ZA200101975B - New carboxylic acid derivatives carrying keto side-chains, their production and their use as endothelin-receptor antagonists. - Google Patents
New carboxylic acid derivatives carrying keto side-chains, their production and their use as endothelin-receptor antagonists. Download PDFInfo
- Publication number
- ZA200101975B ZA200101975B ZA200101975A ZA200101975A ZA200101975B ZA 200101975 B ZA200101975 B ZA 200101975B ZA 200101975 A ZA200101975 A ZA 200101975A ZA 200101975 A ZA200101975 A ZA 200101975A ZA 200101975 B ZA200101975 B ZA 200101975B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- formula
- phenyl
- endothelin
- optionally substituted
- Prior art date
Links
- 229940118365 Endothelin receptor antagonist Drugs 0.000 title claims description 17
- 239000002308 endothelin receptor antagonist Substances 0.000 title claims description 17
- 150000001732 carboxylic acid derivatives Chemical class 0.000 title claims description 13
- 238000004519 manufacturing process Methods 0.000 title claims description 4
- 125000000468 ketone group Chemical group 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims description 62
- 229910052739 hydrogen Inorganic materials 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 30
- 150000002367 halogens Chemical class 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 22
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 16
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 108050009340 Endothelin Proteins 0.000 claims description 13
- 102000002045 Endothelin Human genes 0.000 claims description 13
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 claims description 13
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
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- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims description 8
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 9
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- HXJUTPCZVOIRIF-UHFFFAOYSA-N sulfolane Chemical compound O=S1(=O)CCCC1 HXJUTPCZVOIRIF-UHFFFAOYSA-N 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000007885 tablet disintegrant Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000005147 toluenesulfonyl group Chemical group C=1(C(=CC=CC1)S(=O)(=O)*)C 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- CMMXCVYESRODNH-UHFFFAOYSA-N trichloroepoxyethane Chemical class ClC1OC1(Cl)Cl CMMXCVYESRODNH-UHFFFAOYSA-N 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 230000006442 vascular tone Effects 0.000 description 1
- 239000002525 vasculotropin inhibitor Substances 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 239000005526 vasoconstrictor agent Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19836044A DE19836044A1 (de) | 1998-08-10 | 1998-08-10 | Neue Carbonsäurederivate, die Ketoseitenketten tragen, ihre Herstellung und Verwendung als Endothelin-Rezeptorantagonisten |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200101975B true ZA200101975B (en) | 2002-03-11 |
Family
ID=7876981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200101975A ZA200101975B (en) | 1998-08-10 | 2001-03-09 | New carboxylic acid derivatives carrying keto side-chains, their production and their use as endothelin-receptor antagonists. |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1104410A1 (ja) |
| JP (1) | JP2002522531A (ja) |
| KR (1) | KR20010072378A (ja) |
| CN (1) | CN1323298A (ja) |
| AR (1) | AR020147A1 (ja) |
| AU (1) | AU5374199A (ja) |
| BG (1) | BG105236A (ja) |
| BR (1) | BR9912889A (ja) |
| CA (1) | CA2340167A1 (ja) |
| CO (1) | CO5261504A1 (ja) |
| DE (1) | DE19836044A1 (ja) |
| HK (1) | HK1042086A1 (ja) |
| HR (1) | HRP20010164A2 (ja) |
| HU (1) | HUP0104007A3 (ja) |
| ID (1) | ID27965A (ja) |
| IL (1) | IL140915A0 (ja) |
| NO (1) | NO20010622L (ja) |
| PL (1) | PL345998A1 (ja) |
| SK (1) | SK832001A3 (ja) |
| TR (1) | TR200100427T2 (ja) |
| WO (1) | WO2000009489A1 (ja) |
| ZA (1) | ZA200101975B (ja) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19924892A1 (de) * | 1999-06-01 | 2000-12-07 | Basf Ag | Neue Carbonsäurederivate mit arylsubstituierten Stickstoffheterocyclen, ihre Herstellung und Verwendung als Endothelin Rezeptorantagonisten |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19636046A1 (de) * | 1996-09-05 | 1998-03-12 | Basf Ag | Neue Carbonsäurederivate, ihre Herstellung und Verwendung als gemischte ET¶A¶/ET¶B¶-Rezeptorantagonisten |
-
1998
- 1998-08-10 DE DE19836044A patent/DE19836044A1/de not_active Withdrawn
-
1999
- 1999-08-07 BR BR9912889-6A patent/BR9912889A/pt not_active Application Discontinuation
- 1999-08-07 KR KR1020017001731A patent/KR20010072378A/ko not_active Application Discontinuation
- 1999-08-07 ID IDW20010326A patent/ID27965A/id unknown
- 1999-08-07 HU HU0104007A patent/HUP0104007A3/hu unknown
- 1999-08-07 TR TR2001/00427T patent/TR200100427T2/xx unknown
- 1999-08-07 EP EP99939457A patent/EP1104410A1/de not_active Withdrawn
- 1999-08-07 SK SK83-2001A patent/SK832001A3/sk unknown
- 1999-08-07 CN CN99811981A patent/CN1323298A/zh active Pending
- 1999-08-07 WO PCT/EP1999/005728 patent/WO2000009489A1/de not_active Application Discontinuation
- 1999-08-07 CA CA002340167A patent/CA2340167A1/en not_active Abandoned
- 1999-08-07 AU AU53741/99A patent/AU5374199A/en not_active Abandoned
- 1999-08-07 IL IL14091599A patent/IL140915A0/xx unknown
- 1999-08-07 JP JP2000564942A patent/JP2002522531A/ja active Pending
- 1999-08-07 PL PL99345998A patent/PL345998A1/xx not_active Application Discontinuation
- 1999-08-10 CO CO99050715A patent/CO5261504A1/es not_active Application Discontinuation
- 1999-08-10 AR ARP990103985A patent/AR020147A1/es not_active Application Discontinuation
-
2001
- 2001-02-06 NO NO20010622A patent/NO20010622L/no not_active Application Discontinuation
- 2001-02-09 BG BG105236A patent/BG105236A/xx unknown
- 2001-03-08 HR HR20010164A patent/HRP20010164A2/hr not_active Application Discontinuation
- 2001-03-09 ZA ZA200101975A patent/ZA200101975B/en unknown
-
2002
- 2002-05-15 HK HK02103679.0A patent/HK1042086A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TR200100427T2 (tr) | 2001-07-23 |
| BR9912889A (pt) | 2001-05-08 |
| AU5374199A (en) | 2000-03-06 |
| HUP0104007A3 (en) | 2002-12-28 |
| SK832001A3 (en) | 2001-11-06 |
| BG105236A (en) | 2001-12-29 |
| JP2002522531A (ja) | 2002-07-23 |
| HUP0104007A2 (hu) | 2002-05-29 |
| IL140915A0 (en) | 2002-02-10 |
| NO20010622D0 (no) | 2001-02-06 |
| CN1323298A (zh) | 2001-11-21 |
| ID27965A (id) | 2001-05-03 |
| PL345998A1 (en) | 2002-01-14 |
| WO2000009489A1 (de) | 2000-02-24 |
| CA2340167A1 (en) | 2000-02-24 |
| AR020147A1 (es) | 2002-04-10 |
| CO5261504A1 (es) | 2003-03-31 |
| HRP20010164A2 (en) | 2002-04-30 |
| KR20010072378A (ko) | 2001-07-31 |
| HK1042086A1 (zh) | 2002-08-02 |
| NO20010622L (no) | 2001-02-06 |
| DE19836044A1 (de) | 2000-02-17 |
| EP1104410A1 (de) | 2001-06-06 |
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