Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

HETEROCYCLIC COMPOUNDS AND THEIR USES

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. 5. A compound according to claim 1 , wherein Ris F claim 1 , Cl or Br; and n is 0.6. A compound according to claim 1 , wherein Ris phenyl substituted by 0 or 1 Rsubstituents claim 1 , and the phenyl is additionally substituted by 0 claim 1 , 1 claim 1 , 2 or 3 substituents independently selected from halo claim 1 , nitro claim 1 , cyano claim 1 , Calkyl claim 1 , OCalkyl claim 1 , OChalo alkyl claim 1 , NHCalkyl claim 1 , N(Calkyl)Calkyl and Chalo alkyl.7. A compound according to claim 1 , wherein Ris a direct-bonded or oxygen-linked saturated claim 1 , partially-saturated or unsaturated 5- claim 1 , 6- or 7-membered monocyclic ring containing 1 claim 1 , 2 claim 1 , 3 or 4 atoms selected from N claim 1 , O and S claim 1 , but containing no more than one O or S claim 1 , wherein the available carbon atoms of ...

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS

Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like. 6. The compound of wherein Y is NH claim 1 , N—CH claim 1 , NR claim 1 , or —C(═O).7. The compound of wherein Y is NH.8. The compound of wherein Y is —C(═O).9. The compound of wherein Y is —N—CH—CC—F.10. The compound of wherein Y is —CH—.11. The compound of wherein Y and Rform a 5- to 6-membered ring fused to the ring containing both said Y and R.12. The compound of wherein Xis N or C claim 1 , and each of X claim 1 , X claim 1 , and Xis C.13. The compound of wherein Xis N.14. The compound of wherein Xis C.15. The compound of wherein Z is NH claim 1 , N—Calk claim 1 , N-haloCalk claim 1 , S claim 1 , or —C═.16. The compound of wherein m is 0 or 1.17. The compound of wherein n is 0 or 1.18. The compound of wherein p is 0.19. The compound of wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —OR claim 1 , Calk claim 1 , Chaloalk claim 1 , —C(═O)—O—R claim 1 , —C(═O)NRR claim 1 , —ORand —C(═O)NRR.20. The compound of wherein Ris selected from the group consisting of a saturated 4- claim 1 , 5- claim 1 , 6- claim 1 , or 7-membered monocyclic ring claim 1 , wherein each said ring contains 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3 N atoms and 0 claim 1 , 1 claim 1 , or 2 O atoms claim 1 , and wherein each said ring is substituted by 0 claim 1 , 1 or 2 groups selected from F claim 1 , Cl claim 1 , Br claim 1 , Calk claim 1 , Chaloalk claim 1 , —OR claim 1 , —CN claim 1 , —C(═O)R claim 1 , —C(═O)OR claim 1 , and oxo.22. The compound of wherein Ris selected from the group consisting of a saturated claim 1 , partially-saturated or unsaturated 9- or 10-membered bicyclic ring claim 1 , ...

HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS

Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like. 11H-Benzo[d]imidazol-2-yl)(4-(3-(pyridine-4-yl)pyrazin-2-yloxy)piperidin-1-yl)methanone;1-(4-(3-(1-(1H-Benzo[d]imidazol-2-carbonyl)piperidin-4-yloxy)pyrazin-2-yl)-5,6-dihydropyridin-1(2H)-yl)ethanone;1-(4-(3-(1-(1H-benzo[d]imidazole-2-carbonyl)piperidin-4-yloxy)pyrazin-2-yl)piperidin-1-yl)ethanone;1-(4-(3-(1-(1H-benzo[d]imidazole-2-carbonyl)azetidin-3-yloxy)pyrazin-2-yl)-5,6-dihydropyridin-1(2H)-yl)ethanone;1-(4-(3-(1-(1H-benzo[d]imidazole-2-carbonyl)azetidin-3-yloxy)pyrazin-2-yl)piperidin-1-yl)ethanone;1-(4-(3-(1-(1H-pyrrole-2-carbonyl)azetidin-3-yloxy)pyrazin-2-yl)piperidin-1-yl)ethanone;1-(3-(2-(1-picolinoylazetidin-3-yloxy)pyridin-3-yl)piperidin-1-yl)ethanone;(R) and (S)-1-(3-(2-(1-(1H-benzo[d]imidazole-2-carbonyl)azetidin-3-yloxy)pyridin-3-yl)piperidin-1-yl)ethanone;(1H-benzo[d]imidazol-2-yl)(3-(pyrazin-2-yloxy)azetidin-1-yl)methanone;(1H-benzo[d]imidazol-2-yl)(3-((3-chloropyrazin-2-yl)oxy)azetidin-1-yl)methanone;(R) and (S)-1-(3-(2-(1-(1H-benzo[d]imidazole-2-carbonyl)azetidin-3-yloxy)pyridin-3-yl)piperidin-1-yl)-2-methylpropan-1-one;(1H-benzo[d]imidazol-2-yl)(3-((3-(3,6-dihydro-2H-pyran-4-yl)pyrazin-2-yl)oxy)azetidin-1-yl)methanone;benzyl 3-((3-chloropyrazin-2-yl)oxy)azetidine-1-carboxylate;tert-butyl 3-((3-((1r,4r)-4-hydroxycyclohexyl)pyridin-2-yl)oxy)azetidine-1-carboxylate;(1H-benzo[d]imidazol-2-yl)(3-(3-(tetrahydro-2H-pyran-4-yl)pyridin-2-yloxy)azetidin-1-yl)methanone;(1H-benzo[d]imidazol-2-yl)(3-(3-(tetrahydro-2H-pyran-4-yl)pyrazin-2-yloxy)azetidin-1-yl)methanone;benzyl 3-((3-(1-acetyl-4-hydroxypiperidin-4-yl)pyrazin-2-yl)oxy)azetidine-1-carboxylate;(1H-benzo[d]imidazol-2-yl)(3-((3- ...

