PE64398A1 - Derivados de azetidinona - Google Patents

Derivados de azetidinona

Info

Publication number
PE64398A1
PE64398A1 PE1997000311A PE00031197A PE64398A1 PE 64398 A1 PE64398 A1 PE 64398A1 PE 1997000311 A PE1997000311 A PE 1997000311A PE 00031197 A PE00031197 A PE 00031197A PE 64398 A1 PE64398 A1 PE 64398A1
Authority
PE
Peru
Prior art keywords
formula
compounds
compound
carbonyloxymethyl
conh
Prior art date
Application number
PE1997000311A
Other languages
English (en)
Inventor
Deirdre Mary Bernadette Hickey
Dashyant Dhanak
Robert John Ife
Colin Andrew Leach
Colin Theobald
Original Assignee
Smithkline Beecham Plc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9608646.7A external-priority patent/GB9608646D0/en
Priority claimed from GBGB9623756.5A external-priority patent/GB9623756D0/en
Priority claimed from GBGB9625121.0A external-priority patent/GB9625121D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of PE64398A1 publication Critical patent/PE64398A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • 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

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I) Y A LOS COMPUESTOS INTERMEDIOS DE FORMULA (VI), EN DONDE: R1 ES DE PREFERENCIA H, ISOBUTIRILOXIMETILO, FENILCARBONILOXIMETILO, 4-METOXIFENIL-CARBONILOXIMETILO, TER-BUTILOXICARBONILOXIMETILO, CICLOHEXILOXI-CARBONILOXIMETILO, 1-METILCICLOHEXILOXICARBONILOXIMETILO, N,N-DIMETILAMINOCARBONILMETILO O (5-METIL-2-OXO-1,3-DIOXOLEN-4-IL)METILO; R2, R3 Y R4 SON H O ALQUILO C1-C6; "X" ES X`(CH2)m (m ES 0; 1; 2; 3; 4; 5; 6; 7; 8; 9; 10; 11 o 12, SIENDO m DE PREFERENCIA 6) O ES UNA CADENA ALQUILENO C1-C12 INTERRUMPIDA OPCIONALMENTE POR X', EN DONDE X' ES CO, CONR4, COO, CONR4CO, CONHO o CH2O; "Y" ES FENILO OPCIONALMENTE SUSTITUIDO; SIENDO DE PREFERENCIA DICHA UNION "X-Y" CONH-(CH2)6Ph(4-F)/(4-Cl); R* ES R1 O UN GRUPO PROTECTOR CARBOXI, COMO: ALQUILO C1-C6 O ALQUENILO C2-C6. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LOS COMPUESTOS DE FORMULA (I) EN DONDE "X" ES CONH, QUE COMPRENDE: TRATAR EL COMPUESTO (I) EN DONDE "X-Y" ES COOH, CON NH2(CH2)nY, EN PRESENCIA DE UN AGENTE DE ACTIVACION, Y DEL COMPUESTO INTERMEDIO (VI), QUE COMPRENDE: FORMAR UNA SAL DIASTEROISOMERICA CON UNA BASE QUIRAL TAL COMO (-)-CINCONIDINA. LOS COMPUESTOS DE FORMULA (I) ACTUAN COMO INHIBIDORES DE LA Lp-PLA2, ENZIMA RESPONSABLE DE LA PEROXIDACION DE LA FOSFATIDILCOLINA, SIENDO UTIL EN EL TRATAMIENTO DE LA ATEROSCLEROSIS
PE1997000311A 1996-04-26 1997-04-24 Derivados de azetidinona PE64398A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9608646.7A GB9608646D0 (en) 1996-04-26 1996-04-26 Novel compounds
GBGB9623756.5A GB9623756D0 (en) 1996-11-15 1996-11-15 Novel compounds
GBGB9625121.0A GB9625121D0 (en) 1996-12-03 1996-12-03 Novel compounds

Publications (1)

Publication Number Publication Date
PE64398A1 true PE64398A1 (es) 1999-01-06

Family

ID=27268259

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000311A PE64398A1 (es) 1996-04-26 1997-04-24 Derivados de azetidinona

Country Status (17)

Country Link
EP (1) EP0915843A1 (es)
JP (1) JP2000509049A (es)
AR (1) AR006833A1 (es)
AU (1) AU2698697A (es)
BR (1) BR9709196A (es)
CA (1) CA2252696A1 (es)
CZ (1) CZ341098A3 (es)
HU (1) HUP9901359A3 (es)
ID (1) ID16660A (es)
IL (1) IL126696A0 (es)
MA (1) MA26426A1 (es)
NO (1) NO984939L (es)
NZ (1) NZ332476A (es)
PE (1) PE64398A1 (es)
PL (1) PL329530A1 (es)
TR (1) TR199802160T2 (es)
WO (1) WO1997041098A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001060805A1 (en) 2000-02-16 2001-08-23 Smithkline Beecham P.L.C. Pyrimidine-4-one derivatives as ldl-pla2 inhibitors
IL157552A0 (en) 2001-03-28 2004-03-28 Schering Corp Enantioselective synthesis of azetidinone intermediate compounds
US20030013699A1 (en) * 2001-05-25 2003-01-16 Davis Harry R. Methods for treating alzheimer's disease and/or regulating levels of amyloid beta peptides in a subject
KR101461659B1 (ko) 2007-05-11 2014-11-17 토마스 제퍼슨 유니버시티 신경변성 질환 및 장애의 치료 및 예방 방법
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
WO2008141176A1 (en) 2007-05-11 2008-11-20 The Trustees Of The University Of Pennsylvania Methods of treatment of skin ulcers
JP5886310B2 (ja) 2010-12-06 2016-03-16 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｌｐ−ＰＬＡ２により媒介される疾患または状態の処置における使用のためのピリミジノン化合物
EP2651403B1 (en) 2010-12-17 2020-12-02 Glaxo Group Limited Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases
CN103619831B (zh) 2011-06-27 2016-05-04 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
BR112014001665A2 (pt) 2011-07-27 2017-02-14 Glaxo Group Ltd compostos de 2,3-di-hidroimidazo[1,2-c]pirimidin-5(1h)-ona utilizados como inibidores de lp-plaz
RU2014107486A (ru) 2011-07-27 2015-09-10 Глэксо Груп Лимитед Бициклические пиримидоновые соединения
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
UY35276A (es) 2013-01-25 2014-08-29 Glaxosmithkline Ip Dev Ltd Nuevos compuestos que inhiben la actividad de Lp-PLA2
WO2014114248A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Compounds
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
CN112778331B (zh) 2019-11-09 2022-07-05 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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4680391A (en) * 1983-12-01 1987-07-14 Merck & Co., Inc. Substituted azetidinones as anti-inflammatory and antidegenerative agents
IL89835A0 (en) * 1988-04-11 1989-12-15 Merck & Co Inc Substituted azetidinones,their preparation and pharmaceutical compositions containing them
IL99658A0 (en) * 1990-10-15 1992-08-18 Merck & Co Inc Substituted azetidinones and pharmaceutical compositions containing them
WO1993000332A1 (en) * 1991-06-25 1993-01-07 Merck & Co., Inc. Substituted azetidinones as anti-inflammatory and antidegenerative agents
EP0524595A1 (en) * 1991-07-23 1993-01-27 Schering Corporation Substituted beta-lactam compounds useful as hypocholesterolemic agents and processes for the preparation thereof
MY128261A (en) * 1992-10-27 2007-01-31 Merck Sharp & Dohme New substituted azetidinones as anti-inflammatory and antidegenerative agents
AU5802894A (en) * 1992-12-17 1994-07-04 Merck & Co., Inc. New substituted azetidinones as anti-inflammatory and antidegenerative agents
US5981252A (en) * 1993-06-25 1999-11-09 Smithkline Beecham Lipoprotein associated phospholipase A2, inhibitors thereof and use of the same in diagnosis and therapy
US5641669A (en) * 1993-10-06 1997-06-24 Icos Corporation Platelet-activating factor acetylhydrolase
GB9421816D0 (en) * 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
PL320937A1 (en) * 1994-12-22 1997-11-10 Smithkline Beecham Plc Substituted azetidin-2-ones for treating arterial atheromatosis
WO1996029307A1 (fr) * 1995-03-23 1996-09-26 Japan Tobacco Inc. Composes de diphenylmethyle-azetidinone et inhibiteur d'elastase
PL324240A1 (en) * 1995-07-01 1998-05-11 Smithkline Beecham Plc Derivatives of azetidinone for treating atherosclerosis
WO1997021676A1 (en) * 1995-12-08 1997-06-19 Smithkline Beecham Plc Azetidinone compounds for the treatment of atherosclerosis

Also Published As

Publication number Publication date
JP2000509049A (ja) 2000-07-18
NZ332476A (en) 2000-06-23
HUP9901359A2 (hu) 1999-08-30
NO984939D0 (no) 1998-10-23
CZ341098A3 (cs) 1999-03-17
WO1997041098A1 (en) 1997-11-06
EP0915843A1 (en) 1999-05-19
AU2698697A (en) 1997-11-19
PL329530A1 (en) 1999-03-29
NO984939L (no) 1998-12-23
HUP9901359A3 (en) 2000-03-28
IL126696A0 (en) 1999-08-17
ID16660A (id) 1997-10-30
TR199802160T2 (xx) 1999-04-21
BR9709196A (pt) 1999-05-25
CA2252696A1 (en) 1997-11-06
AR006833A1 (es) 1999-09-29
MA26426A1 (fr) 2004-12-20

Similar Documents

Publication Publication Date Title
PE64398A1 (es) Derivados de azetidinona
PE20001047A1 (es) METODO PARA TRATAR ATEROESCLEROSIS EMPLEANDO UN INHIBIDOR DE aP2 Y COMBINACION
NO20020214D0 (no) Substituerte oksozaheterocyklylforbindelser
ATE226193T1 (de) Substituierte zyklische amine als metalloproteaseinhibitoren
PE44599A1 (es) Inhibidores de la enzima acido nitrico sintasa
MXPA04001323A (es) Dihidro-3-halo-1h-pirazol-5-carboxilatos sustituidos, su preparacion y uso.
KR100263496B1 (ko) 탁솔 유도체 및 이의 제조방법
ES2185054T3 (es) Derivados de benzopirano.
ID26622A (id) Senyawa-senyawa pengganti 2-benzylamino-2-phenyl-acetamide
DE69730817D1 (de) Dihydrobenzofuranderivate verwendbar als entzündungshemmende mittel
NO970340L (no) Organiske forbindelser
ES2163730T3 (es) Derivados espirocetales y su uso como agentes terapeuticos.
NO983531L (no) Dihydrobenzofuranforbindelser anvendelig som anti-inflammatoriske midler
NZ505200A (en) Carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists
FR2798931B1 (fr) Nouveaux composes indoliques, leur utilisation pour la teinture et le maquillage des matieres keratiniques, compositions les contenant et procedes de teinture
PT1280779E (pt) Novos indanilimidazois policiclicos com actividade adrenergica alfa2
EA199800931A1 (ru) Способ получения ингибиторов фосфодиэстеразы iv
MA25495A1 (fr) Compositions contenant des esters pour traiter les infestations parasitiques d'organismes
ECSP982365A (es) Antagonistas de taquiquinina
ATE346615T1 (de) Mittel zur verbesserung der gewebepenetration

Legal Events

Date Code Title Description
FA Abandonment or withdrawal