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 of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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(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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
C07D 221/04 - Ortho- or peri-condensed ring systems
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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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
05 - Pharmaceutical, veterinary and sanitary products
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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 - Pharmaceutical, veterinary and sanitary products
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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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
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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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Pharmaceutical, veterinary and sanitary products
Goods & 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 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present disclosure relates to certain diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer.
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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.
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
C07D 209/56 - Ring systems containing three or more rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
The present disclosure relates to certain macrocyclic kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same to treat disease.
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 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
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 of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
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.
