HUP9904696A2 - Indene inhibitors of cox-2 - Google Patents
Indene inhibitors of cox-2Info
- Publication number
- HUP9904696A2 HUP9904696A2 HU9904696A HUP9904696A HUP9904696A2 HU P9904696 A2 HUP9904696 A2 HU P9904696A2 HU 9904696 A HU9904696 A HU 9904696A HU P9904696 A HUP9904696 A HU P9904696A HU P9904696 A2 HUP9904696 A2 HU P9904696A2
- Authority
- HU
- Hungary
- Prior art keywords
- hydrogen
- alkyl
- cox
- atom
- alkyloxy
- Prior art date
Links
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Chemical compound C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 title 2
- 101150071146 COX2 gene Proteins 0.000 title 1
- 101100114534 Caenorhabditis elegans ctc-2 gene Proteins 0.000 title 1
- 101150000187 PTGS2 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000003454 indenyl group Chemical class C1(C=CC2=CC=CC=C12)* 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000012659 Joint disease Diseases 0.000 abstract 1
- 102100038280 Prostaglandin G/H synthase 2 Human genes 0.000 abstract 1
- 108050003267 Prostaglandin G/H synthase 2 Proteins 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 230000001093 anti-cancer Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/60—Two oxygen atoms, e.g. succinic anhydride
-
- 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
- A61P25/28—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
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
A találmány COX-2 enzim inbitőraként viselkedő, így gyűlladásgátló ésrákelleni hatású indénszármazékőkra és ilyen vegyületeket tartalmazógyógyászati készítményekre, valamint az indénszármazékők gyógyászatikészítmények előállítására való alkalmazására vőnatkőzik. A találmányszerinti vegyületek elsősőrban ízületi megbetegedések, kőlőrektálisrák és Alzheimer-kór kezelhető. A találmány szerinti vegyületek (1)általánős képletében R1 jelentése hidrőgén- vagy halőgénatőm vagy alkil-, alkőxi-,flűőralkőxi-, triflűőrmetil-, alkiltiő- vagy triflűőrmetiltiőcsőpőrt; R2 és R3 egymástól függetlenül hidrőgénatőmőt vagy alkilcsőpőrtőtjelentenek, vagy együtt telített ciklőalkilgyűrűt alkőthatnak; tővábbá R4, R5, R6, R7 és R8 egymástól függetlenül hidrőgén- vagyhalőgénatőmőt, vagy alkil-, alkőxi-, alkiltiő-, alkilszűlfinil-,alkilszűlfőnil-, flűőr-alkőxi-, triflűőrmetil- vagytriflűőrmetiltiőcsőpőrtőt jelentenek. ŕThe invention relates to indene derivatives acting as COX-2 enzyme inhibitors, thus having anti-inflammatory and anticancer effects, and to medicinal preparations containing such compounds, as well as to the use of indene derivatives for the production of medicinal preparations. The compounds according to the invention are primarily used to treat joint diseases, colorectal cancer and Alzheimer's disease. In the general formula (1) of the compounds according to the invention, R1 is a hydrogen or halogen atom or an alkyl, alkyloxy, fluoroalkyl, trifluoromethyl, alkylthio or trifluoromethylthio group; R 2 and R 3 independently represent a hydrogen atom or an alkyl ring atom, or together they can form a saturated cyclic alkyl ring; furthermore, R4, R5, R6, R7 and R8 independently represent a hydrogen or halogen atom, or an alkyl, alkyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, fluoroalkyl, trifluoromethyl or trifluoromethylthio group. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74794896A | 1996-11-12 | 1996-11-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP9904696A2 true HUP9904696A2 (en) | 2000-05-28 |
Family
ID=25007366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9904696A HUP9904696A2 (en) | 1996-11-12 | 1997-11-10 | Indene inhibitors of cox-2 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP0948493A1 (en) |
| JP (1) | JP2001504118A (en) |
| KR (1) | KR20000053227A (en) |
| CN (1) | CN1237162A (en) |
| AU (1) | AU5105598A (en) |
| BR (1) | BR9713346A (en) |
| CA (1) | CA2269035A1 (en) |
| HU (1) | HUP9904696A2 (en) |
| WO (1) | WO1998021195A1 (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1246621A4 (en) | 1999-12-23 | 2004-11-24 | Nitromed Inc | Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use |
| AU2004237439B2 (en) | 2003-05-07 | 2009-09-10 | Osteologix A/S | Treating cartilage/bone conditions with water-soluble strontium salts |
| EP1968616A4 (en) | 2006-01-04 | 2009-10-21 | Southern Res Inst | Derivatives of sulindac, use thereof and preparation thereof |
| CN104592091B (en) * | 2015-01-27 | 2017-07-04 | 冉瑞琼 | A kind of compound and its application containing heteroauxin core texture |
| WO2022195579A1 (en) | 2021-03-15 | 2022-09-22 | Saul Yedgar | Hyaluronic acid-conjugated dipalmitoyl phosphatidyl ethanolamine in combination with non-steroidal anti-inflammatory drugs (nsaids) for treating or alleviating inflammatory diseases |
| CA3235127A1 (en) * | 2021-10-15 | 2023-04-20 | Yao XU | 2,3-dimethoxy-5-methyl-1,4-benzoquinone alkyl alcohol derivative and use thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3647858A (en) * | 1970-05-01 | 1972-03-07 | Merck & Co Inc | Process for preparing 1-benzylidene-3-indenyl acetic acids |
| MX9302419A (en) * | 1992-04-28 | 1994-03-31 | American Home Prod | DERIVATIVES OF TETRONIC ACID, TIOTETRONIC AND TETRAMIC. |
| GB9403857D0 (en) * | 1994-03-01 | 1994-04-20 | Scotia Holdings Plc | Fatty acid derivatives |
-
1997
- 1997-11-10 BR BR9713346-9A patent/BR9713346A/en not_active Application Discontinuation
- 1997-11-10 KR KR1019990704202A patent/KR20000053227A/en not_active Application Discontinuation
- 1997-11-10 AU AU51055/98A patent/AU5105598A/en not_active Abandoned
- 1997-11-10 CN CN97199655A patent/CN1237162A/en active Pending
- 1997-11-10 CA CA002269035A patent/CA2269035A1/en not_active Abandoned
- 1997-11-10 HU HU9904696A patent/HUP9904696A2/en unknown
- 1997-11-10 JP JP52266398A patent/JP2001504118A/en active Pending
- 1997-11-10 WO PCT/US1997/020231 patent/WO1998021195A1/en not_active Application Discontinuation
- 1997-11-10 EP EP97945622A patent/EP0948493A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CN1237162A (en) | 1999-12-01 |
| CA2269035A1 (en) | 1998-05-22 |
| BR9713346A (en) | 2000-05-09 |
| AU5105598A (en) | 1998-06-03 |
| EP0948493A1 (en) | 1999-10-13 |
| WO1998021195A1 (en) | 1998-05-22 |
| JP2001504118A (en) | 2001-03-27 |
| KR20000053227A (en) | 2000-08-25 |
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