HUP9700595A1 - Fluor-alkil- és fluor-alkoxicsoporttal helyettesített heterociklikus bradikinin-antagonisták, eljárás ezek előállítására, valamint ezek alkalmazása - Google Patents
Fluor-alkil- és fluor-alkoxicsoporttal helyettesített heterociklikus bradikinin-antagonisták, eljárás ezek előállítására, valamint ezek alkalmazásaInfo
- Publication number
- HUP9700595A1 HUP9700595A1 HU9700595A HUP9700595A HUP9700595A1 HU P9700595 A1 HUP9700595 A1 HU P9700595A1 HU 9700595 A HU9700595 A HU 9700595A HU P9700595 A HUP9700595 A HU P9700595A HU P9700595 A1 HUP9700595 A1 HU P9700595A1
- Authority
- HU
- Hungary
- Prior art keywords
- ring
- alkyl
- fluoro
- substituted
- atom
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 125000004434 sulfur atom 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 compound 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
- 101100516563 Caenorhabditis elegans nhr-6 gene 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
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003118 aryl 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
- 125000003709 fluoroalkyl 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)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
(I) általánős képletű heterőciklikűs flűőr-alkil- és flűőr-alkőxi-származékők bradikininantagőnista hatással, melyben X1-X3=N vagy CR5;R1 és R2=H vagy halőgénatőm; R3 és R4=H, halőgénatőm, alkil- vagyalkenilcsőpőrt; R5=H, halőgénatőm, (helyettesített) alkilcsőpőrt, O-R6csőpőrt, S-R6 csőpőrt, NHR6 csőpőrt, (helyettesített) arilcsőpőrt,(helyettesített) aril-alkil-csőpőrt, -C(O)-OR6 csőpőrt vagy -C(O)-Hcsőpőrt; R6 és R8=H, alkil-, alkenil- vagy aril-alkil-csőpőrt;R=(helyettesített) alkil- vagy (helyettesített) alkőxicsőpőrt;B=aminőkarbőnsav; D=alkén-diil-, alkán-diil- vagy -(CH2)n-Yp-(CH2)mcsőpőrt; E=őxigénatőm vagy kénatőm; Y=őxigénatőm, kénatőm vagy NR8; nés m=0-3; és p=0vagy 1, valamint ezek fiziőlógiai szempőntbólelfőgadható sói, és eljárás ezek előállítására. ŕ
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 (2)
| Publication Number | Publication Date |
|---|---|
| HU9700595D0 HU9700595D0 (en) | 1997-05-28 |
| HUP9700595A1 true HUP9700595A1 (hu) | 2000-08-28 |
Family
ID=7788755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9700595A HUP9700595A1 (hu) | 1996-03-19 | 1997-03-17 | Fluor-alkil- és fluor-alkoxicsoporttal helyettesített heterociklikus bradikinin-antagonisták, eljárás ezek előállítására, valamint ezek alkalmazása |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US5859025A (hu) |
| EP (1) | EP0796848B1 (hu) |
| JP (1) | JP4199315B2 (hu) |
| KR (1) | KR970065522A (hu) |
| AR (1) | AR006261A1 (hu) |
| AT (1) | ATE242215T1 (hu) |
| AU (1) | AU1628397A (hu) |
| BR (1) | BR9701332A (hu) |
| CA (1) | CA2199925A1 (hu) |
| CZ (1) | CZ81097A3 (hu) |
| DE (2) | DE19610784A1 (hu) |
| DK (1) | DK0796848T3 (hu) |
| ES (1) | ES2196207T3 (hu) |
| HR (1) | HRP970155A2 (hu) |
| HU (1) | HUP9700595A1 (hu) |
| ID (1) | ID16274A (hu) |
| IL (1) | IL120477A0 (hu) |
| NO (1) | NO971238L (hu) |
| PL (1) | PL318924A1 (hu) |
| PT (1) | PT796848E (hu) |
| SI (1) | SI0796848T1 (hu) |
| SK (1) | SK34897A3 (hu) |
| TR (1) | TR199700206A2 (hu) |
| ZA (1) | ZA972328B (hu) |
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 |
| TR200400220T4 (tr) * | 1999-12-10 | 2004-02-23 | Pfizer Inc. | Bradikinin antagonistleri olarak, 5 üyeli heteroaril ile ikame edilmiş 1,4-dihidropiridin bileşikleri. |
| AU2003226188A1 (en) * | 2002-04-10 | 2003-10-27 | 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 |
| WO2006094034A1 (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 |
| CN111433196B (zh) | 2017-11-24 | 2023-06-06 | 法瓦里斯荷兰有限责任公司 | 缓激肽b2受体拮抗剂及其用途 |
| UY38707A (es) | 2019-05-23 | 2020-12-31 | Pharvaris Gmbh | Nuevos antagonistas cíclicos del receptor b2 de bradiquinina |
| UY38706A (es) | 2019-05-23 | 2020-12-31 | Pharvaris Gmbh | Antagonistas cíclicos del receptor b2 de bradiquinina |
| PT4203919T (pt) | 2021-08-05 | 2024-04-23 | Pharvaris Gmbh | Composição à base de lípidos para administração oral de antagonistas do recetor b2 da bradicinina |
| AU2023241243A1 (en) | 2022-03-25 | 2024-11-07 | Pharvaris Gmbh | Solid composition comprising solubilised 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 |
| EP4499100A1 (en) | 2022-03-25 | 2025-02-05 | Pharvaris GmbH | Therapeutic uses of bradykinin b2-receptor antagonists |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5216165A (en) * | 1990-10-03 | 1993-06-01 | American Home Products Corporation | N-substituted aminoquinolines as analgesic agents |
| US5212182A (en) * | 1990-10-03 | 1993-05-18 | American Home Products Corpooration | Substituted quinolinyl- and naphthalenylbenzamides or benzylamines and related compounds useful as analgesics |
| 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 (fr) * | 1994-08-17 | 1996-02-22 | Nippon Hypox Laboratories Inc. | Derive de l'imidazoquinoleine |
| WO1996013485A1 (en) * | 1994-10-27 | 1996-05-09 | Fujisawa Pharmaceutical Co., Ltd. | Pyridopyrimidones, quinolines and fused n-heretocycles as bradykinin antagonists |
-
1996
- 1996-03-19 DE DE19610784A patent/DE19610784A1/de not_active Withdrawn
-
1997
- 1997-03-05 DE DE59710191T patent/DE59710191D1/de not_active Expired - Lifetime
- 1997-03-05 EP EP97103611A patent/EP0796848B1/de not_active Expired - Lifetime
- 1997-03-05 ES ES97103611T patent/ES2196207T3/es not_active Expired - Lifetime
- 1997-03-05 SI SI9730572T patent/SI0796848T1/xx unknown
- 1997-03-05 DK DK97103611T patent/DK0796848T3/da active
- 1997-03-05 AT AT97103611T patent/ATE242215T1/de not_active IP Right Cessation
- 1997-03-05 PT PT97103611T patent/PT796848E/pt unknown
- 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 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 CZ CZ97810A patent/CZ81097A3/cs unknown
- 1997-03-17 SK SK348-97A patent/SK34897A3/sk unknown
- 1997-03-17 TR TR97/00206A patent/TR199700206A2/xx unknown
- 1997-03-17 KR KR1019970008899A patent/KR970065522A/ko not_active Withdrawn
- 1997-03-18 NO NO971238A patent/NO971238L/no unknown
- 1997-03-18 ZA ZA9702328A patent/ZA972328B/xx unknown
- 1997-03-18 IL IL12047797A patent/IL120477A0/xx unknown
- 1997-03-18 US US08/819,351 patent/US5859025A/en not_active Expired - Lifetime
- 1997-03-18 HR HR19610784.9A patent/HRP970155A2/xx not_active Application Discontinuation
- 1997-03-18 JP JP06474897A patent/JP4199315B2/ja not_active Expired - Lifetime
- 1997-03-18 BR BR9701332A patent/BR9701332A/pt not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA972328B (en) | 1997-09-19 |
| JP4199315B2 (ja) | 2008-12-17 |
| DE59710191D1 (de) | 2003-07-10 |
| HRP970155A2 (en) | 1998-04-30 |
| DE19610784A1 (de) | 1997-09-25 |
| SK34897A3 (en) | 1998-01-14 |
| CA2199925A1 (en) | 1997-09-19 |
| TR199700206A2 (xx) | 1997-10-21 |
| EP0796848B1 (de) | 2003-06-04 |
| US5859025A (en) | 1999-01-12 |
| AR006261A1 (es) | 1999-08-11 |
| DK0796848T3 (da) | 2003-09-22 |
| PL318924A1 (en) | 1997-09-29 |
| BR9701332A (pt) | 1998-08-18 |
| ID16274A (id) | 1997-09-18 |
| MX9702028A (es) | 1997-09-30 |
| CZ81097A3 (en) | 1997-10-15 |
| EP0796848A1 (de) | 1997-09-24 |
| ES2196207T3 (es) | 2003-12-16 |
| HU9700595D0 (en) | 1997-05-28 |
| NO971238L (no) | 1997-09-22 |
| NO971238D0 (no) | 1997-03-18 |
| PT796848E (pt) | 2003-08-29 |
| AU1628397A (en) | 1997-09-25 |
| SI0796848T1 (en) | 2003-12-31 |
| IL120477A0 (en) | 1997-07-13 |
| JPH107656A (ja) | 1998-01-13 |
| ATE242215T1 (de) | 2003-06-15 |
| KR970065522A (ko) | 1997-10-13 |
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