C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Torrente De Haro, Esther
Paonessa, Giacomo
Ontoria Ontoria, Jesus Maria
Montalbetti, Chrisian
Corio, Alessandra
Ievoli, Giovanni
Abstract
The present invention pertains to compounds that inhibit Flavivirus NS2B-NS3 proteases and are potent and selective inhibitors of the West Nile virus and Zika virus. The compounds of the invention can be used alone or in combination with other agents to treat infections caused by these viruses. Additionally, the invention relates to pharmaceutical compositions containing these compounds.
C07D 413/10 - 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 carbon chain containing aromatic 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
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Petrocchi, Alessia
Montalbetti, Christian
Di Fabio, Romano
Ciammaichella, Alina
Rossetti, Ilaria
Abstract
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase. Compounds of the invention can be used for the treatment of disorders associated with SHP2 deregulation. The present invention also relates to pharmaceutical compositions containing said compounds and to their method of synthesis.
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 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
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
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Alli, Cristina
Bresciani, Alberto
Di Fabio, Romano
Montalbetti, Christian A.G.N.
Ontoria Ontoria, Jesus Maria
Paonessa, Giacomo
Quotadamo, Antonio
Torrente De Haro, Esther
Bencheva, Leda
Amaudrut, Jerome
Corio, Alessandra
Ferrigno, Federica
Abstract
The invention relates to compounds that are inhibitors of Flavivirus NS2B-NS3 proteases and inhibit replication of flavivirus in cells. Compounds of this invention are useful alone or in combination with other agents for use in the treatment of infections caused by Flaviviruses, in particular by Dengue, West Nile, Zika, Japan Encephalitis viruses.
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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 31/4545 - 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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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
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 413/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 413/10 - 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 carbon chain containing aromatic 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 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 417/12 - 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
42 - Scientific, technological and industrial services, research and design
Goods & Services
Scientific and technological services and research and design relating thereto; Industrial analysis, of industrial research and of industrial design; quality control and authentication services; Design and development of computer hardware and software; Research in the chemical-pharmaceutical sector; Medical research; Biological research; Clinical research; Analysis of human serum for medical research; Analysis of human tissues for medical research; Providing medical research information in the field of genetics; Providing medical research information in the field of pharmaceuticals; Providing medical and scientific research information in the field of pharmaceuticals and clinical trials.
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Ontoria Ontoria, Jesus Maria
Montalbetti, Christian
Quotadamo, Antonio
Torrente De Haro, Esther
Corio, Alessandra
Ievoli, Giovanni
Di Fabio, Romano
Bencheva, Leda Ivanova
Amaudrut, Jerome
Abstract
The invention relates to compounds that are inhibitors of Flavivirus NS2B-NS3 proteases and inhibit replication of flavivirus in cells. Compounds of this invention are useful alone or in combination with other agents for use in the treatment of infections caused by Flaviviruses, in particular by Dengue, West Nile, Zika, Japan Encephalitis viruses.
(S)-1-(5-((PYRIDIN-3-YL)THIO)PYRAZIN-2-YL)-4'H,6'H-SPIRO[PIPERIDINE-4,5'-PYRROLO [1,2-B]PYRAZOL]-4'-AMINE DERIVATIVES AND SIMILAR COMPOUNDS AS SHP2 INHIBITORS FOR THE TREATMENT OF E.G. CANCER
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
IRBM S.p.A. (Italy)
Inventor
Di Fabio, Romano
Montalbetti, Christian
Petrocchi, Alessia
Grillo, Alessandro
Randazzo, Pietro
Rossetti, Ilaria
Ciammaichella, Alina
Abstract
The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
UNIVERSITÄTSMEDIZIN DER JOHANNES GUTENBERG-UNIVERSITÄT MAINZ (Germany)
THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIVERSITY (Canada)
ISTITUTO SUPERIORE DI SANITÀ (Italy)
CONSIGLIO NAZIONALE DELLE RICERCHE (Italy)
IRBM S.P.A. (Italy)
Inventor
Martino, Gianvito
Panina, Paola
Nait-Oumesmar, Brahim
Baron-Van Evercooren, Anne
Kuhlmann, Tanja
Baranzini, Sergio
Goebels, Norbert
Zipp, Frauke
Hanuscheck, Nicholas
Antel, Jack
Agresti, Cristina
Abbracchio, Maria Pia
Eberini, Ivano
Parravicini, Chiara
Olla, Stefania
Bresciani, Alberto
Abstract
The present invention provides compounds able to induce neuroprotection of damaged neurons and boost the remyelination potential of oligodendrocytes. The compounds have been identified through methods of pharmacological screening of a small molecule library consisting of known pharmacologically active compounds and approved drugs. The screening method is also included in the invention.
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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 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
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Petrocchi, Alessia
Montalbetti, Christian
Di Fabio, Romano
Ciammaichella, Alina
Rossetti, Ilaria
Abstract
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase. Compounds of the invention can be used for the treatment of disorders associated with SHP2 deregulation. The present invention also relates to pharmaceutical compositions containing said compounds and to their method of synthesis.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Petrocchi, Alessia
Montalbetti, Christian
Di Fabio, Romano
Ciammaichella, Alina
Rossetti, Ilaria
Abstract
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase. Compounds of the invention can be used for the treatment of disorders associated with SHP2 deregulation. The present invention also relates to pharmaceutical compositions containing said compounds and to their method of synthesis.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Ciammaichella, Alina
Di Fabio, Romano
Ferrigno, Federica
Fezzardi, Paola
Montalbetti, Christian
Petrocchi, Alessia
Relitti, Nicola
Rossetti, Ilaria
Sferrazza, Alessio
Torrente, Esther
Ferrante, Luca
Grillo, Alessandro
Abstract
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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 401/14 - 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 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 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
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
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Alli, Cristina
Bresciani, Alberto
Di Fabio, Romano
Montalbetti, Christian A.G.N.
Ontoria Ontoria, Jesus Maria
Paonessa, Giacomo
Quotadamo, Antonio
Torrente De Haro, Esther
Bencheva, Leda
Amaudrut, Jerome
Corio, Alessandra
Ferrigno, Federica
Abstract
The invention relates to compounds that are inhibitors of Flavivirus NS2B-NS3 proteases and inhibit replication of flavivirus in cells. Compounds of this invention are useful alone or in combination with other agents for use in the treatment of infections caused by Flaviviruses, in particular by Dengue, West Nile, Zika, Japan Encephalitis viruses.
C07D 413/10 - 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 carbon chain containing aromatic 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 413/10 - 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 carbon chain containing aromatic 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
(S)-1-(5-((PYRIDIN-3-YL)THIO)PYRAZIN-2-YL)-4'H,6'H-SPIRO[PIPERIDINE-4,5'-PYRROLO [1,2-B]PYRAZOL]-4'-AMINE DERIVATIVES AND SIMILAR COMPOUNDS AS SHP2 INHIBITORS FOR THE TREATMENT OFE.G. CANCE
C.N.C.C.S. SCARL COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
IRBM S.P.A. (Italy)
Inventor
Di Fabio, Romano
Montalbetti, Christian
Petrocchi, Alessia
Grillo, Alessandro
Randazzo, Pietro
Rossetti, Ilaria
Ciammaichella, Alina
Abstract
The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-4lH,6'H-spiro[piperidine-4,5'-pyrrolo[l,2-b]pyrazol]-4l- amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
15.
(S)-1-(5-((PYRIDIN-3-YL)THIO)PYRAZIN-2-YL)-4'H,6'H-SPIRO[PIPERIDINE-4,5'-PYRROLO [1,2-B]PYRAZOL]-4'-AMINE DERIVATIVES AND SIMILAR COMPOUNDS AS SHP2 INHIBITORS FOR THE TREATMENT OF E.G. CANCER
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
IRBM S.P.A. (Italy)
Inventor
Di Fabio, Romano
Montalbetti, Christian
Petrocchi, Alessia
Grillo, Alessandro
Randazzo, Pietro
Rossetti, Ilaria
Ciammaichella, Alina
Abstract
The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-4lH,6'H-spiro[piperidine-4,5'-pyrrolo[l,2-b]pyrazol]-4l- amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
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
C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING (Italy)
Inventor
Ciammaichella, Alina
Ferrigno, Federica
Ontoria Ontoria, Jesus Maria
Petrocchi, Alessia
Ponzi, Simona
Rossetti, Ilaria
Sferrazza, Alessio
Torrente, Esther
Abstract
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).
The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
17.
COMPOUNDS FOR USE IN PROGRESSIVE MULTIPLE SCLEROSIS
UNIVERSITÄTSMEDIZIN DER JOHANNES GUTENBERG-UNIVERSITÄT MAINZ (Germany)
THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIVERSITY (Canada)
ISTITUTO SUPERIORE DI SANITÀ (Italy)
CONSIGLIO NAZIONALE DELLE RICERCHE (Italy)
IRBM S.P.A. (Italy)
Inventor
Martino, Gianvito
Panina, Paola
Nait-Oumesmar, Brahim
Baron-Van Evercooren, Anne
Kuhlmann, Tanja
Baranzini, Sergio
Goebels, Norbert
Zipp, Frauke
Hanuscheck, Nicholas
Antel, Jack
Agresti, Cristina
Abbracchio, Maria Pia
Eberini, Ivano
Parravicini, Chiara
Olla, Stefania
Bresciani, Alberto
Abstract
The present invention provides compounds able to induce neuroprotection of damaged neurons and boost the remyelination potential of oligodendrocytes. Said compounds have been identified through methods of pharmacological screening on a small molecule library consisting of known pharmacologically active compounds and approved drugs. The screening method is also included in the invention.
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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 31/40 - 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
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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 31/4462 - Non-condensed piperidines, e.g. piperocaine only substituted in position 3
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 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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 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 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
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 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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Prandi, Adolfo
Randazzo, Pietro
Gornati, Davide
Grillo, Alessandro
Ferrante, Luca
Bencheva, Leda Ivanova
De Matteo, Marilenia
Ferrara, Marco
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing the compounds.
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 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
Inventor
Di Fabio, Romano
Summa, Vincenzo
Bencheva, Leda Ivanova
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Prandi, Adolfo
De Matteo, Marilenia
Randazzo, Pietro
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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 403/04 - 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 403/14 - 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 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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 413/14 - 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 31/4545 - 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
22.
OXALAMIDO-SUBSTITUTED TRICYCLIC INHIBITORS OF HEPATITIS B VIRUS
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
OSPEDALE SAN RAFFAELE S.R.L. (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Prandi, Adolfo
Randazzo, Pietro
Ivanova Bencheva, Leda
De Matteo, Marilenia
Ferrante, Luca
Gornati, Davide
Grillo, Alessandro
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/437 - 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
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
OSPEDALE SAN RAFFAELE S.R.L. (Italy)
IRBM S.P.A. (Italy)
PROMIDIS S.R.L. (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Prandi, Adolfo
Randazzo, Pietro
Ivanova Bencheva, Leda
De Matteo, Marilenia
Ferrante, Luca
Gornati, Davide
Grillo, Alessandro
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
IRBM S.P.A. (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Prandi, Adolfo
Randazzo, Pietro
Gornati, Davide
Grillo, Alessandro
Ferrante, Luca
Bencheva, Leda Ivanova
De Matteo, Marilenia
Ferrara, Marco
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Prandi, Adolfo
Randazzo, Pietro
Gornati, Davide
Grillo, Alessandro
Ferrante, Luca
Bencheva, Leda Ivanova
De Matteo, Marilenia
Ferrara, Marco
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
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 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
Inventor
De Francesco, Raffaele
Prandi, Adolfo
Randazzo, Pietro
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Bencheva, Leda Ivanova
De Matteo, Marilenia
Ferrante, Luca
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
C07C 311/44 - 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 having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 207/14 - Nitrogen atoms not forming part of a nitro radical
C07D 211/58 - Nitrogen atoms attached in position 4
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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 ring atoms
ISTITUTO NAZIONALE DI GENETICA MOLECOLARE - INGM (Italy)
Inventor
De Francesco, Raffaele
Donnici, Lorena
Guidotti, Luca
Iannacone, Matteo
Di Fabio, Romano
Summa, Vincenzo
Bencheva, Leda Ivanova
De Matteo, Marilenia
Ferrante, Luca
Prandi, Adolfo
Randazzo, Pietro
Abstract
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
C07D 285/28 - 1,2,4-ThiadiazinesHydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached in position 3
C07D 291/08 - Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems