FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Substituted benzamides and substituted pyridinecarboxamides as Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

Factor XIa Inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 3. The compound of wherein Ris aryl claim 1 , which optionally is substituted with one to three substituents independently selected from the group consisting of halo claim 1 , cyano claim 1 , R claim 1 , ORand heteroaryl which is optionally substituted with R; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with one to two substituents independently selected from the group consisting of halo and tetrazolyl; or a pharmaceutically acceptable salt thereof.5. The compound of wherein Ris aryl claim 1 , which optionally is substituted with one to three halo groups; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with halo; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.8. The compound of wherein Ris cyclopropyl; or a pharmaceutically acceptable salt thereof.9. The compound of wherein Ris R claim 1 , which optionally is substituted with halo claim 1 , (C═O)ORor NH(C═O)OR claim 1 , or a pharmaceutically acceptable salt thereof.11. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.12. A method for inhibiting thrombus formation in blood or treating thrombus formation in blood comprising administering a composition of to a mammal in need of thereof.13. A method for preventing thrombus formation in blood comprising administering a composition of to a mammal in need thereof.14. A method of ...

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa Inhibitors

The present invention provides a compound of Formula (I) (Formula(I)) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 3. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with two or three substituents independently selected from the group consisting of halo and heteroaryl; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with halo and tetrazolyl; or a pharmaceutically acceptable salt thereof.5. The compound of where in Ris phenyl claim 1 , which optionally is substituted with three halo; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris hydroxy; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris phenyl claim 1 , which is optionally substituted with one to three substituents independently selected from the group consisting of (C═O)ORand NH(C═O)R; or a pharmaceutically acceptable salt thereof.8. The compound of wherein Ris phenyl claim 1 , which is substituted with (C═O)OR; or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.11. A method for inhibiting thrombus formation in blood or treating thrombus formation in blood comprising administering a composition of to a mammal in need of thereof.12. A method for preventing thrombus formation in blood comprising administering a composition of to a mammal in need thereof.13. A method of treating venous thromboembolism and pulmonary embolism in a mammal comprising administering a composition of to a mammal in need thereof.14. A method of treating deep vein thrombosis in a mammal comprising ...

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 4. The compound of wherein Ris phenyl claim 1 ,which optionally is substituted with two or three substituents independently selected from the group consisting of halo and heteroaryl; or a pharmaceutically acceptable salt thereof.5. The compound of wherein Ris phenyl claim 1 ,which optionally is substituted with halo and tetrazolyl; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with three halo; or a pharmaceutically acceptable salt thereof.7. The compound of wherein is imidazolyl claim 1 , oxazolyl claim 1 , oxadiazolyl claim 1 , benzimidazolyl or pyrazolyl claim 1 , wherein said imidazolyl is optionally substituted with methyl or halo; or a pharmaceutically acceptable salt thereof.8. The compound of wherein is phenyl claim 1 , which is optionally substituted with halo; or a pharmaceutically acceptable salt thereof.9. The compound of wherein is phenyl; or a pharmaceutically acceptable salt thereof.10. The compound of selected from:methyl [4-(2-{3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-1-oxido-6,7-dihydro-5H-cyclopenta[b]pyridin-7-yl}-1H-imidazol-4-yl)phenyl]carbamate;methyl [4-(2-{3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-1-oxido-6,7-dihydro-5H-cyclopenta[b]pyridin-7-yl}-4-methyl-1H-imidazol-5-yl)phenyl]carbamate;3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-7-[4-(3-fluorophenyl)-1H-imidazol-2-yl]-6,7-dihydro-5H-cyclopenta[b]pyridine 1-oxide;methyl 4-(2-{3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-1-oxido-6,7-dihydro-5H-cyclopenta[b]pyridin-7-yl}-1H-imidazol-4-yl)-3-fluorothiophene-2-carboxylate;3-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-7-[4-(3- ...

