AR102722A2 - Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kit - Google Patents
Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kitInfo
- Publication number
- AR102722A2 AR102722A2 ARP150103780A ARP150103780A AR102722A2 AR 102722 A2 AR102722 A2 AR 102722A2 AR P150103780 A ARP150103780 A AR P150103780A AR P150103780 A ARP150103780 A AR P150103780A AR 102722 A2 AR102722 A2 AR 102722A2
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- cycloalkyl
- alkyl
- group selected
- heterocyclylalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/28—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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
-
- 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
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—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—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- AIDS & HIV (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Se revelan derivados de pirazolo-quinazolina de fórmula (1) ó (2) como se definen en la memoria y sales farmacéuticamente aceptables de los mismos, un procedimiento para su preparación y composiciones farmacéuticas que los comprenden; estos compuestos pueden ser útiles, en terapéutica, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como cáncer. Reivindicación 1: Un derivado de pirazolo-quinazolina representado por la fórmula (1) ó (2), caracterizado porque: R es hidrógeno o un grupo opcionalmente sustituido seleccionado entre amino, alquilo C₁₋₆ lineal o ramificado, cicloalquilo C₃₋₁₀, arilo, arilalquilo, heterociclilo o heterociclilalquilo; X es un enlace simple o un radical divalente seleccionado entre -NR-, -CONR-, -NH-CO-NH-, -O-, -S- o -SO₂, en donde R es hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C₁₋₆ lineal o ramificado, cicloalquilo C₃₋₆ arilo, arilalquilo, heterociclilo, heterociclilalquilo o, junto con el átomo de nitrógeno al cual están unidos, R y R pueden formar un grupo heteroarilo o heterociclilo de 5 a 6 miembros, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, O ó S; R¹ ligado a uno cualquiera de los átomos de nitrógeno del anillo pirazol según la fórmula (1) ó (2), representa un átomo de hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C₁₋₆ lineal o ramificado, cicloalquilo C₃₋₆, arilo, arilalquilo, heterociclilo o heterociclilalquilo o, en la fórmula (2), R¹ es un grupo -(CH₂)ₙ-NH- divalente que está ligado a R², en donde n es 2 ó 3; R² es un grupo seleccionado entre -NRR, -N(OH)R, -OR o -R, en donde R y R son, cada uno independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C₁₋₆ lineal o ramificado, cicloalquilo C₃₋₆, o cicloalquilo-alquilo, arilo, arilalquilo, heterociclilo o heterociclilalquilo o, junto con el átomo de nitrógeno al cual están unidos, R y R pueden formar un grupo heteroarilo o heterociclilo de 5 a 6 miembros, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, O ó S; A es un grupo divalente seleccionado entre -CH₂-, -(CH₂)₂-, -CH₂-C(CH₃)₂-, -C(CH₃)₂-CH₂- o -CH=CH-; o una sal farmacéuticamente aceptable de los mismos. Reivindicación 26: Un compuesto de fórmula (3) ó (4), como se definió en el paso (p.3) de la reivindicación 24 en donde R¹ es un átomo de hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C₁₋₆ lineal o ramificado, cicloalquilo C₃₋₆, arilo, arilalquilo, heterociclilo o heterociclilalquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47266103P | 2003-05-22 | 2003-05-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102722A2 true AR102722A2 (es) | 2017-03-22 |
