BR9510420A - Azetidin-2-onas substituìdas para o tratamento de aterosclerose - Google Patents
Azetidin-2-onas substituìdas para o tratamento de ateroscleroseInfo
- Publication number
- BR9510420A BR9510420A BR9510420-8A BR9510420A BR9510420A BR 9510420 A BR9510420 A BR 9510420A BR 9510420 A BR9510420 A BR 9510420A BR 9510420 A BR9510420 A BR 9510420A
- Authority
- BR
- Brazil
- Prior art keywords
- azetidin
- ones
- replaced
- atherosclerosis
- treatment
- Prior art date
Links
- 201000001320 Atherosclerosis Diseases 0.000 title abstract 3
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical class O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 102000016752 1-Alkyl-2-acetylglycerophosphocholine Esterase Human genes 0.000 abstract 1
- 108010024976 Asparaginase Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
- C07D205/09—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a sulfur atom directly attached in position 4
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"AZETIDIN-2-ONAS SUBSTITUìDAS PARA O TRATAMENTO DE ATEROSCLEROSE". Compostos de fórmula (I) em que R1 e R2 podem ser iguais ou diferentes, é cada selecionado dentre hidrogênio, halogênio, ou alquila C1-8, R3 é arila ou aril alquila C(1-4), que podem ser opcionalmente substituídos, X é um grupo ligador, Y é um grupo arila opcionalmente substituído, e n é 0, 1 ou 2, são inibidores da enzima Lp-PLA2 e seu uso no tratamento de aterosclerose.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9426020.5A GB9426020D0 (en) | 1994-12-22 | 1994-12-22 | Novel compounds |
| GBGB9426030.4A GB9426030D0 (en) | 1994-12-23 | 1994-12-23 | Novel compounds |
| GBGB9511600.0A GB9511600D0 (en) | 1995-06-08 | 1995-06-08 | Novel compounds |
| GBGB9511599.4A GB9511599D0 (en) | 1995-06-08 | 1995-06-08 | Novel compounds |
| PCT/EP1995/005130 WO1996019451A1 (en) | 1994-12-22 | 1995-12-20 | Substituted azetidin-2-ones for treatment of atherosclerosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9510420A true BR9510420A (pt) | 2004-04-20 |
Family
ID=27451242
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9510420-8A BR9510420A (pt) | 1994-12-22 | 1995-12-20 | Azetidin-2-onas substituìdas para o tratamento de aterosclerose |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US5990102A (pt) |
| EP (1) | EP0799200A1 (pt) |
| JP (1) | JPH11500415A (pt) |
| CN (1) | CN1175246A (pt) |
| AP (1) | AP9701007A0 (pt) |
| AR (1) | AR002012A1 (pt) |
| AU (1) | AU704407B2 (pt) |
| BG (1) | BG101687A (pt) |
| BR (1) | BR9510420A (pt) |
| CA (1) | CA2208530A1 (pt) |
| CZ (1) | CZ192297A3 (pt) |
| DZ (1) | DZ1958A1 (pt) |
| FI (1) | FI972584L (pt) |
| HU (1) | HUT77089A (pt) |
| IL (1) | IL116485A0 (pt) |
| MA (1) | MA23834A1 (pt) |
| MX (1) | MX9704736A (pt) |
| NO (1) | NO972909L (pt) |
| NZ (1) | NZ298416A (pt) |
| OA (1) | OA10737A (pt) |
| PL (1) | PL320937A1 (pt) |
| SK (1) | SK80397A3 (pt) |
| TR (1) | TR199501655A2 (pt) |
| WO (1) | WO1996019451A1 (pt) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1197452A (zh) * | 1995-07-01 | 1998-10-28 | 史密丝克莱恩比彻姆有限公司 | 用于治疗动脉粥样硬化的氮杂环丁烷酮衍生物 |
| JP2000505063A (ja) * | 1995-12-08 | 2000-04-25 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | アテローム性動脈硬化症の治療のためのアゼチジノン化合物 |
| JP2000502079A (ja) * | 1995-12-08 | 2000-02-22 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | アテローム性動脈硬化症の治療のための単環β―ラクタム誘導体 |
| CA2252696A1 (en) * | 1996-04-26 | 1997-11-06 | Deirdre Mary Bernadette Hickey | Azetidinone derivatives for the treatment of atherosclerosis |
| GB9608649D0 (en) * | 1996-04-26 | 1996-07-03 | Smithkline Beecham Plc | Novel compounds |
| AU4654199A (en) * | 1998-07-23 | 2000-02-14 | Shionogi & Co., Ltd. | Monocyclic beta-lactam compounds and chymase inhibitors containing the same |
| AU2001235466B2 (en) | 2000-02-16 | 2004-04-22 | Glaxo Group Limited | Pyrimidine-4-one derivatives as LDL-PLA2 inhibitors |
| GB0024808D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| US6982251B2 (en) * | 2000-12-20 | 2006-01-03 | Schering Corporation | Substituted 2-azetidinones useful as hypocholesterolemic agents |
| SI1413331T1 (sl) | 2001-01-26 | 2008-02-29 | Schering Corp | Kombinacije fenofibrata peroksisomskega proliferator aktivirajocega receptorja (PPAR) z ezetimib zaviralcem absorpcije sterola za vaskularne indikacije |
| RS50406B (sr) | 2001-01-26 | 2009-12-31 | Schering Corporation, | Upotreba supstituisanih jedinjenja azetidinona za lečenje sitosterolemije |
| US7071181B2 (en) | 2001-01-26 | 2006-07-04 | Schering Corporation | Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors |
| MXPA04002573A (es) | 2001-09-21 | 2004-06-18 | Schering Corp | Tratamiento de xantoma con derivados de azetidinona como inhibidores de la absorcion de esterol. |
| US7053080B2 (en) | 2001-09-21 | 2006-05-30 | Schering Corporation | Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors |
| EP1562582A1 (en) | 2002-11-06 | 2005-08-17 | Schering Corporation | Cholesterol absorption inhibitors for the treatment of demyelination |
| US7192944B2 (en) * | 2003-03-07 | 2007-03-20 | Schering Corp. | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| JP4589919B2 (ja) | 2003-03-07 | 2010-12-01 | シェーリング コーポレイション | 高コレステロール血症の処置のための、置換アゼチジノン化合物、これらの処方物および使用 |
| ES2311806T3 (es) | 2003-03-07 | 2009-02-16 | Schering Corporation | Compuesto de azetidinona sustituidos, fornulaciones y usos de los mismos para el tratamiento de hipercolesterolemia. |
| US7459442B2 (en) | 2003-03-07 | 2008-12-02 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| EP1747014A4 (en) * | 2004-05-03 | 2007-09-12 | Ilypsa Inc | MODULATION OF LYSOPHOSPHATIDYLCHOLINE AND TREATMENT OF CONDITIONS INDUCED BY A DIET |
| BRPI0810336A2 (pt) | 2007-05-11 | 2019-03-19 | The Trustees Of The University Of Pennsylvania | "método para tratar e/ou prevenir úlceras de pele em um indivíduo" |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| KR101730290B1 (ko) | 2007-05-11 | 2017-04-25 | 토마스 제퍼슨 유니버시티 | 신경변성 질환 및 장애의 치료 및 예방 방법 |
| CA2820408C (en) | 2010-12-06 | 2018-03-06 | Glaxo Group Limited | Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp-pla2 |
| WO2012080497A2 (en) | 2010-12-17 | 2012-06-21 | Glaxo Group Limited | Methods of treatment and prevention of eye diseases |
| WO2013000267A1 (zh) | 2011-06-27 | 2013-01-03 | 中国科学院上海药物研究所 | 唑类杂环化合物、其制备方法、药物组合物和用途 |
| JP2014521611A (ja) | 2011-07-27 | 2014-08-28 | グラクソ グループ リミテッド | Lp−PLA2阻害剤としての2,3−ジヒドロイミダゾ[1,2−c]ピリミジン−5(1H)−オン化合物の使用 |
| JP2014521625A (ja) | 2011-07-27 | 2014-08-28 | グラクソ グループ リミテッド | 二環式ピリミドン化合物 |
| WO2014114694A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors |
| JP2016505053A (ja) | 2013-01-25 | 2016-02-18 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | Lp‐PLA2の阻害剤としての二環式ピリミドン化合物 |
| CA2899124A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| WO2015179293A1 (en) * | 2014-05-18 | 2015-11-26 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Small molecule activators and inhibitors of lecithin: cholesterol acyltransferase |
| WO2016012917A1 (en) | 2014-07-22 | 2016-01-28 | Glaxosmithkline Intellectual Property Development Limited | 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2 |
| WO2016012916A1 (en) | 2014-07-22 | 2016-01-28 | Glaxosmithkline Intellectual Property Development Limited | 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2 |
| WO2021089032A1 (zh) | 2019-11-09 | 2021-05-14 | 上海赛默罗生物科技有限公司 | 三环二氢咪唑并嘧啶酮衍生物、其制备方法、药物组合物和用途 |
| CN115304620A (zh) | 2021-05-07 | 2022-11-08 | 上海赛默罗生物科技有限公司 | 嘧啶酮衍生物、其制备方法、药物组合物和用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0010358A1 (en) * | 1978-09-20 | 1980-04-30 | Glaxo Group Limited | Beta-lactam compounds, processes for their preparation, compositions containing them, intermediates of use in their preparation and methods for the production thereof |
| US4680391A (en) * | 1983-12-01 | 1987-07-14 | Merck & Co., Inc. | Substituted azetidinones as anti-inflammatory and antidegenerative agents |
| IL99658A0 (en) * | 1990-10-15 | 1992-08-18 | Merck & Co Inc | Substituted azetidinones and pharmaceutical compositions containing them |
-
1995
- 1995-12-20 SK SK803-97A patent/SK80397A3/sk unknown
- 1995-12-20 CN CN95197606A patent/CN1175246A/zh active Pending
- 1995-12-20 CA CA002208530A patent/CA2208530A1/en not_active Abandoned
- 1995-12-20 US US08/860,162 patent/US5990102A/en not_active Expired - Fee Related
- 1995-12-20 JP JP8519527A patent/JPH11500415A/ja active Pending
- 1995-12-20 PL PL95320937A patent/PL320937A1/xx unknown
- 1995-12-20 EP EP95942734A patent/EP0799200A1/en not_active Withdrawn
- 1995-12-20 DZ DZ950141A patent/DZ1958A1/fr active
- 1995-12-20 BR BR9510420-8A patent/BR9510420A/pt unknown
- 1995-12-20 MA MA24105A patent/MA23834A1/fr unknown
- 1995-12-20 MX MX9704736A patent/MX9704736A/es unknown
- 1995-12-20 AU AU43898/96A patent/AU704407B2/en not_active Ceased
- 1995-12-20 FI FI972584A patent/FI972584L/fi unknown
- 1995-12-20 WO PCT/EP1995/005130 patent/WO1996019451A1/en not_active Ceased
- 1995-12-20 CZ CZ971922A patent/CZ192297A3/cs unknown
- 1995-12-20 AP APAP/P/1997/001007A patent/AP9701007A0/en unknown
- 1995-12-20 HU HU9701948A patent/HUT77089A/hu unknown
- 1995-12-20 NZ NZ298416A patent/NZ298416A/xx unknown
- 1995-12-20 AR ARP950100660A patent/AR002012A1/es unknown
- 1995-12-21 IL IL11648595A patent/IL116485A0/xx unknown
- 1995-12-22 TR TR95/01655A patent/TR199501655A2/xx unknown
-
1997
- 1997-06-20 NO NO972909A patent/NO972909L/no unknown
- 1997-06-20 OA OA70034A patent/OA10737A/en unknown
- 1997-06-26 BG BG101687A patent/BG101687A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| FI972584A0 (fi) | 1997-06-17 |
| HUT77089A (hu) | 1998-03-02 |
| IL116485A0 (en) | 1996-08-04 |
| TR199501655A2 (tr) | 1996-07-21 |
| MX9704736A (es) | 1997-10-31 |
| AU704407B2 (en) | 1999-04-22 |
| CA2208530A1 (en) | 1996-06-27 |
| OA10737A (en) | 2002-12-10 |
| BG101687A (bg) | 1998-02-27 |
| PL320937A1 (en) | 1997-11-10 |
| FI972584A7 (fi) | 1997-08-19 |
| CN1175246A (zh) | 1998-03-04 |
| EP0799200A1 (en) | 1997-10-08 |
| AU4389896A (en) | 1996-07-10 |
| SK80397A3 (en) | 1998-01-14 |
| FI972584L (fi) | 1997-08-19 |
| NO972909L (no) | 1997-08-20 |
| US5990102A (en) | 1999-11-23 |
| NO972909D0 (no) | 1997-06-20 |
| DZ1958A1 (fr) | 2002-02-17 |
| NZ298416A (en) | 1999-03-29 |
| JPH11500415A (ja) | 1999-01-12 |
| MA23834A1 (fr) | 1996-10-01 |
| AP9701007A0 (en) | 1997-07-31 |
| CZ192297A3 (en) | 1997-11-12 |
| WO1996019451A1 (en) | 1996-06-27 |
| AR002012A1 (es) | 1998-01-07 |
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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] |