HETEROCYCLIC COMPOUNDS AND THEIR USES

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. 5. A method according to claim 1 , wherein Ris F claim 1 , Cl or Br; and n is 0.6. A method according to claim 1 , wherein Ris phenyl substituted by 0 or 1Rsubstituents claim 1 , and the phenyl is additionally substituted by 0 claim 1 , 1 claim 1 , 2 or 3 substituents independently selected from halo claim 1 , nitro claim 1 , cyano claim 1 , Calkyl claim 1 , OCalkyl claim 1 , OChaloalkyl claim 1 , NHCalkyl claim 1 , N(Calkyl)Calkyl and Chaloalkyl.7. A method of wherein Ris a direct bonded saturated claim 1 , partially-saturated or unsaturated 5- claim 1 , 6- or 7-membered monocyclic ring containing 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 or 4 atoms selected from N claim 1 , O and S claim 1 , but containing no more than one O or S claim 1 , wherein the available carbon atoms of the ring are substituted by 0 ...

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES

The present invention relates to compounds of formula I or II, 3. A compound of or , or a pharmaceutically acceptable salt thereof , wherein Ris phenyl , substituted phenyl , pyridyl , substituted pyridyl , thienyl , substituted thienyl , pyrimidinyl or substituted pyrimidinyl.4. A compound of or , or a pharmaceutically acceptable salt thereof , wherein Ris benzofuranyl , substituted benzofuranyl , benzothiophenyl , substituted benzothiophenyl , benzothiazolyl , substituted benzothiazolyl , thieno[2 ,3-c]pyridinyl , substituted thieno[2 ,3-c]pyridinyl , benzoxazolyl , substituted benzoxazolyl , thieno[3 ,2-c]pyridinyl , substituted , thieno[3 ,2-c]pyridinyl , quinolinyl , substituted quinolinyl , naphthalenyl , substituted naphthalenyl , thieno[3 ,2-b]pyridinyl , substituted thieno[3 ,2-b]pyridinyl , thieno[2 ,3-b]pyridinyl , substituted thieno[2 ,3-b]pyridinyl , [1 ,3]thiazolo[5 ,4-b]pyridinyl , or substituted [1 ,3]thiazolo[5 ,4-b]pyridinyl.5. A compound of or , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen or halogen.6. A compound of or , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen.7. A compound of or , or a pharmaceutically acceptable salt thereof , that has the R configuration at the stereocenter designated with a *.8. A compound of or , or a pharmaceutically acceptable salt thereof , that is a mixture of the R and S configurations at the stereocenter designated with a *.9. A compound of or , or a pharmaceutically acceptable salt thereof , that is a racemic mixture of the R and S configurations at the stereocenter designated with a *.10. A compound of or , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '1', 'Ris phenyl, substituted phenyl, pyridyl, substituted pyridyl, thienyl, substituted thienyl, pyrimidinyl or substituted pyrimidinyl; and'}{'sup': '2', 'Ris benzofuranyl, substituted benzofuranyl, benzothiophenyl, substituted benzothiophenyl, benzothiazolyl, substituted benzothiazolyl, thieno[2, ...

HETEROCYCLIC COMPOUNDS AND THEIR USES

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. 218-. (canceled) This application is a divisional of U.S. Ser. No. 13/468,234, filed May 10, 2012, which claims the benefit of U.S. Ser. No. 12/079,406, filed Mar. 24, 2008 and U.S. Provisional Application No. 60/919,568, filed Mar. 23, 2007, which are hereby incorporated by reference in their entireties for all purposes.The present invention relates generally to phosphatidylinositol 3-kinase (PI3K) enzymes, and more particularly to selective inhibitors of PI3K activity and to methods of using such materials.Cell signaling via 3′-phosphorylated phosphoinositides has been implicated in a variety of cellular processes, e.g., malignant transformation, growth factor signaling, inflammation, and immunity (see Rameh et al., J. Biol Chem, 274:8347-8350 (1999) for a review). The enzyme responsible for generating ...

Benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein

The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors

Pyridine and pyrimidine compounds: (I); or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; (II); or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and (III); or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Benzodioxepine and benzodioxine compounds that interact with glucokinase regulatory protein for the treatment of diabetes

The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Heteroaryloxyheterocyclyl compounds as pde10 inhibitors

Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.

Heterocyclic modulators of PKB

The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors

Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X1 is C(R9) or N; X2 is C(R10) or N; Y is N(R11), O or S; which are useful to inhibit the biological activity of human PI3K.delta. and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110.delta. activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo- dysplastic syndrome (MDS) myeloproliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on, or associated with p110 activity, including but not restricted to leukemias, such as acute myeloid leukaemia (AML), myelo-dysplastic syndrome (MDS), myelo-proliferative diseases (MPD), chronic myeloid leukemia (CML), T-cell acute lymphoblastic leukaemia (T-ALL), B-cell acute lymphoblastic leukaemia (B-ALL), non Hodgkins lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.

Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors

Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Heterocyclic modulators of PKB

3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors

Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X1 is C(R9) or N; X2 is C(R10) or N; Y is N(R11), O or S; which are useful to inhibit the biological activity of human PI3K.delta. and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110.delta. activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo- dysplastic syndrome (MDS) myeloproliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on, or associated with p110 activity, including but not restricted to leukemias, such as acute myeloid leukaemia (AML), myelo-dysplastic syndrome (MDS), myelo-proliferative diseases (MPD), chronic myeloid leukemia (CML), T-cell acute lymphoblastic leukaemia (T-ALL), B-cell acute lymphoblastic leukaemia (B-ALL), non Hodgkins lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.

Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase ( pi3k) inhibitors

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors

Heterocyclic compounds and their uses

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors

Thiadiazole modulators of PKB

PIRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS 10

La presente invención se refiere a compuestos de piridina y pirimidina y composiciones que los contienen, y proceso para preparar tales compuestos.

Delta3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase ( PI3K) inhibitors

Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X is C(R) or N; X is C(R) or N; Y is N(R), O or S; which are useful to inhibit the biological activity of human PI3Kδ and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo- dysplastic syndrome (MDS) myeloproliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer.

La presente invención se refiere a heteroarilos bicíclicos substituidos y las composiciones que los contienen, para el tratamiento de la inflamación general, artritis, enfermedades reumáticas, osteoartritis, enfermedades inflamatorias del intestino, trastornos inflamatorios de los ojos, trastornos inflamatorios de la vejiga o trastornos de vejiga inestable, psoriasis, enfermedades de la piel con componentes inflamatorios, afecciones inflamatorias crónicas, incluyendo pero sin estar restringido a las enfermedades autoinmunitarias tales como lupus eritematoso sistémico (SLE), miastenia grave, artritis reumatoide, encefalomielitis diseminada aguda, púrpura trombocitopénica idiopática, esclerosis múltiple, síndrome de Sjoegren y anemia hemolítica autoinmune, afecciones alérgicas que incluyen todas las formas de hipersensibilidad. La presente invención también hace posibles métodos para el tratamiento de los cánceres que están meaiados, dependen de o están asociados con la actividad de pilO, incluyendo pero sin estar restringidos a las leucemias, tales como la leucemia mieloide aguda (AML), síndrome mielodisplásico (MDS), enfermedades mieloproliferativas (MPD), leucemia mieloide crónica (CML), leucemia linfoblástica aguda de las células T (T-ALL), leucemia linfoblástica aguda de las células B (B-ALL), linfoma no de Hodgkin (NHL), linfoma de las células B y tumores sólidos, tales como el cáncer de mama.

Schienenauszugsvorrichtung für ein Hausgerät sowie Hausgerät mit einer Schienenauszugsvorrichtung

Schienenauszugsvorrichtung (14, 15, 16, 17) für ein Hausgerät (1), mit einer ersten Schiene (18) und zumindest einer relativ dazu bewegbaren zweiten Schiene (19), wobei eine Sperreinrichtung (21) ausgebildet ist, mit welcher die Schienen (18, 19) im ausgezogenen Zustand positionsstabil zueinander gehalten sind, wobei die Sperreinrichtung (21) einen Sperrhebel (22) aufweist, der an einer Lagerstelle (23) an einer der Schienen (18, 19) angeordnet ist und zur positionsstabilen Halterung der Schienen (18, 19) um eine Schwenkachse (B, C) an der Lagerstelle (23) verschwenkbar ist, und zumindest eine Anlagestütze (32) beabstandet zur Schwenkachse (B, C) angeordnet ist, welche mit dem Sperrhebel (22) zu dessen Führung der Schwenkbewegung verbunden ist, dadurch gekennzeichnet, dass- die Anlagestütze (32) in eine der Schienen (18, 19) integriert ist und- die Anlagestütze (32) in der Schiene (18, 19) angeordnet ist, in der sich auch die Lagerstelle (23) für den Sperrhebel (22) befindet.