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)
- 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)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 |
|---|---|---|---|---|
| CA2518465A1 (en) * | 2003-03-25 | 2004-10-14 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US20060281088A1 (en) * | 2003-05-21 | 2006-12-14 | Wright Matthew B | Markers for lxr activation |
| EP1646615B1 (de) | 2003-06-06 | 2009-08-26 | Vertex Pharmaceuticals Incorporated | 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) |
| 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) |
| EP1776350B1 (de) * | 2004-08-06 | 2013-01-23 | Janssen Pharmaceutica NV | NEUE, ALS INHIBITOREN VON ß-SECRETASE (BACE) NÜTZLICHE 2-AMINO-CHINAZOLINDERIVATE |
| US8426429B2 (en) | 2004-08-06 | 2013-04-23 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| WO2006045010A2 (en) * | 2004-10-20 | 2006-04-27 | Resverlogix Corp. | Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases |
| US7989179B2 (en) | 2005-06-28 | 2011-08-02 | Daiichi Sankyo Company, Limited | LXR ligand testing method |
| US8410109B2 (en) * | 2005-07-29 | 2013-04-02 | Resverlogix Corp. | Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices |
| EP1966198B1 (de) | 2005-10-25 | 2011-03-16 | Janssen Pharmaceutica NV | Als inhibitoren von beta-sekretase (bace) geeignete 2-amino-3,4-dihydropyrido[3,4-d]pyrimidinderivate |
| US7932261B2 (en) | 2006-02-06 | 2011-04-26 | Janssen Pharmaceutica Nv | Macrocycle derivatives useful as inhibitors of β-secretase (BACE) |
| US7868022B2 (en) | 2006-02-06 | 2011-01-11 | Janssen Pharmaceutica Nv | 2-amino-quinoline 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) |
| KR20090086084A (ko) | 2006-11-30 | 2009-08-10 | 코와 가부시키가이샤 | 치환 카르비놀 화합물 |
| 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) |
| EP2240472B1 (de) | 2008-01-29 | 2012-11-21 | Janssen Pharmaceutica NV | Als inhibitoren von beta-sekretase (bace) geeignete 2-aminochinolinderivate |
| 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 |
| JP5371118B2 (ja) | 2008-04-30 | 2013-12-18 | 興和株式会社 | キノリン化合物 |
| AU2009252615B2 (en) | 2008-05-29 | 2013-08-15 | Kowa Company, Ltd. | Substituted carbinol compound having cyclic linker |
| SI2346837T1 (sl) | 2008-06-26 | 2015-05-29 | Resverlogix Corporation | Postopki pripravljanja kinazolinonskih derivatov |
| US8952021B2 (en) | 2009-01-08 | 2015-02-10 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular disease |
| KR101913109B1 (ko) | 2009-03-18 | 2018-10-31 | 리스버로직스 코퍼레이션 | 신규한 소염제 |
| EP2414521B1 (de) * | 2009-03-31 | 2016-10-26 | The General Hospital Corporation | Regulierung von mir-33-mikrornas bei der behandlung cholesterinspiegelbedingter erkrankungen |
| US9757368B2 (en) | 2009-04-22 | 2017-09-12 | Resverlogix Corp. | Anti-inflammatory agents |
| KR101671046B1 (ko) | 2009-04-29 | 2016-10-31 | 코와 가부시키가이샤 | 헤테로환 링커를 갖는 카르비놀 화합물 |
| WO2012033353A2 (ko) | 2010-09-07 | 2012-03-15 | 서울대학교 산학협력단 | 세스터터핀 화합물 및 이들 물질의 용도 |
| EP2545964A1 (de) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Neuartige FXR- (NR1H4)-Binde- und -Aktivitätsmodulationsverbindungen |
| CA2851996C (en) | 2011-11-01 | 2020-01-07 | Resverlogix Corp. | Pharmaceutical compositions for substituted quinazolinones |
| 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 |
| WO2015106164A1 (en) | 2014-01-10 | 2015-07-16 | Rgenix, Inc. | Lxr agonists and uses thereof |
| US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
| EP3402477A4 (de) | 2016-01-11 | 2019-08-21 | The Rockefeller University | Verfahren zur behandlung von erkrankungen im zusammenhang mit aus myeloid abgeleiteten suppressorzellen |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| SI4122464T1 (sl) | 2017-03-28 | 2024-07-31 | Gilead Sciences, Inc. | Terapevtske kombinacije za zdravljenje bolezni jeter |
| CA3078981A1 (en) | 2017-11-21 | 2019-05-31 | Rgenix, Inc. | Polymorphs and uses thereof |
| KR20210039368A (ko) | 2018-07-26 | 2021-04-09 | 도메인 테라퓨틱스 | 치환된 퀴나졸리논 유도체 및 mGluR4의 양성 알로스테릭 조절인자로서의 이의 용도 |
| PT3911647T (pt) | 2019-01-15 | 2024-03-04 | Gilead Sciences Inc | Composto de isoxazole como agonista de fxr e composições farmacêuticas que o contenham |
| JP2022519906A (ja) | 2019-02-19 | 2022-03-25 | ギリアード サイエンシーズ， インコーポレイテッド | Ｆｘｒアゴニストの固体形態 |
| TWI888447B (zh) | 2019-12-13 | 2025-07-01 | 美商因思博納公司 | 金屬鹽及其用途 |
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 |
| WO1994026722A1 (en) * | 1993-05-12 | 1994-11-24 | E.I. Du Pont De Nemours And Company | Fungicidal fused bicyclic pyrimidinones |
| AU7692996A (en) * | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Receptor antagonists |
| EP1347982B1 (de) * | 2000-12-12 | 2005-11-16 | Neurogen Corporation | Spiro[isobenzofuran-1,4'-piperidin]-3-one und 3h-spiroisobenzofuran-1,4'-piperidine |
| JP2004520393A (ja) * | 2001-02-05 | 2004-07-08 | ドクター・レディーズ・ラボラトリーズ・リミテッド | ヘテロ環化号物の薬学的に許容可能な塩 |
| 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 AU AU2003296861A patent/AU2003296861A1/en not_active Abandoned
- 2003-07-02 CA CA002498655A patent/CA2498655A1/en not_active Abandoned
- 2003-07-02 WO PCT/EP2003/007067 patent/WO2004024162A1/en not_active Ceased
- 2003-07-02 JP JP2004535046A patent/JP2006502169A/ja not_active Withdrawn
- 2003-09-10 AT AT03753402T patent/ATE325609T1/de not_active IP Right Cessation
- 2003-09-10 WO PCT/EP2003/010036 patent/WO2004024161A1/en not_active Ceased
- 2003-09-10 EP EP03753402A patent/EP1536799B1/de not_active Expired - Lifetime
- 2003-09-10 DE DE60305193T patent/DE60305193T2/de not_active Expired - Lifetime
- 2003-09-10 AU AU2003271595A patent/AU2003271595A1/en not_active Abandoned
-
2005
- 2005-03-09 US US11/076,163 patent/US20050261319A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003296861A1 (en) | 2004-04-30 |
| EP1536799B1 (de) | 2006-05-10 |
| JP2006502169A (ja) | 2006-01-19 |
| CA2498655A1 (en) | 2004-03-25 |
| WO2004024162A1 (en) | 2004-03-25 |
| DE60305193T2 (de) | 2007-06-14 |
| DE60305193D1 (de) | 2006-06-14 |
| US20050261319A1 (en) | 2005-11-24 |
| WO2004024161A1 (en) | 2004-03-25 |
| AU2003271595A1 (en) | 2004-04-30 |
| EP1536799A1 (de) | 2005-06-08 |
| 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 |