BTK INHIBITORS

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I 3. The compound of claim 1 , wherein ring K is defined as:{'sub': 1', '2', '3', '4, 'sup': 7', '8', '9', '10, 'Bis C(R), Bis C(R), Bis C(R), and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 9', '10, 'Bis N, Bis N, Bis C(R), and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 8', '10, 'Bis N, Bis C(R), Bis N, and Bis C(R); or'}{'sub': 1', '2', '3', '4, 'sup': 8', '9, 'Bis N, Bis C(R), Bis C(R), and Bis N; or'}{'sub': 1', '2', '3', '4, 'sup': 7', '8, 'Bis C(R), Bis C(R), Bis N, and Bis N; or'}{'sub': 1', '2', '3', '4, 'sup': 7', '9, 'Bis C(R), Bis N, Bis C(R), and Bis N.'}4. The compound of claim 3 , wherein ring K is defined as: Bis C(R) claim 3 , Bis C(R) claim 3 , Bis C(R) claim 3 , and Bis C(R) claim 3 , and wherein R claim 3 , R claim 3 , Rand Reach are H claim 3 , halogen claim 3 , (1-3C)alkyl claim 3 , (1-3C)alkoxy or halo(1-3C)alkyl; any alkoxy may optionally be substituted with one claim 3 , two or three halogen.5. The compound of claim 1 , wherein ring L is selected from the group consisting of phenyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , pyridazyl claim 1 , triazinyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , thiadiazolyl claim 1 , and isothiazolyl.7. The compound of claim 5 , wherein ring L is pyridyl.8. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , CN claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , oxetanyl claim 1 , (1-3C)alkyl claim 1 , (1-5C) alkoxy claim 1 , and (1-5C)cycloalkoxy; the alkyl claim 1 , alkoxy claim 1 , cycloalkyl and cycloalkoxy of which are optionally substituted with one or more halogen.9. The compound of claim 8 , wherein Ris selected from the group consisting of hydrogen claim 8 , fluorine claim 8 , methyl claim 8 , ethyl claim 8 , propyl claim 8 , cyclopropyl ...

Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

FACTOR XIA INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein. 5. The compound of wherein Ris aryl claim 1 , which optionally is substituted with one to four substituents independently selected from the group consisting of chloro claim 1 , fluoro claim 1 , iodo claim 1 , methyl claim 1 , cyclopropyl claim 1 , OCF claim 1 , OCF claim 1 , CF claim 1 , CF claim 1 , and heteroaryl (which is optionally substituted with halo claim 1 , cyano claim 1 , cyclopropyl claim 1 , C(O)OH claim 1 , methyl claim 1 , CFor CF); or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with one to three substituents independently selected from the group consisting of halo claim 1 , cyclopropyl and tetrazolyl; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris hydrogen or hydroxy; or a pharmaceutically acceptable salt thereof.9. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.10. A method for inhibiting thrombus formation in blood or treating thrombus formation in blood comprising administering a composition of to a mammal in need of thereof.11. A method for preventing thrombus formation in blood comprising administering a composition of to a mammal in need thereof.12. A method of treating venous thromboembolism and pulmonary embolism in a mammal comprising administering a composition of to a mammal in need thereof.13. A method of treating deep vein thrombosis in a mammal comprising administering a composition of to a mammal in need thereof.14. A method of treating thromboembolic stroke in a human comprising ...

Ophthalmic compositions for treating ocular hypertension

Ophthalmic compositions for treating ocular hypertension

This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Factor XIa inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.

Triaryl and diaryl compounds, their analogues and uses thereof

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Ophthalmic compositions for treating ocular hypertension

This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Factor XIa inhibitors

The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Substituted 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes

The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. Compounds of the invention include the compound of formula I (see formula I)

Substituted 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Pyrazole carboxamides as inhibitors of 11-β-hydroxysteroid dehydrogenase-1

Pyrazole carboxamides of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Triaryl and diaryl compounds, their analogues and uses thereof

Spiro-indolines as y5 receptor antagonists

Compounds of general structural formula (I) such as that shown in structural formula (II) are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.

Use of substituted diphenyl indanone, indane and indole compounds for the treatment or prevention of sickle cell disease, inflammatory diseases characterized by abnormal cell proliferation, diarrhe and scours

Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes

The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Bicyclic pyrimidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes

The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Spiro-indolines as Y5 receptor antagonists

Spiro-indolines as y5 receptor antagonists

Ophthalmic compositions for treating ocular hypertension

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Factor xia inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Ophthalmic compositions for treating ocular hypertension

This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

FACTOR XIa INHIBITORS

compound, pharmaceutical composition, methods for inhibiting blood thrombus formation or treating blood thrombus formation, preventing blood thrombus formation, treating venous thromboembolism and pulmonary embolism, treating deep vein thrombosis and treating thromboembolic attack , and, use of a compound

a presente invenção provê um composto de fórmula i i e composições farmacêuticas, compreendendo um ou mais dos ditos compostos, e métodos para usar os ditos compostos para tratar ou prevenir a trombose, embolias, hipercoagulabilidade ou alterações fibróticas. os compostos são inibidores seletivos do fator xia ou inibidores duplos do fator xia e da calicreína plasmática. The present invention provides a compound of formula II and pharmaceutical compositions, comprising one or more of said compounds, and methods for using said compounds to treat or prevent thrombosis, embolisms, hypercoagulability or fibrotic disorders. The compounds are selective factor xia inhibitors or dual factor xia and plasma kallikrein inhibitors.

Substituted diazepine sulfonamides as bombesin receptor subtype-3 modulators

Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

Factor xi activation inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

Factor xi activation inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

Pyrazole carboxamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Pyrazole carboxamides of structural formula (I) are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Substituted diazepine sulfonamides as bombesin receptor subtype-3 modulators

Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

Substitute 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 11-phenyl-dibenzazepine compounds that are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Pyrazole carboxamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Plasma kallikrein inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

TRIARYLMETHANE COMPOUNDS FOR THE TREATMENT OF CANCER, ACTINIC KERATOSIS AND KAPOSIARCOMA

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Heterobicyclic compounds as ep4 receptor antagonists

The invention is directed to a series of novel heterobicyclic amide derivatives as EP4 receptor antagonists which are useful for treating diseases or conditions mediated by the action of PGE2 at EP4 receptors, such as pain, an inflammatory disease and cancer. Also within the scope of this invention are pharmaceutical compositions containing such compounds and methods of use of these compounds for treating a subject suffering from a condition mediated by the action of PGE2 at EP4 receptors.

Macrocyclic compounds as factor xia inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.

Substituierte 11-phenyl-dibenzazepin-verbindungen,die nützlich sind zur behandlung oder vorbeugung von durch abnormale zellproliferation gekennzeichneten krankheiten

Factor xia inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor xia inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos

compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos. a presente invenção proporciona um composto de fórmula (i) e composições farmacêuticas compreendendo um ou mais dos referidos compostos, e métodos para usar os referidos compostos para tratar ou prevenir tromboses, embolias, hipercoagulabilidade ou alterações fibróticas. os compostos são inibidores seletivos do fator xia ou inibidores duais do fator xia e calicreína plasmática.

Bicyclische pyrimidine als dipeptidylpeptidase-iv-hemmer zur behandlung bzw. prävention von diabetes

Compostos inibidores do fator XIA, composição farmacêutica e usos dos mesmos

COMPOSTOS INIBIDORES DO FATOR XIA, COMPOSIÇÃO FARMACÊUTICA E USOS DOS MESMOS. A presente invenção proporciona um composto de Fórmula (I) e composições farmacêuticas compreendendo um ou mais dos referidos compostos, e métodos para usar os referidos compostos para tratar ou prevenir tromboses, embolias, hipercoagulabilidade ou alterações fibróticas. Os compostos são inibidores seletivos do Fator XIa ou inibidores duais do Fator XIa e Calicreína plasmática.

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Use of substituted 11-phenyl-dibenzazepine compounds for the treatment or prevention of sickle cell disease, inflammatory diseases characterized by abnormal cell proliferation, diarrhea and scour

The present invention provides substituted 11-phenyl-dibenzazepine compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of the Ca2+-activated potassium channel (Gardos channel) of erythrocytes, of mammalian cell proliferation and/or of secretagogue-stimulated transepithelial electrogenic chloride secretion in intestinal cells. The compounds can be used to reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation in situ as a therapeutic approach towards the treatment or prevention of sickle cell disease. The compounds can also be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation. Furthermore, the compounds can also be used to inhibit chloride secretion in intestinal cells as a therapeutic approach towards the treatment of diarrhea and scours.

Factor xi activation inhibitors

Spiro-indole als y5-rezeptor antagonisten

Plasma kallikrein inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Inhibidores de calicreina plasmatica.

La presente invención proporciona un compuesto de Fórmula I (ver Fórmula) I y composiciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos para usar dichos compuestos para tratamiento o prevención de uno o más estados de enfermedad que podrían beneficiarse de la inhibición de calicreína plasmática, que incluyen angioedema hereditario, uveítis, uveítis posterior, edema macular húmedo relacionado con la edad, edema macular diabético, retinopatía diabética y oclusión de la vena retiniana. Los compuestos son inhibidores selectivos de calicreína plasmática.

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Inhibidores del factor xia.

La presente invención proporciona un compuesto de la Fórmula I (ver Fórmula) y composiciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos por los que se utilizan dichos compuestos para tratar o prevenir trombosis, embolias, hipercoagulabilidad o cambios fibróticos. Los compuestos son inhibidores selectivos del Factor XIa o inhibidores dobles del Factor XIa y la calicreína plasmática.

Substituierte diphenylindanone, -indane und -indolverbindungen und deren analogue zur verwendung in der prophylaxe und behandlung von krankheiten die sich durch anormale zellproliferation auszeichnen

Inhibidores de la calicreina plasmatica.

La presente invención proporciona un compuesto de la Fórmula I (ver Fórmula) y composiciones farmacéuticas que comprende uno o más de tales compuestos, y métodos para usarse tales compuestos para tratamiento o prevención de uno o más estados patológicos que podrían beneficiarse de la inhibición de calicreína plasmática, incluyendo angioedema hereditario, uveítis, uveítis posterior, edema macular húmedo relacionado con la edad, edema macular diabético, retinopatía diabética y oclusión de la vena retiniana. Los compuestos son inhibidores selectivos de calicreína plasmática.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Factor xi activation inhibitors

Plasma kallikrein inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation.

Substituierte diphenylindanone, -indane und - indolverbindungen und deren analogue zur verwendung in der prophylaxe und behandlung von krankheiten die sich durch anormale zellproliferation auszeichnen

Substituierte diphenylindanone, -indane und -indolverbindungen und deren analogue zur verwendung in der prophylaxe und behandlung von krankheiten die sich durch anormale zellproliferation auszeichnen

Plasma kallikrein inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

Factor xia inhibitors

The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Plasma kallikrein inhibitors

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment of prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Use of triaryl methane compounds for inhibiting unwanted cellular proliferation associated with inflammatory disease

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Inhibidores de calicreina plasmatica.

La presente invención proporciona un compuesto de la Fórmula I (ver Fórmula) y composiciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos para usar dichos compuestos para tratar o prevenir uno o más estados de enfermedad que podrían beneficiarse por la inhibición de la calicreína plasmática, incluyendo angioedema hereditario, uveítis, uveítis posterior, degeneración macular húmeda relacionada con la edad, edema macular diabético, retinopatía diabética y oclusión de la vena de la retina. Los compuestos son inhibidores selectivos de calicreína plasmática.

Plasma kallikrein inhibitors

Factor XIa inhibitors

The present invention provides a compound of Formula (I) (Formula (I)) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.