Family
ID=33476970
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101748A AR044543A1 (es) | 2003-05-22 | 2004-05-20 | Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa |
| ARP150103780A AR102722A2 (es) | 2003-05-22 | 2015-11-20 | Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kit |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101748A AR044543A1 (es) | 2003-05-22 | 2004-05-20 | Derivados de pirazolo-quinazolina, un procedimiento para su preparacion y su uso como inhibidor de quinasa |
Country Status (36)
| Country | Link |
|---|---|
| US (9) | US7482354B2 (es) |
| EP (1) | EP1636236B1 (es) |
| JP (1) | JP5043432B2 (es) |
| KR (1) | KR101084871B1 (es) |
| CN (2) | CN102079746A (es) |
| AP (1) | AP2064A (es) |
| AR (2) | AR044543A1 (es) |
| AU (1) | AU2004240772B2 (es) |
| BR (2) | BRPI0410563B8 (es) |
| CA (1) | CA2526578C (es) |
| CO (1) | CO5721006A2 (es) |
| CR (1) | CR8102A (es) |
| CY (1) | CY1114708T1 (es) |
| DK (1) | DK1636236T3 (es) |
| EA (1) | EA010904B1 (es) |
| EC (1) | ECSP056194A (es) |
| ES (1) | ES2436524T3 (es) |
| GE (1) | GEP20094664B (es) |
| HR (1) | HRP20050967B8 (es) |
| IL (1) | IL172046A (es) |
| IS (1) | IS2939B (es) |
| ME (1) | ME00142B (es) |
| MX (1) | MXPA05012573A (es) |
| MY (1) | MY142019A (es) |
| NO (1) | NO334992B1 (es) |
| NZ (1) | NZ543661A (es) |
| OA (1) | OA13170A (es) |
| PL (1) | PL1636236T3 (es) |
| PT (1) | PT1636236E (es) |
| RS (2) | RS52899B (es) |
| SI (1) | SI1636236T1 (es) |
| TN (1) | TNSN05298A1 (es) |
| TW (1) | TWI349672B (es) |
| UA (1) | UA80763C2 (es) |
| WO (1) | WO2004104007A1 (es) |
| ZA (1) | ZA200509486B (es) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0410563B8 (pt) * | 2003-05-22 | 2021-05-25 | Nerviano Medical Sciences Srl | compostos de pirazol-quinazolina, seus processos de preparação e composições farmacêuticas |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| US7572914B2 (en) | 2003-12-19 | 2009-08-11 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| US7772232B2 (en) | 2004-04-15 | 2010-08-10 | Bristol-Myers Squibb Company | Quinazolinyl compounds as inhibitors of potassium channel function |
| ITMI20041033A1 (it) * | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Composti farmaceutici |
| US7550598B2 (en) | 2004-08-18 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| EP1812439B2 (en) | 2004-10-15 | 2017-12-06 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| US8084027B2 (en) * | 2006-02-10 | 2011-12-27 | Nerviano Medical Sciences S.R.L. | Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic |
| MX2008014292A (es) * | 2006-05-09 | 2008-11-18 | Novartis Ag | Combinacion que comprende un quelante de hierro y un agente anti-neoplastico, y uso de la misma. |
| WO2007149395A2 (en) * | 2006-06-20 | 2007-12-27 | Amphora Discovery Corporation | 2,5-substituted oxazole derivatives as protein kinase inhibitors for the treatment of cancer |
| US7517882B2 (en) * | 2006-09-18 | 2009-04-14 | Polaris Group | Protein kinase inhibitors |
| BRPI0719883A2 (pt) | 2006-10-09 | 2015-05-05 | Takeda Pharmaceutical | Inibidores de quinase |
