AR006261A1 - Antagonistas de bradiquinina heterociclicos, sustituidos con fluoroalquilo fluoroalcoxi, procedimiento para su preparacion y su utilizacion para lapreparacion de un medicamento y dicho medicamento - Google Patents
Antagonistas de bradiquinina heterociclicos, sustituidos con fluoroalquilo fluoroalcoxi, procedimiento para su preparacion y su utilizacion para lapreparacion de un medicamento y dicho medicamentoInfo
- Publication number
- AR006261A1 AR006261A1 ARP970101058A ARP970101058A AR006261A1 AR 006261 A1 AR006261 A1 AR 006261A1 AR P970101058 A ARP970101058 A AR P970101058A AR P970101058 A ARP970101058 A AR P970101058A AR 006261 A1 AR006261 A1 AR 006261A1
- Authority
- AR
- Argentina
- Prior art keywords
- preparation
- substituted
- medicinal product
- alkyl
- fluoroalkyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 2
- 239000005557 antagonist Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- YYQGUWHFXVXQOO-GFCCVEGCSA-N 2-chloro-4-[[3-[(2R)-2-hydroxybutyl]-1-methyl-2-oxobenzimidazol-5-yl]amino]pyridine-3-carbonitrile Chemical group ClC1=C(C#N)C(=CC=N1)NC1=CC2=C(N(C(N2C[C@@H](CC)O)=O)C)C=C1 YYQGUWHFXVXQOO-GFCCVEGCSA-N 0.000 abstract 1
- 101800004538 Bradykinin Proteins 0.000 abstract 1
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 abstract 1
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 abstract 1
- 102100035792 Kininogen-1 Human genes 0.000 abstract 1
- -1 R3 and R4 are H Chemical class 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 abstract 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/18—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/08—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/10—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D257/12—Six-membered rings having four nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describenn derivados heterocíclicos de fluoroalquilo y fluoroalcoxi de la fórmula (1) con un efecto antagonista de bradiquinina en la que X1-X3son N ó CR5; R1 y R2 son H o halógeno, R3 y R4 son H, halógeno, alquilo o alquenilo; R5 es H, halógeno, alquilo (sustituido); O-R6, S-R6, NH6R, arilo(sustituído) aril (sustituido), alquilo, -C(O)-OR6 o -C(O)-H, R6 y R8 son H, alquilo, alquenilo o aril-alquilo; R7 son alquilo (sustituido) o alcoxi(sustituido); B es un ácido aminocarboxílico;D es alquenodiílo, alcanodiílo o -(CH2)n-Yp-(CH2)m; E es oxígeno o azufre; Y es oxígeno, azufre o NR8; n y m sonun número de 1-3; o significa un número de 1-3 y p significa 0 ó 1, así como sus sales fisiológicamente compatibles, un procedimientopara su preparación,utilización de dichos derivados para la preparación de un medicamento y dicho medicamento.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19610784A DE19610784A1 (de) | 1996-03-19 | 1996-03-19 | Fluoralkyl- und Fluoralkoxysubstituierte heterocyclische Bradykinin-Antagonisten, Verfahren zu ihrer Herstellung und ihre Verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR006261A1 true AR006261A1 (es) | 1999-08-11 |
Family
ID=7788755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970101058A AR006261A1 (es) | 1996-03-19 | 1997-03-17 | Antagonistas de bradiquinina heterociclicos, sustituidos con fluoroalquilo fluoroalcoxi, procedimiento para su preparacion y su utilizacion para lapreparacion de un medicamento y dicho medicamento |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US5859025A (es) |
| EP (1) | EP0796848B1 (es) |
| JP (1) | JP4199315B2 (es) |
| KR (1) | KR970065522A (es) |
| AR (1) | AR006261A1 (es) |
| AT (1) | ATE242215T1 (es) |
| AU (1) | AU1628397A (es) |
| BR (1) | BR9701332A (es) |
| CA (1) | CA2199925A1 (es) |
| CZ (1) | CZ81097A3 (es) |
| DE (2) | DE19610784A1 (es) |
| DK (1) | DK0796848T3 (es) |
| ES (1) | ES2196207T3 (es) |
| HR (1) | HRP970155A2 (es) |
| HU (1) | HUP9700595A1 (es) |
| ID (1) | ID16274A (es) |
| IL (1) | IL120477A0 (es) |
| NO (1) | NO971238L (es) |
| PL (1) | PL318924A1 (es) |
| PT (1) | PT796848E (es) |
| SI (1) | SI0796848T1 (es) |
| SK (1) | SK34897A3 (es) |
| TR (1) | TR199700206A2 (es) |
| ZA (1) | ZA972328B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19712960A1 (de) * | 1997-03-27 | 1998-10-01 | Hoechst Ag | Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten |
| ATE257479T1 (de) * | 1999-12-10 | 2004-01-15 | Pfizer | 5-ring heteroarylsubstituierte 1,4- dihydropyridine als bradykinin antagonisten |
| CA2481855A1 (en) | 2002-04-10 | 2003-10-23 | Ortho-Mcneil Pharmaceutical, Inc. | Novel heteroaryl alkylamide derivatives useful as bradykinin receptor modulators |
| EP1914236A1 (en) | 2002-04-10 | 2008-04-23 | Ortho-McNeil Pharmaceutical, Inc. | Novel heteroaryl alkylamide derivatives useful as bradykinin receptor modulators |
| ITMI20021247A1 (it) * | 2002-06-07 | 2003-12-09 | Menarini Ricerche Spa | Antagonisti basici non peptidici della bradichinina e loro impiego informulazioni farmaceutiche |
| US7256207B2 (en) * | 2003-08-20 | 2007-08-14 | Irm Llc | Inhibitors of cathepsin S |
| AU2006218661A1 (en) | 2005-03-01 | 2006-09-08 | Wyeth | Cinnoline compounds and their use as liver X receptor modilators |
| TWI407960B (zh) | 2007-03-23 | 2013-09-11 | Jerini Ag | 小分子緩激肽ｂ２受體調節劑 |
| AR085073A1 (es) * | 2012-01-11 | 2013-09-11 | Richmond Sa Com Ind Y Financiera Lab | Compuestos con actividad antibacteriana, un procedimiento para su obtencion y composiciones farmaceuticas que los comprenden |
| SI3713928T1 (sl) | 2017-11-24 | 2022-09-30 | Pharvaris Netherlands B.V. | Novi antagonisti receptorja bradikinina B2 |
| AR118982A1 (es) | 2019-05-23 | 2021-11-17 | Pharvaris Gmbh | Antagonistas cíclicos del receptor b2 de bradiquinina |
| AR118983A1 (es) | 2019-05-23 | 2021-11-17 | Pharvaris Gmbh | Antagonistas cíclicos del receptor b2 de bradiquinina |
| EP4203919B1 (en) | 2021-08-05 | 2024-01-31 | Pharvaris GmbH | Lipid-based composition for oral administration of bradykinin b2-receptor antagonists |
| US20250268887A1 (en) | 2022-03-25 | 2025-08-28 | Pharvaris Gmbh | Therapeutic uses of bradykinin b2-receptor antagonists |
| TW202345810A (zh) | 2022-03-25 | 2023-12-01 | 瑞士商帕法瑞斯有限責任公司 | 包含緩激肽ｂ２受體拮抗劑之固態延長釋放組成物 |
| CA3250835A1 (en) | 2022-03-25 | 2023-09-28 | Pharvaris Gmbh | SOLID COMPOSITION COMPRISING SOLUBILIZED BRADYKININ B2 RECEPTOR ANTAGONISTS |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5212182A (en) * | 1990-10-03 | 1993-05-18 | American Home Products Corpooration | Substituted quinolinyl- and naphthalenylbenzamides or benzylamines and related compounds useful as analgesics |
| US5216165A (en) * | 1990-10-03 | 1993-06-01 | American Home Products Corporation | N-substituted aminoquinolines as analgesic agents |
| US5438064A (en) * | 1991-12-23 | 1995-08-01 | American Home Products Corporation | Derivatives of 4-anilinoquinoline-3-carboxamide as analgesic agents |
| AU680870B2 (en) * | 1993-04-28 | 1997-08-14 | Astellas Pharma Inc. | New heterocyclic compounds |
| WO1996005202A1 (en) * | 1994-08-17 | 1996-02-22 | Nippon Hypox Laboratories Inc. | Imidazoquinoline derivative |
| KR970707098A (ko) * | 1994-10-27 | 1997-12-01 | 후지야마 아키라 | 브라디키닌 길항제로서 피리도피리미돈, 퀴놀린 및 융합된 N-헤테로사이클(Pyridopyrimidones, quinolines and fused N-heterocycles as bradykinin antagonists) |
-
1996
- 1996-03-19 DE DE19610784A patent/DE19610784A1/de not_active Withdrawn
-
1997
- 1997-03-05 PT PT97103611T patent/PT796848E/pt unknown
- 1997-03-05 AT AT97103611T patent/ATE242215T1/de not_active IP Right Cessation
- 1997-03-05 EP EP97103611A patent/EP0796848B1/de not_active Expired - Lifetime
- 1997-03-05 SI SI9730572T patent/SI0796848T1/xx unknown
- 1997-03-05 DE DE59710191T patent/DE59710191D1/de not_active Expired - Lifetime
- 1997-03-05 DK DK97103611T patent/DK0796848T3/da active
- 1997-03-05 ES ES97103611T patent/ES2196207T3/es not_active Expired - Lifetime
- 1997-03-12 PL PL97318924A patent/PL318924A1/xx unknown
- 1997-03-13 CA CA002199925A patent/CA2199925A1/en not_active Abandoned
- 1997-03-17 ID IDP970863A patent/ID16274A/id unknown
- 1997-03-17 TR TR97/00206A patent/TR199700206A2/xx unknown
- 1997-03-17 CZ CZ97810A patent/CZ81097A3/cs unknown
- 1997-03-17 KR KR1019970008899A patent/KR970065522A/ko not_active Withdrawn
- 1997-03-17 HU HU9700595A patent/HUP9700595A1/hu unknown
- 1997-03-17 AR ARP970101058A patent/AR006261A1/es unknown
- 1997-03-17 AU AU16283/97A patent/AU1628397A/en not_active Abandoned
- 1997-03-17 SK SK348-97A patent/SK34897A3/sk unknown
- 1997-03-18 HR HR19610784.9A patent/HRP970155A2/xx not_active Application Discontinuation
- 1997-03-18 NO NO971238A patent/NO971238L/no unknown
- 1997-03-18 JP JP06474897A patent/JP4199315B2/ja not_active Expired - Lifetime
- 1997-03-18 ZA ZA9702328A patent/ZA972328B/xx unknown
- 1997-03-18 US US08/819,351 patent/US5859025A/en not_active Expired - Lifetime
- 1997-03-18 IL IL12047797A patent/IL120477A0/xx unknown
- 1997-03-18 BR BR9701332A patent/BR9701332A/pt not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| HU9700595D0 (en) | 1997-05-28 |
| US5859025A (en) | 1999-01-12 |
| DE59710191D1 (de) | 2003-07-10 |
| CZ81097A3 (en) | 1997-10-15 |
| ZA972328B (en) | 1997-09-19 |
| IL120477A0 (en) | 1997-07-13 |
| ATE242215T1 (de) | 2003-06-15 |
| PT796848E (pt) | 2003-08-29 |
| JP4199315B2 (ja) | 2008-12-17 |
| HRP970155A2 (en) | 1998-04-30 |
| MX9702028A (es) | 1997-09-30 |
| JPH107656A (ja) | 1998-01-13 |
| EP0796848A1 (de) | 1997-09-24 |
| NO971238L (no) | 1997-09-22 |
| ES2196207T3 (es) | 2003-12-16 |
| TR199700206A2 (xx) | 1997-10-21 |
| AU1628397A (en) | 1997-09-25 |
| HUP9700595A1 (hu) | 2000-08-28 |
| KR970065522A (ko) | 1997-10-13 |
| SK34897A3 (en) | 1998-01-14 |
| SI0796848T1 (en) | 2003-12-31 |
| DE19610784A1 (de) | 1997-09-25 |
| DK0796848T3 (da) | 2003-09-22 |
| ID16274A (id) | 1997-09-18 |
| BR9701332A (pt) | 1998-08-18 |
| PL318924A1 (en) | 1997-09-29 |
| NO971238D0 (no) | 1997-03-18 |
| EP0796848B1 (de) | 2003-06-04 |
| CA2199925A1 (en) | 1997-09-19 |
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