HUP9901153A2 - Atherosclerosis kezelésére alkalmas szubsztituált 2-oxo-azetidinek, előállításuk és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Atherosclerosis kezelésére alkalmas szubsztituált 2-oxo-azetidinek, előállításuk és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP9901153A2 HUP9901153A2 HU9901153A HUP9901153A HUP9901153A2 HU P9901153 A2 HUP9901153 A2 HU P9901153A2 HU 9901153 A HU9901153 A HU 9901153A HU P9901153 A HUP9901153 A HU P9901153A HU P9901153 A2 HUP9901153 A2 HU P9901153A2
- Authority
- HU
- Hungary
- Prior art keywords
- substituted
- alkylene
- heteroarylalkyl
- aryl
- alkyl
- Prior art date
Links
- 201000001320 Atherosclerosis Diseases 0.000 title 1
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical class O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000002947 alkylene group Chemical group 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 102000016752 1-Alkyl-2-acetylglycerophosphocholine Esterase Human genes 0.000 abstract 1
- 108010024976 Asparaginase Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000004419 alkynylene group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 125000001424 substituent 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
-
- 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
- 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
- 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
- C07D205/085—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 nitrogen atom directly attached in position 3
-
- 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
- C07D205/095—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 and with a nitrogen atom directly attached in position 3
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
A találmány szerinti (I) általánős képletű vegyületek (I) - amelyek képletében R1 és R2 egymástól függetlenül hidrőgén-,halőgénatőm vagy alkilcsőpőrt; R4 és R5 egymástól függetlenül hidrőgénatőm, alkil-, alkenil-, aril-,aril-alkil- és heterőaril-alkil-csőpőrt, amelyek mindegyike adőttesetben szűbsztitűált lehet, vagy R4 és R5 a közös szénatőmmal együtt ciklőalkiléncsőpőrtőt képez; X közvetlen kötés, -X1(CH2)m-, amelyben X1 -CO-, -COO-, -CONR6-, -CONR6CO- vagy -CONR6O-, ahől R6 hidrőgénatőmvagy alkilcsőpőrt, és X2 alkiléncsőpőrt, amelyet az alkilénláncőn belül vagy az Yszűbsztitűenssel szőmszédős láncvégen egy vagy több alkenilén- vagyalkiniléncsőpőrt, vagy alkiléncsőpőrttal megszakítőtt lehet, Y adőtt esetben szűbsztitűált arilcsőpőrt; Z őxigénatőm, és R3 alkil-, ciklőalkil-, ciklőalkil-alkil-, heterőaril-, heterőaril-alkil-, aril- vagy aril-alkil-csőpőrt, amelyek mindegyike adőttesetben szűbsztitűált lehet, vagy Z -S(O)n-, amelyben R3 heterőaril- vagy heterőaril-alkil-csőpőrt, amelyek mindegyike adőttesetben szűbsztitűált lehet -, amelyek az Lp PLA2 enzim inhibitőrai. ŕ
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9513442.5A GB9513442D0 (en) | 1995-07-01 | 1995-07-01 | Novel compounds |
GBGB9515056.1A GB9515056D0 (en) | 1995-07-22 | 1995-07-22 | Novel compounds |
GBGB9515206.2A GB9515206D0 (en) | 1995-07-25 | 1995-07-25 | Novel compounds |
GBGB9516985.0A GB9516985D0 (en) | 1995-08-18 | 1995-08-18 | Novel compounds |
GBGB9525132.8A GB9525132D0 (en) | 1995-12-08 | 1995-12-08 | Novel compounds |
GBGB9608650.9A GB9608650D0 (en) | 1996-04-26 | 1996-04-26 | Novel compounds |
GBGB9608651.7A GB9608651D0 (en) | 1996-04-26 | 1996-04-26 | Novel compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP9901153A2 true HUP9901153A2 (hu) | 1999-08-30 |
HUP9901153A3 HUP9901153A3 (en) | 1999-11-29 |
Family
ID=27562921
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU9901153A HUP9901153A3 (en) | 1995-07-01 | 1996-06-20 | Azetidinone derivatives for the treatment of atherosclerosis, their production and pharmaceutical compositions containing them |
Country Status (23)
Country | Link |
---|---|
EP (1) | EP0840725A1 (hu) |
JP (1) | JP2002515852A (hu) |
KR (1) | KR19990028630A (hu) |
CN (1) | CN1197452A (hu) |
AP (1) | AP728A (hu) |
AU (1) | AU708032B2 (hu) |
BG (1) | BG102214A (hu) |
BR (1) | BR9609445A (hu) |
CA (1) | CA2225627A1 (hu) |
CZ (1) | CZ422197A3 (hu) |
EA (1) | EA199800109A1 (hu) |
HU (1) | HUP9901153A3 (hu) |
IL (1) | IL122650A0 (hu) |
MA (1) | MA23922A1 (hu) |
MX (1) | MX9800186A (hu) |
NO (1) | NO976158L (hu) |
NZ (1) | NZ311684A (hu) |
OA (1) | OA10648A (hu) |
PE (1) | PE8998A1 (hu) |
PL (1) | PL324240A1 (hu) |
SK (1) | SK178497A3 (hu) |
TR (1) | TR199701762T1 (hu) |
WO (1) | WO1997002242A1 (hu) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
BR9709196A (pt) * | 1996-04-26 | 1999-05-25 | Smithkline Beecham Plc | Derivados de azetidinona para o tratamento de aterosclerose |
GB9608649D0 (en) * | 1996-04-26 | 1996-07-03 | Smithkline Beecham Plc | Novel compounds |
WO2001060805A1 (en) | 2000-02-16 | 2001-08-23 | Smithkline Beecham P.L.C. | Pyrimidine-4-one derivatives as ldl-pla2 inhibitors |
GB0024808D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
KR101461659B1 (ko) | 2007-05-11 | 2014-11-17 | 토마스 제퍼슨 유니버시티 | 신경변성 질환 및 장애의 치료 및 예방 방법 |
WO2008141176A1 (en) | 2007-05-11 | 2008-11-20 | The Trustees Of The University Of Pennsylvania | Methods of treatment of skin ulcers |
US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
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 |
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 |
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 |
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 (5)
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 |
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 |
-
1996
- 1996-06-20 PL PL96324240A patent/PL324240A1/xx unknown
- 1996-06-20 NZ NZ311684A patent/NZ311684A/xx unknown
- 1996-06-20 CA CA002225627A patent/CA2225627A1/en not_active Abandoned
- 1996-06-20 AU AU63050/96A patent/AU708032B2/en not_active Ceased
- 1996-06-20 HU HU9901153A patent/HUP9901153A3/hu unknown
- 1996-06-20 SK SK1784-97A patent/SK178497A3/sk unknown
- 1996-06-20 JP JP50477297A patent/JP2002515852A/ja active Pending
- 1996-06-20 WO PCT/EP1996/002765 patent/WO1997002242A1/en not_active Application Discontinuation
- 1996-06-20 TR TR97/01762T patent/TR199701762T1/xx unknown
- 1996-06-20 BR BR9609445A patent/BR9609445A/pt unknown
- 1996-06-20 CZ CZ974221A patent/CZ422197A3/cs unknown
- 1996-06-20 KR KR1019970709952A patent/KR19990028630A/ko not_active Application Discontinuation
- 1996-06-20 CN CN96196661A patent/CN1197452A/zh active Pending
- 1996-06-20 AP APAP/P/1997/001161A patent/AP728A/en active
- 1996-06-20 EA EA199800109A patent/EA199800109A1/ru unknown
- 1996-06-20 EP EP96922030A patent/EP0840725A1/en not_active Withdrawn
- 1996-06-20 IL IL12265096A patent/IL122650A0/xx unknown
- 1996-06-28 PE PE1996000496A patent/PE8998A1/es not_active Application Discontinuation
- 1996-06-28 MA MA24298A patent/MA23922A1/fr unknown
-
1997
- 1997-12-30 NO NO976158A patent/NO976158L/no unknown
- 1997-12-31 OA OA70172A patent/OA10648A/en unknown
-
1998
- 1998-01-07 MX MX9800186A patent/MX9800186A/es unknown
- 1998-01-28 BG BG102214A patent/BG102214A/xx unknown
Also Published As
Publication number | Publication date |
---|---|
NO976158L (no) | 1998-02-25 |
SK178497A3 (en) | 1998-07-08 |
JP2002515852A (ja) | 2002-05-28 |
PL324240A1 (en) | 1998-05-11 |
EP0840725A1 (en) | 1998-05-13 |
WO1997002242A1 (en) | 1997-01-23 |
BG102214A (en) | 1998-08-31 |
CN1197452A (zh) | 1998-10-28 |
AU708032B2 (en) | 1999-07-29 |
EA199800109A1 (ru) | 1998-10-29 |
AU6305096A (en) | 1997-02-05 |
HUP9901153A3 (en) | 1999-11-29 |
PE8998A1 (es) | 1998-03-20 |
KR19990028630A (ko) | 1999-04-15 |
CA2225627A1 (en) | 1997-01-23 |
NO976158D0 (no) | 1997-12-30 |
CZ422197A3 (cs) | 1998-06-17 |
BR9609445A (pt) | 1999-04-06 |
IL122650A0 (en) | 1998-08-16 |
TR199701762T1 (xx) | 1998-05-21 |
MA23922A1 (fr) | 1996-12-31 |
AP9701161A0 (en) | 1998-01-31 |
MX9800186A (es) | 1998-07-31 |
OA10648A (en) | 2002-09-25 |
AP728A (en) | 1999-01-29 |
NZ311684A (en) | 2000-04-28 |
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