| PT2125822E (pt) * | 2006-12-21 | 2015-01-30 | Nerviano Medical Sciences Srl | Derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase |
| ZA200904912B (en) * | 2006-12-21 | 2010-09-29 | Nerviano Medical Sciences Srl | Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors |
| EP2213673B1 (en) | 2007-10-23 | 2013-06-05 | Msd K.K. | Pyridone-substituted-dihydropyrazolopyrimidinone derivative |
| KR20100095020A (ko) * | 2007-12-19 | 2010-08-27 | 암젠 인크 | 세포 주기 억제제로서의 융합된 피리딘, 피리미딘 및 트리아진 화합물 |
| AU2009233951B2 (en) * | 2008-04-07 | 2014-02-27 | Amgen Inc. | Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors |
| TWI426074B (zh) * | 2008-04-30 | 2014-02-11 | Nerviano Medical Sciences Srl | ５－（２－胺基－嘧啶－４－基）－２－芳基－１ｈ－吡咯－３－羧醯胺之製造方法 |
| US8846701B2 (en) * | 2008-06-26 | 2014-09-30 | Nerviano Medical Sciences S.R.L. | Pyrazolo-quinazolines |
| CN102105151B (zh) * | 2008-07-29 | 2013-12-18 | 内尔维阿诺医学科学有限公司 | Cdk抑制剂在治疗神经胶质瘤中的应用 |
| CN102105152B (zh) * | 2008-07-29 | 2012-10-17 | 内尔维阿诺医学科学有限公司 | 包含cdks抑制剂和抗肿瘤剂的治疗组合 |
| US8653097B2 (en) * | 2008-10-17 | 2014-02-18 | Boehringer Ingelheim International Gmbh | Tetra-aza-heterocycles as phosphatidylinositol-3-kinases (P13-kinases) inhibitor |
| WO2010058006A1 (en) | 2008-11-24 | 2010-05-27 | Nerviano Medical Sciences S.R.L. | Cdk inhibitor for the treatment of mesothelioma |
| IT1395724B1 (it) * | 2009-02-25 | 2012-10-19 | Neuroscienze Pharmaness S C A R L | Composti farmaceutici |
| ES2445896T3 (es) * | 2009-03-20 | 2014-03-05 | Nerviano Medical Sciences S.R.L. | Uso de un inhibidor de quinasa para el tratamiento del timoma |
| EP2421872B1 (en) | 2009-04-22 | 2015-06-10 | Boehringer Ingelheim International GmbH | Thia-triaza-as-indacenes as pi3-kinases inhibitors for the treatment of cancer |
| US8586598B2 (en) | 2009-04-29 | 2013-11-19 | Nerviano Medical Sciences S.R.L. | CDK inhibitor salts |
| AR076784A1 (es) | 2009-05-26 | 2011-07-06 | Nerviano Medical Sciences Srl | Combinacion terapeutica que comprende un inhibidor de plk1 y un agente antineoplasico |
| ES2553114T3 (es) * | 2009-07-29 | 2015-12-04 | Nerviano Medical Sciences S.R.L. | Sales de inhibidor de plk |
| AU2011210765A1 (en) | 2010-01-28 | 2012-09-13 | President And Fellows Of Harvard College | Compositions and methods for enhancing proteasome activity |
| US8735386B2 (en) * | 2010-07-23 | 2014-05-27 | Boehringer Ingelheim International Gmbh | Aminopyrazoloquinazolines |
| WO2012013557A1 (en) | 2010-07-30 | 2012-02-02 | Nerviano Medical Sciences S.R.L. | Isoxazolo-quinazolines as modulators of protein kinase activity |
| EP2619181A1 (en) | 2010-09-23 | 2013-07-31 | Syngenta Participations AG | Novel microbiocides |
| HUE030714T2 (en) * | 2010-10-25 | 2017-05-29 | G1 Therapeutics Inc | Cdk inhibitors |
| MX342873B (es) * | 2010-12-17 | 2016-10-17 | Nerviano Medical Sciences S R L * | Derivados de pirazolo-quinazolina sustituidos como inhibidores de cinasa. |
| JP5925809B2 (ja) * | 2011-01-26 | 2016-05-25 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 三環系ピロロ誘導体、その調製方法およびそのキナーゼ阻害剤としての使用 |
| JP5925808B2 (ja) * | 2011-01-26 | 2016-05-25 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用 |
| WO2012117021A2 (en) | 2011-03-03 | 2012-09-07 | Syngenta Participations Ag | Novel microbiocidal oxime ethers |
| MY161199A (en) | 2011-03-23 | 2017-04-14 | Amgen Inc | Fused tricyclic dual inhibitors of cdk 4/6 and flt3 |
| US9556166B2 (en) | 2011-05-12 | 2017-01-31 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
| WO2013092460A1 (en) | 2011-12-20 | 2013-06-27 | Syngenta Participations Ag | Cyclic bisoxime microbicides |
| EP2807166B1 (en) | 2012-01-23 | 2016-04-06 | Boehringer Ingelheim International GmbH | 5,8-dihydro-6h-pyrazolo[3,4-h]quinazolines as igf-1r/ir inhibitors |
| EP2641901A1 (en) | 2012-03-22 | 2013-09-25 | Syngenta Participations AG. | Novel microbiocides |
| CN104870446B (zh) | 2012-11-07 | 2019-08-13 | 内尔维阿诺医学科学有限公司 | 取代的嘧啶基和吡啶基吡咯并吡啶酮类、其制备方法及其作为激酶抑制剂的用途 |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| SI2968290T1 (sl) | 2013-03-15 | 2020-02-28 | G1 Therapeutics, Inc., | Prehodna zaščita normalnih celic med kemoterapijo |
| EP2967050A4 (en) | 2013-03-15 | 2016-09-28 | G1 Therapeutics Inc | HIGH-ACTIVE ANTINEOPLASTIC AND ANTIPROLIFERATIVE AGENTS |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| HUE043108T2 (hu) | 2014-04-07 | 2019-07-29 | Netherlands Translational Res Center B V | (5,6-dihidro)pirimido[4,5-e]indolizinek |
| US9717735B2 (en) | 2014-04-17 | 2017-08-01 | G1 Therapeutics, Inc. | Tricyclic lactams for use in HSPC-sparing treatments for RB-positive abnormal cellular proliferation |
| DK3148532T3 (en) | 2014-05-28 | 2021-04-26 | Piramal Entpr Ltd | Pharmaceutical Combination Comprising a CDK Inhibitor and a Thioredoxin Reductase Inhibitor for the Treatment of Cancer |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| CA2992161A1 (en) | 2015-07-17 | 2017-01-26 | Institut Pasteur | 5-hydroxytryptamine 1b receptor-stimulating agent for use as a promoter of satellite cells self-renewal and/or differentiation |
| BR112019000706A8 (pt) | 2016-07-15 | 2022-12-06 | Pasteur Institut | Agente de estímulo do receptor 1b de 5-hidroxitriptamina para reparo de pele e/ou cabelo |
| CN113264935B (zh) * | 2016-11-11 | 2022-09-20 | 上海海雁医药科技有限公司 | 吡啶胺取代的杂三环化合物及其中间体和医药上的用途 |
| CN110997678B (zh) * | 2017-07-11 | 2023-02-21 | 内尔维亚诺医疗科学公司 | 作为胆碱激酶抑制剂的吡唑并喹唑啉衍生物 |
| CN107383019B (zh) * | 2017-07-28 | 2019-10-15 | 江苏艾凡生物医药有限公司 | 吡唑并[4,3-h]喹唑啉类化合物及其用途 |
| ES2923415T3 (es) | 2017-08-11 | 2022-09-27 | Shengke Pharmaceuticals Jiangsu Ltd | Compuesto de 1H-pirazolo[4,3-H]quinazolina que sirve como inhibidor de proteína quinasa |
| JP7581244B2 (ja) * | 2019-06-06 | 2024-11-12 | アーカス バイオサイエンシズ インコーポレイティド | アミノピリミジン化合物の調製方法 |
| US20220363690A1 (en) * | 2019-09-05 | 2022-11-17 | Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd. | Isoxazolo[5,4-h]quinazoline compounds as protein kinase inhibitors |
| WO2021084541A1 (en) * | 2019-10-31 | 2021-05-06 | Sol-Gel Technologies Ltd. | Treatment of hair loss disorders with a topical egfr inhibitor |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| CN116547280A (zh) * | 2020-10-08 | 2023-08-04 | 雷多纳治疗公司 | 用于治疗癌症的苯并[h]喹唑啉-4-胺和噻吩并[3,2-h]喹唑啉-4-胺衍生物 |
| US20230416271A1 (en) * | 2020-11-26 | 2023-12-28 | Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd. | Heteroarylquinazoline compounds as protein kinase inhibitors |
| CN114685520B (zh) * | 2020-12-25 | 2024-08-30 | 武汉誉祥医药科技有限公司 | 三并环化合物及其药物组合物和应用 |
| WO2022143576A1 (zh) * | 2020-12-31 | 2022-07-07 | 恒元生物医药科技(苏州)有限公司 | 一种吡唑并喹唑啉类化合物、其制备方法及应用 |
| CN116761806B (zh) * | 2021-02-08 | 2025-10-10 | 上海复星医药产业发展有限公司 | 5，6-二氢噻吩并[3，4-h]喹唑啉类化合物 |
| IL309569A (en) * | 2021-06-22 | 2024-02-01 | Taxis Pharmaceuticals Inc | Therapeutic compounds |
| CN113527310B (zh) * | 2021-07-30 | 2022-09-23 | 上海市肺科医院 | 用于减轻自身免疫性疾病患者不良炎性反应的小分子化合物及其应用 |
| EP4446325A4 (en) * | 2021-12-10 | 2025-04-16 | Shandong Luye Pharmaceutical Co., Ltd. | Protein kinase inhibitors, manufacturing processes therefor and use thereof |
| WO2024153110A1 (zh) * | 2023-01-17 | 2024-07-25 | 北京哲源科技有限责任公司 | 吡唑并喹唑啉类化合物的立体异构体和氘代衍生物及应用 |
| AU2024284206A1 (en) * | 2023-06-08 | 2025-12-11 | Shandong Luye Pharmaceutical Co., Ltd. | Salt form and crystal form of plk1 kinase inhibitor, and preparation method therefor and use thereof |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2119975A (en) * | 1936-08-26 | 1938-06-07 | Beatrice S Nazel | Fluid pressure hammer |
| JP3907220B2 (ja) * | 1994-06-30 | 2007-04-18 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 複素環含有化合物 |
| MX9709867A (es) | 1995-06-07 | 1998-03-31 | Pfizer | Derivados de pirimidina condensados con un anillo heterociclico, composiciones que contienen los mismos, y uso de los mismos. |
| EP0946523A1 (en) | 1996-12-23 | 1999-10-06 | Celltech Therapeutics Limited | Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors |
| GB9713087D0 (en) | 1997-06-20 | 1997-08-27 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9911053D0 (en) | 1999-05-12 | 1999-07-14 | Pharmacia & Upjohn Spa | 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| EA005373B1 (ru) | 1999-08-12 | 2005-02-24 | Фармация Италия С.П.А. | Производные 3(5)-аминопиразола, способ их получения и их применение в качестве противоопухолевых средств |
| BR0113176A (pt) | 2000-08-10 | 2003-06-17 | Pharmacia Italia Spa | Compostos biciclo-pirazol, composições farmacêuticas compreendendo os compostos, uso dos compostos na fabricação de medicamentos, processos para a preparação dos compostos, coleção quìmica combinatória e métodos para o tratamento de mamìferos incluindo humanos utilizando os compostos |
| ATE385498T1 (de) | 2000-08-11 | 2008-02-15 | Boehringer Ingelheim Pharma | Heterozyklische verbindungen als inhibitoren von tyrosin-kinasen |
| AU2002215053A1 (en) | 2000-11-27 | 2002-06-24 | Pharmacia Italia S.P.A. | Phenylacetamido- pyrazole derivatives and their use as antitumor agents |
| US20040116497A1 (en) | 2001-01-26 | 2004-06-17 | Gabriella Traquandi | Chromane derivatives, process for their preparation and their use as antitumor agents |
| US20030100594A1 (en) * | 2001-08-10 | 2003-05-29 | Pharmacia Corporation | Carbonic anhydrase inhibitor |
| JP2005501083A (ja) * | 2001-08-10 | 2005-01-13 | ファルマシア・コーポレーション | 炭酸脱水酵素阻害剤 |
| EA007430B1 (ru) | 2001-09-26 | 2006-10-27 | Фармация Италия С.П.А. | Производные аминоиндазола, активные в качестве ингибиторов киназ, способ их получения и содержащая их фармацевтическая композиция |
| EP1476431A1 (en) * | 2002-02-19 | 2004-11-17 | Pharmacia Corporation | Tricyclic pyrazole derivatives for the treatment of inflammation |
| BRPI0410563B8 (pt) | 2003-05-22 | 2021-05-25 | Nerviano Medical Sciences Srl | compostos de pirazol-quinazolina, seus processos de preparação e composições farmacêuticas |
| PT2125822E (pt) * | 2006-12-21 | 2015-01-30 | Nerviano Medical Sciences Srl | Derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase |
-
2004
- 2004-04-27 BR BRPI0410563A patent/BRPI0410563B8/pt not_active IP Right Cessation
- 2004-04-27 AU AU2004240772A patent/AU2004240772B2/en not_active Expired
- 2004-04-27 HR HRP20050967AA patent/HRP20050967B8/hr not_active IP Right Cessation
- 2004-04-27 PL PL04741483T patent/PL1636236T3/pl unknown
- 2004-04-27 DK DK04741483.4T patent/DK1636236T3/da active
- 2004-04-27 EA EA200501849A patent/EA010904B1/ru unknown
- 2004-04-27 UA UAA200512347A patent/UA80763C2/uk unknown
- 2004-04-27 SI SI200432118T patent/SI1636236T1/sl unknown
- 2004-04-27 RS RS20050944A patent/RS52899B/sr unknown
- 2004-04-27 BR BR122019010200A patent/BR122019010200B8/pt active IP Right Grant
- 2004-04-27 GE GEAP20049128A patent/GEP20094664B/en unknown
- 2004-04-27 NZ NZ543661A patent/NZ543661A/xx not_active IP Right Cessation
- 2004-04-27 EP EP04741483.4A patent/EP1636236B1/en not_active Expired - Lifetime
- 2004-04-27 ME MEP-2008-259A patent/ME00142B/me unknown
- 2004-04-27 US US10/557,565 patent/US7482354B2/en not_active Expired - Lifetime
- 2004-04-27 PT PT47414834T patent/PT1636236E/pt unknown
- 2004-04-27 JP JP2006530168A patent/JP5043432B2/ja not_active Expired - Lifetime
- 2004-04-27 WO PCT/EP2004/050612 patent/WO2004104007A1/en not_active Ceased
- 2004-04-27 KR KR1020057022355A patent/KR101084871B1/ko not_active Expired - Lifetime
- 2004-04-27 OA OA1200500329A patent/OA13170A/fr unknown
- 2004-04-27 AP AP2005003452A patent/AP2064A/xx active
- 2004-04-27 MX MXPA05012573A patent/MXPA05012573A/es active IP Right Grant
- 2004-04-27 CA CA2526578A patent/CA2526578C/en not_active Expired - Lifetime
- 2004-04-27 CN CN2010105863199A patent/CN102079746A/zh active Pending
- 2004-04-27 ES ES04741483.4T patent/ES2436524T3/es not_active Expired - Lifetime
- 2004-04-27 RS YUP-2005/0944A patent/RS20050944A/sr unknown
- 2004-04-27 CN CNA2004800210752A patent/CN1826343A/zh active Pending
- 2004-05-04 TW TW093112449A patent/TWI349672B/zh not_active IP Right Cessation
- 2004-05-13 MY MYPI20041795A patent/MY142019A/en unknown
- 2004-05-20 AR ARP040101748A patent/AR044543A1/es active IP Right Grant
-
2005
- 2005-11-18 IS IS8132A patent/IS2939B/is unknown
- 2005-11-20 IL IL172046A patent/IL172046A/en active IP Right Grant
- 2005-11-21 TN TNP2005000298A patent/TNSN05298A1/fr unknown
- 2005-11-21 NO NO20055496A patent/NO334992B1/no unknown
- 2005-11-22 CO CO05118410A patent/CO5721006A2/es active IP Right Grant
- 2005-11-22 CR CR8102A patent/CR8102A/es unknown
- 2005-11-23 ZA ZA200509486A patent/ZA200509486B/xx unknown
- 2005-11-30 EC EC2005006194A patent/ECSP056194A/es unknown
-
2008
- 2008-10-31 US US12/262,933 patent/US8541429B2/en not_active Expired - Lifetime
-
2013
- 2013-08-21 US US13/972,659 patent/US8981089B2/en not_active Expired - Lifetime
- 2013-12-09 CY CY20131101108T patent/CY1114708T1/el unknown
-
2015
- 2015-02-18 US US14/625,093 patent/US9464090B2/en not_active Expired - Lifetime
- 2015-11-20 AR ARP150103780A patent/AR102722A2/es unknown
-
2016
- 2016-09-06 US US15/256,916 patent/US9637497B2/en not_active Expired - Fee Related
-
2017
- 2017-03-23 US US15/467,323 patent/US10280176B2/en not_active Expired - Lifetime
-
2019
- 2019-03-04 US US16/291,323 patent/US20190194214A1/en not_active Abandoned
-
2020
- 2020-10-30 US US17/084,862 patent/US20210300935A1/en not_active Abandoned
-
2023
- 2023-12-22 US US18/394,122 patent/US20250011333A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR102722A2 (es) | Un derivado de pirazolo-quinazolina, su uso, un procedimiento para prepararlos, composiciones farmacéuticas que los comprenden, compuestos utilizables en su preparación, una biblioteca de dos o más compuestos, y un producto o kit | |
| BR0010520A (pt) | Novos compostos farmaceuticamente ativos | |
| JOP20220069A1 (ar) | عوامل محللة لـ brd9 ثنائية الوظيفة وطرق لاستخدامها | |
| YU40394A (sh) | Fenil heterociklična jedinjenja kao cox-2 inhibitori - | |
| BR0014137A (pt) | Composto, método para inibir a aurora 2 quinase em um animal de sangue quente, uso de um composto, e, composição farmacêutica | |
| PH12021551256A1 (en) | Pantetheine derivatives and uses thereof | |
| BR0307409A (pt) | Compostos de hidrazida de ácido 2-furanocarboxìlico, composições farmacêuticas contendo os mesmos e uso dos mesmos para preparação de um agente preventivo ou terapêutico | |
| ATE307810T1 (de) | Imidazol-2-carbonsäureamid derivate als raf- kinase-inhibitoren | |
| AR034270A1 (es) | 1-aril- o 1-alquilsulfonil-heterociclilbenzazoles como ligandos de 5-hidroxitriptamina-6, un metodo para su preparacion, una composicion farmaceutica y el uso de los mismos para la manufactura de un medicamento | |
| BR0311806A (pt) | Derivados heteroaril benzocondensado-amida de tienopiridinas úteis como agentes terapêuticos, composições farmacêuticas que os incluem e métodos para o seu uso | |
| ATE517882T1 (de) | Chinolinderivate | |
| BR0014116A (pt) | Uso de um composto, composto, métodos para preparação de um composto, e para inibir aurora 2 quinase em um animal de sangue quente, e, composição farmacêutica | |
| EA200501332A1 (ru) | Производные пиримидин-4-она и их применение в качестве модуляторов киназы p38 | |
| NO20062905L (no) | Nye hydroksaminsyreestere og farmasoytisk anvendelse derav | |
| NO20076425L (no) | Fremgangsmater for behandling av drug-resistent cancer | |
| BR0311535A (pt) | Uso de cianopirrolidinas substituìdas e preparações de combinações contendo as mesmas para o tratamento da hiperlipidemia e doenças associadas | |
| EA201992090A1 (ru) | ДЕЙТЕРИРОВАННЫЕ СОЕДИНЕНИЯ ИМИДАЗО[4,5-c]ХИНОЛИН-2-ОНА И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ РАКА | |
| DK0521768T3 (da) | Nye triazolopyrimidin-derivater som er angiotensin II-receptor-antagonister, fremgangsmåder til deres fremstilling og farmaceutiske præparater med indhold deraf | |
| SG145570A1 (en) | 4-æ7-halo-2-quino(xa-)linyloxy!phenoxy-propionic acid derivatives as antineoplastic agents | |
| UY28688A1 (es) | Derivados de amida | |
| EA200400896A1 (ru) | Терапевтические акридоновые и акридиновые соединения | |
| DK1723138T3 (da) | Substituerede benzimidazoler og deres anvendelse til at inducere apoptose | |
| EA200400219A1 (ru) | Производные хинолина и их использование в качестве противоопухолевых средств | |
| AR119143A1 (es) | Compuesto de 1h-pirrolo[3,2-b]piridin-5-ilo, composición farmacéutica que lo comprende y su uso para fabricar un medicamento | |
| CO2025004701A2 (es) | Métodos de tratamiento del cáncer usando derivados de isoquinolina o 6-aza-quinolina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |