RU2018140051A - Производные нестероидных противовоспалительных средств - Google Patents
Производные нестероидных противовоспалительных средств Download PDFInfo
- Publication number
- RU2018140051A RU2018140051A RU2018140051A RU2018140051A RU2018140051A RU 2018140051 A RU2018140051 A RU 2018140051A RU 2018140051 A RU2018140051 A RU 2018140051A RU 2018140051 A RU2018140051 A RU 2018140051A RU 2018140051 A RU2018140051 A RU 2018140051A
- Authority
- RU
- Russia
- Prior art keywords
- inflammatory
- steroidal anti
- derivatives
- inflammatory drugs
- aceclofenac
- Prior art date
Links
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 4
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 4
- MNIPYSSQXLZQLJ-UHFFFAOYSA-N Biofenac Chemical compound OC(=O)COC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl MNIPYSSQXLZQLJ-UHFFFAOYSA-N 0.000 claims 2
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 2
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims 2
- 229960004420 aceclofenac Drugs 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 230000003110 anti-inflammatory effect Effects 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 231100000433 cytotoxic Toxicity 0.000 claims 2
- 230000001472 cytotoxic effect Effects 0.000 claims 2
- 229960001259 diclofenac Drugs 0.000 claims 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims 2
- 229960001680 ibuprofen Drugs 0.000 claims 2
- 229960000905 indomethacin Drugs 0.000 claims 2
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims 2
- 229960000991 ketoprofen Drugs 0.000 claims 2
- 229960004752 ketorolac Drugs 0.000 claims 2
- OZWKMVRBQXNZKK-UHFFFAOYSA-N ketorolac Chemical compound OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 claims 2
- 229960002009 naproxen Drugs 0.000 claims 2
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 2
- 230000000324 neuroprotective effect Effects 0.000 claims 2
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 2
- 229960000894 sulindac Drugs 0.000 claims 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
Classifications
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/30—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/02—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring monocyclic with no unsaturation outside the aromatic ring
- C07C39/06—Alkylated phenols
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (8)
1. Соединения общей формулы (I):
где R = остаток нестероидного противовоспалительного средства, содержащих карбоксильную группу и присоединенных амидной связью, а Х=(CH2)3CONHCH2 или CH2CH2O(CO)NHCH2, обладающие противовоспалительной, цитотоксической и нейрозащитной активностью.
2. Соединения по п. 1, где противовоспалительное средство представляет собой диклофенак, ибупрофен, напроксен, кетопрофен, сулиндак, кеторолак, ацеклофенак, индометацин.
3. Соединения общей формулы (I):
где R = остаток нестероидного противовоспалительного средства, содержащих карбоксильную группу и присоединенных амидной связью, а X=СН2, обладающие противовоспалительной, цитотоксической и нейрозащитной активностью.
4. Соединения по п. 3, где противовоспалительное средство представляет собой диклофенак, ибупрофен, напроксен, кетопрофен, сулиндак, кеторолак, ацеклофенак, индометацин.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2018140051A RU2732297C2 (ru) | 2018-11-14 | 2018-11-14 | Производные нестероидных противовоспалительных средств |
| PCT/RU2019/050212 WO2020101543A1 (ru) | 2018-11-14 | 2019-11-12 | Производные нестероидных противовоспалительных средств |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2018140051A RU2732297C2 (ru) | 2018-11-14 | 2018-11-14 | Производные нестероидных противовоспалительных средств |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2018140051A true RU2018140051A (ru) | 2020-05-14 |
| RU2018140051A3 RU2018140051A3 (ru) | 2020-05-14 |
| RU2732297C2 RU2732297C2 (ru) | 2020-09-15 |
Family
ID=70730725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018140051A RU2732297C2 (ru) | 2018-11-14 | 2018-11-14 | Производные нестероидных противовоспалительных средств |
Country Status (2)
| Country | Link |
|---|---|
| RU (1) | RU2732297C2 (ru) |
| WO (1) | WO2020101543A1 (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102669063B1 (ko) * | 2021-06-29 | 2024-05-23 | 난징 헤론 파마슈티컬 사이언스 앤 테크놀로지 컴퍼니 리미티드 | 이부프로펜 에스테르 유도체 및 그 에멀젼 제제 |
| EP4396305A1 (en) | 2021-09-01 | 2024-07-10 | Empathibio, Inc. | Synthesis of mdma or its optically active (r)- or (s)-mdma isomers |
| US11845736B2 (en) | 2021-10-01 | 2023-12-19 | Empathbio, Inc. | Prodrugs of MDMA, MDA, and derivatives thereof |
| US11912680B2 (en) | 2021-12-28 | 2024-02-27 | Empathbio, Inc. | Nitric oxide releasing prodrugs of MDA and MDMA |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5612369A (en) * | 1995-06-07 | 1997-03-18 | 3-Dimensional Pharmaceuticals, Inc. | Thrombin inhibitors |
| SE9600070D0 (sv) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral pharmaceutical dosage forms |
| KR19990082330A (ko) * | 1996-02-06 | 1999-11-25 | 미즈노 마사루 | 신규 화합물 및 이의 의약 용도 |
| SK286779B6 (sk) * | 1997-02-19 | 2009-05-07 | Berlex Laboratories, Inc. | N-Heterocyklické deriváty ako inhibítory NOS, spôsob ich prípravy, farmaceutické prostriedky s ich obsahom a ich použitie |
| SE9801526D0 (sv) * | 1998-04-29 | 1998-04-29 | Astra Ab | New compounds |
| US20070208087A1 (en) * | 2001-11-02 | 2007-09-06 | Sanders Virginia J | Compounds, compositions and methods for the treatment of inflammatory diseases |
| EP1511736A4 (en) * | 2002-06-07 | 2006-06-07 | Cortical Pty Ltd | THERAPEUTIC MOLECULES AND METHOD 1 |
| RU2447060C2 (ru) * | 2005-06-17 | 2012-04-10 | Эпоуджи Биотекнолоджи Корпорейшн | Ингибиторы сфингозинкиназы |
| AU2011329233A1 (en) * | 2010-11-15 | 2013-05-23 | Abbvie Deutschland Gmbh & Co Kg | NAMPT and ROCK inhibitors |
| US9193762B2 (en) * | 2010-12-01 | 2015-11-24 | University Of Mississippi | Selective inhibitors of prolylcarboxypeptidase |
| WO2014018913A2 (en) * | 2012-07-27 | 2014-01-30 | University Of Connecticut | Santacruzamate a compositions and analogs and methods of use |
| WO2015050379A1 (ko) * | 2013-10-01 | 2015-04-09 | 광주과학기술원 | 신규한 퀴놀리논 유도체 및 이의 용도 |
| WO2015162216A1 (en) * | 2014-04-24 | 2015-10-29 | Universita' Degli Studi Di Siena | Biaryl amide or urea derivatives as trpv1 ligands |
| RU2568603C1 (ru) * | 2015-01-15 | 2015-11-20 | Федеральное агентство научных организаций (ФАНО России) Федеральное государственное бюджетное учреждение науки Институт биоорганической химии им. академиков М.М. Шемякина и Ю.А. Овчинникова Российской академии наук (ИБХ РАН) | Производные простагландина, обладающие противовоспалительной и анальгезирующей активностью |
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2018
- 2018-11-14 RU RU2018140051A patent/RU2732297C2/ru active
-
2019
- 2019-11-12 WO PCT/RU2019/050212 patent/WO2020101543A1/ru active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020101543A1 (ru) | 2020-05-22 |
| RU2018140051A3 (ru) | 2020-05-14 |
| RU2732297C2 (ru) | 2020-09-15 |
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