BRPI0611960A2 - modulaÇço sinergÍstica de flt3 cinase empregando tienopirimidina e moduladores de tienopiridina cinase - Google Patents
modulaÇço sinergÍstica de flt3 cinase empregando tienopirimidina e moduladores de tienopiridina cinaseInfo
- Publication number
- BRPI0611960A2 BRPI0611960A2 BRPI0611960-3A BRPI0611960A BRPI0611960A2 BR PI0611960 A2 BRPI0611960 A2 BR PI0611960A2 BR PI0611960 A BRPI0611960 A BR PI0611960A BR PI0611960 A2 BRPI0611960 A2 BR PI0611960A2
- Authority
- BR
- Brazil
- Prior art keywords
- kinase
- flt3
- thienopyrimidine
- thienopyridine
- modulators
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- 230000002195 synergetic effect Effects 0.000 title abstract 2
- DBDCNCCRPKTRSD-UHFFFAOYSA-N thieno[3,2-b]pyridine Chemical compound C1=CC=C2SC=CC2=N1 DBDCNCCRPKTRSD-UHFFFAOYSA-N 0.000 title abstract 2
- RBNBDIMXFJYDLQ-UHFFFAOYSA-N thieno[3,2-d]pyrimidine Chemical compound C1=NC=C2SC=CC2=N1 RBNBDIMXFJYDLQ-UHFFFAOYSA-N 0.000 title abstract 2
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 title 1
- 229940125670 thienopyridine Drugs 0.000 title 1
- 239000002175 thienopyridine Substances 0.000 title 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 abstract 5
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 2
- 229940124226 Farnesyltransferase inhibitor Drugs 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 abstract 1
- 230000001603 reducing effect Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4743—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having sulfur as a ring hetero atom
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- 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
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
MODULAÇçO SINERGISTICA DE FLT3 CINASE EMPREGANDO TIENOPIRIMIDINA E MODULADORES DE TIENOPIRIDINA CINASE. A presente invenção refere-se a um método para inibição da atividade ou expressão de FLT3 tirosina cinase, ou para redução da atividade, ou para expressão da atividade de FLT3 cinase em uma célula ou um indivíduo, compreendendo a administração de um inibidor de farnesil transferase e um inibidor de FLT3 cinase selecionado da tienopirimidina e compostos de tienopiridina da Fórmula I' e Fórmula II': em que R~ 1~, R~ 3~, B, Z, Q, p, q e X são conforme definidos aqui. Incluídos na presente invenção temos ambos os métodos profiláticos e terapêuticos para tratamento de um indivíduo em risco de (ou suscetível ao) desenvolvimento de um distúrbio proliferativo celular ou um distúrbio relativo a FLT3.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68940905P | 2005-06-10 | 2005-06-10 | |
| PCT/US2006/022101 WO2006135630A1 (en) | 2005-06-10 | 2006-06-07 | Synergistic modulation of flt3 kinase using thienopyrimidine and thienopyridine kinase modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0611960A2 true BRPI0611960A2 (pt) | 2009-01-27 |
Family
ID=37067880
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0611960-3A BRPI0611960A2 (pt) | 2005-06-10 | 2006-06-07 | modulaÇço sinergÍstica de flt3 cinase empregando tienopirimidina e moduladores de tienopiridina cinase |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20060281769A1 (pt) |
| EP (1) | EP1893215A1 (pt) |
| JP (1) | JP2008543756A (pt) |
| KR (1) | KR20080028919A (pt) |
| CN (1) | CN101242846A (pt) |
| AU (1) | AU2006258040A1 (pt) |
| BR (1) | BRPI0611960A2 (pt) |
| CA (1) | CA2611680A1 (pt) |
| MX (1) | MX2007015740A (pt) |
| WO (1) | WO2006135630A1 (pt) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060281788A1 (en) * | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor |
| US20070004660A1 (en) * | 2005-06-10 | 2007-01-04 | Baumann Christian A | Synergistic Modulation of Flt3 Kinase Using Alkylquinolines and Alkylquinazolines |
| US20060281768A1 (en) * | 2005-06-10 | 2006-12-14 | Gaul Michael D | Thienopyrimidine and thienopyridine kinase modulators |
| KR101367645B1 (ko) | 2006-04-20 | 2014-02-27 | 얀센 파마슈티카 엔.브이. | C-fms 키나제의 저해제로서의 복소환식 화합물 |
| EP2016070B1 (en) | 2006-04-20 | 2016-01-13 | Janssen Pharmaceutica N.V. | Inhibitors of c-fms kinase |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| TW200924781A (en) | 2007-09-14 | 2009-06-16 | Janssen Pharmaceutica Nv | Thieno- and furo-pyrimidine modulators of the histamine H4 receptor |
| JO3240B1 (ar) | 2007-10-17 | 2018-03-08 | Janssen Pharmaceutica Nv | c-fms مثبطات كيناز |
| AU2010289321A1 (en) * | 2009-09-04 | 2012-04-05 | The Regents Of The University Of Michigan | Compositions and methods for treatment of leukemia |
| ES2607807T3 (es) | 2012-08-07 | 2017-04-04 | Janssen Pharmaceutica Nv | Procedimiento para la preparación de los inibidores de las quinasas c-fms |
| AU2013299922B2 (en) | 2012-08-07 | 2018-06-21 | Janssen Pharmaceutica Nv | Process for the preparation of heterocyclic ester derivatives |
| WO2015160192A1 (ko) * | 2014-04-15 | 2015-10-22 | 연세대학교 산학협력단 | 티에노피리미딘 유도체 또는 이의 약학적으로 허용가능한 염을 포함하는 백혈병 치료 및 예방용 약학 조성물 |
| USRE49687E1 (en) | 2014-09-09 | 2023-10-10 | The Regents Of The University Of Michigan | Thienopyrimidine and thienopyridine compounds and methods of use thereof |
| WO2016197027A1 (en) | 2015-06-04 | 2016-12-08 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with mll proteins |
| TWI703150B (zh) | 2015-06-04 | 2020-09-01 | 美商庫拉腫瘤技術股份有限公司 | 用於抑制menin及mll蛋白之交互作用的方法及組合物 |
| WO2017161028A1 (en) | 2016-03-16 | 2017-09-21 | Kura Oncology, Inc. | Substituted inhibitors of menin-mll and methods of use |
| US10752639B2 (en) | 2016-03-16 | 2020-08-25 | Kura Oncology, Inc. | Bridged bicyclic inhibitors of menin-MLL and methods of use |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| US11542248B2 (en) | 2017-06-08 | 2023-01-03 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| TW201920170A (zh) | 2017-09-20 | 2019-06-01 | 美商庫拉腫瘤技術股份有限公司 | 經取代之menin-mll 抑制劑及使用方法 |
| ES2974634T3 (es) | 2018-12-21 | 2024-06-28 | Celgene Corp | Inhibidores de tienopiridinas de RIPK2 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6117432A (en) * | 1995-04-20 | 2000-09-12 | Societe D'exploitation De Produits Pour Les Industries Chimiques (S.E.P.P.I.C.) | Therapeutic composition comprising an antigen or an in vivo generator of a compound comprising an amino acid sequence |
| TW349948B (en) * | 1995-10-31 | 1999-01-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 2-quinolone derivatives |
| DE69635966T2 (de) * | 1995-12-08 | 2006-11-30 | Janssen Pharmaceutica N.V. | (Imidazol-5-yl)Methyl-2-Chinolinonderivate als Farnesyl Protein transferase Inhibitoren |
| US5874442A (en) * | 1995-12-22 | 1999-02-23 | Schering-Plough Corporation | Tricyclic amides useful for inhibition of G-protein function and for treatment of proliferative disease |
| TW591030B (en) * | 1997-03-10 | 2004-06-11 | Janssen Pharmaceutica Nv | Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles |
| PT1140935E (pt) * | 1998-12-23 | 2003-10-31 | Janssen Pharmaceutica Nv | Derivados da quinolina 1,2-ciclizada |
| US6776796B2 (en) * | 2000-05-12 | 2004-08-17 | Cordis Corportation | Antiinflammatory drug and delivery device |
| GB0326601D0 (en) * | 2003-11-14 | 2003-12-17 | Novartis Ag | Organic compounds |
-
2006
- 2006-06-06 US US11/422,400 patent/US20060281769A1/en not_active Abandoned
- 2006-06-07 JP JP2008515864A patent/JP2008543756A/ja not_active Withdrawn
- 2006-06-07 AU AU2006258040A patent/AU2006258040A1/en not_active Abandoned
- 2006-06-07 WO PCT/US2006/022101 patent/WO2006135630A1/en not_active Ceased
- 2006-06-07 CN CNA200680029399XA patent/CN101242846A/zh active Pending
- 2006-06-07 KR KR1020087000696A patent/KR20080028919A/ko not_active Withdrawn
- 2006-06-07 MX MX2007015740A patent/MX2007015740A/es unknown
- 2006-06-07 BR BRPI0611960-3A patent/BRPI0611960A2/pt not_active IP Right Cessation
- 2006-06-07 CA CA002611680A patent/CA2611680A1/en not_active Abandoned
- 2006-06-07 EP EP06772424A patent/EP1893215A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006258040A1 (en) | 2006-12-21 |
| US20060281769A1 (en) | 2006-12-14 |
| CA2611680A1 (en) | 2006-12-21 |
| KR20080028919A (ko) | 2008-04-02 |
| EP1893215A1 (en) | 2008-03-05 |
| MX2007015740A (es) | 2008-04-29 |
| CN101242846A (zh) | 2008-08-13 |
| WO2006135630A1 (en) | 2006-12-21 |
| JP2008543756A (ja) | 2008-12-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 4A, 5A E 6A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012. |