ATE398125T1 - Chinazolin-derivate als tgf-beta-inhibitoren - Google Patents
Chinazolin-derivate als tgf-beta-inhibitorenInfo
- Publication number
- ATE398125T1 ATE398125T1 AT04718542T AT04718542T ATE398125T1 AT E398125 T1 ATE398125 T1 AT E398125T1 AT 04718542 T AT04718542 T AT 04718542T AT 04718542 T AT04718542 T AT 04718542T AT E398125 T1 ATE398125 T1 AT E398125T1
- Authority
- AT
- Austria
- Prior art keywords
- tgf beta
- quinazoline derivatives
- beta inhibitors
- mediated disease
- tgf
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 abstract 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 abstract 1
- 125000003258 trimethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])[*:1] 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45416403P | 2003-03-12 | 2003-03-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE398125T1 true ATE398125T1 (de) | 2008-07-15 |
Family
ID=32990876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT04718542T ATE398125T1 (de) | 2003-03-12 | 2004-03-08 | Chinazolin-derivate als tgf-beta-inhibitoren |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7189733B2 (de) |
| EP (1) | EP1603908B1 (de) |
| AT (1) | ATE398125T1 (de) |
| DE (1) | DE602004014347D1 (de) |
| ES (1) | ES2305744T3 (de) |
| WO (1) | WO2004081009A1 (de) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY27224A1 (es) * | 2001-03-23 | 2002-10-31 | Bayer Corp | Inhibidores de la rho-quinasa |
| PE20020958A1 (es) * | 2001-03-23 | 2002-11-14 | Bayer Corp | Inhibidores de la rho-quinasa |
| CL2004000409A1 (es) * | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
| JP4895806B2 (ja) * | 2003-04-09 | 2012-03-14 | エクセリクシス, インク. | Tie−2モジュレータと使用方法 |
| US8283354B2 (en) * | 2004-09-02 | 2012-10-09 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7718658B2 (en) * | 2004-09-02 | 2010-05-18 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7928107B2 (en) * | 2004-09-02 | 2011-04-19 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| ATE549314T1 (de) * | 2004-12-17 | 2012-03-15 | Vertex Pharma | Verfahren zur herstellung von 4-aminochinazolinen |
| EP1891039A1 (de) | 2005-05-20 | 2008-02-27 | Vertex Pharmaceuticals Incorporated | Chinolinderivate als modulatoren von ionenkanälen |
| EP2079739A2 (de) | 2006-10-04 | 2009-07-22 | Pfizer Products Inc. | Pyrido[4,3-d]pyrimidin-4(3h)-onderivate als kalziumrezeptorantagonisten |
| AR070127A1 (es) * | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| WO2009146301A1 (en) * | 2008-05-27 | 2009-12-03 | Yale University | TARGETING TGF-β AS A THERAPY FOR ALZHEIMER'S DISEASE |
| US20100087486A1 (en) * | 2008-05-30 | 2010-04-08 | Hiroshi Nakamura | Methods for using tgf-b receptor inhibitors or activin-like kinase (alk) 5 inhibitors a-83-01 and sb-431542 to treat eye disease and wound healing conditions |
| CN102695511A (zh) * | 2009-04-17 | 2012-09-26 | 舒玛健康系统有限责任公司 | 抑制眼部瘢痕形成的转化生长因子-β受体抑制剂的用途 |
| EP2496234A1 (de) | 2009-11-07 | 2012-09-12 | Merck Patent GmbH | Heteroarylaminochinoline als tgf-beta-rezeptorkinase-inhibitoren |
| BR112012018954A2 (pt) * | 2010-02-05 | 2016-04-12 | Merck Patent Gmbh | derivados de hetaril-[1,8]naftiridina |
| TW201210597A (en) * | 2010-06-09 | 2012-03-16 | Gilead Sciences Inc | Inhibitors of hepatitis C virus |
| AU2011273931B2 (en) * | 2010-06-28 | 2015-04-23 | Merck Patent Gmbh | 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer |
| ES2542647T3 (es) * | 2011-03-09 | 2015-08-07 | Merck Patent Gmbh | Derivados de pirido[2,3 b]pirazina y sus usos terapéuticos |
| US20150275306A1 (en) | 2012-10-10 | 2015-10-01 | Stichting Het Nederlands Kanker Instituut Antoni van Leeuwenhoek Ziekenhuis | Methods and means for predicting resistance to anti-cancer treatment |
| PL2970890T3 (pl) | 2013-03-14 | 2020-11-16 | The Brigham And Women's Hospital, Inc. | Kompozycje i sposoby ekspansji i hodowli nabłonkowych komórek macierzystych |
| KR101658111B1 (ko) * | 2013-05-13 | 2016-09-20 | 제일모직 주식회사 | 유기광전자소자용 화합물, 이를 포함하는 유기발광소자 및 상기 유기발광소자를 포함하는 표시장치 |
| CN103570632B (zh) * | 2013-07-22 | 2015-09-30 | 成都理工大学 | 无催化剂的4(3h)-喹唑啉酮的合成方法 |
| PL3089971T3 (pl) | 2014-01-01 | 2021-01-25 | Medivation Technologies Llc | Związki i sposoby ich zastosowania |
| EP3189134A1 (de) | 2014-09-03 | 2017-07-12 | The Brigham and Women's Hospital, Inc. | Zusammensetzungen, systeme und verfahren zur erzeugung von innenohrhaarzellen zur behandlung von gehörverlust |
| US10626094B2 (en) | 2014-10-14 | 2020-04-21 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof |
| US10669528B2 (en) | 2015-06-25 | 2020-06-02 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| US10399987B2 (en) | 2015-07-28 | 2019-09-03 | Bristol-Myer Squibb Company | TGF beta receptor antagonists |
| US11021687B2 (en) | 2016-01-08 | 2021-06-01 | The Brigham And Women's Hospital, Inc. | Production of differentiated enteroendocrine cells and insulin producing cells |
| US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| EP4049665B1 (de) | 2016-03-15 | 2025-03-12 | The Children's Medical Center Corporation | Verfahren und zusammensetzungen im zusammenhang mit der expansion hämatopoetischer stammzellen |
| EP3562827A1 (de) | 2016-12-30 | 2019-11-06 | Frequency Therapeutics, Inc. | 1h-pyrrol-2,5-dion-verbindungen und verfahren zur verwendung davon zur induktion der selbsterneuerung von unterstützenden stamm-/vorläuferzellen |
| WO2018204176A1 (en) | 2017-05-01 | 2018-11-08 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitors of low molecular weight protein tyrosine phosphatase (lmptp) and uses thereof |
| CN109096254B (zh) * | 2017-06-20 | 2021-07-06 | 江西师范大学 | 喹唑啉衍生物及其制备方法和应用 |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| US20210254006A1 (en) | 2018-06-06 | 2021-08-19 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| JP2021533788A (ja) | 2018-08-17 | 2021-12-09 | フリークエンシー セラピューティクス インコーポレイテッド | Jag−1を上方制御することにより有毛細胞を生成するための組成物及び方法 |
| WO2020142485A1 (en) | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| EP4681774A3 (de) | 2021-03-29 | 2026-03-25 | Gilead Sciences, Inc. | Khk-hemmer |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5776963A (en) * | 1989-05-19 | 1998-07-07 | Hoechst Marion Roussel, Inc. | 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility |
| US5223501A (en) * | 1991-05-10 | 1993-06-29 | Merck & Co., Inc. | Substituted pyrimidinones bearing acidic functional groups as angiotensin ii antagonists |
| US6225318B1 (en) * | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
| US6184226B1 (en) * | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| AU2003229305A1 (en) | 2002-05-17 | 2003-12-02 | Scios, Inc. | TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS |
| EP1575506A4 (de) | 2002-07-25 | 2008-04-23 | Scios Inc | Verfahren zur verbesserung der lungenfunktion mit tgf-beta hemmern |
-
2004
- 2004-03-08 DE DE602004014347T patent/DE602004014347D1/de not_active Expired - Lifetime
- 2004-03-08 WO PCT/US2004/007090 patent/WO2004081009A1/en not_active Ceased
- 2004-03-08 AT AT04718542T patent/ATE398125T1/de not_active IP Right Cessation
- 2004-03-08 US US10/795,538 patent/US7189733B2/en not_active Expired - Fee Related
- 2004-03-08 ES ES04718542T patent/ES2305744T3/es not_active Expired - Lifetime
- 2004-03-08 EP EP04718542A patent/EP1603908B1/de not_active Expired - Lifetime
-
2007
- 2007-01-16 US US11/653,679 patent/US8268857B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20040204431A1 (en) | 2004-10-14 |
| ES2305744T3 (es) | 2008-11-01 |
| US8268857B2 (en) | 2012-09-18 |
| WO2004081009A1 (en) | 2004-09-23 |
| EP1603908A1 (de) | 2005-12-14 |
| EP1603908B1 (de) | 2008-06-11 |
| US20070142408A1 (en) | 2007-06-21 |
| DE602004014347D1 (de) | 2008-07-24 |
| US7189733B2 (en) | 2007-03-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |