; the bond represents a normalized bond within the aromatic ring containing both an N and X, which formally is represented by a C=C bond when X is C and a single bond when X is N; ring A is of the formula (A-l) or (A-2): wherein El and E2 are rings; their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Cyclopropylamines as lsd1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Bicyclic heterocycles as fgfr inhibitors.

La presente invención se refiere a heterociclos bicíclicos y composiciones farmacéuticas de estos, que son inhibidores de una o más enzimas del FGFR y son útiles en el tratamiento de enfermedades relacionadas con el FGFR, como el cáncer.

Heterocyclic compounds as LSD1 inhibitors

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

COMPOUNDS OF THIAZOLACARBOXAMIDES AND PYRIDINECARBOXAMIDE, COMPOSITION COMPRISING THE SAME, METHOD OF INHIBITION OF THE ENZYME PIM1, PIM2, OR PIM3, AND USES OF SUCH COMPOUNDS

a presente invenção descreve derivados de tiazol e piridina carboxamida da fórmula (i) ou um sal farmaceuticamente aceitável do mesmo, em que: x é c ou n; a, b e d são anéis; a ligação? representa uma ligação normalizada dentro do anel aromático contendo ambos um n e x, o qual formalmente é representado por uma ligação c=c quando x for c e uma ligação única, quando x for n; anel a é da fórmula (a-1) ou (a-2): em que e1 e e2 são anéis; suas composições e métodos de uso. os compostos inibem a atividade das quinases pim e são úteis no tratamento de doenças relacionadas à atividade de quinases pim incluindo, por exemplo, câncer e outras doenças.

Heterocyclic compounds as immunomodulators

【課題】がんまたは感染症などの疾患または障害の治療、予防、または改善に有用である、免疫調節剤として使用する化合物、及びかかる化合物を含む薬学的組成物を提供する。【解決手段】式（Ｉ）の化合物を使用する。TIFF2022058400000106.tif3786【選択図】なし

CYCLOPROPYLAMINES AS LSD1 INHIBITORS, THEIR USE, PHARMACEUTICAL COMPOSITION INCLUDING THEM AND LSD1 INHIBITION METHOD

CICLOPROPILAMINAS COMO INIBIDORES DE LSD1, SEU USO, COMPOSIÇÃO FARMACÊUTICA QUE OS COMPREENDE E MÉTODO DE INIBIÇÃO DE LSD1. A presente invenção é direcionada a derivados de ciclopro-pilamina que são inibidores de LSD1 úteis no tratamento de doenças como o câncer. CYCLOPROPYLAMINES AS LSD1 INHIBITORS, THEIR USE, PHARMACEUTICAL COMPOSITION INCLUDING THEM AND LSD1 INHIBITION METHOD. The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Thiazolecarboxamides and pyridinecarboxamide compounds useful as PIM kinase inhibitors

La presente descripción describe derivados de carboxamida de tiazol y piridina, sus composiciones y métodos de uso. Los compuestos inhiben la actividad de las quinasas Pim y son útiles en el tratamiento de enfermedades relacionadas con la actividad de las quinasas Pim que incluyen, por ejemplo, cáncer y otras enfermedades. (Traducción automática con Google Translate, sin valor legal) The present description describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of Pim kinases and are useful in the treatment of diseases related to Pim kinase activity including, for example, cancer and other diseases. (Automatic translation with Google Translate, without legal value)

Pyridinecarboxamide compound useful as pim kinase inhibitor

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS

COMPOSTOS HETEROCÍCLICOS COMO INIBIDORES DE LSD1, SEU USO, COMPOSIÇÃO FARMACÊUTICA QUE OS COMPREENDE E MÉTODO PARA INIBIR A DEMETILASE LISINA-ESPECÍFICA 1 (LSD1) IN VITRO. A presente invenção refere-se aos compostos da Fórmula I que são inibidores da LSD1 úteis no tratamento de doenças, tais como o câncer. HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS, THEIR USE, PHARMACEUTICAL COMPOSITION COMPRISING THEM AND METHOD TO INHIBIT THE SPECIFIC LYSINE DEMETHYLASE 1 (LSD1) IN VITRO. The present invention relates to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Heterocyclic compounds as lsd1 inhibitors

The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Cyclopropylamines as LSD1 inhibitors

