AR042525A1 - Derivados de pirrolo-pirazoles sustituidos como inhibidores de quinasa - Google Patents
Derivados de pirrolo-pirazoles sustituidos como inhibidores de quinasaInfo
- Publication number
- AR042525A1 AR042525A1 ARP030104702A ARP030104702A AR042525A1 AR 042525 A1 AR042525 A1 AR 042525A1 AR P030104702 A ARP030104702 A AR P030104702A AR P030104702 A ARP030104702 A AR P030104702A AR 042525 A1 AR042525 A1 AR 042525A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- formula
- alkyl
- cycloalkyl
- atom
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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]
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Radiology & Medical Imaging (AREA)
- Pathology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se revelan compuestos representados por las fórmula (1a) o (1b) y en donde R y R1 son como se definieron en la descripción, y sales farmacéuticamente aceptables de los mismo; dichos compuestos son útiles en el tratamiento de trastornos proliferativos del ciclo celular, por ej.,cáncer, asociados con una actividad alterada de la quinasa dependiente del ciclo celular. Reivindicación 11: Un compuesto representado por la fórmula (1a) o (1b); caracterizado porque: R es un grupo -CORa, -CONHRa o -CONRaRb, en donde Ra y Rb son, cada uno independientemente, H o un grupo opcionalmente sustituido seleccionado entre heterociclilalquilo, heterociclilo, arilalquilo, arilo, cicloalquilo C3-6 o alquilo C1-6 lineal o ramificado, o junto con el átomo de N al cual están unidos, Ra y Rb pueden formar un heterociclo de 5 o 6 miembros opcionalmente sustituido que contiene opcionalmente un heteroátomo o un grupo heteroatómico adicional seleccionado entre N, NH, O o S; R1 es seleccionado entre el grupo que consiste en: a) alquilo C3-4 lineal o ramificado; b) cicloalquilo, cicloalquilo-alquilo o alquilo-cicloalquilo, en donde la parte cicloalquilo comprende cualquier grupo cicloalquilo C3-6 y en donde la parte alquilo comprende cualquier grupo alquilo C1-4 lineal o ramificado; c) 3-metiltienil-2-ilo; 2-tienilo; fenilo; 2,6-difluorofenilo, 4-(aminosulfonil)-fenilo; 4-(dimetilaminometil)fenilo; 4-(4-metilpiperazinil)metilfenilo; d) un grupo de la fórmula (2a) o (2b), en donde, en la fórmula (2a), el ciclo representa un anillo heterocíclico de 5 a 7 miembros, en donde X, ligado directamente al resto de la molécula, representa un átomo de N o C; Y es un átomo de C, N, O o S o es un grupo NH, con la condición de que por lo menos uno de X e Y es distinto que un átomo de C; Rc es, independientemente uno de otro, y en una cualquiera de las posiciones libres del anillo heterocíclico de fórmula (2a), un átomo de halógeno o un grupo hidroxi o es un grupo opcionalmente sustituido seleccionado entre arilcarbonilo, alquilcarbonilo, alcoxicarbonilo, oxo (=O), carboxi, aminocarbonilo, amino, heterociclilalquilo, heterociclilo, arilalquilo, arilo,. Cicloalquilo C3-6 o alquilo C1-6 lineal o ramificado; y n es 0 o un número entero de 1 a 4; e) un grupo de fórmula (2c) o (2d) en donde Rd, R´d y Re representan, iguales o diferentes e independientemente uno de otro, un átomo de H o un alquilo C1-6 lineal o ramificado opcionalmente sustituido por uno o más grupos seleccionados entre hidroxi (-OH), aminocarbonilo (-CONH2) o metilaminocarbonilo (-CONHCH3), con la condición de que la fórmula (1a), cuando R1 es un grupo de fórmula (2c) y uno de Rd o R´d es un átomo de H mientras el otro de Rd o R´d es etilo o n-butilo, entonces R es distinto de -CORa con Ra como 3-bromofenilo, bencilo, 4-tert-butilfenilo, 4-tert-butilfenilmetilo, 4-fluorofenilmetilo, ciclopropilo o 2-naftilmetilo; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43495202P | 2002-12-19 | 2002-12-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR042525A1 true AR042525A1 (es) | 2005-06-22 |
