AR038915A1 - Derivados de aminoindazoles, procedimiento de preparacion e intermedios de este procedimiento, medicamentos y composiciones farmaceuticas que contienen al compuesto - Google Patents
Derivados de aminoindazoles, procedimiento de preparacion e intermedios de este procedimiento, medicamentos y composiciones farmaceuticas que contienen al compuestoInfo
- Publication number
- AR038915A1 AR038915A1 ARP030100808A ARP030100808A AR038915A1 AR 038915 A1 AR038915 A1 AR 038915A1 AR P030100808 A ARP030100808 A AR P030100808A AR P030100808 A ARP030100808 A AR P030100808A AR 038915 A1 AR038915 A1 AR 038915A1
- Authority
- AR
- Argentina
- Prior art keywords
- aryl
- alkyl
- heteroaryl
- formula
- nr8r9
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 5
- 238000002360 preparation method Methods 0.000 title abstract 5
- 239000003814 drug Substances 0.000 title abstract 2
- 239000002131 composite material Substances 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 150000003839 salts Chemical class 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- -1 trifluoromethylsulfanyl Chemical group 0.000 abstract 3
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 abstract 2
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 238000006243 chemical reaction Methods 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000005592 polycycloalkyl group Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 201000011240 Frontotemporal dementia Diseases 0.000 abstract 1
- 206010019196 Head injury Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 abstract 1
- 208000024571 Pick disease Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 230000010933 acylation Effects 0.000 abstract 1
- 238000005917 acylation reaction Methods 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 238000009795 derivation Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 150000002825 nitriles Chemical class 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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
- C07D401/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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
- C07D405/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Virology (AREA)
- Psychology (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Estos compuestos pueden ser utilizados para prevenir y tratar enfermedades que pueden resultar de una actividad normal de kinasas, como por ejemplo, las enfermedades neurodegenerativas (tales como enfermedades de Alzheimer, Parkinson, Pick, la demencia frontoparietal, los accidentes cerebrovasculares y los traumatismos craneales, entre otras). Reivindicación 1: Compuestos de fórmula (1), en la que: R es bien O, S o NH; R3 es un radical alquilo (C1-6), arilo, arilo-alquilo(C1-6), heteroarilo, heteroarilo-alquilo(C1-6), arilo o heteroarilo fusionado con un cicloalquilo (C1-10), heterociclo, cicloalquilo, adamantilo, policicloalquilos, alquenilo, alquinilo; estando estos radicales, eventualmente, sustituidos por 1 o varios sustituyentes elegidos entre halógeno, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, -O-C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, C(S)NR8R9, NHC(S)R8, -O-SO2R8, -SO2-O-R8, arilo, heteroarilo, formilo, triflúormetilo, triflúormetilsulfanilo, trifluormetoxi; R4, R5, R6 y R7 son elegidos, independientemente entre sí, entre los radicales siguientes hidrógeno, halógeno, CN, NO2, NH2, OH, COOH, C(O)OR8, -O-C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, -O-SO2R8, -SO2-O-R8, triflúormetilo, triflúormetoxi, alquilo (C1-6),alcoxi (C1-6), arilo, arilo-alquilo(C1-6), heteroarilo, heteroarilo-alquilo(C1-6), heterociclo, cicloalquilo, alquenilo, alquinilo, adamantilo, policicloalquilos; estando sustituidos estos radicales, eventualmente, por 1 o varios sustituyentes elegidos entre halógeno, CN, NO2, NH2, OH, OR10, COOH, C(O)OR10, -O-C(O)R10, NR10R11, NHC(O)R10, C(O)NR10R11, NHC(S)R10, C(S)NR10R11, SR10, S(O)R10, SO2R10, NHSO2R10, SO2NR10R11, -O-SO2R10, -SO2-O-R10, arilo, heteroarilo, formilo, triflúormetilo, triflúormetoxi; R8, R9, R10, R11 son, independientemente entre sí, un hidrógeno, alquilo (C1-6), arilo, alquenilo, alquinilo, heteroarilo estando a su vez, eventualmente sustituidos por 1 o varios sustituyentes elegidos entre halógeno, alquilo(C1-6), alcoxi (C1-6), CN, NO2, NH2, OH, COOH, COOalquilo, CONH2, formilo, triflúormetilo, triflúormetoxi; sus racémicos, enantiómeros, diastereoisómeros y sus mezclas, sus tautómeros y sus sales farmacéuticamente aceptables para preparar un medicamento. Reivindicación 13: Procedimiento para la preparación de los compuestos de fórmula (1) tales como los que se han definido en la reivindicación 1 en los que R es oxígeno caracterizado porque se efectúa una acilación del derivado amina de fórmula (2), en la que R4, R5, R6, R7 tienen los mismos significados que en la reivindicación 1, transformándose, eventualmente, en sal farmacéuticamente aceptable. Reivindicación 14: Procedimiento para la preparación de los compuestos de fórmula (1) tales como los que se han definido en la reivindicación 1 y en los que R es un azufre caracterizado porque se efectúa una tionación del derivado en el que R es un oxígeno, transformándose, eventualmente, en sal farmacéuticamente aceptable. Reivindicación 15: Procedimiento para la preparación de los compuestos de fórmula (1) tales como los que se han definido en la reivindicación 1 y en los que R es NH, caracterizado porque se efectúa una reacción del derivado de fórmula (2) con un nitrilo o sal de Merwein en la que R4, R5, R6, R7 tienen los mismos significados que en la reivindicación 1 transformándose, eventualmente, en sal farmacéuticamente aceptable. Reivindicación 16: Procedimiento de preparación según las reivindicaciones 13 y 15 caracterizado porque el derivado de fórmula (2) se obtiene a partir del derivado de fórmula (3) por reacción con hidrazina.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0202997A FR2836915B1 (fr) | 2002-03-11 | 2002-03-11 | Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant |
Publications (1)
Publication Number | Publication Date |
---|---|
AR038915A1 true AR038915A1 (es) | 2005-02-02 |
Family
ID=27763685
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030100808A AR038915A1 (es) | 2002-03-11 | 2003-03-10 | Derivados de aminoindazoles, procedimiento de preparacion e intermedios de este procedimiento, medicamentos y composiciones farmaceuticas que contienen al compuesto |
Country Status (30)
Country | Link |
---|---|
US (1) | US6949579B2 (es) |
EP (1) | EP1487804B1 (es) |
JP (2) | JP4648630B2 (es) |
KR (1) | KR101068770B1 (es) |
CN (2) | CN1656078A (es) |
AR (1) | AR038915A1 (es) |
AU (1) | AU2003242809B8 (es) |
BR (1) | BR0308373A (es) |
CA (1) | CA2478542C (es) |
FR (1) | FR2836915B1 (es) |
GT (1) | GT200300057A (es) |
HR (1) | HRP20040824B1 (es) |
IL (2) | IL163831A0 (es) |
JO (1) | JO2326B1 (es) |
MA (1) | MA27230A1 (es) |
ME (2) | MEP16108A (es) |
MX (1) | MXPA04007478A (es) |
MY (1) | MY138269A (es) |
NO (1) | NO329384B1 (es) |
NZ (1) | NZ535147A (es) |