Un compuesto de Fórmula II:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: el anillo A es arilo C6-10 o heteroarilo de 5-10 miembros que comprende carbono y 1, 2, 3 o 4 heteroátomos seleccionados de N, O y S; X es -CH2- o -CH2-CH2-; X es -CH2- o -CH2-CH2-; en donde cada R2 está sustituido en cualquier átomo de carbono que forma el anillo del anillo en la Fórmula II que contiene X e Y excepto el átomo de carbono que forma el anillo al que está unido RZ; el anillo C es heterocicloalquilo de 4-7 miembros monocíclico que comprende carbono y 1, 2, 3 o 4 heteroátomos seleccionados de N, O, y S; cada R1 se selecciona independientemente de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5 a 10 miembros, heterocicloalquilo de 4-10 miembros, arilo C6-10- alquilo C1-4-, cicloalquilo C3-10-alquilo C1-4-, (heteroarilo de 5-10 miembros)-alquilo C1-4-, (heterocicloalquilo de 4-10 miembros)-alquilo C1-4-, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, y S(O)2NRcRd, en donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5 a 10 miembros, heterocicloalquilo de 4-10 miembros, arilo C6-10-alquilo C1-4-, cicloalquilo C3-10-alquilo C1-4-, (heteroarilo de 5- 10 miembros)-alquilo C1-4-, y (heterocicloalquilo de 4-10 miembros)-alquilo C1-4-, están cada uno opcionalmente sustituidos con 1, 2, 3, o 4 sustituyentes seleccionados independientemente de halo, alquilo C1-4, haloalquilo C1-4, cianoalquilo C1-4, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, y S(O)2NRcRd; cada R2 se selecciona independientemente de halo, ...

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula (I) and (II) are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

CYCLOPROPYLAMINE AS INHIBITORS OF LSD1

La presente invención está dirigida a los derivados de la ciclopropilamina que son inhibidores de la LSD1 eficaces para el tratamiento de enfermedades como el cáncer.

Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors

The present application provides pyrazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula (I) or Formula (II): enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula (I) and (II) are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

Cyclopropylamines as LSD1 inhibitors

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

N-phenyl-pyridine-2-carboxamide derivatives and their use as pd-1/pd-l1 protein/protein interaction modulators

HETEROCYCLIC COMPOUNDS USED AS LSD1 INHIBITORS

Bicyclic heterocyclics as FGFR inhibitors

Un compuesto de Fórmula IIa: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en donde: R2 es halo; R5 es halo R6 es H, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, C(=NRe2)Rb2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 o S(O)2NRc2Rd2; en donde dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5-10 miembros, y heterocicloalquilo de 4-10 miembros están cada uno opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente de R6a; cada R6a se selecciona independientemente de Cy1, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1- 6, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, y S(O)2 NRc2Rd2, en donde dicho alquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están cada uno opcionalmente sustituidos con 1, 2, o 3 sustituyentes seleccionados independientemente de Cy1, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2 NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 y S(O)2NRc2Rd2; R7 y R8 se seleccionan cada uno independientemente de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -C(O)RA, S(O)RA, S(O)2RA, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros, arilo C6-10-alquilo C1-4, cicloalquilo C3-10-alquilo C1-4, (heteroarilo de 5-10 miembros)- ...

Benzooxazole derivatives as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors.

La presente solicitud se refiere a compuestos de la Fórmula (I):<br /> (I), o estereoisómeros o sales farmacéuticamente aceptables de estos, que modulan la actividad de los receptores de adenosina, tales como los subtipos A2A y A2B, y son útiles para el tratamiento de enfermedades relacionadas con la actividad de los receptores de adenosina, que incluyen, por ejemplo, cáncer, enfermedades inflamatorias, enfermedades cardiovasculares y enfermedades neurodegenerativas. The present application refers to compounds of Formula (I): <br /> (I), or stereoisomers or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as the A2A and A2B subtypes, and they are useful for the treatment of diseases related to the activity of adenosine receptors, including, for example, cancer, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases.

Bicyclic heterocycles as fgfr inhibitors

The present invention relates to bicyclic heterocycles of formula I, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Tricyclic compounds as inhibitors of KRAS

Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer. (I)

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

Cyclopropylamines as lsd1 inhibitors

The present invention is directed to compounds of Formula II: (see formula II) and pharmaceutically acceptable salts thereof, which are LSD1 inhibitors and therefore may be useful in the treatment of diseases such as cancer.

Aza spiro alkane derivatives as inhibitors of metalloproteases

The present invention provides a compound of Formula (I) or Formula (II): enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula (I) and (II) are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

Η παρούσα εφεύρεση κατευθύνεται σε παράγωγα κυκλοπροπυλαμίνης που είναι αναστολείς LSD1 χρήσιμοι στη θεραπεία ασθενειών όπως καρκίνου. The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Azaspiralane derivatives as inhibitors of metal processes

Heterocyclic compounds derivatives as pd-l1 internalization inducers

Disclosed are compounds of Formula (I'), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

HETEROCYCLIC COMPOUNDS USED AS IMMUNOMODULATORS

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Cyclopropylamines as LSD1 inhibitors

Un compuesto de Fórmula I: **Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: el anillo A es arilo C6-10 o heteroarilo de 5-10 miembros que comprende carbono y 1, 2, 3 o 4 heteroátomos seleccionados entre N, O y S; el anillo B es heterocicloalquilo de 4-10 miembros que comprende carbono y 1, 2 o 3 heteroátomos seleccionados de N, O y S; RZ es Cy1, CN, C(O)ORa, C(O)NRcRd, ORa, SRa, C(O)Rb, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)2Rb, S(O)Rb, S(O)NRcRd, S(O)2Rb o S(O)2NRcRd; cada R1 se selecciona independientemente entre halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros, arilo C6-10-alquilo C1-4-, cicloalquilo C3-10-alquilo C1-4-, (heteroarilo de 5-10 miembros)-alquilo C1-4-, (heterocicloalquilo de 4-10 miembros)-alquilo C1-4-, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, C(>=NRe1)Rb1, C(>=NRe1)NRc1Rd1, NRc1C(>=NRe1)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRC1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRC1Rd1, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo C6-10, cicloalquilo C3-10, heteroarilo de 5-10 miembros, heterocicloalquilo de 4-10 miembros, arilo C6-10-alquilo C1-4-, cicloalquilo C3-10-alquilo C1-4-, (heteroarilo de 5-10 miembros)-alquilo C1-4-, y (heterocicloalquilo de 4-10 miembros)-alquilo C1-4 están cada uno opcionalmente sustituidos con 1, 2, 3 o 4 sustituyentes seleccionados independientemente de halo, alquilo C1-4, haloalquilo C1-4, cianoalquilo C1-4, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(>=NRe1)NRc1Rd1, NRc1C(>=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRC1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRC1Rd1; cada RB se selecciona independientemente de Cy, halo, ...

Bicyclic heterocycles as fgfr inhibitors

The present invention relates to bicyclic heterocycles of Formula IIIa, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Cyclopropylamines as lsd1 inhibitors

La presente invención está dirigida a los derivados de la ciclopropilamina que son inhibidores de la LSD1 eficaces para el tratamiento de enfermedades como el cáncer.

Benzooxazole derivatives as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Bicyclic heterocycles as fgfr inhibitors

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Imidazopyrimidines and triazolopyrimidines as A2A/A2B inhibitors

【課題】アデノシン受容体、例えば、サブタイプＡ２Ａ及びＡ２Ｂの活性を調節し、例えば、がんの治療に有用な化合物を提供する。【解決手段】式（Ｉ）の化合物またはその薬学的に許容可能な塩もしくは立体異性体。TIFF2023123569000219.tif3453式中、Ｘは、ＣＲ３；Ｒ３は、Ｈ、Ｄ、ハロ、Ｃ１－６アルキル、Ｃ２－６アルケニル、Ｃ６－１４アリール、Ｃ３－１４シクロアルキル、５～１４員ヘテロアリール、４～１４員ヘテロシクロアルキル等；Ｒ１は、Ｈ、Ｃ１－６アルキル、Ｃ２－６アルケニル等；Ｒ２は、Ｈ、Ｄ、ハロ、Ｃ１－６アルキル、Ｃ２－６アルケニル等；Ｃｙ１は、Ｃ６－１４アリール、Ｃ３－１４シクロアルキル、または５～１４員ヘテロアリール；Ｃｙ２は、Ｃ６－１４アリール、Ｃ３－１４シクロアルキル、５～１４員ヘテロアリール、または４～１４員ヘテロシクロアルキルである。【選択図】なし

thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

abstract the present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. the compounds inhibit the activity of the pim kinases and are useful in the treatment of diseases related to the activity of pim kinases including, e.g., cancer and other diseases. tradução do resumo resumo "compostos de tiazolacarboxamidas e piridinacarboxamida úteis como inibidores de quinase pim" a presente divulgação descreve derivados de tiazola e piridina carboxamida da fórmula (i) ou um sal farmaceuticamente aceitável do mesmo, em que: x é c ou n; a, b e d são anéis; a ligação- representa uma ligação normalizada dentro do anel aromático contendo ambos um n e x, o qual formalmente é representado por uma ligação c=c quando x é c e uma ligação única quando x é n; anel a é da fórmula (a-1) ou (a-2): em que e1 e e2 são anéis; suas composições e métodos de uso. os compostos inibem a atividade das quinases pim e são úteis no tratamento de doenças relacionadas à atividade de quinases pim incluindo, por exemplo, câncer e outras doenças. abstract the present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. the compounds inhibit the activity of the pim kinases and are useful in the treatment of diseases related to the activity of pim kinases including, e.g., cancer and other diseases. "thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors" The present disclosure describes thiazole and pyridine carboxamide derivatives of formula (i) or a pharmaceutically acceptable salt thereof, wherein: x is c or n; a, b and d are rings; the bond represents a normalized bond within the aromatic ring containing both an n and x, which is formally represented by a bond c = c when x is c and a single bond when x is n; ring a is of formula (a-1) or (a-2): wherein e1 and e2 are rings; their compositions and methods of use. The compounds inhibit the activity of ...

Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos

compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos. a presente invenção refere-se a compostos da fórmula (i) ou sais ou estereoisômeros farmaceuticamente aceitáveis dos mesmos, que modulam a atividade de receptores de adenosina, tais como receptores dos subtipos a2a e a2b, e são úteis no tratamento de doenças relacionadas à atividade de receptores de adenosina incluindo, por exemplo, câncer, doenças inflamatórias, doenças cardiovasculares e doenças neurodegenerativas.