The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
This disclosure relates to the use of certain diaryl macrocycle compounds in the treatment of disease in mammals. This disclosure also relates to compositions including such compounds, and to methods of using such compositions in the treatment of diseases in mammals, especially in humans.
This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10] benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07C 271/16 - Esters des acides carbamiques ayant des atomes d'oxygène de groupes carbamate liés à des atomes de carbone acycliques avec les atomes d'azote des groupes carbamate liés à des atomes d'hydrogène ou à des atomes de carbone acycliques à des atomes de carbone de radicaux hydrocarbonés substitués par des atomes d'oxygène liés par des liaisons simples
The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with a KRAS inhibitor, such as an inhibitor of KRAS G12C.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.
This disclosure relates to the use of certain diaryl macrocycle compounds, specifically (7S13R)-11-fluoro-7,13-di-methyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one in the treatment of disease in mammals. This disclosure also relates to compositions including such compounds, and to methods of using such compositions in the treatment of diseases in mammals, especially in humans.
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07C 271/16 - Esters des acides carbamiques ayant des atomes d'oxygène de groupes carbamate liés à des atomes de carbone acycliques avec les atomes d'azote des groupes carbamate liés à des atomes d'hydrogène ou à des atomes de carbone acycliques à des atomes de carbone de radicaux hydrocarbonés substitués par des atomes d'oxygène liés par des liaisons simples
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, heart failure, thrombosis, stroke, cancer, respiratory diseases, auto-immune diseases, rheumatoid arthritis, lupus, inflammatory bowel disease, solid organ transplant rejection, hepatitis, fibrosis, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; pharmaceutical preparations for human use for the treatment and prevention of metabolic disorders, namely, diabetes, obesity, hyperlipidemia, insulin resistance, metabolic syndrome; pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, anti-inflammatories, anti-infectives, central nervous system depressants, central nervous system stimulants, anti-psychotics, cytokine inhibitory drugs, anticoagulants; pharmaceutical preparations for human use, namely, pharmaceutical antibodies for the treatment of cancer, respiratory diseases, auto-immune diseases, and for the prevention and treatment of solid organ transplant rejection; pharmaceutical preparations for human use, namely, pharmaceutical antibodies for use as anti-infectives, and for use as anti-inflammatories; diagnostic pharmaceutical preparations for human use for increasing the heart rate and for use as medical imaging contrast agents; pharmaceutical preparations for human use that modulate the immune system; pharmaceutical preparations for human use, namely, immunotherapies for the treatment of cancer; pharmaceutical and biological preparations for human use for use in immunotherapies; pharmaceutical and biological preparations for human use for use in T-cell immunotherapy; pharmaceutical and biological preparations for human use for use in cell therapy; pharmaceutical and biological preparations for human use namely T-cells for medical purposes and T-cells for clinical laboratory use; pharmaceutical preparations for human use namely diagnostic kits consisting primarily of cells for medical laboratory use; Pharmaceutical preparations for human use for treatment and prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use namely antivirals for treatment and prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; pharmaceutical preparations for human use namely monoclonal antibodies; pharmaceutical preparations for human use for the treatment of neuropsychiatric disorders; therapeutic radiopharmaceutical preparations for human use for the treatment of cancer and solid tumors; diagnostic radiopharmaceutical preparations for human use; pharmaceutical preparations for human use namely radiopharmaceutical imaging and detection agents for diagnosing and monitoring cancer; pharmaceutical preparations for human use namely radio-isotope markers for therapeutic or diagnostic use; radiopharmaceuticals for human use; Pharmaceutical preparations for human use for the treatment of Cystic Fibrosis
The present disclosure provides new methods of preparing a compound of Formula (I). Such methods can prepare the compound at any scale, including gram and kilogram scale.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
C07D 221/04 - Systèmes cycliques condensés en ortho ou en péri
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
This disclosure relates to polymorphs of (3aR,11S,20aS)-7-fluoro-11-methyl-2,3,3a,12,13,20a-hexahydro-1H,5H-17,19-(metheno)cyclopenta[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment and prevention of obesity, incontinence, cardiovascular diseases, central nervous system diseases and disorders, metabolic disorders, stroke, cancer, inflammation and inflammatory diseases, respiratory and infectious diseases, auto-immune diseases, solid organ transplant rejection, beta thalassemia and myelodysplastic syndromes, myeloproliferative diseases, myelofibrosis, leukemia, lymphoma, multiple myeloma, autoinflammatory disease, blood disease, tumors, multiple sclerosis, ulcerative colitis, arthritis, and musculoskeletal and skin diseases; Pharmaceutical preparations for human use, namely, antibiotics, anti-fungals, anti-virals, immunosuppressants, pharmaceutical antibodies, immunotherapies for the treatment of cancer, cytokine inhibitory drugs; Pharmaceutical preparations for human use that modulate the immune system; Pharmaceutical and biological preparations for human use for immunotherapy, namely T Cell therapy; Pharmaceutical preparations for human use, namely, stem cells for medical or clinical use; Pharmaceutical preparations for human use for the treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, antivirals for treatment or prevention of covid-19, coronavirus disease, and respiratory diseases and disorders; Pharmaceutical preparations for human use, namely, monoclonal antibodies for medical use
The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
This disclosure relates to the use of certain diaryl macrocycle compounds in the treatment of disease in mammals. This disclosure also relates to compositions including such compounds, and to methods of using such compositions in the treatment of diseases in mammals, especially in humans.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with a KRAS inhibitor, such as an inhibitor of KRAS G12C.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
The present disclosure relates to certain diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with a KRAS inhibitor, such as an inhibitor of KRAS G12C.
