HUP0102981A2 - Pirrolo[1,2-a]pirazin-származékok és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Pirrolo[1,2-a]pirazin-származékok és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0102981A2 HUP0102981A2 HU0102981A HUP0102981A HUP0102981A2 HU P0102981 A2 HUP0102981 A2 HU P0102981A2 HU 0102981 A HU0102981 A HU 0102981A HU P0102981 A HUP0102981 A HU P0102981A HU P0102981 A2 HUP0102981 A2 HU P0102981A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- atoms
- hydrogen atom
- pyrrolo
- formula
- Prior art date
Links
- QSLLFYVBWXWUQT-UHFFFAOYSA-N 7-Azaindolizine Chemical class C1=NC=CN2C=CC=C21 QSLLFYVBWXWUQT-UHFFFAOYSA-N 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 2
- -1 oxamoyl- Chemical group 0.000 abstract 2
- 102000005473 Secretory Phospholipases A2 Human genes 0.000 abstract 1
- 108010031873 Secretory Phospholipases A2 Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Abstract
A találmány tárgyát, általános képletű sPLA2 inhibitor hatásúpirrolo[1,2-a] pirazin-származékok - ahol előnyösen R1 hidrogénatomvagy -(L1)-R6 általános képletű csoport, amelyben L1 1-18 atomos híd,és R6 adott esetben szubsztituált karbociklusos vagy heterociklusoscsoport; R2 hidrogénatom vagy a hidrogénatomoktól eltekintvelegfeljebb 4 atomos csoport, főként alkil- vagy cikloalkilcsoport; R3- (L2) - (sav) általános képletű csoport, amelyben L2 1-5 atomhosszúságú híd, főleg -O-CH2- képletű csoport, a sav pedig karboxi-,szulfo- vagy foszfonocsoport; R4 és R5 hidrogénatom vagy közömbösszubsztituens; és RA oxamoil-, karbamoil-metil- vagy karbazoil-metilcsoport - és prodrugjaik, gyógyszerészetileg elfogadható sóikvagy szolvátjaik, ezeket tartalmazó gyógyszerkészítmények képezik. Afenti vegyületek a gyógyászatban SPLA2 inhibitorként különösengyulladásos betegségek kezelésére vagy megelőzésére alkalmazhatók. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP8599798 | 1998-03-31 | ||
JP24473598 | 1998-08-31 | ||
PCT/JP1999/001670 WO1999051605A1 (en) | 1998-03-31 | 1999-03-31 | PYRROLO[1,2-a]PYRAZINE sPLA2 INHIBITOR |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0102981A2 true HUP0102981A2 (hu) | 2002-01-28 |
HUP0102981A3 HUP0102981A3 (en) | 2002-10-28 |
Family
ID=26427020
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0102981A HUP0102981A3 (en) | 1998-03-31 | 1999-03-31 | Pyrrolo[1,2-a]pyrazine derivatives and pharmaceutical compositions thereof |
Country Status (11)
Country | Link |
---|---|
US (1) | US6407104B1 (hu) |
EP (1) | EP1066290A1 (hu) |
JP (1) | JP4412521B2 (hu) |
KR (1) | KR20010042307A (hu) |
CN (1) | CN1303384A (hu) |
AU (1) | AU3054399A (hu) |
BR (1) | BR9909345A (hu) |
CA (1) | CA2326522A1 (hu) |
HU (1) | HUP0102981A3 (hu) |
NO (1) | NO20004881L (hu) |
WO (1) | WO1999051605A1 (hu) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE329619T1 (de) | 1998-10-14 | 2006-07-15 | Shionogi & Co | Spla2-inhibitoren zur behandlung von ischämischen reperfusionsschäden |
WO2001005789A1 (fr) | 1999-07-19 | 2001-01-25 | Shionogi & Co., Ltd. | Composes tricycliques a action inhibitrice a l'encontre de spla¿2? |
US6787545B1 (en) | 1999-08-23 | 2004-09-07 | Shiongi & Co., Ltd. | Pyrrolotriazine derivatives having spla2-inhibitory activities |
AU7559600A (en) * | 1999-10-15 | 2001-04-23 | Shionogi & Co., Ltd. | V type and/or x type spla2 inhibitors |
WO2001036420A1 (fr) * | 1999-11-15 | 2001-05-25 | Shionogi & Co., Ltd. | Derives d'aza-indolizine tricyclique ayant un effet inhibiteur sur spla¿2? |
WO2002000256A1 (en) | 2000-06-29 | 2002-01-03 | Shionogi & Co., Ltd. | Remedies for cirrhosis |
US7026318B2 (en) | 2000-06-29 | 2006-04-11 | Shionogi & Co., Ltd. | Compounds exhibiting X-type sPLA2 inhibiting effect |
AUPQ876400A0 (en) * | 2000-07-14 | 2000-08-03 | University Of Queensland, The | Compositions and method of using them |
WO2002012249A2 (en) * | 2000-08-04 | 2002-02-14 | Eli Lilly And Company | Substituted pyrrole compounds and their use as spla2 inhibitors |
TWI314457B (hu) | 2001-03-19 | 2009-09-11 | Shionogi & Co | |
US6730694B1 (en) | 2001-07-20 | 2004-05-04 | Eli Lilly And Company | sPLA2 inhibitors |
DE10155727A1 (de) * | 2001-11-13 | 2003-05-28 | Morphochem Ag | Serin Protease Inhibitoren |
AUPS282602A0 (en) | 2002-06-07 | 2002-06-27 | Garvan Institute Of Medical Research | Method of inhibiting cell proliferation |
AU2006278396A1 (en) * | 2005-08-04 | 2007-02-15 | Sirtris Pharmaceuticals, Inc. | Benzimidazole derivatives as sirtuin modulators |
CL2008001822A1 (es) * | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras. |
EP2424521A4 (en) | 2009-04-29 | 2015-03-04 | Amarin Pharmaceuticals Ie Ltd | PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND CARDIOVASCULAR AGENT AND METHODS OF USE |
CN105622616A (zh) * | 2016-02-25 | 2016-06-01 | 上海雅本化学有限公司 | 一种4-氯吡咯并嘧啶的制备方法 |
WO2023042716A1 (ja) * | 2021-09-17 | 2023-03-23 | 三井化学株式会社 | (メタ)アクリルアミド化合物の製造方法 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL109309A (en) * | 1993-04-16 | 2000-06-29 | Lilly Co Eli | 1-H-indole-3-acetic acid hydrazide SPLA2 inhibitors and pharmaceutical compositions containing them |
IL109311A0 (en) | 1993-04-16 | 1994-07-31 | Lilly Co Eli | 1H-indole-3-acetamide sPla2 inhibitors |
ES2377223T3 (es) | 1994-04-01 | 2012-03-23 | Eli Lilly And Company | Éster metÃlico de ácido [[3-(2-amino-1,2-dioxoetil)-2-etil-1-(fenilmetil)-11H-indol-4-IL]oxi]acético como inhibidor de sPLA2 |
US6214876B1 (en) * | 1994-07-21 | 2001-04-10 | Eli Lilly And Company | Indene-1-acetamide sPLA2 inhibitors |
CN1158121A (zh) * | 1994-07-21 | 1997-08-27 | 伊莱利利公司 | 吲哚嗪sPLA2抑制剂 |
US5641800A (en) | 1994-07-21 | 1997-06-24 | Eli Lilly And Company | 1H-indole-1-functional sPLA2 inhibitors |
AU1289797A (en) | 1995-12-13 | 1997-07-03 | Eli Lilly And Company | Naphthyl acetamides as spla2 inhibitors |
AU1149797A (en) | 1995-12-13 | 1997-07-03 | Eli Lilly And Company | Naphthyl glyoxamides as spla2 inhibitors |
TR199900956T2 (xx) | 1996-10-30 | 1999-07-21 | Eli Lilly And Company | S�bstit�e edilmi� trisiklik bile�imler. |
US5916922A (en) | 1996-12-03 | 1999-06-29 | Eli Lilly And Company | Phenyl glyoxamides as SPLA2 inhibitors |
US6353128B1 (en) | 1996-12-03 | 2002-03-05 | Eli Lilly And Company | Phenyl acetamides as sPLA2 inhibitors |
ID18983A (id) | 1996-12-04 | 1998-05-28 | Lilly Co Eli | Pirazola sebagai inhibitor sekresi fosfolipase a2 non-pankreas pada manusia |
US5919774A (en) | 1996-12-10 | 1999-07-06 | Eli Lilly And Company | Pyrroles as sPLA2 inhibitors |
TW455581B (en) | 1997-06-26 | 2001-09-21 | Lilly Co Eli | Process for preparing 4-substituted-1H-indole-3-glyoxamides |
-
1999
- 1999-03-31 KR KR1020007010855A patent/KR20010042307A/ko not_active Application Discontinuation
- 1999-03-31 JP JP2000542326A patent/JP4412521B2/ja not_active Expired - Fee Related
- 1999-03-31 CN CN99806627A patent/CN1303384A/zh active Pending
- 1999-03-31 AU AU30543/99A patent/AU3054399A/en not_active Abandoned
- 1999-03-31 WO PCT/JP1999/001670 patent/WO1999051605A1/en not_active Application Discontinuation
- 1999-03-31 CA CA002326522A patent/CA2326522A1/en not_active Abandoned
- 1999-03-31 BR BR9909345-6A patent/BR9909345A/pt not_active IP Right Cessation
- 1999-03-31 US US09/623,591 patent/US6407104B1/en not_active Expired - Fee Related
- 1999-03-31 HU HU0102981A patent/HUP0102981A3/hu unknown
- 1999-03-31 EP EP99912066A patent/EP1066290A1/en not_active Ceased
-
2000
- 2000-09-28 NO NO20004881A patent/NO20004881L/no unknown
Also Published As
Publication number | Publication date |
---|---|
HUP0102981A3 (en) | 2002-10-28 |
NO20004881L (no) | 2000-11-28 |
WO1999051605A1 (en) | 1999-10-14 |
CN1303384A (zh) | 2001-07-11 |
BR9909345A (pt) | 2000-12-12 |
EP1066290A1 (en) | 2001-01-10 |
NO20004881D0 (no) | 2000-09-28 |
US6407104B1 (en) | 2002-06-18 |
KR20010042307A (ko) | 2001-05-25 |
JP2002530268A (ja) | 2002-09-17 |
CA2326522A1 (en) | 1999-10-14 |
JP4412521B2 (ja) | 2010-02-10 |
AU3054399A (en) | 1999-10-25 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HUP0102981A2 (hu) | Pirrolo[1,2-a]pirazin-származékok és ezeket tartalmazó gyógyszerkészítmények | |
DK1106612T3 (da) | Quinolinderivater, der er nyttige til inhibering af farnesylproteintransferase | |
DE69529614T2 (de) | Heterobizyklische derivate | |
HUP0101146A2 (hu) | Foszfolipáz enzim inhibitor hatású indolszármazékok, valamint a vegyületeket tartalmazó gyógyászati készítmények | |
HUP0002353A2 (hu) | IV típusú foszfodiészteráz inhibitor hatású 1-cikloalkil-1,8-naftiridin-4-on-származékok és ezeket a vegyületeket tartalmazó gyógyszerkészítmények | |
TR200201505T2 (tr) | Terapötik maddeler olarak pirazolopirimidinler | |
DE69200766T2 (de) | Phenylamidinderivate als plättchenaggregationsinhibitoren. | |
HUP0202490A2 (hu) | Indazolszármazékok és ezeket tartalmazó protein-kináz gátló hatású gyógyszerkészítmények | |
HUP0100156A2 (hu) | Foszfolipáz-A2 inhibitor hatású indolszármazékok és alkalmazásuk gyógyászati készítmények előállítására | |
WO2004016614A3 (en) | Pyrrolopyrazines as kinase inhibitors | |
ATE443063T1 (de) | Ä1,2,4ütriazoloä4,3-aüpyridin-derivative zur behandlung hyperproliferativer erkrankungen | |
DK260588A (da) | Heterocykliske ketoner | |
HUP0001269A2 (hu) | 2-Oxo-1-azetidin-szulfonsav-származékok és ezeket tartalmazó kombinált gyógyszerkészítmények | |
NO20062692L (no) | Heterosykliske MEK inhibitorer og fremgangsmater for anvendelse derav | |
HUP0301690A2 (hu) | Szinergikus eljárások és készítmények rák kezelésére | |
HUP0002495A1 (hu) | VLA-4 Által közvetített leukocita adhéziót gátló dipeptidszármazékok és rokon vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
DK0705254T3 (da) | Phenylheterocykliske forbindelser som cyclooxygenase-2-inhibitorer | |
EA200200708A1 (ru) | Производные бензазола и их применение в качестве модуляторов jnk | |
HUP0102563A2 (hu) | Indolszármazékok és alkalmazásuk rosszindulatú és egyéb, patológiás sejtproliferáción alapuló megbetegedések kezelésére | |
GEP20084357B (en) | Pyrimidine derivatives for the treatment of abnormal cell growth | |
HUP0202381A2 (hu) | MEK-inhibitor hatású fenil-amino-benzoesav-származékok alkalmazása krónikus fájdalom kezelésére szolgáló gyógyszerkészítmények előállítására | |
NO931317L (no) | Et terapeutisk middel for parkinson's sykdom | |
HUP0203422A2 (hu) | Foszfodiészteráz VII inhibitor hatású imidazolszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
HUP0004142A2 (hu) | 5-HT1F agonista hatású karboxamidszármazékok és a vegyületeket tartalmazó gyógyászati készítmények | |
NO20045351L (no) | 1-[(indol-3-yl)karbonyl] piperazin-derivater |