ATE325609T1 - Neue 2-amino-4-oxochinazolone als partielle lxr- kernrezeptoragonisten - Google Patents
Neue 2-amino-4-oxochinazolone als partielle lxr- kernrezeptoragonistenInfo
- Publication number
- ATE325609T1 ATE325609T1 AT03753402T AT03753402T ATE325609T1 AT E325609 T1 ATE325609 T1 AT E325609T1 AT 03753402 T AT03753402 T AT 03753402T AT 03753402 T AT03753402 T AT 03753402T AT E325609 T1 ATE325609 T1 AT E325609T1
- Authority
- AT
- Austria
- Prior art keywords
- amino
- alkyl
- new
- substituted
- alkylphenyl
- Prior art date
Links
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- -1 carboxy, carboxymethyl Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 abstract 3
- 102000004311 liver X receptors Human genes 0.000 abstract 3
- 108090000865 liver X receptors Proteins 0.000 abstract 3
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 3
- SDTFBAXSPXZDKC-UHFFFAOYSA-N 2-imino-1,2,3,4-tetrahydroquinazolin-4-one Chemical class C1=CC=C2C(=O)NC(N)=NC2=C1 SDTFBAXSPXZDKC-UHFFFAOYSA-N 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 230000023603 positive regulation of transcription initiation, DNA-dependent Effects 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 101000603962 Homo sapiens Oxysterols receptor LXR-alpha Proteins 0.000 abstract 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 abstract 1
- 102100038476 Oxysterols receptor LXR-alpha Human genes 0.000 abstract 1
- 108700008625 Reporter Genes Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000001539 anorectic effect Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 206010061428 decreased appetite Diseases 0.000 abstract 1
- 231100000673 dose–response relationship Toxicity 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 102000006255 nuclear receptors Human genes 0.000 abstract 1
- 108020004017 nuclear receptors Proteins 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 230000035897 transcription Effects 0.000 abstract 1
- 238000013518 transcription Methods 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Adhesive Tapes (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20020020255 EP1407774A1 (de) | 2002-09-10 | 2002-09-10 | 2-Amino-4-chinazolinone, die an den LXR Kernrezeptor binden |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE325609T1 true ATE325609T1 (de) | 2006-06-15 |
Family
ID=31985024
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03753402T ATE325609T1 (de) | 2002-09-10 | 2003-09-10 | Neue 2-amino-4-oxochinazolone als partielle lxr- kernrezeptoragonisten |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20050261319A1 (de) |
| EP (2) | EP1407774A1 (de) |
| JP (1) | JP2006502169A (de) |
| AT (1) | ATE325609T1 (de) |
| AU (2) | AU2003296861A1 (de) |
| CA (1) | CA2498655A1 (de) |
| DE (1) | DE60305193T2 (de) |
| WO (2) | WO2004024162A1 (de) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040242568A1 (en) | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| EP1639129A2 (de) * | 2003-05-21 | 2006-03-29 | F. Hoffmann-La Roche Ag | Marker zur lxr-aktivierung |
| ATE440825T1 (de) | 2003-06-06 | 2009-09-15 | Vertex Pharma | Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern |
| WO2005101007A1 (en) * | 2004-04-15 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with liver x receptor beta (lxrb) |
| CN101035770B (zh) * | 2004-08-06 | 2011-02-23 | 詹森药业有限公司 | 可用作β-分泌酶(BACE)抑制剂的2-氨基-喹唑啉衍生物 |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8383637B2 (en) | 2004-08-06 | 2013-02-26 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8426429B2 (en) | 2004-08-06 | 2013-04-23 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US7846915B2 (en) * | 2004-10-20 | 2010-12-07 | Resverlogix Corporation | Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases |
| ES2438739T3 (es) | 2005-06-28 | 2014-01-20 | Daiichi Sankyo Company, Limited | Procedimiento de prueba de ligando LXR |
| WO2007016525A2 (en) * | 2005-07-29 | 2007-02-08 | Resverlogix Corp. | Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices |
| ES2360957T3 (es) | 2005-10-25 | 2011-06-10 | Janssen Pharmaceutica Nv | Derivados de 2-amino-3,4-dihidro-pirido(3,4-d)-pirimidina utiles como inhibidores de la beta-secretasa (bace). |
| WO2007092854A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| US7932261B2 (en) | 2006-02-06 | 2011-04-26 | Janssen Pharmaceutica Nv | Macrocycle derivatives useful as inhibitors of β-secretase (BACE) |
| US7776882B2 (en) | 2006-02-06 | 2010-08-17 | Baxter Ellen W | 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8168666B2 (en) | 2006-11-30 | 2012-05-01 | Kowa Company, Ltd. | Substituted carbinol compound |
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| WO2009097278A1 (en) | 2008-01-28 | 2009-08-06 | Janssen Pharmaceutica N.V. | 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| ES2397682T3 (es) | 2008-01-29 | 2013-03-08 | Janssen Pharmaceutica Nv | Derivados de 2-amino-quinolina útiles como inhibidores de la beta-secretasa (BACE) |
| US7919509B2 (en) | 2008-02-29 | 2011-04-05 | Kowa Company, Ltd. | 2-oxochromene derivatives |
| US7951822B2 (en) | 2008-03-31 | 2011-05-31 | Kowa Company, Ltd. | 1,3-dihydroisobenzofuran derivatives |
| US8008306B2 (en) | 2008-04-30 | 2011-08-30 | Kowa Company, Ltd. | Quinoline compounds |
| WO2009144961A1 (ja) | 2008-05-29 | 2009-12-03 | 興和株式会社 | 環状リンカーを有する置換カルビノール化合物 |
| US8114995B2 (en) | 2008-06-26 | 2012-02-14 | Resverlogix Corp. | Methods of preparing quinazolinone derivatives |
| ES2542835T3 (es) | 2009-01-08 | 2015-08-12 | Resverlogix Corporation | Compuestos para la prevención y el tratamiento de enfermedades cardiovasculares |
| NZ617779A (en) | 2009-03-18 | 2015-08-28 | Resverlogix Corp | Novel anti-inflammatory agents |
| WO2010120508A2 (en) * | 2009-03-31 | 2010-10-21 | The General Hospital Corporation | Regulation of mir-33 micrornas in the treatment of cholesterol-related disorders |
| US9757368B2 (en) | 2009-04-22 | 2017-09-12 | Resverlogix Corp. | Anti-inflammatory agents |
| CN102438991B (zh) | 2009-04-29 | 2015-08-26 | 兴和株式会社 | 具有杂环连接基的甲醇化合物 |
| CA2811145A1 (en) | 2010-09-07 | 2012-03-15 | Snu R&Db Foundation | Sesterterpene compound and use thereof |
| EP2545964A1 (de) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Neuartige FXR- (NR1H4)-Binde- und -Aktivitätsmodulationsverbindungen |
| PT2773354T (pt) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Formulações orais de libertação imediata para quinazolinonas substituídas |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| UY35675A (es) | 2013-07-24 | 2015-02-27 | Novartis Ag | Derivados sustituidos de quinazolin-4-ona |
| AU2015204572B2 (en) | 2014-01-10 | 2020-07-30 | Inspirna, Inc. | LXR agonists and uses thereof |
| CN114984016A (zh) | 2015-03-13 | 2022-09-02 | 雷斯韦洛吉克斯公司 | 用于治疗补体相关疾病之组合物及治疗方法 |
| AU2017207291B2 (en) | 2016-01-11 | 2023-06-15 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| ES2982801T3 (es) | 2017-03-28 | 2024-10-17 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas |
| EP3713575A4 (de) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | Polymorphe und ihre verwendung |
| CA3102326A1 (en) | 2018-07-26 | 2020-01-30 | Domain Therapeutics | Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4 |
| KR102692309B1 (ko) | 2019-01-15 | 2024-08-07 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| JP7689964B2 (ja) | 2019-12-13 | 2025-06-09 | インスピルナ，インコーポレーテッド | 金属塩及びその使用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1062357A (en) * | 1965-03-23 | 1967-03-22 | Pfizer & Co C | Quinazolone derivatives |
| BE792206A (de) * | 1971-12-02 | 1973-06-01 | Byk Gulden Lomberg Chem Fab | |
| US3867384A (en) * | 1972-09-01 | 1975-02-18 | Greg A Bullock | 2-Amino-4(3H)-quinazolinones |
| RU2139862C1 (ru) * | 1993-05-12 | 1999-10-20 | Е.И. Дю Пон де Немурс энд Компани | Замещенные 4(3н)-хиназолиноны, обладающие фунгицидными свойствами, композиции на их основе и способы борьбы с мучнистой росой |
| AU7692996A (en) * | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Receptor antagonists |
| JP2004520299A (ja) * | 2000-12-12 | 2004-07-08 | ニューロジェン・コーポレーション | スピロ［イソベンゾフラン−１，４’−ピペリジン］−３−オン類及び３ｈ−スピロイソベンゾフラン−１，４’−ピペリジン類 |
| EP1363913A2 (de) * | 2001-02-05 | 2003-11-26 | Dr. Reddy's Laboratories Ltd. | Salze von pyrimidin derivaten zur verwendung gegen coronare herzkrankheit und atherosclerose |
| PT1551834E (pt) * | 2002-05-23 | 2010-09-30 | Novartis Vaccines & Diagnostic | Compostos de quinazolinona substituídos |
-
2002
- 2002-09-10 EP EP20020020255 patent/EP1407774A1/de not_active Withdrawn
-
2003
- 2003-07-02 WO PCT/EP2003/007067 patent/WO2004024162A1/en not_active Ceased
- 2003-07-02 JP JP2004535046A patent/JP2006502169A/ja not_active Withdrawn
- 2003-07-02 AU AU2003296861A patent/AU2003296861A1/en not_active Abandoned
- 2003-07-02 CA CA002498655A patent/CA2498655A1/en not_active Abandoned
- 2003-09-10 WO PCT/EP2003/010036 patent/WO2004024161A1/en not_active Ceased
- 2003-09-10 AU AU2003271595A patent/AU2003271595A1/en not_active Abandoned
- 2003-09-10 DE DE60305193T patent/DE60305193T2/de not_active Expired - Lifetime
- 2003-09-10 EP EP03753402A patent/EP1536799B1/de not_active Expired - Lifetime
- 2003-09-10 AT AT03753402T patent/ATE325609T1/de not_active IP Right Cessation
-
2005
- 2005-03-09 US US11/076,163 patent/US20050261319A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1536799A1 (de) | 2005-06-08 |
| DE60305193T2 (de) | 2007-06-14 |
| JP2006502169A (ja) | 2006-01-19 |
| EP1536799B1 (de) | 2006-05-10 |
| DE60305193D1 (de) | 2006-06-14 |
| CA2498655A1 (en) | 2004-03-25 |
| AU2003271595A1 (en) | 2004-04-30 |
| WO2004024161A1 (en) | 2004-03-25 |
| AU2003296861A1 (en) | 2004-04-30 |
| WO2004024162A1 (en) | 2004-03-25 |
| US20050261319A1 (en) | 2005-11-24 |
| EP1407774A1 (de) | 2004-04-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |