AR093579A1 - Inhibidores de bmi-1 de pirimidina inversa sustituida - Google Patents
Inhibidores de bmi-1 de pirimidina inversa sustituidaInfo
- Publication number
- AR093579A1 AR093579A1 ARP130104300A ARP130104300A AR093579A1 AR 093579 A1 AR093579 A1 AR 093579A1 AR P130104300 A ARP130104300 A AR P130104300A AR P130104300 A ARP130104300 A AR P130104300A AR 093579 A1 AR093579 A1 AR 093579A1
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- alkyl
- amino
- carbonyl
- alkoxy
- halo
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- 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
- C07D405/14—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 three or more hetero rings
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- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61P35/00—Antineoplastic agents
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- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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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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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pathology (AREA)
- Radiology & Medical Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hematology (AREA)
- Oncology (AREA)
Abstract
En el presente documento se describen compuestos de pirimidina sustituidos con amina y formas de estos que inhiben la función y reducen el nivel de proteína del sitio 1 de integración del virus de la leucemia murina de Moloney específico de linfocitos B (Bmi-1) y métodos para su uso para inhibir la función de Bmi-1 y reducir el nivel de Bmi-1 para tratar un cáncer mediado por Bmi-1. Reivindicación 1: Un compuesto de la fórmula (1), o una forma de este, donde R¹ es heteroarilo o heterociclilo opcionalmente sustituido en un miembro de átomo de carbono del anillo con uno, dos, tres o cuatro sustituyentes R⁵, o en un miembro de átomo de nitrógeno del anillo con un sustituyente de átomo de oxígeno para formar u N-óxido; X es N o N sustituido con un sustituyente de átomo de oxigeno para formar un N-óxido; R² es hidrógeno, ciano, halo, hidroxilo, nitro, alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, hidroxil-amino, hidroxil-alquil C₁₋₈-amino, alcoxi C₁₋₈-alquil C₁₋₈-amino, alquil C₁₋₈-tio, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-amino, amino-carbonilo, alquil C₁₋₈-amino-carbonilo, (alquil C₁₋₈)₂-amino-carbonilo, amino-carbonil-amino, alquil C₁₋₈-amino-carbonilamino, (alquil C₁₋₈)₂-amino-carbonil-amino, alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈-carbonil-amino, amino-sulfonilo, alquil C₁₋₈-amino-sulfonilo, (alquil C₁₋₈)₂-amino-sulfonilo, amino-sulfonil-amino, alquil C₁₋₈-amino-sulfonil-amino, (alquil C₁₋₈)₂-amino-sulfonil-amino, P(O)(R⁷)₂-amino o heteroarilo, donde el heteroarilo está opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes alquilo C₁₋₈; R³ es hidrógeno, ciano, halo, alquilo C₁₋₈, amino, alquil C₁₋₈-amino o (alquil C₁₋₈)₂-amino; R⁴ es cicloalquilo C₃₋₁₄, arilo, heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes R⁶; R⁵ se selecciona independientemente entre ciano, halo, hidroxilo, nitro, oxo, alquilo C₁₋₈, ciano-alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, halo-alcoxi C₁₋₈, alquenilo C₂₋₈, alcoxi C₁₋₈-alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈-alquinilo C₂₋₈, carboxilo, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, amino-alquilo C₁₋₈, alquil C₁₋₈-amino-alquilo C₁₋₈, (alquil C₁₋₈)₂-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino-alquil C₁₋₈-amino, alquil C₁₋₈-tio, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-amino, alquil C₁₋₈-carboniloxi, alquil C₁₋₈-carbonil-oxi-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈-carbonil-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilamino, alquil C₁₋₈-sulfonilo, cicloalquilo C₃₋₁₄, arilo, aril-alquilo C₁₋₈, aril-amino, aril-alquil C₁₋₈-amino, heteroarilo, heteroaril-alquilo C₁₋₈ o heterociclilo, donde cicloalquilo C₃₋₁₄, arilo, heteroarilo o heterociclilo, y las porciones arilo y heteroarilo de aril-alquilo C₁₋₈, aril-amino, aril-alquil C₁₋₈-amino y heteroaril-alquilo C₁₋₈ están cada una opcionalmente sustituidas con uno, dos, tres o cuatro sustituyentes halo, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, halo-alcoxi C₁₋₈, hidroxil-alcoxi C₁₋₈ o carboxilo; R⁶ se selecciona independientemente entre ciano, halo, hidroxilo, nitro, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, halo-alcoxi C₁₋₈, alquenilo C₂₋₈, alcoxi C₁₋₈-alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈-alquinilo C₂₋₈, carboxilo, formilo, formiloxi, alquil C₁₋₈-carbonilo, halo-alquil C₁₋₈-carbonilo, alquil C₁₋₈-tio, halo-alquil C₁₋₈-tio, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-oxi, alquil C₁₋₈-carbonil-oxi-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilo, halo-alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈-carbonil-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilamino, alcoxi C₁₋₈-carbonil-amino-alquilo C₁₋₈, amino-carbonilo, alquil C₁₋₈-amino-carbonilo, (alquil C₁₋₈)₂-amino-carbonilo, alquil C₁₋₈-carbonil-amino, alquil C₁₋₈-carbonil-amino- alquilo C₁₋₈, amino-alquilo C₁₋₈, alquil C₁₋₈-amino-alquilo C₁₋₈, (alquil C₁₋₈)₂-amino-alquilo C₁₋₈, amino-alquil C₁₋₈-amino, alquil C₁₋₈-amino-alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino-alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino-alquil C₁₋₈-amino, imino-alquilo C₁₋₈, hidroxil-imino-alquilo C₁₋₈, alcoxi C₁₋₈-imino-alquilo C₁₋₈, alquil C₁₋₈-sulfonilo, halo-alquil C₁₋₈-sulfonilo, amino-sulfonilo, alquil C₁₋₈-amino-sulfonilo, (alquil C₁₋₈)₂-amino-sulfonilo, B(OR⁸)₂, cicloalquilo C₃₋₁₄, heterociclil-arilo o heteroarilo, donde cicloalquilo C₃₋₁₄, heterociclilo, arilo y heteroarilo están cada uno opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes halo o alquilo C₁₋₈; R⁷ es independientemente hidroxilo o (alcoxi C₁₋₈)ₙ, donde n representa un número entero de 1 a 5; y R⁸ es independientemente hidrógeno o alquilo C₁₋₈; donde la forma del compuesto se selecciona entre un ácido libre, base libre, sal, éster, hidrato, solvato, quelato, clatrato, polimorfo, isotopólogo, estereoisómero, racemato, enantiómero, diastereómero o tautómero de este.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261728907P | 2012-11-21 | 2012-11-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR093579A1 true AR093579A1 (es) | 2015-06-10 |
Family
ID=50776672
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104300A AR093579A1 (es) | 2012-11-21 | 2013-11-21 | Inhibidores de bmi-1 de pirimidina inversa sustituida |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US10428050B2 (es) |
| EP (1) | EP2922828B1 (es) |
| JP (3) | JP6412503B2 (es) |
| KR (4) | KR20220143164A (es) |
| CN (2) | CN104918919A (es) |
| AR (1) | AR093579A1 (es) |
| AU (1) | AU2013348009C1 (es) |
| BR (1) | BR112015011760B1 (es) |
| CA (1) | CA2892045C (es) |
| CL (1) | CL2015001377A1 (es) |
| CR (1) | CR20150294A (es) |
| CU (1) | CU24387B1 (es) |
| DK (1) | DK2922828T3 (es) |
| EA (2) | EA031405B1 (es) |
| EC (1) | ECSP15019948A (es) |
| ES (1) | ES2821529T3 (es) |
| HK (1) | HK1215032A1 (es) |
| IL (2) | IL238871B (es) |
| MA (1) | MA38208B1 (es) |
| MX (2) | MX2015006469A (es) |
| NI (1) | NI201500072A (es) |
| NZ (2) | NZ746607A (es) |
| PE (1) | PE20151413A1 (es) |
| PH (1) | PH12015501130A1 (es) |
| PL (1) | PL2922828T3 (es) |
| PT (1) | PT2922828T (es) |
| SA (1) | SA517381847B1 (es) |
| SG (2) | SG10201600149VA (es) |
| TW (1) | TWI623531B (es) |
| UA (1) | UA118094C2 (es) |
| WO (1) | WO2014081906A2 (es) |
| ZA (1) | ZA201503642B (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2922828T3 (pl) | 2012-11-21 | 2020-12-28 | Ptc Therapeutics, Inc. | Pochodne 4,6-diaminopirymidynowe jako inhibitory bmi-1 w leczeniu raka |
| WO2015003360A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| EP3019480B1 (en) * | 2013-07-11 | 2020-05-06 | Agios Pharmaceuticals, Inc. | 2,4- or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer |
| WO2015003355A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| TWI692477B (zh) | 2013-08-30 | 2020-05-01 | 美商Ｐｔｃ治療公司 | 經取代嘧啶ｂｍｉ-１抑制劑 |
| US10584115B2 (en) | 2013-11-21 | 2020-03-10 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine BMI-1 inhibitors |
| JP7001593B2 (ja) | 2015-08-11 | 2022-01-19 | コグノア， インコーポレイテッド | 人工知能およびユーザ入力を用いて発達進度を判定するための方法および装置 |
| US10851082B2 (en) | 2015-10-28 | 2020-12-01 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2) |
| US11972336B2 (en) | 2015-12-18 | 2024-04-30 | Cognoa, Inc. | Machine learning platform and system for data analysis |
| CA3010615C (en) * | 2016-01-14 | 2024-02-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
| CA3053245A1 (en) | 2017-02-09 | 2018-08-16 | Cognoa, Inc. | Platform and system for digital personalized medicine |
| EP3664803A4 (en) | 2017-08-01 | 2021-05-05 | PTC Therapeutics, Inc. | DHODH INHIBITOR FOR USE IN THE TREATMENT OF HEMATOLOGICAL CANCERS |
| EP3564235A1 (en) * | 2018-05-03 | 2019-11-06 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2) |
| AU2019340402A1 (en) | 2018-08-17 | 2021-03-25 | Ptc Therapeutics, Inc. | Method for treating pancreatic cancer |
| CN109988172B (zh) * | 2019-01-10 | 2020-09-29 | 石家庄学院 | 一种吡唑并[1,5-a]嘧啶类杂环化合物及衍生物的合成方法 |
| US20220096473A1 (en) * | 2019-01-15 | 2022-03-31 | Ptc Therapeutics, Inc. | Method for treating an acute myeloid leukemia |
| AU2020227748A1 (en) * | 2019-02-28 | 2021-09-16 | Ptc Therapeutics, Inc. | Method for treating a multiple myeloma |
| SG11202109503TA (en) * | 2019-03-11 | 2021-09-29 | Ptc Therapeutics Inc | Compound form having enhanced bioavailability and formulations thereof |
| BR112021018770A2 (pt) | 2019-03-22 | 2022-02-15 | Cognoa Inc | Métodos e dispositivos de terapia digital personalizada |
| JP2022519930A (ja) * | 2019-03-27 | 2022-03-25 | ピーティーシー セラピューティクス， インコーポレイテッド | 肉腫を治療する方法に有用な組み合わせ |
| US20220177459A1 (en) * | 2019-04-02 | 2022-06-09 | Hinova Pharmaceuticals Inc. | Aromatic amine compound and use thereof in preparation of ar and brd4 dual inhibitors and regulators |
Family Cites Families (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH593266A5 (es) | 1973-09-20 | 1977-11-30 | Delalande Sa | |
| ES2201112T3 (es) | 1994-08-13 | 2004-03-16 | Yuhan Corporation | Nuevos derivados de pirimidina y procedimientos para su preparacion. |
| IN188411B (es) | 1997-03-27 | 2002-09-21 | Yuhan Corp | |
| KR100272471B1 (ko) | 1998-11-17 | 2000-11-15 | 김선진 | 신규의 피리미딘 유도체 및 그의 제조방법 |
| GB9905075D0 (en) * | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| ATE253915T1 (de) | 1999-06-30 | 2003-11-15 | Merck & Co Inc | Src-kinase hemmende verbindungen |
| GB9919778D0 (en) | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| WO2001025220A1 (en) | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
| WO2001030778A1 (en) | 1999-10-27 | 2001-05-03 | Novartis Ag | Thiazole and imidazo [4,5-b] pyridine compounds and their pharmaceutical use |
| HUP0301117A3 (en) | 2000-02-17 | 2004-01-28 | Amgen Inc Thousand Oaks | Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them |
| CN100355751C (zh) | 2000-03-29 | 2007-12-19 | 西克拉塞尔有限公司 | 2－取代的4－杂芳基－嘧啶、其组合物及其用途 |
| HUP0302173A2 (hu) | 2000-09-15 | 2003-09-29 | Vertex Pharmaceuticals Incorporated | Protein kináz inhibitorokként alkalmazható pirazolvegyületek |
| EP1330452B1 (en) | 2000-09-20 | 2008-11-26 | Ortho-McNeil Pharmaceutical, Inc. | Pyrazine derivatives as modulators of tyrosine kinases |
| AU2002228922A1 (en) * | 2000-12-12 | 2002-06-24 | Cytovia, Inc. | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| US6716851B2 (en) * | 2000-12-12 | 2004-04-06 | Cytovia, Inc. | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof |
| EP1377573B1 (en) | 2000-12-15 | 2005-07-27 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| IL156784A0 (en) | 2001-02-20 | 2004-02-08 | Astrazeneca Ab | 2-arylamino-pyrimidines for the treatment of gsk3-related disorders |
| DE60239097D1 (de) | 2001-03-02 | 2011-03-17 | Gpc Biotech Ag | Drei-hybrid-assaysystem |
| US7196095B2 (en) | 2001-06-25 | 2007-03-27 | Merck & Co., Inc. | (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds |
| ES2271283T3 (es) | 2001-07-03 | 2007-04-16 | Vertex Pharmaceuticals Incorporated | Isoxazolil-pirimidinas como inhibidores de las proteinas quinasas src y lck. |
| US7109204B2 (en) | 2001-08-01 | 2006-09-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| WO2003075828A2 (en) | 2002-03-11 | 2003-09-18 | Zetiq Technologies Ltd. | Compounds useful in the treatment of cancer |
| IL165262A0 (en) | 2002-05-23 | 2005-12-18 | Cytopia Pty Ltd | Kinase inhibitors |
| CN100343237C (zh) | 2002-06-28 | 2007-10-17 | 日本新药株式会社 | 酰胺衍生物及医药品 |
| GB0215844D0 (en) | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
| US7060850B2 (en) * | 2002-07-11 | 2006-06-13 | Fluorous Technologies Incorporated | Fluorous tagging and scavenging reactants and methods of synthesis and use thereof |
| US20040110821A1 (en) * | 2002-08-07 | 2004-06-10 | Konkel Michael J. | GAL3 receptor antagonists for the treatment of affective disorders |
| UA80296C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Imidazolopyridines and methods of making and using the same |
| WO2004035588A1 (en) | 2002-10-15 | 2004-04-29 | Smithkline Beecham Corporation | Pyradazine compounds as gsk-3 inhibitors |
| US7169781B2 (en) | 2003-10-17 | 2007-01-30 | Hoffmann-La Roche Inc. | Imidazole derivatives and their use as pharmaceutical agents |
| GB2424882B (en) | 2004-01-12 | 2008-08-06 | Cytopia Res Pty Ltd | Selective kinase inhibitors |
| US20070117818A1 (en) | 2004-02-04 | 2007-05-24 | Masaichi Hasegawa | Pyrimidinone compounds useful as kinase inhibitors |
| ES2398712T3 (es) * | 2004-03-30 | 2013-03-21 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de JAK y otras proteínas quinasas |
| JP2006045119A (ja) | 2004-08-04 | 2006-02-16 | Toray Ind Inc | ピラジン誘導体及びそれを有効成分とする腎炎治療薬 |
| WO2006050076A1 (en) | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| BRPI0607062A2 (pt) | 2005-02-28 | 2009-08-04 | Japan Tobacco Inc | composto de aminopiridina com atividade inibidora de syk, composição farmacêutica e agente terapêutico compreendendo os mesmos |
| CA2601257A1 (en) | 2005-03-10 | 2006-09-21 | Bayer Pharmaceuticals Corporation | Pyrimidine derivatives for treatment of hyperproliferative disorders |
| WO2007147874A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| CN101516873A (zh) * | 2006-10-03 | 2009-08-26 | 神经研究公司 | 用作钾通道调节剂的吲唑基衍生物 |
| CA2665398A1 (en) | 2006-10-03 | 2008-04-10 | Neurosearch A/S | Indazolyl derivatives useful as potassium channel modulating agents |
| BRPI0717773A2 (pt) * | 2006-10-19 | 2013-11-05 | Signal Pharm Llc | Composto, composição farmacêutica, e, métodos para tratar ou prevenir câncer, uma condição inflamatória, uma condição imunológica ou uma condição metabólica, e para inibir uma quinase em uma célula que expressa a dita quinase |
| AU2007336933A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as CDK inhibitors for the treatment of cancer, inflammation and viral infections |
| TW200902010A (en) | 2007-01-26 | 2009-01-16 | Smithkline Beecham Corp | Anthranilamide inhibitors of aurora kinase |
| WO2008099210A2 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| TW200846344A (en) | 2007-04-25 | 2008-12-01 | Astrazeneca Ab | Chemical compounds |
| GB0714573D0 (en) | 2007-07-26 | 2007-09-05 | Imp Innovations Ltd | Marker gene |
| EP2203436A1 (en) | 2007-09-17 | 2010-07-07 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| MX2010005300A (es) | 2007-11-16 | 2010-06-25 | Incyte Corp | 4-pirazolil-n-arilpirimidin-2-aminas y 4-pirazolil-n-heteroarilpir imidin-2-aminas como inhibidores de cinasas janus. |
| JP2011506303A (ja) | 2007-12-07 | 2011-03-03 | ノバルティス アーゲー | ピラゾール誘導体およびサイクリン依存性キナーゼの阻害剤としてのその使用 |
| DE102008005493A1 (de) | 2008-01-22 | 2009-07-23 | Merck Patent Gmbh | 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate |
| GB0801416D0 (en) | 2008-01-25 | 2008-03-05 | Piramed Ltd | Pharmaceutical compounds |
| JP2011518219A (ja) | 2008-04-22 | 2011-06-23 | ポートラ ファーマシューティカルズ， インコーポレイテッド | タンパク質キナーゼの阻害剤 |
| ES2605815T3 (es) | 2008-07-01 | 2017-03-16 | Ptc Therapeutics, Inc. | Moduladores de la expresión de la proteína Bmi-1 |
| EP2328890B1 (en) | 2008-08-06 | 2012-01-25 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
| US8618099B2 (en) | 2008-09-02 | 2013-12-31 | Ataxion, Inc. | Pyrazolyl-pyrimidine derivatives and their use as potassium channel modulators |
| TW201028399A (en) * | 2008-11-27 | 2010-08-01 | Shionogi & Co | Pyrimidine derivative and pyridine derivative both having pi3k inhibitory activity |
| KR20110120286A (ko) | 2009-02-12 | 2011-11-03 | 아스텔라스세이야쿠 가부시키가이샤 | 헤테로환 유도체 |
| CN102448958B (zh) | 2009-03-27 | 2015-10-21 | 维特Dc公司 | 嘧啶基和1,3,5-三嗪基苯并咪唑磺酰胺和其在癌症治疗中的用途 |
| ES2453097T3 (es) | 2009-05-27 | 2014-04-04 | Abbvie Inc. | Inhibidores de pirimidina de actividad quinasa |
| TW201102387A (en) | 2009-06-08 | 2011-01-16 | Medicinova Inc | Substituted pyrazolo[1,5-a]pyridine compounds having multi-target activity |
| KR101702609B1 (ko) * | 2009-06-17 | 2017-02-03 | 버텍스 파마슈티칼스 인코포레이티드 | 인플루엔자 바이러스 복제의 억제제 |
| CA2767008C (en) | 2009-07-07 | 2018-01-30 | Pathway Therapeutics, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
| US8435980B2 (en) | 2009-07-15 | 2013-05-07 | Abbvie Inc. | Pyrrolopyridine inhibitors of kinases |
| ES2483594T3 (es) | 2009-07-15 | 2014-08-06 | Abbott Laboratories | Pirrolopirazinas inhibidoras de quinasas |
| JP2011136925A (ja) * | 2009-12-28 | 2011-07-14 | Dainippon Sumitomo Pharma Co Ltd | 含窒素二環性化合物 |
| MX2012008083A (es) | 2010-01-12 | 2012-08-15 | Ab Science | Inhibidores de triazol y oxazol quinaza. |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| ES2365960B1 (es) | 2010-03-31 | 2012-06-04 | Palobiofarma, S.L | Nuevos antagonistas de los receptores de adenosina. |
| EP2606126B1 (en) * | 2010-08-19 | 2016-05-18 | F.Hoffmann-La Roche Ag | Conversion of somatic cells to induced reprogrammed neural stem cells (irnscs) |
| CN103221408A (zh) | 2010-09-13 | 2013-07-24 | 诺瓦提斯公司 | 三嗪-*二唑类化合物 |
| US20140088056A1 (en) | 2010-09-28 | 2014-03-27 | President And Fellows Of Harvard College | Cardiac glycosides are potent inhibitors of interferon-beta gene expression |
| EP2649065A1 (en) | 2010-12-09 | 2013-10-16 | Amgen Inc. | Bicyclic compounds as pim inhibitors |
| US9850227B2 (en) | 2011-02-25 | 2017-12-26 | Yuhan Corporation | Diaminopyrimidine derivatives and processes for the preparation thereof |
| US9199962B2 (en) | 2011-07-07 | 2015-12-01 | Merck Patent Gmbh | Substituted azaheterocycles for the treatment of cancer |
| US9695228B2 (en) | 2012-11-21 | 2017-07-04 | Janssen Biotech, Inc. | EGFR and c-Met fibronectin type III domain binding molecules |
| UY35148A (es) | 2012-11-21 | 2014-05-30 | Amgen Inc | Immunoglobulinas heterodiméricas |
| PL2922828T3 (pl) * | 2012-11-21 | 2020-12-28 | Ptc Therapeutics, Inc. | Pochodne 4,6-diaminopirymidynowe jako inhibitory bmi-1 w leczeniu raka |
| CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
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