PA (1) | PA8568301A1 (es) |
PE (1) | PE20040155A1 (es) |
PL (1) | PL370478A1 (es) |
RS (1) | RS52396B (es) |
RU (1) | RU2345070C2 (es) |
SV (1) | SV2003001494A (es) |
TW (1) | TWI329103B (es) |
UY (1) | UY27713A1 (es) |
WO (1) | WO2003078403A2 (es) |
ZA (1) | ZA200406687B (es) |
Families Citing this family (78)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2836914B1 (fr) * | 2002-03-11 | 2008-03-14 | Aventis Pharma Sa | Indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
MXPA04011417A (es) * | 2002-05-17 | 2005-02-14 | Pharmacia Italia Spa | Derivados de aminoindazol activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden. |
BR0314098A (pt) | 2002-09-05 | 2005-07-19 | Aventis Pharma Sa | Derivados da aminoindazóis a tìtulo de medicamentos e composições farmacêuticas que os contêm |
CA2507074A1 (en) * | 2002-12-02 | 2004-06-17 | F. Hoffmann-La Roche Ag | Indazole derivatives as crf antagonists |
FR2848554A1 (fr) * | 2002-12-12 | 2004-06-18 | Aventis Pharma Sa | Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant |
WO2004062662A1 (fr) | 2002-12-12 | 2004-07-29 | Aventis Pharma S.A. | Derives d'aminoindazoles et leur utilisation comme inhibiteurs de kinases |
US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
WO2005077912A1 (ja) * | 2004-02-12 | 2005-08-25 | Mitsubishi Pharma Corporation | インダゾール化合物及びその医薬用途 |
FR2871158A1 (fr) * | 2004-06-04 | 2005-12-09 | Aventis Pharma Sa | Indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
RU2007101488A (ru) | 2004-08-03 | 2008-09-10 | Вайет (Us) | Индазолы для лечения сердечно-сосудистых заболеваний |
WO2007032936A2 (en) * | 2005-09-09 | 2007-03-22 | Schering Corporation | Azafused cyclin dependent kinase inhibitors |
ATE542800T1 (de) | 2006-01-31 | 2012-02-15 | Array Biopharma Inc | Kinasehemmer und ihre anwendungsverfahren |
CA2666193A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use |
CN101594862B (zh) * | 2006-12-20 | 2015-11-25 | 内尔维阿诺医学科学有限公司 | 作为激酶抑制剂的取代吲唑衍生物 |
DE102007022565A1 (de) * | 2007-05-14 | 2008-11-20 | Merck Patent Gmbh | Heterocyclische Indazolderivate |
SG183049A1 (en) * | 2007-07-20 | 2012-08-30 | Nerviano Medical Sciences Srl | Substituted indazole derivatives active as kinase inhibitors |
EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
CN101977905B (zh) | 2008-01-23 | 2014-07-02 | 百时美施贵宝公司 | 4-吡啶酮化合物及其对于癌症的用途 |
UY31968A (es) | 2008-07-09 | 2010-01-29 | Sanofi Aventis | Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos |
WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
WO2010069966A1 (en) * | 2008-12-18 | 2010-06-24 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
KR101679642B1 (ko) | 2009-04-30 | 2016-11-25 | 글락소 그룹 리미티드 | Pi3키나아제 억제제로서 옥사졸 치환된 인다졸 |
CN102482312A (zh) | 2009-08-26 | 2012-05-30 | 赛诺菲 | 新颖的杂芳族氟代糖苷结晶水合物、含有这些化合物的药物和它们的用途 |
EP2937345B1 (en) | 2009-12-29 | 2018-03-21 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
BR112012023021A2 (pt) * | 2010-03-16 | 2016-05-31 | Dana Farber Cancer Inst Inc | compostos de indazol e seus usos |
US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
EP2835131B1 (en) * | 2010-12-14 | 2017-09-06 | Electrophoretics Limited | Casein kinase 1delta (CK1delta) inhibitors |
WO2012120055A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
WO2012120053A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
EP2683698B1 (de) | 2011-03-08 | 2017-10-04 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
EP2683702B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