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.
F24F 5/00 - Systèmes ou appareils de conditionnement d'air non couverts par ou
F25B 23/00 - Machines, installations ou systèmes ayant un seul principe de fonctionnement non compris dans les groupes , p. ex. utilisant l'effet de radiation sélective
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.
This disclosure relates to the use of certain diaryl macrocycle compounds, specifically (7S13R)-11-fluoro-7,13-di-methyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one in the treatment of disease in mammals. This disclosure also relates to compositions including such compounds, and to methods of using such compositions in the treatment of diseases in mammals, especially in humans.
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer. Also provided are methods of inhibiting receptor tyrosine kinases such as RET or SRC using the macrocyclic derivatives. The macrocyclic compounds have a tetracyclic heterocyclic core moiety, such as, cylopenta[5,6][1,4]oxazino[3,4-j] pyrazolo[4,3-g][1,5,9,11]benzoxatriazacyclotetradecin-15-one.
aRSSaHHilHH)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with at least one other cancer therapeutic, such as an EGFR inhibitor.
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
83.
Chiral diaryl macrocycles as modulators of protein kinases
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, of the formula I:
pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/4353 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques
C07D 209/56 - Systèmes cycliques contenant au moins trois cycles
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
The present disclosure relates to certain macrocyclic kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same to treat disease.
This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07C 271/16 - Esters des acides carbamiques ayant des atomes d'oxygène de groupes carbamate liés à des atomes de carbone acycliques avec les atomes d'azote des groupes carbamate liés à des atomes d'hydrogène ou à des atomes de carbone acycliques à des atomes de carbone de radicaux hydrocarbonés substitués par des atomes d'oxygène liés par des liaisons simples
The present disclosure relates to certain chiral diaryl macrocyclic derivatives of the formula I
pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
C07C 233/57 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
The present invention relates to certain diaryl macrocyclic compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
The present invention relates to certain diaryl macrocyclic compounds, such as
compounds of of Formula (IV): and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods of using them. The compounds have activity against tyrosine kinases, such as ALK or Trks, and as such may be useful for treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
C07D 491/12 - Composés hétérocycliques contenant dans le système cyclique condensé, à la fois un ou plusieurs cycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle, et un ou plusieurs cycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus dans les groupes , , ou dans lesquels le système condensé contient trois hétérocycles
The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.
F24F 5/00 - Systèmes ou appareils de conditionnement d'air non couverts par ou
F25B 23/00 - Machines, installations ou systèmes ayant un seul principe de fonctionnement non compris dans les groupes , p. ex. utilisant l'effet de radiation sélective
This disclosure relates to the use of certain diaryl macrocycle compounds, specifically (7S13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one in the treatment of disease in mammals. This disclosure also relates to compositions including such compounds, and to methods of using such compositions in the treatment of diseases in mammals, especially in humans.
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with at least one other cancer therapeutic, such as an EGFR inhibitor.
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/529 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime formant une partie de systèmes cycliques pontés
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with a KRAS inhibitor, such as an inhibitor of KRAS G12C.
The present disclosure relates to certain diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Composés hétérocycliques contenant dans le système condensé au moins un hétérocycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle dans lesquels le système condensé contient au moins quatre hétérocycles
