The present invention relates to novel fluoroallylamine sulfone derivatives that are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for the treatment of a variety of indications, e.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
The present invention relates to novel bioprobes which are capable of binding to certain amine oxidase enzymes. These bioprobes are useful in methods of detecting and determining the concentration of certain amine oxidase enzymes in a sample as well as in methods for the quantitative assessment of inhibition of certain amine oxidases.
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 novel compounds which are capable of inhibiting semicarbazide-sensitive amine oxidase (SSAO/VAP-1) and monoamine oxidase B (MAO-B). These compounds are useful for treatment of a variety of neuromuscular diseases, such as muscular dystrophies, and neuroinflammatory diseases, including both peripheral and central disorders in human subjects, as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
4.
DIFLUOROHALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES, METHODS OF PREPARATION, AND USES THEREOF
The present invention relates to methods for preparing a variety of difluorohaloallylamine derivatives. The present invention also relates to novel difluorohaloallylamine derivatives that are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for the treatment of a variety of indications, e.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof.
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 317/20 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
C07D 279/12 - 1,4-ThiazinesHydrogenated 1,4-thiazines not condensed with other rings
C07C 317/36 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atoms of the amino groups bound to hydrogen atoms or to carbon atoms
C07B 59/00 - Introduction of isotopes of elements into organic compounds
C07B 45/04 - Formation or introduction of functional groups containing sulfur of sulfonyl or sulfinyl groups
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 295/116 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings with the doubly bound oxygen or sulfur atoms directly attached to a carbocyclic ring
The present invention relates to novel compounds which are capable of inhibiting semicarbazide-sensitive amine oxidase (SSAO/VAP-1) and monoamine oxidase B (MAO-B). These compounds are useful for treatment of a variety of neuromuscular diseases, such as muscular dystrophies, and neuroinflammatory diseases, including both peripheral and central disorders in human subjects, as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07C 217/46 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and unsaturated
The present invention relates to novel bioprobes which are capable of binding to certain amine oxidase enzymes. These bioprobes are useful in methods of detecting and determining the concentration of certain amine oxidase enzymes in a sample as well as in methods for the quantitative assessment of inhibition of certain amine oxidases.
e.ge.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof.
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 317/20 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
C07C 315/02 - Preparation of sulfonesPreparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
C07B 45/04 - Formation or introduction of functional groups containing sulfur of sulfonyl or sulfinyl groups
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to methods for preparing a variety of difluorohaloallylamine derivatives. The present invention also relates to novel difluorohaloallylamine derivatives that are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for the treatment of a variety of indications, e.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof.
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
C07B 45/04 - Formation or introduction of functional groups containing sulfur of sulfonyl or sulfinyl groups
C07C 315/02 - Preparation of sulfonesPreparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
C07C 317/20 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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
9.
HALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to novel compounds such as those of formula I(see formula I)which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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 405/04 - 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 directly linked by a ring-member-to-ring- member bond
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
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
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 405/04 - 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 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 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 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.
C07D 209/24 - 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 with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:
The invention also relates to methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
C07C 235/46 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 323/62 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
C07C 311/37 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 323/63 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
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 311/16 - 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 hydrogen atoms or to an acyclic carbon atom
16.
Substituted 3-haloallylamine inhibitors of ASSAO and uses thereof
The preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I:
is described. Methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer, are also described.
C07C 311/37 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 235/46 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 323/62 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
C07C 323/63 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
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
17.
SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF SSAO AND USES THEREOF
The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula (I), as defined in the specification. The invention also relates to methods of using compounds of Formula (I), or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
C07C 235/46 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 311/28 - 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 ring other than a six-membered aromatic ring
C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
18.
SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF SSAO AND USES THEREOF
The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula (I), as defined in the specification. The invention also relates to methods of using compounds of Formula (I), or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
C07C 233/11 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
C07C 311/16 - 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 hydrogen atoms or to an acyclic carbon atom
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A delivery device (100,200) is disclosed, which comprises a container (80) containing a dose of greater than 40mg of a powder and having at least one exit orifice (92) for dispensing the dose from the container (80), and a chamber (110) adapted to receive the container (80) in an operative configuration, the delivery device (100,200) further comprising at least one gas inlet (26) by which gas may enter the chamber (110) and at least one gas outlet (72) by which gas and entrained powder may exit the chamber (110), wherein the delivery device (100,200) is operable to generate a gas flow through the chamber (110) between the at least one gas inlet (26) and the at least one gas outlet (72), which brings about orbital motion of the container (80) within the chamber (110) in that at least a central region of the container (80) orbits a central axis of the chamber (110).
A delivery device (100,200) is disclosed, which comprises a container (80) containing a dose of a powder, a chamber (110) adapted to receive the container (80), at least one gas inlet (26) by which gas may enter the chamber (110), and at least one gas outlet (72) by which gas and entrained powder may exit the chamber (110) for inhalation, the delivery device (100,200) having a pre-use configuration in which the container (80) is accommodated, at least partially, within a storage enclosure in a wall of the chamber (110), the delivery device (100,200) having a deployment member (60) adapted to put the delivery device (100,200) in an operative configuration by displacing the container (80) from the storage enclosure into the chamber (110), such that the container (80) is movable within the chamber (110), in use, the deployment member (60) being adapted to at least partially occupy the storage enclosure in the operative configuration.
A delivery device (100,200) is disclosed, which comprises a container (80) containing a dose of greater than 40mg of a powder and having at least one exit orifice (92) for dispensing the dose from the container (80), and a chamber (110) adapted to receive the container (80) in an operative configuration, the delivery device (100,200) further comprising at least one gas inlet (26) by which gas may enter the chamber (110) and at least one gas outlet (72) by which gas and entrained powder may exit the chamber (110), wherein the delivery device (100,200) is operable to generate a gas flow through the chamber (110) between the at least one gas inlet (26) and the at least one gas outlet (72), which brings about orbital motion of the container (80) within the chamber (110) in that at least a central region of the container (80) orbits a central axis of the chamber (110).
A delivery device (100,200) is disclosed, which comprises a container (80) containing a dose of a powder and having at least one exit orifice (98) for dispensing the dose from the container (80), and a chamber (110) adapted to receive the container (80) in an operative configuration, the device (100,200) further comprising at least one gas inlet (26) by which gas may enter the chamber (110) and at least one gas outlet (72) by which gas and entrained powder may exit the chamber (110), wherein the delivery device (100,200) is operable to generate a gas flow through the chamber (110) between the at least one gas inlet (26) and the at least one gas outlet (72), which brings about orbital motion of the container (80) within the chamber (110) in that at least a central region of the container (80) orbits a central axis of the chamber (110), wherein the volume occupied by the container (80) is at least 25% of the volume of the chamber (110).
A delivery device (100,200) is disclosed, which comprises a container (80) containing a dose of a powder and having at least one exit orifice (98) for dispensing the dose from the container (80), and a chamber (110) adapted to receive the container (80) in an operative configuration, the device (100,200) further comprising at least one gas inlet (26) by which gas may enter the chamber (110) and at least one gas outlet (72) by which gas and entrained powder may exit the chamber (110), wherein the delivery device (100,200) is operable to generate a gas flow through the chamber (110) between the at least one gas inlet (26) and the at least one gas outlet (72), which brings about orbital motion of the container (80) within the chamber (110) in that at least a central region of the container (80) orbits a central axis of the chamber (110), wherein the volume occupied by the container (80) is at least 25% of the volume of the chamber (110).
A delivery device comprises a free-standing container containing a dose of powder. There is a chamber adapted to receive the container, at least one gas inlet by which gas may enter the chamber, and at least one gas outlet by which gas and entrained powder may exit the chamber for inhalation. The delivery device has a pre-use configuration in which the container is accommodated, at least partially, within a storage enclosure in a wall of the chamber a deployment member adapted to put the delivery device in an operative configuration by displacing the container from the storage enclosure into the chamber, such that the container is freely movable within the chamber, in the operative configuration, to permit orbital motion of the container driven by gas flow within the chamber. The deployment member is adapted to at least partially occupy the storage enclosure in the operative configuration.
There is provided herein, an oligonucleotide directed against a target gene, wherein the oligonucleotide is capable of hybridizing to at least a portion of a nucleic acid sequence encoding the gene under stringent conditions, and wherein, at least one nucleotide of the oligonucleotide is 2-amino-2'- deoxyadenosine (DAP); and the internucleoside linkages of the oligonucleotide comprises at least three alternating segments, each segment consisting of either at least one phosphorothioate or at least one phosphodiester bond.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/7125 - Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
There is provided oligonucleotides directed against the CCR3 receptor and the common beta sub-unit of IL-3, IL-5 and GM-CSF receptors. The oligonucleotides are useful to inhibit general inflammation, including inflammation associated with asthma, COPD, allergy, Cystic fibrosis (CF), hypereosinophilia and neoplastic cell proliferation such as cancer.
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
27.
NO-DONATING CORDICOSTEROID WITH IMPROVED PHARMACOKINETIC, ANTI-INFLAMMATORY AND VASODILATORY PROPERTIES
The present invention involves the use of a steroid linked to nitric oxide (preferred steroid is budesonide) for treating respirator}' diseases by decreasing neutrophil sputum levels and decreasing plasma CRP levels Respiratory diseases treated include asthma, COPD (chronic obstructive pulmonary disorder), eosinophilic cough, bronchitis, sarcoidosis, pulmonary fibrosis, rhinitis, pulmonary hypertension, cystic fibrosis, bronchiectasis and sinusitis
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
A61P 11/00 - Drugs for disorders of the respiratory system
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations and substances; pharmaceutical
reagents and antibodies, chemical reagents for
pharmaceutical, medical and diagnostic purposes; diagnostic
preparations and substances for medical use; inhalers filled
with pharmaceutical preparations, diagnostic preparations.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations to treat and prevent diseases and disorders associated with the respiratory system; pharmaceutical preparations to treat and prevent chronic obstructive pulmonary diseases and disorders; pharmaceutical preparations for the treatment and prevention of bronchiectasis; pharmaceutical preparations for the treatment and prevention of chronic bronchitis; and pharmaceutical preparations for the treatment and prevention of cystic fibrosis; pharmaceutical preparations and substances for the treatment of cystic fibrosis
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations and substances; pharmaceutical
reagents and antibodies, chemical reagents for
pharmaceutical, medical and diagnostic purposes; diagnostic
preparations and substances for medical use. Inhalers; medical inhalers; filters for inhalers; apparatus
for administering drugs or pharmaceutical preparations by
inhalation; drug delivery apparatus; parts and fittings for
the aforementioned goods. Research and development including research and development
for new products in the fields of pharmaceuticals and drug
discovery; medical and scientific research, including,
conducting clinical and diagnostic trials; pharmaceutical
and drug development services; consultancy and reporting in
the fields of biotechnology research and development;
provision of information in relation to the aforesaid
services.
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations and substances; pharmaceutical
reagents and antibodies, chemical reagents for
pharmaceutical, medical and diagnostic purposes; diagnostic
preparations and substances for medical use. Inhalers; medical inhalers; filters for inhalers; apparatus
for administering drugs or pharmaceutical preparations by
inhalation; drug delivery apparatus; parts and fittings for
the aforementioned goods. Research and development including research and development
for new products in the fields of pharmaceuticals and drug
discovery; medical and scientific research, including,
conducting clinical and diagnostic trials; pharmaceutical
and drug development services; consultancy and reporting in
the fields of biotechnology research and development;
provision of information in relation to the aforesaid
services.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations to treat and prevent diseases and disorders associated with the respiratory system; pharmaceutical preparations to treat and prevent chronic obstructive pulmonary diseases and disorders; pharmaceutical preparations for the treatment and prevention of bronchiectasis; pharmaceutical preparations for the treatment and prevention of chronic bronchitis; and pharmaceutical preparations for the treatment and prevention of cystic fibrosis.
34.
OLIGONUCLEOTIDES AFFECTING EXPRESSION OF PHOSPHODIESTERASES
The invention relates to therapeutic antisense oligonucleotides directed against genes encoding phosphodiesterases (PDE) and the use of these antisense oligonucleotides in combination. These antisense oligonucleotides may be used as analytical tools and/or as therapeutic agents in the treatment of disease associated with reduced cellular cAMP in a patient, such as inflammatory diseases of the respiratory tract including, for example, asthma, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome, bronchitis, chronic bronchitis, silicosis, pulmonary fibrosis, lung allograft rejection, allergic rhinitis and chronic sinusitis as well as other conditions in which an increase in cyclic AMP or a decrease in PDE levels is beneficial.
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
35.
SMALL INTERFERING RIBONUCLEIC ACID DUPLEXES COMPRISING ARABINOSE MODIFIED NUCLEOTIDES
Small interfering ribonucleic acid duplexes (siRNA) comprising at least one arabinose modified nucleotide that inhibit gene expression are Provided. In one embodiment, the duplexes contain ribonucleotides wherein at least one arabinose modified nucleotide is a 2'-deoxy-2'- fluoroarabinonucleotide (FANA).
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations and substances; pharmaceutical reagents and antibodies, chemical reagents for pharmaceutical, medical and diagnostic purposes; diagnostic preparations and substances for medical use, none of the aforementioned goods/services being for animals or veterinary purposes. Inhalers; medical inhalers; filters for inhalers; apparatus for administering drugs or pharmaceutical preparations by inhalation; drug delivery apparatus; parts and fittings for the aforementioned goods. Research and development including research and development for new products in the fields of pharmaceuticals and drug discovery; medical and scientific research, including, conducting clinical and diagnostic trials; pharmaceutical and drug development services; consultancy and reporting in the fields of biotechnology research and development; provision of information in relation to the aforesaid services, none of the aforementioned goods/services being for animals or veterinary purposes.
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations to treat and prevent diseases and disorders associated with the respiratory system; [ pharmaceutical preparations to treat and prevent chronic obstructive pulmonary diseases and disorders; ] pharmaceutical preparations for the treatment and prevention of bronchiectasis; [ pharmaceutical preparations for the treatment and prevention of chronic bronchitis; ] and pharmaceutical preparations for the treatment and prevention of cystic fibrosis; inhalers filled with pharmaceutical preparations to treat and prevent diseases and disorders associated with the respiratory system; [ inhalers filled with pharmaceutical preparations to treat and prevent chronic obstructive pulmonary diseases and disorders; ] inhalers filled with pharmaceutical preparations for the treatment and prevention of bronchiectasis; [ inhalers filled with pharmaceutical preparations for the treatment and prevention of chronic bronchitis; ] inhalers filled with pharmaceutical preparations for the treatment and prevention of cystic fibrosis Inhalers for medical purposes, sold empty; inhalers for therapeutic purposes, sold empty; [ pressurized metered dose medical inhalers, sold empty; ] dry powder inhalers for medical or therapeutic use, sold empty; medical inhalers sold empty; apparatus for administering drugs or pharmaceutical preparations by inhalation, namely, nebulizers for respiration therapy and medical apparatus for facilitating the inhalation of pharmaceutical preparations; and drug delivery apparatus, namely, drug delivery systems; replacement parts and fittings for the aforementioned goods
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations to aid in the diagnosis and management of asthma; pharmaceutical preparations to assist in the diagnosis and prevention of diseases, disorders, conditions or ailments associated with the respiratory system; pharmaceutical preparations to assist in the diagnosis and management of chronic obstructive pulmonary diseases and disorders.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Diagnostic pharmaceutical preparations for medical purposes in evaluating and managing asthma; diagnostic pharmaceutical preparations for medical purposes to assist in the diagnosis of diseases, disorders, conditions or ailments associated with the respiratory system [ ; diagnostic pharmaceutical preparations for medical purposes to assist in the diagnosis and management of chronic obstructive pulmonary diseases and disorders ]
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Inhalable pharmaceutical products in powder or capsule form for the management (namely assesment) and diagnosis of respiratory diseases, supplied under prescription only, and administered only under the direct supervision of a medical or healthcare professional; but not including cosmetic and pharmaceutical tooth and mouth care preparations.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations to treat and prevent diseases and disorders associated with the respiratory system; pharmaceutical preparations to treat and prevent chronic obstructive pulmonary diseases and disorders; pharmaceutical preparations for the treatment and prevention of bronchiectasis; pharmaceutical preparations for the treatment and prevention of chronic bronchitis; and pharmaceutical preparations for the treatment [and prevention] of cystic fibrosis