US8846666B2 (en) | 2011-03-08 | 2014-09-30 | Sanofi | Oxathiazine derivatives which are substituted with benzyl or heteromethylene groups, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
EP2683703B1 (de) | 2011-03-08 | 2015-05-27 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
JP6165733B2 (ja) | 2011-09-16 | 2017-07-19 | ノバルティス アーゲー | N−置換ヘテロシクリルカルボキサミド類 |
EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
AU2012340200B2 (en) | 2011-11-17 | 2017-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-Terminal Kinase (JNK) |
EP2797879B1 (en) * | 2011-12-27 | 2018-12-26 | Bio-Pharm Solutions Co., Ltd. | Phenyl carbamate compounds for use in alleviating or treating pain and neuropathic pain |
WO2014063068A1 (en) | 2012-10-18 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
EP3057956B1 (en) | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
AU2014337122B2 (en) | 2013-10-18 | 2019-01-03 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
CN103739550B (zh) * | 2014-01-02 | 2016-06-01 | 中国药科大学 | 2,3-二甲基-6-脲-2h-吲唑类化合物及其制备方法与应用 |
CA2937111A1 (en) * | 2014-01-24 | 2015-07-30 | Abbvie Inc. | 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use |
TWI672141B (zh) | 2014-02-20 | 2019-09-21 | 美商醫科泰生技 | 投予ros1突變癌細胞之分子 |
US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
WO2015164614A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
KR101731624B1 (ko) * | 2014-07-01 | 2017-05-04 | 광주과학기술원 | 세포 리프로그래밍 유도용 조성물 |
PE20170774A1 (es) * | 2014-08-19 | 2017-07-04 | Shanghai Haihe Pharmaceutical Co Ltd | Compuestos de indazol como inhibidores de cinasa fgfr, preparacion y uso de los mismos |
CN107207471B (zh) | 2014-12-02 | 2020-06-26 | 伊尼塔公司 | 用于治疗神经母细胞瘤的组合 |
EP3233840B1 (en) | 2014-12-16 | 2018-11-21 | Eudendron S.r.l. | Heterocyclic derivatives modulating activity of certain protein kinases |
US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
WO2016160617A2 (en) | 2015-03-27 | 2016-10-06 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
CN106279119B (zh) * | 2015-05-27 | 2020-06-16 | 上海海和药物研究开发有限公司 | 一种新型激酶抑制剂的制备及其应用 |
CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
GB201511382D0 (en) | 2015-06-29 | 2015-08-12 | Imp Innovations Ltd | Novel compounds and their use in therapy |
US11142507B2 (en) | 2015-09-09 | 2021-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2017068064A1 (en) * | 2015-10-22 | 2017-04-27 | Selvita S.A. | Pyridone derivatives and their use as kinase inhibitors |
CN105467027B (zh) * | 2015-11-18 | 2021-09-21 | 北京万全德众医药生物技术有限公司 | 一种用气相色谱法分离测定米诺膦酸中间体有关物质的方法 |
WO2017106492A1 (en) | 2015-12-18 | 2017-06-22 | Ignyta, Inc. | Combinations for the treatment of cancer |
CA3069339A1 (en) | 2017-07-19 | 2019-01-24 | Ignyta, Inc. | Pharmaceutical compositions comprising entrectinib |
PE20201028A1 (es) | 2017-08-01 | 2020-10-05 | Theravance Biopharma Randd Ip Llc | Compuestos biciclicos de pirazol y triazolo como inhibidores de las cinasas jak |
JP7311498B2 (ja) | 2017-10-17 | 2023-07-19 | イグナイタ インコーポレイテッド | 薬学的組成物および剤形 |
CN110117278B (zh) * | 2018-02-07 | 2022-07-19 | 石家庄以岭药业股份有限公司 | 烷氧基苯并五元(六元)杂环胺类化合物及其药物用途 |
WO2020086503A1 (en) * | 2018-10-24 | 2020-04-30 | Bristol-Myers Squibb Company | Substituted indole and indazole compounds |
EP3870589B1 (en) | 2018-10-24 | 2023-09-06 | Bristol-Myers Squibb Company | Substituted indole dimer compounds |
EP3914348A1 (en) | 2019-01-23 | 2021-12-01 | Theravance Biopharma R&D IP, LLC | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
CN115003666A (zh) * | 2019-12-04 | 2022-09-02 | 先正达农作物保护股份公司 | 杀有害生物活性的稠合二环杂芳香族氨基化合物 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3133081A (en) * | 1964-05-12 | J-aminoindazole derivatives | ||
