The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers, isotopologues, or N-oxides thereof. The present invention is further concerned with inter alia the use of such a compound or salt, stereoisomer, tautomer, isotopologues, or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.
The present invention relates to compounds of formula (I) and salts, stereoisomers, atropisomers, rotamers, tautomers or N-oxides thereof that are useful as PRMT5 inhibitors. The present invention further relates to the compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising said compounds.
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
Substituted tetrazole derivatives are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
A61K 31/437 - 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 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 41/17 - Inactivation or decontamination of a medicinal preparation prior to administration to an animal or a person by ultraviolet [UV] or infrared [IR] light, X-rays or gamma rays
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
The present invention relates to compounds of formula (I) and salts, stereoisomers, atrop-isomers, rotamers, tautomers or N- oxides thereof that are useful as PRMT5 inhibitors. The present invention further relates to the compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising said compounds.
C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention is inter alia concerned with a combination of (i) a FLT3-inhibitor and (ii) SEL24/MEN1703 for use as medicament, preferably for use in the treatment of a patient suffering from cancer. The present invention is also concerned with a kit of dosage forms comprising (i) a dosage form comprising a FLT3-inhibitor and (ii) a dosage form comprising SEL24/MEN1703; as well as dosage form comprising (i) a FLT3-inhibitor and (ii) SEL24/MEN1703.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
6.
CANCER COMBINATION THERAPY INCLUDING A BCL-2 INHIBITOR
The present invention is inter alia concerned with a combination of (i) a BCL-2 inhibitor and (ii) SEL24/MEN1703 for use as medicament, preferably for use in the treatment of a patient suffering from cancer. The present invention is also concerned with a kit of dosage forms comprising (i) a dosage form comprising a BCL-2 inhibitor and (ii) a dosage form comprising SEL24/MEN1703; as well as dosage form comprising (i) a BCL-2 inhibitor and (ii) SEL24/MEN1703.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
7.
CANCER COMBINATION THERAPY INCLUDING A BCL-2 INHIBITOR
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
8.
CANCER COMBINATION THERAPY INCLUDING A FLT3-INHIBITOR
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
Substituted amide derivatives are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Compounds of the formula I
Compounds of the formula I
Compounds of the formula I
are inhibitors of HIF-2α, and can be employed for the treatment of diseases such as cancer.
C07D 333/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
13.
Modulators of stimulator of interferon genes (STING)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention relates to substituted amide derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
A61K 31/437 - 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 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The present invention relates to substituted tetrazole derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
A61K 31/437 - 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 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The present invention relates to substituted amide derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
Compounds of the formula I
1 denotes a mono- or bicyclic aromatic, unsaturated or saturated heterocycle having 1 to 4 N, O, and/or S atoms, and Hal denotes F, Cl, Br, or I, are inhibitors of HIF-2α, and can be employed for the treatment of diseases such as cancer.
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
20.
FUNCTIONALIZED HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61P 37/00 - Drugs for immunological or allergic disorders
The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
23.
CONDENSED THIOPHENE DERIVATIVES AS HYPOXIA INDUCIBLE FACTOR (HIF) INHIBITORS
Compounds of the formula I in which R1, R2, R3, R4, R5, n and m have the meanings indicated in Claim 1, are inhibitors of HIF-2a, and can be employed for the treatment of diseases such as cancer.
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
24.
CONDENSED THIOPHENE DERIVATIVES AS HYPOXIA INDUCIBLE FACTOR (HIF) INHIBITORS
Compounds of the formula I in which R1, R2, R3, R4, R5, n and m have the meanings indicated in Claim 1, are inhibitors of HIF-2α, and can be employed for the treatment of diseases such as cancer.
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
26.
NEXT-GENERATION MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention relates to the compounds of formula (I) and salts, stereoisomers, tautomers, isotopologues, or N-oxides thereof. The present invention is further concerned with the use of such a compounds or salt, stereoisomer, tautomer, isotopologues, or N- oxide thereof as modulators of the adenosine A2A receptor in the treatment of cancer and a pharmaceutical composition comprising said compounds.
The present invention relates to disubstituted alkyne derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
C07C 311/14 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 317/12 - SulfonesSulfoxides having sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 317/14 - SulfonesSulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 307/79 - Benzo [b] furansHydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 333/62 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to disubstituted alkyne derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
C07D 333/62 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07C 311/14 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07C 317/12 - SulfonesSulfoxides having sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 317/14 - SulfonesSulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 307/79 - Benzo [b] furansHydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical preparations for use in the manufacture of
pharmaceuticals; chemical preparations for scientific
purposes, other than for medical or veterinary use; chemical
products for biotechnological purposes [industrial];
chemicals for use in the agrochemical industry. Chemico-pharmaceutical preparations; chemical preparations
for pharmaceutical purposes; pharmaceutical preparations and
substances for use in oncology; pharmaceutical preparations
and substances for the treatment of cancer; biotechnological
preparations for medical use; medicines for human purposes;
adjuvants for medical purposes; biological tissue cultures
for medical purposes; biological preparations for veterinary
purposes; biological preparations for medical purposes; drug
delivery agents that facilitate the delivery of
pharmaceutical preparations; medical preparations;
diagnostic preparations and materials; chemical preparations
for medical purposes; immunomodulators; immunostimulants;
immunoassay reagents for medical use; chemotherapeutics;
chemical reagents for medical or veterinary purposes;
biological preparations for the treatment of cancer; mixed
biological preparations for medical purposes;
pharmaceuticals; pharmaceutical preparations and substances;
anti-cancer drugs; dietetic foods adapted for medical
purposes; dietetic food preparations adapted for medical
use. Scientific apparatus and instruments; software; computer
software for use in medical decision support systems;
instruments for diagnosis [for scientific use]; scientific
research and laboratory apparatus, educational apparatus and
simulators. Research and development services in the field of
immunology; chemistry services; chemical laboratories;
chemistry consultation; testing of chemicals; chemical
analysis; scientific research relating to chemistry;
chemical research laboratory services; research and
development services in the field of chemistry; provision of
scientific information relating to the chemical industry;
preparation of reports relating to chemical research;
research and development in the pharmaceutical and
biotechnology fields; laboratory research services relating
to pharmaceuticals; information technology consultancy
services for the pharmaceutical and healthcare industries;
scientific research; computer aided scientific research
services; biochemical research and analysis; genetic
research; clinical research; biological research; biological
analysis; scientific research relating to biology;
preparation of biological samples for research purposes;
medical research; research to develop new products; research
in the field of gene therapy; research and development in
the field of diagnostic preparations; information on the
subject of scientific research in the field of biochemistry
and biotechnology; consultancy relating to pharmaceutical
research and development; scientific research for medical
purposes in the area of cancerous diseases; pharmaceutical
products development; pharmaceutical product evaluation;
testing of pharmaceuticals; conducting clinical trials for
pharmaceutical products; research on the subject of
pharmaceuticals; scientific laboratory services; scientific
services relating to the isolation and cultivation of human
tissues and cells; computer aided scientific testing;
scientific and technological design; software design and
development; design and development of medical technology;
design and development of software for database management;
pharmaceutical research and development; providing
information about the results of clinical trials for
pharmaceutical products; technological research; engineering
services relating to computers; computer analysis.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical preparations for use in the manufacture of
pharmaceuticals; chemical preparations for scientific
purposes, other than for medical or veterinary use; chemical
products for biotechnological purposes [industrial];
chemicals for use in the agrochemical industry. Chemico-pharmaceutical preparations; chemical preparations
for pharmaceutical purposes; pharmaceutical preparations and
substances for use in oncology; pharmaceutical preparations
and substances for the treatment of cancer; biotechnological
preparations for medical use; medicines for human purposes;
adjuvants for medical purposes; biological tissue cultures
for medical purposes; biological preparations for veterinary
purposes; biological preparations for medical purposes; drug
delivery agents that facilitate the delivery of
pharmaceutical preparations; medical preparations;
diagnostic preparations and materials; chemical preparations
for medical purposes; immunomodulators; immunostimulants;
immunoassay reagents for medical use; chemotherapeutics;
chemical reagents for medical or veterinary purposes;
biological preparations for the treatment of cancer; mixed
biological preparations for medical purposes;
pharmaceuticals; pharmaceutical preparations and substances;
anti-cancer drugs; dietetic foods adapted for medical
purposes; dietetic food preparations adapted for medical
use. Scientific apparatus and instruments; software; computer
software for use in medical decision support systems;
instruments for diagnosis [for scientific use]; scientific
research and laboratory apparatus, educational apparatus and
simulators. Research and development services in the field of
immunology; chemistry services; chemical laboratories;
chemistry consultation; testing of chemicals; chemical
analysis; scientific research relating to chemistry;
chemical research laboratory services; research and
development services in the field of chemistry; provision of
scientific information relating to the chemical industry;
preparation of reports relating to chemical research;
research and development in the pharmaceutical and
biotechnology fields; laboratory research services relating
to pharmaceuticals; information technology consultancy
services for the pharmaceutical and healthcare industries;
scientific research; computer aided scientific research
services; biochemical research and analysis; genetic
research; clinical research; biological research; biological
analysis; scientific research relating to biology;
preparation of biological samples for research purposes;
medical research; research to develop new products; research
in the field of gene therapy; research and development in
the field of diagnostic preparations; information on the
subject of scientific research in the field of biochemistry
and biotechnology; consultancy relating to pharmaceutical
research and development; scientific research for medical
purposes in the area of cancerous diseases; pharmaceutical
products development; pharmaceutical product evaluation;
testing of pharmaceuticals; conducting clinical trials for
pharmaceutical products; research on the subject of
pharmaceuticals; scientific laboratory services; scientific
services relating to the isolation and cultivation of human
tissues and cells; computer aided scientific testing;
scientific and technological design; software design and
development; design and development of medical technology;
design and development of software for database management;
pharmaceutical research and development; providing
information about the results of clinical trials for
pharmaceutical products; technological research; engineering
services relating to computers; computer analysis.
32.
MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical preparations being additives for use in the manufacture of pharmaceuticals; chemical preparations for scientific purposes, other than for medical or veterinary use; chemical products for biotechnological purposes, namely, chemicals for use in biotechnological research and product development; chemicals for use in the agrochemical industry Chemico-pharmaceutical preparations, namely, chemical preparations for pharmaceutical purposes, namely, for the treatment of cancer and for use in immunology and oncology; chemical preparations for pharmaceutical purposes for the treatment of cancer and for use in immunology and oncology; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations and substances for the treatment of cancer; biotechnological preparations for medical use in the nature of biological preparations for the treatment of cancer and for use immunology and oncology; medicines for human purposes, namely, medicines for the treatment of cancer and for use in immunology and oncology; adjuvants for medical purposes; biological tissue cultures for medical purposes; biological preparations being biological tissue cultures for veterinary purposes; biological preparations for medical purposes, namely, for treatment of cancer and for use in immunology and oncology; drug delivery agents consisting of compounds that facilitate the delivery of pharmaceutical preparations; medical preparations, namely, for treatment of cancer and for use in oncology; diagnostic preparations and materials being diagnostic preparations for medical purposes; chemical preparations for medical purposes namely, for treatment of cancer and for use in immunology and oncology; immunomodulators being a type of pharmaceutical preparation for the treatment of cancer; immunostimulants; immunoassay reagents for medical use; chemotherapeutics; chemical reagents for medical or veterinary purposes; biological preparations for the treatment of cancer; mixed biological preparations for medical purposes, namely, for the treatment of cancer; pharmaceuticals for the treatment of cancer; pharmaceutical preparations and substances, namely, for treatment of cancer and for use in immunology and oncology; anti-cancer preparations Downloadable computer software for use with medical diagnosis, research, and treatment, namely, for analyzing medical data and diagnosing medical conditions, for evaluation of suggested medical treatment, analyzing and evaluating medical data for mitigation or prevention of disease, for processing data related to clinical trials, and for use with the development, production, and research of pharmaceuticals, namely, data processing, data analysis and data evaluation, processing and analyzing data related to clinical trials, evaluating and analyzing pharmaceutical ingredients and facilitating formulation and administration of pharmaceuticals Research and development services in the field of immunology; chemistry services, namely, research in the field of immunology and oncology; chemical laboratories; chemistry consultation; testing of chemicals; chemical analysis; scientific research relating to chemistry; chemical research laboratory services; research and development services in the field of chemistry; provision of scientific information relating to the chemical industry; preparation of reports relating to chemical research; research and development in the pharmaceutical and biotechnology fields; laboratory research services relating to pharmaceuticals; information technology consultancy services for the pharmaceutical and healthcare industries; scientific research; computer aided scientific research services; biochemical research and analysis; genetic research; clinical research in the field of immunology and oncology; biological research; biological analysis; scientific research relating to biology; custom development of biological samples for research purposes; medical research; research to develop new products; research in the field of gene therapy; research and development in the field of diagnostic preparations; information on the subject of scientific research in the field of biochemistry and biotechnology; consultancy relating to pharmaceutical research; scientific research for medical purposes in the area of cancerous diseases; pharmaceutical products development; pharmaceutical product evaluation; testing of pharmaceuticals; conducting clinical trials for others for pharmaceutical products; research on the subject of pharmaceuticals; scientific laboratory services; scientific research services relating to the isolation and cultivation of human tissues and cells; computer aided scientific testing in the field of immunology and oncology; scientific and technological design, namely, design in the fields of biochemistry and biotechnology, namely, custom design of pharmaceuticals, chemicals, biological preparations, scientific software, pharmaceutical software, medical software, medical instruments and devices; software design and development; design and development of medical technology, namely, technology research in the field of medical instruments and devices; design and development of software for database management; pharmaceutical research and development; providing scientific information about the results of clinical trials for pharmaceutical products; technological research, namely, research in the field of pharmaceuticals; engineering services relating to computers, namely, computer-aided engineering services for the biotechnology industry; computer systems analysis
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical preparations being additives for use in the manufacture of pharmaceuticals; chemical preparations for scientific purposes, other than for medical or veterinary use; chemical products for biotechnological purposes, namely, chemicals for use in biotechnological research and product development; chemicals for use in the agrochemical industry Chemico-pharmaceutical preparations, namely, chemical preparations for pharmaceutical purposes, namely, for the treatment of cancer and for use in immunology and oncology; chemical preparations for pharmaceutical purposes for the treatment of cancer and for use in immunology and oncology; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations and substances for the treatment of cancer; biotechnological preparations for medical use in the nature of biological preparations for the treatment of cancer and for use immunology and oncology; medicines for human purposes, namely, medicines for the treatment of cancer and for use in immunology and oncology; adjuvants for medical purposes; biological tissue cultures for medical purposes; biological preparations being biological tissue cultures for veterinary purposes; biological preparations for medical purposes, namely, for treatment of cancer and for use in immunology and oncology; drug delivery agents consisting of compounds that facilitate the delivery of pharmaceutical preparations; medical preparations, namely, for treatment of cancer and for use in oncology; diagnostic preparations and materials being diagnostic preparations for medical purposes; chemical preparations for medical purposes namely, for treatment of cancer and for use in immunology and oncology; immunomodulators being a type of pharmaceutical preparation for the treatment of cancer; immunostimulants; immunoassay reagents for medical use; chemotherapeutics; chemical reagents for medical or veterinary purposes; biological preparations for the treatment of cancer; mixed biological preparations for medical purposes, namely, for the treatment of cancer; pharmaceuticals for the treatment of cancer; pharmaceutical preparations and substances, namely, for treatment of cancer and for use in immunology and oncology; anti-cancer preparations Downloadable computer software for use with medical diagnosis, research, and treatment, namely, for analyzing medical data and diagnosing medical conditions, for evaluation of suggested medical treatment, analyzing and evaluating medical data for mitigation or prevention of disease, for processing data related to clinical trials, and for use with the development, production, and research of pharmaceuticals, namely, data processing, data analysis and data evaluation, processing and analyzing data related to clinical trials, evaluating and analyzing pharmaceutical ingredients and facilitating formulation and administration of pharmaceuticals Research and development services in the field of immunology; chemistry services, namely, research in the field of immunology and oncology; chemical laboratories; chemistry consultation; testing of chemicals; chemical analysis; scientific research relating to chemistry; chemical research laboratory services; research and development services in the field of chemistry; provision of scientific information relating to the chemical industry; preparation of reports relating to chemical research; research and development in the pharmaceutical and biotechnology fields; laboratory research services relating to pharmaceuticals; information technology consultancy services for the pharmaceutical and healthcare industries; scientific research; computer aided scientific research services; biochemical research and analysis; genetic research; clinical research in the field of immunology and oncology; biological research; biological analysis; scientific research relating to biology; custom development of biological samples for research purposes; medical research; research to develop new products; research in the field of gene therapy; research and development in the field of diagnostic preparations; information on the subject of scientific research in the field of biochemistry and biotechnology; consultancy relating to pharmaceutical research; scientific research for medical purposes in the area of cancerous diseases; pharmaceutical products development; pharmaceutical product evaluation; testing of pharmaceuticals; conducting clinical trials for others for pharmaceutical products; research on the subject of pharmaceuticals; scientific laboratory services; scientific research services relating to the isolation and cultivation of human tissues and cells; computer aided scientific testing in the field of immunology and oncology; scientific and technological design, namely, design in the fields of biochemistry and biotechnology, namely, custom design of pharmaceuticals, chemicals, biological preparations, scientific software, pharmaceutical software, medical software, medical instruments and devices; software design and development; design and development of medical technology, namely, technology research in the field of medical instruments and devices; design and development of software for database management; pharmaceutical research and development; providing scientific information about the results of clinical trials for pharmaceutical products; technological research, namely, research in the field of pharmaceuticals; engineering services relating to computers, namely, computer-aided engineering services for the biotechnology industry; computer systems analysis
Compounds of the formula (I) in which R1, R2, R3, R4 and n have the meanings indicated in Claim 1, are inhibitors of HIF-2a, and can be employed for the treatment of diseases such as cancer.
C07D 333/78 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
10 - Medical apparatus and instruments
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemical preparations for use in the manufacture of pharmaceuticals; Chemical preparations for scientific purposes, other than for medical or veterinary use; Chemical products for biotechnological purposes [industrial]; Biochemicals for in vitro and in vivo scientific use; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Chemicals for use in the agrochemical industry; Laboratory chemicals for scientific use; Chemical compositions and materials for use in science; Chemical test reagents [other than medical or veterinary]; Chemicals for use in scientific analysis [other than medical or veterinary]; Chemicals for use in scientific research [other than medical or veterinary]; Chemical reagents for use in science, other than for medical or veterinary use; Chemical reagents for molecular biology, other than for medical or veterinary use; Chemical reagents for laboratory use, other than for medical or veterinary use; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Biological preparations for use in science. Chemico-pharmaceutical preparations; Chemical preparations for pharmaceutical purposes; Pharmaceutical preparations and substances for use in oncology; Pharmaceutical preparations and substances for the treatment of cancer; Biotechnological preparations for medical use; Medicines for human purposes; Adjuvants for medical purposes; Biological tissue cultures for medical purposes; Biological preparations for veterinary purposes; Biological preparations for medical purposes; Drug delivery agents that facilitate the delivery of pharmaceutical preparations; Medical preparations; Diagnostic preparations and materials; Chemical preparations for medical purposes; Immunomodulators; Immunostimulants; Immunoassay reagents for medical use; Chemotherapeutics; Chemical reagents for medical or veterinary purposes; Biological preparations for the treatment of cancer; Mixed biological preparations for medical purposes; Pharmaceuticals; Pharmaceutical preparations and substances; Anti-cancer drugs; Dietetic foods adapted for medical purposes; Dietetic food preparations adapted for medical use. Scientific apparatus and instruments; Software; Computer software for use in medical decision support systems; Instruments for diagnosis [for scientific use]; Scientific research and laboratory apparatus, educational apparatus and simulators. Medical apparatus for introducing pharmaceutical preparations into the human body; Diagnostic, examination, and monitoring equipment; Applicators for pharmaceutical preparations; Testing apparatus for medical purposes; Medication injectors; Medical apparatus for facilitating the inhalation of pharmaceutical preparations; Inhalers; Apparatus for administering pharmaceuticals; Infusion pumps to deliver medication; Applicators for medications. Education services relating to health; Educational services in the healthcare sector; Conducting educational support programmes for patients; Conducting educational support programmes for healthcare professionals; Arranging and conducting conferences and seminars; Publishing of medical publications; Organization of seminars and conventions in the field of medicine; Organisation of conferences and symposia in the field of medical science; Medical education services; Running seminars in the field of oncology. Research and development services in the field of immunology; Chemistry services; Chemical laboratories; Chemical research; Chemistry consultation; Chemical analytical examinations; Chemical technological research; Testing of chemicals; Chemical analysis; Scientific research relating to chemistry; Chemical research laboratory services; Laboratory research in the field of chemistry; Research and development services in the field of chemistry; Provision of scientific information relating to the chemical industry; Preparation of reports relating to chemical research; Research and development for the pharmaceutical industry; Research and development in the pharmaceutical and biotechnology fields; Laboratory research services relating to pharmaceuticals; Information technology services for the pharmaceutical and healthcare industries; Scientific research; Computer aided scientific research services; Biochemical research and analysis; Genetic research; Clinical research; Biological research; Biological analysis; Scientific research relating to biology; Preparation of biological samples for research purposes; Biological development services; Preparation of biological samples for analysis in research laboratories; Biological research, clinical research and medical research; Research laboratories; Medical research; Research into new products; Research in the field of gene therapy; Research and development in the field of diagnostic preparations; Information on the subject of scientific research in the field of biochemistry and biotechnology; Consultancy relating to pharmaceutical research and development; Scientific research for medical purposes in the area of cancerous diseases; Pharmaceutical products development; Pharmaceutical product evaluation; Testing of pharmaceuticals; Conducting clinical trials for pharmaceutical products; Research on the subject of pharmaceuticals; Scientific laboratory services; Scientific research conducted using databases; Scientific services relating to the isolation and cultivation of human tissues and cells; Computer aided scientific testing; Scientific and technological design; Software design and development; Design and development of medical technology; Design and development of software for database management; Working on and evaluation of chemical analyses; Research and development services; Pharmaceutical research and development; Providing information about the results of clinical trials for pharmaceutical products; Technological research; Engineering services relating to computers; Computer analysis. Advice relating to immunology; Consultancy and information services relating to pharmaceutical products; Medical services in the field of oncology; Medical testing for diagnostic or treatment purposes; Providing on-line information relating to oncology; Pharmacy advice; Provision of pharmaceutical information.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
10 - Medical apparatus and instruments
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemical preparations for use in the manufacture of pharmaceuticals; Chemical preparations for scientific purposes, other than for medical or veterinary use; Chemical products for biotechnological purposes [industrial]; Biochemicals for in vitro and in vivo scientific use; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Chemicals for use in the agrochemical industry; Laboratory chemicals for scientific use; Chemical compositions and materials for use in science; Chemical test reagents [other than medical or veterinary]; Chemicals for use in scientific analysis [other than medical or veterinary]; Chemicals for use in scientific research [other than medical or veterinary]; Chemical reagents for use in science, other than for medical or veterinary use; Chemical reagents for molecular biology, other than for medical or veterinary use; Chemical reagents for laboratory use, other than for medical or veterinary use; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Biological preparations for use in science. Chemico-pharmaceutical preparations; Chemical preparations for pharmaceutical purposes; Pharmaceutical preparations and substances for use in oncology; Pharmaceutical preparations and substances for the treatment of cancer; Biotechnological preparations for medical use; Medicines for human purposes; Adjuvants for medical purposes; Biological tissue cultures for medical purposes; Biological preparations for veterinary purposes; Biological preparations for medical purposes; Drug delivery agents that facilitate the delivery of pharmaceutical preparations; Medical preparations; Diagnostic preparations and materials; Chemical preparations for medical purposes; Immunomodulators; Immunostimulants; Immunoassay reagents for medical use; Chemotherapeutics; Chemical reagents for medical or veterinary purposes; Biological preparations for the treatment of cancer; Mixed biological preparations for medical purposes; Pharmaceuticals; Pharmaceutical preparations and substances; Anti-cancer drugs; Dietetic foods adapted for medical purposes; Dietetic food preparations adapted for medical use. Scientific apparatus and instruments; Software; Computer software for use in medical decision support systems; Instruments for diagnosis [for scientific use]; Scientific research and laboratory apparatus, educational apparatus and simulators. Medical apparatus for introducing pharmaceutical preparations into the human body; Diagnostic, examination, and monitoring equipment; Applicators for pharmaceutical preparations; Testing apparatus for medical purposes; Medication injectors; Medical apparatus for facilitating the inhalation of pharmaceutical preparations; Inhalers; Apparatus for administering pharmaceuticals; Infusion pumps to deliver medication; Applicators for medications. Education services relating to health; Educational services in the healthcare sector; Conducting educational support programmes for patients; Conducting educational support programmes for healthcare professionals; Arranging and conducting conferences and seminars; Publishing of medical publications; Organization of seminars and conventions in the field of medicine; Organisation of conferences and symposia in the field of medical science; Medical education services; Running seminars in the field of oncology. Research and development services in the field of immunology; Chemistry services; Chemical laboratories; Chemical research; Chemistry consultation; Chemical analytical examinations; Chemical technological research; Testing of chemicals; Chemical analysis; Scientific research relating to chemistry; Chemical research laboratory services; Laboratory research in the field of chemistry; Research and development services in the field of chemistry; Provision of scientific information relating to the chemical industry; Preparation of reports relating to chemical research; Research and development for the pharmaceutical industry; Research and development in the pharmaceutical and biotechnology fields; Laboratory research services relating to pharmaceuticals; Information technology services for the pharmaceutical and healthcare industries; Scientific research; Computer aided scientific research services; Biochemical research and analysis; Genetic research; Clinical research; Biological research; Biological analysis; Scientific research relating to biology; Preparation of biological samples for research purposes; Biological development services; Preparation of biological samples for analysis in research laboratories; Biological research, clinical research and medical research; Research laboratories; Medical research; Research into new products; Research in the field of gene therapy; Research and development in the field of diagnostic preparations; Information on the subject of scientific research in the field of biochemistry and biotechnology; Consultancy relating to pharmaceutical research and development; Scientific research for medical purposes in the area of cancerous diseases; Pharmaceutical products development; Pharmaceutical product evaluation; Testing of pharmaceuticals; Conducting clinical trials for pharmaceutical products; Research on the subject of pharmaceuticals; Scientific laboratory services; Scientific research conducted using databases; Scientific services relating to the isolation and cultivation of human tissues and cells; Computer aided scientific testing; Scientific and technological design; Software design and development; Design and development of medical technology; Design and development of software for database management; Working on and evaluation of chemical analyses; Research and development services; Pharmaceutical research and development; Providing information about the results of clinical trials for pharmaceutical products; Technological research; Engineering services relating to computers; Computer analysis. Advice relating to immunology; Consultancy and information services relating to pharmaceutical products; Medical services in the field of oncology; Medical testing for diagnostic or treatment purposes; Providing on-line information relating to oncology; Pharmacy advice; Provision of pharmaceutical information.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
10 - Medical apparatus and instruments
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemical preparations for use in the manufacture of pharmaceuticals; Chemical preparations for scientific purposes, other than for medical or veterinary use; Chemical products for biotechnological purposes [industrial]; Biochemicals for in vitro and in vivo scientific use; Diagnostic reagents for in vitro use in biochemistry, clinical chemistry and microbiology; Chemicals for use in the agrochemical industry; Laboratory chemicals for scientific use; Chemical compositions and materials for use in science; Chemical test reagents [other than medical or veterinary]; Chemicals for use in scientific analysis [other than medical or veterinary]; Chemicals for use in scientific research [other than medical or veterinary]; Chemical reagents for use in science, other than for medical or veterinary use; Chemical reagents for molecular biology, other than for medical or veterinary use; Chemical reagents for laboratory use, other than for medical or veterinary use; Chemical reagents for use in diagnostic tests, other than for medical or veterinary use; Biological preparations for use in science. Chemico-pharmaceutical preparations; Chemical preparations for pharmaceutical purposes; Pharmaceutical preparations and substances for use in oncology; Pharmaceutical preparations and substances for the treatment of cancer; Biotechnological preparations for medical use; Medicines for human purposes; Adjuvants for medical purposes; Biological tissue cultures for medical purposes; Biological preparations for veterinary purposes; Biological preparations for medical purposes; Drug delivery agents that facilitate the delivery of pharmaceutical preparations; Medical preparations; Diagnostic preparations and materials; Chemical preparations for medical purposes; Immunomodulators; Immunostimulants; Immunoassay reagents for medical use; Chemotherapeutics; Chemical reagents for medical or veterinary purposes; Biological preparations for the treatment of cancer; Mixed biological preparations for medical purposes; Pharmaceuticals; Pharmaceutical preparations and substances; Anti-cancer drugs; Dietetic foods adapted for medical purposes; Dietetic food preparations adapted for medical use. Scientific apparatus and instruments; Software; Computer software for use in medical decision support systems; Instruments for diagnosis [for scientific use]; Scientific research and laboratory apparatus, educational apparatus and simulators. Medical apparatus for introducing pharmaceutical preparations into the human body; Diagnostic, examination, and monitoring equipment; Applicators for pharmaceutical preparations; Testing apparatus for medical purposes; Medication injectors; Medical apparatus for facilitating the inhalation of pharmaceutical preparations; Inhalers; Apparatus for administering pharmaceuticals; Infusion pumps to deliver medication; Applicators for medications. Education services relating to health; Educational services in the healthcare sector; Conducting educational support programmes for patients; Conducting educational support programmes for healthcare professionals; Arranging and conducting conferences and seminars; Publishing of medical publications; Organization of seminars and conventions in the field of medicine; Organisation of conferences and symposia in the field of medical science; Medical education services; Running seminars in the field of oncology. Research and development services in the field of immunology; Chemistry services; Chemical laboratories; Chemical research; Chemistry consultation; Chemical analytical examinations; Chemical technological research; Testing of chemicals; Chemical analysis; Scientific research relating to chemistry; Chemical research laboratory services; Laboratory research in the field of chemistry; Research and development services in the field of chemistry; Provision of scientific information relating to the chemical industry; Preparation of reports relating to chemical research; Research and development for the pharmaceutical industry; Research and development in the pharmaceutical and biotechnology fields; Laboratory research services relating to pharmaceuticals; Information technology services for the pharmaceutical and healthcare industries; Scientific research; Computer aided scientific research services; Biochemical research and analysis; Genetic research; Clinical research; Biological research; Biological analysis; Scientific research relating to biology; Preparation of biological samples for research purposes; Biological development services; Preparation of biological samples for analysis in research laboratories; Biological research, clinical research and medical research; Research laboratories; Medical research; Research into new products; Research in the field of gene therapy; Research and development in the field of diagnostic preparations; Information on the subject of scientific research in the field of biochemistry and biotechnology; Consultancy relating to pharmaceutical research and development; Scientific research for medical purposes in the area of cancerous diseases; Pharmaceutical products development; Pharmaceutical product evaluation; Testing of pharmaceuticals; Conducting clinical trials for pharmaceutical products; Research on the subject of pharmaceuticals; Scientific laboratory services; Scientific research conducted using databases; Scientific services relating to the isolation and cultivation of human tissues and cells; Computer aided scientific testing; Scientific and technological design; Software design and development; Design and development of medical technology; Design and development of software for database management; Working on and evaluation of chemical analyses; Research and development services; Pharmaceutical research and development; Providing information about the results of clinical trials for pharmaceutical products; Technological research; Engineering services relating to computers; Computer analysis. Advice relating to immunology; Consultancy and information services relating to pharmaceutical products; Medical services in the field of oncology; Medical testing for diagnostic or treatment purposes; Providing on-line information relating to oncology; Pharmacy advice; Provision of pharmaceutical information.
The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
C07D 235/24 - BenzimidazolesHydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
C07D 235/30 - Nitrogen atoms not forming part of a nitro radical
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 235/14 - Radicals substituted by nitrogen atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
C07D 235/24 - BenzimidazolesHydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
C07D 235/30 - Nitrogen atoms not forming part of a nitro radical
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 235/14 - Radicals substituted by nitrogen atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
41.
NOVEL BENZIMIDAZOLE DERIVATIVES AS KINASE INHIBITORS
The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceuticalcompositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3-and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 235/24 - BenzimidazolesHydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
C07D 235/30 - Nitrogen atoms not forming part of a nitro radical
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
42.
SUBSTITUTED TRICYCLIC BENZIMIDAZOLES AS KINASE INHIBITORS
Disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (I) or pharmaceutically acceptable salts thereof. The compounds of the invention selectively inhibit CDK8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hematological malignancies, autoimmune diseases and inflammatory diseases. Also disclosed are processes for preparing these compounds.