Family
ID=32682128
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030104702A AR042525A1 (es) | 2002-12-19 | 2003-12-18 | Derivados de pirrolo-pirazoles sustituidos como inhibidores de quinasa |
Country Status (33)
| Country | Link |
|---|---|
| US (5) | US7407971B2 (es) |
| EP (2) | EP2266987B1 (es) |
| JP (2) | JP4739761B2 (es) |
| KR (2) | KR101223826B1 (es) |
| CN (1) | CN1726217B (es) |
| AP (1) | AP2005003343A0 (es) |
| AR (1) | AR042525A1 (es) |
| AU (1) | AU2003300255B9 (es) |
| BR (1) | BR0317455A (es) |
| CA (1) | CA2508069C (es) |
| CR (2) | CR7880A (es) |
| CU (1) | CU23550B7 (es) |
| EA (1) | EA010596B1 (es) |
| EC (1) | ECSP055864A (es) |
| ES (2) | ES2605848T3 (es) |
| GE (1) | GEP20084435B (es) |
| HR (1) | HRP20050562A2 (es) |
| IL (2) | IL169019A (es) |
| IS (1) | IS7857A (es) |
| MA (1) | MA27569A1 (es) |
| ME (1) | MEP52408A (es) |
| MX (1) | MXPA05006791A (es) |
| MY (1) | MY141196A (es) |
| NO (1) | NO333178B1 (es) |
| NZ (1) | NZ540644A (es) |
| OA (1) | OA13015A (es) |
| PL (1) | PL377285A1 (es) |
| RS (1) | RS20050462A (es) |
| TN (1) | TNSN05163A1 (es) |
| TW (1) | TWI327470B (es) |
| UA (1) | UA81790C2 (es) |
| WO (1) | WO2004056827A2 (es) |
| ZA (1) | ZA200504298B (es) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL153997A0 (en) * | 2000-08-10 | 2003-07-31 | Pharmacia Italia Spa | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| UA81790C2 (uk) * | 2002-12-19 | 2008-02-11 | Фармация Италия С.П.А. | Заміщені піролопіразольні похідні як інгібітори кінази |
| SI1611131T1 (sl) | 2003-02-27 | 2011-03-31 | Palau Pharma Sa | Pirazolopiridinski derivati |
| CA2518395A1 (en) * | 2003-03-11 | 2004-09-23 | Pharmacia Italia S.P.A. | Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| AU2004276341B2 (en) | 2003-09-23 | 2011-04-14 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrrole derivatives as protein kinase inhibitors |
| EP1694686A1 (en) | 2003-12-19 | 2006-08-30 | Takeda San Diego, Inc. | Kinase inhibitors |
| CA2559221A1 (en) * | 2004-03-18 | 2005-09-29 | Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| EP1732549A4 (en) * | 2004-03-18 | 2009-11-11 | Brigham & Womens Hospital | METHOD FOR THE TREATMENT OF SYNUCLEINOPATHIES |
| WO2005089515A2 (en) * | 2004-03-18 | 2005-09-29 | The Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| EP1744751A4 (en) * | 2004-03-18 | 2010-03-10 | Brigham & Womens Hospital | METHOD FOR THE TREATMENT OF SYNUCLEINOPATHIES |
| US20070293539A1 (en) * | 2004-03-18 | 2007-12-20 | Lansbury Peter T | Methods for the treatment of synucleinopathies |
| EP1778669A2 (en) | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| DE602005023333D1 (de) | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| CA2589271A1 (en) | 2004-12-07 | 2006-06-15 | Locus Pharmaceuticals, Inc. | Urea inhibitors of map kinases |
| US7612200B2 (en) | 2004-12-07 | 2009-11-03 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| AP2007004061A0 (en) * | 2005-01-10 | 2007-08-31 | Galloway & Company | Pyrrolopyrazoles, potent kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| EA015513B1 (ru) * | 2005-12-21 | 2011-08-30 | Пфайзер Продактс Инк. | Карбониламинопирролопиразолы в качестве эффективных ингибиторов киназ |
| CN101346382B (zh) * | 2005-12-21 | 2011-07-06 | 辉瑞产品公司 | 一种有效的羰基氨基吡咯并吡唑激酶抑制剂 |
| EP1999131B1 (en) | 2006-03-03 | 2013-10-23 | Nerviano Medical Sciences S.r.l. | Bicyclo-pyrazoles active as kinase inhibitors |
| EA200970361A1 (ru) | 2006-10-09 | 2010-02-26 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы киназы |
| WO2008043745A1 (en) * | 2006-10-11 | 2008-04-17 | Nerviano Medical Sciences S.R.L. | Substituted pyrrolo-pyrazole derivatives as kinase inhibitors |
| WO2008096260A1 (en) | 2007-02-07 | 2008-08-14 | Pfizer Inc. | 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors |
| UA96618C2 (en) * | 2007-02-07 | 2011-11-25 | Пфайзер Инк. | 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors |
| CN104370914B (zh) * | 2007-04-12 | 2018-09-07 | 辉瑞大药厂 | 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物 |
| WO2009151683A2 (en) * | 2008-03-12 | 2009-12-17 | Link Medicine Corporation | Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications |
| US20110060005A1 (en) * | 2008-11-13 | 2011-03-10 | Link Medicine Corporation | Treatment of mitochondrial disorders using a farnesyl transferase inhibitor |
| US20100331363A1 (en) * | 2008-11-13 | 2010-12-30 | Link Medicine Corporation | Treatment of mitochondrial disorders using a farnesyl transferase inhibitor |
| NZ593090A (en) * | 2008-11-13 | 2013-06-28 | Link Medicine Corp | Azaquinolinone derivatives and uses thereof |
| EP2519517B1 (en) | 2009-12-29 | 2015-03-25 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| US9382239B2 (en) | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2014063061A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| AU2014337044A1 (en) | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| WO2015164604A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| CN105377852B (zh) * | 2014-05-23 | 2018-08-28 | 深圳明赛瑞霖药业有限公司 | 自身免疫疾病的治疗 |
| CA2966164C (en) * | 2014-10-31 | 2023-10-17 | Ube Industries, Ltd. | Substituted dihydropyrrolopyrazole compound |
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| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
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| KR101845931B1 (ko) * | 2015-06-18 | 2018-04-05 | 한국화학연구원 | 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 |
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| US3526633A (en) * | 1968-03-06 | 1970-09-01 | American Cyanamid Co | Substituted 2,4,5,6-tetrahydropyrrolo(3,4-c)pyrazoles |
| 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 |
| EE200200065A (et) | 1999-08-12 | 2003-04-15 | Pharmacia Italia S.P.A. | 3-aminopürasooli derivaadid, nende valmistamine ja kasutamine vähivastaste toimeainetena ning neid sisaldav farmatseutiline kompositsioon |
| IL153997A0 (en) * | 2000-08-10 | 2003-07-31 | Pharmacia Italia Spa | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| JP2004517840A (ja) * | 2000-11-27 | 2004-06-17 | フアルマシア・イタリア・エツセ・ピー・アー | フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用 |
| NZ527767A (en) * | 2001-01-26 | 2004-11-26 | Pharmacia Italia S | Chromane derivatives, process for their preparation and their use as antitumor agents |
| CN1556702A (zh) | 2001-09-26 | 2004-12-22 | 具有作为激酶抑制剂的活性的氨基吲唑衍生物、它们的制备方法和含有它们的药物组合物 | |
| UA81790C2 (uk) * | 2002-12-19 | 2008-02-11 | Фармация Италия С.П.А. | Заміщені піролопіразольні похідні як інгібітори кінази |
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