US2971842A (en) * | 1956-03-21 | 1961-02-14 | Gen Aniline & Film Corp | Light sensitive layers for photomechanical reproduction |
GB965511A (en) * | 1961-11-30 | 1964-07-29 | Smith Kline French Lab | Improvements in or relating to 3-aminoindazole derivatives |
DE1280878B (de) * | 1961-11-30 | 1968-10-24 | Smith Kline French Lab | 3-Aminoindazole |
BE626284A (es) * | 1962-04-28 | |||
US3720671A (en) * | 1970-10-05 | 1973-03-13 | Ciba Geigy Ag | Polycyclic dyestuffs |
FR2111641A2 (en) * | 1970-10-09 | 1972-06-09 | Geigy Ag J R | Polycyclic cpds as dispersion dyestuffs for - hydrophobic organic fibres |
DE2458965C3 (de) * | 1974-12-13 | 1979-10-11 | Bayer Ag, 5090 Leverkusen | 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel |
JPS51143010A (en) * | 1975-06-04 | 1976-12-09 | Kao Corp | Stable bleaching detergent composition |
SU742430A1 (ru) * | 1978-11-09 | 1980-06-25 | Предприятие П/Я А-7850 | Способ получени 3-амино-5-нитроиндазола |
JPS58159473A (ja) * | 1982-03-17 | 1983-09-21 | Asahi Chem Ind Co Ltd | ベンゼン環置換基を有する新規な1位置換インダゾ−ル誘導体およびその製造法 |
EP0090972B1 (en) * | 1982-03-17 | 1990-05-30 | Asahi Kasei Kogyo Kabushiki Kaisha | Indazole derivatives |
KR940021073A (ko) * | 1993-03-02 | 1994-10-17 | 미야베 요시가즈 | 알쯔하이머병의 예방 또는 치료제, 그 스크리닝 방법 및 인간 유래의 타우 단백질 키나아제 i |
KR100423899B1 (ko) * | 2000-05-10 | 2004-03-24 | 주식회사 엘지생명과학 | 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸 |
-
2002
- 2002-03-11 FR FR0202997A patent/FR2836915B1/fr not_active Expired - Fee Related
-
2003
- 2003-02-28 PA PA20038568301A patent/PA8568301A1/es unknown
- 2003-03-03 SV SV2003001494A patent/SV2003001494A/es not_active Application Discontinuation
- 2003-03-06 TW TW092104839A patent/TWI329103B/zh not_active IP Right Cessation
- 2003-03-06 JO JO200323A patent/JO2326B1/en active
- 2003-03-07 ME MEP-161/08A patent/MEP16108A/xx unknown
- 2003-03-07 RU RU2004129780/04A patent/RU2345070C2/ru not_active IP Right Cessation
- 2003-03-07 PL PL03370478A patent/PL370478A1/xx unknown
- 2003-03-07 JP JP2003576409A patent/JP4648630B2/ja not_active Expired - Fee Related
- 2003-03-07 KR KR1020047014199A patent/KR101068770B1/ko not_active IP Right Cessation
- 2003-03-07 IL IL16383103A patent/IL163831A0/xx unknown
- 2003-03-07 CN CNA038053667A patent/CN1656078A/zh active Pending
- 2003-03-07 PE PE2003000234A patent/PE20040155A1/es not_active Application Discontinuation
- 2003-03-07 WO PCT/FR2003/000752 patent/WO2003078403A2/fr active Application Filing
- 2003-03-07 AU AU2003242809A patent/AU2003242809B8/en not_active Ceased
- 2003-03-07 MX MXPA04007478A patent/MXPA04007478A/es active IP Right Grant
- 2003-03-07 EP EP03744396.7A patent/EP1487804B1/fr not_active Expired - Lifetime
- 2003-03-07 BR BR0308373-0A patent/BR0308373A/pt not_active IP Right Cessation
- 2003-03-07 CN CN2010102771547A patent/CN101962365A/zh active Pending
- 2003-03-07 CA CA2478542A patent/CA2478542C/fr not_active Expired - Fee Related
- 2003-03-07 RS YU79504A patent/RS52396B/en unknown
- 2003-03-07 NZ NZ535147A patent/NZ535147A/en not_active IP Right Cessation
- 2003-03-07 ME MEP-2008-161A patent/ME00058B/me unknown
- 2003-03-10 AR ARP030100808A patent/AR038915A1/es unknown
- 2003-03-11 US US10/385,871 patent/US6949579B2/en not_active Expired - Lifetime
- 2003-03-11 UY UY27713A patent/UY27713A1/es unknown
- 2003-03-11 GT GT200300057A patent/GT200300057A/es unknown
- 2003-03-11 MY MYPI20030839A patent/MY138269A/en unknown
-
2004
- 2004-08-05 MA MA27814A patent/MA27230A1/fr unknown
- 2004-08-23 ZA ZA2004/06687A patent/ZA200406687B/en unknown
- 2004-08-31 IL IL163831A patent/IL163831A/en not_active IP Right Cessation
- 2004-09-10 HR HRP20040824AA patent/HRP20040824B1/hr not_active IP Right Cessation
- 2004-09-29 NO NO20044137A patent/NO329384B1/no not_active IP Right Cessation
-
2010
- 2010-04-06 JP JP2010087830A patent/JP5315287B2/ja not_active Expired - Fee Related
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR038915A1 (es) | Derivados de aminoindazoles, procedimiento de preparacion e intermedios de este procedimiento, medicamentos y composiciones farmaceuticas que contienen al compuesto | |
NZ610312A (en) | 6-amino-2-phenylamino-1h-benzimidazole-5-carboxamide- derivatives and their use as microsomal prostaglandin e2 synthase-1 inhibitors | |
HUP0402376A2 (hu) | Imidazol-4-karboxamid-származékok, előállításuk és az ezeket tartalmazó, elhízás kezelésére alkalmas gyógyszerkészítmények | |
AR045389A1 (es) | Inhibidores del c-kit con estructura de pirazolil-amidil-benzoimidazolilo n-sustituido | |
AR058546A1 (es) | Derivados de 2- adamantilurea como inhibidores selectivos de 11 beta - hsd1 | |
AR079541A1 (es) | Compuestos sustituidos de n-(1h-indazol-4-il) imidazo (1,2-a) piridin-3-carboxamida como inhibidores de cfms | |
RS28004A (en) | Azabicycle-substituted fused- heteroaryl compounds for the treatment of disease | |
CY1112326T1 (el) | Παραγωγα της 6-(πυριδινυλ)-4-πυριμιδονης ως αναστολεις της κινασης 1 tau πρωτεϊνης | |
TW200716531A (en) | Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia | |
MY134666A (en) | Pyridinoylpiperidines as 5-ht1f agonists | |
PE20091974A1 (es) | Derivados de indazoles sustituidos con fenil o piridinilo | |
ATE545413T1 (de) | Antagonisten des opioidrezeptors | |
SE0104332D0 (sv) | Therapeutic agents | |
PE20071132A1 (es) | Compuestos macrociclicos como inhibidores del factor viia | |
MX2010001080A (es) | Pirrolidin-aril-eteres como antagonistas de receptor de nk3. | |
AR034203A1 (es) | Derivados de 1-aril- o 1-alquilsulfonilbenzazol como ligandos de 5-hidroxitriptamina-6, un metodo para su preparacion, composicion farmaceutica y el uso de los mismos para la fabricacion de un medicamento | |
ATE540037T1 (de) | Triazolopyridine als phosphodiesterasehemmer zur behandlung von hautkrankheiten | |
ECSP066415A (es) | 2-carbonilamino-6-piperidinaminopiridinas sustituidas y 1-carbonilamino-3-piperidinaminobenzenos sustituidos como 5-ht1f agonistas | |
AR068116A1 (es) | Compuestos 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu, proceso de preparacion de los mismos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de disfunciones intestinales inducidas por opioides o ileo posquirurgico. | |
PE20081169A1 (es) | Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp | |
HUP0302770A2 (hu) | Tripeptidil peptidáz inhibitorok, eljárás az előállítására és ezeket tartalmazó gyógyszerkészítmények | |
TW200500343A (en) | Caspase inhibitors and uses thereof | |
NO20025640D0 (no) | Substituerte 1-aminoalkyl-laktamer og deres anvendelse som muscarin-reseptor-antagonister | |
AR074128A1 (es) | Derivados de 4-[2-(2-fluorofenoximetil)fenil] piperidina, composiciones farmaceuticas que los contienen, metodo de preparacion, compuestos intermediarios de dicho proceso y uso de los mismos para el tratamiento de dolores neuropaticos, mal de alzheimer y otras enfermedades relacionadas con el snc. | |
AR062941A1 (es) | Compuestos para el tratamiento de desordenes metabolicos |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |