ATE197305T1 - Endothelin antagonisten - Google Patents
Endothelin antagonistenInfo
- Publication number
- ATE197305T1 ATE197305T1 AT92120225T AT92120225T ATE197305T1 AT E197305 T1 ATE197305 T1 AT E197305T1 AT 92120225 T AT92120225 T AT 92120225T AT 92120225 T AT92120225 T AT 92120225T AT E197305 T1 ATE197305 T1 AT E197305T1
- Authority
- AT
- Austria
- Prior art keywords
- group
- lower alkyl
- formula
- alkyl group
- atom
- Prior art date
Links
- 102000002045 Endothelin Human genes 0.000 title 1
- 108050009340 Endothelin Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 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 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 17
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- -1 1-adamantyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000004149 thio group Chemical group *S* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06043—Leu-amino acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Crystallography & Structural Chemistry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP34767091 | 1991-12-04 | ||
| JP35373891 | 1991-12-18 | ||
| JP23420792 | 1992-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE197305T1 true ATE197305T1 (de) | 2000-11-15 |
Family
ID=27332096
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT92120225T ATE197305T1 (de) | 1991-12-04 | 1992-11-26 | Endothelin antagonisten |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP0555537B1 (https=) |
| AT (1) | ATE197305T1 (https=) |
| AU (1) | AU657585B2 (https=) |
| CA (1) | CA2084163C (https=) |
| DE (1) | DE69231546T2 (https=) |
| TW (1) | TW217417B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2121724A1 (en) | 1993-04-21 | 1994-10-22 | Toshifumi Watanabe | Methods and compositions for the prophylactic and/or therapeutic treatment of organ hypofunction |
| CA2135151A1 (en) * | 1993-11-08 | 1995-05-09 | Mitsuhiro Wakimasu | Cyclic hexapeptides, their production and use |
| US6017887A (en) * | 1995-01-06 | 2000-01-25 | Sibia Neurosciences, Inc. | Peptide, peptide analog and amino acid analog protease inhibitors |
| AU5687396A (en) * | 1995-04-21 | 1996-11-07 | Novarits Ag | N-aroylamino acid amides as endothelin inhibitors |
| CA2229263A1 (en) * | 1995-09-26 | 1997-04-03 | Toshifumi Watanabe | Peptide derivatives, their production and use |
| US7115664B2 (en) | 2000-03-16 | 2006-10-03 | Sepracor Inc. | Peptidomimetic ligands for cellular receptors and ion channels |
| DE10105077A1 (de) * | 2001-02-05 | 2002-08-08 | Febit Ferrarius Biotech Gmbh | Hybrid-Schutzgruppe |
| DE60120104T2 (de) | 2001-03-20 | 2006-09-21 | Schwarz Pharma Ag | Neue Verwendung von Peptidverbindungen bei der Behandlung von nicht-neuropathischem Entzündungsschmerz |
| DK1243263T3 (da) | 2001-03-21 | 2003-03-17 | Sanol Arznei Schwarz Gmbh | Hidtil ukendt anvendelse af en klasse af peptidforbindelser til behandling af allodyni eller andre forskellige typer af kronisk- eller fantomsmerte |
| JP4664924B2 (ja) | 2003-12-02 | 2011-04-06 | ウーツェーベー ファルマ ゲーエムベーハー | 中枢神経因性疼痛の治療のためのペプチド化合物の新規使用 |
| AU2005232395B2 (en) | 2004-04-16 | 2010-09-09 | Schwarz Pharma Ag | Use of peptidic compounds for the prophylaxis and treatment of chronic headache |
| EP1604655A1 (en) | 2004-06-09 | 2005-12-14 | Schwarz Pharma Ag | Novel use of peptide compounds for treating pain in trigeminal neuralgia |
| EA014055B1 (ru) | 2004-08-27 | 2010-08-30 | Шварц Фарма Аг | Применение пептидных соединений для лечения боли при раке кости, а также боли, вызванной химиотерапией и нуклеозидами |
| EA019757B1 (ru) | 2006-06-15 | 2014-06-30 | ЮСиБи ФАРМА ГМБХ | Фармацевтическая композиция с синергетическим противосудорожным эффектом |
| US10695400B2 (en) | 2015-08-03 | 2020-06-30 | Enb Therapeutics, Inc. | Compositions and methods for treating cancers associated with ETBR activation |
| GB201712282D0 (en) * | 2017-07-31 | 2017-09-13 | Nodthera Ltd | Selective inhibitors of NLRP3 inflammasome |
| AU2019206652B2 (en) | 2018-01-12 | 2024-11-14 | Enb Therapeutics, Inc. | Deuterated compounds, compositions, and methods for treating cancers associated with ETBR activation |
| EP3746110A4 (en) * | 2018-03-30 | 2022-03-02 | ENB Therapeutics, Inc. | ETBR ANTAGONIST COMPOUNDS, COMPOSITIONS AND USES |
| EP4089102A1 (en) * | 2021-05-14 | 2022-11-16 | Insusense ApS | Modulators of sortilin activity |
| CN120271660B (zh) * | 2025-06-09 | 2025-08-19 | 杭州肽佳生物科技有限公司 | 一种高效选择性拮抗剂bq-788的制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5284828A (en) * | 1990-05-14 | 1994-02-08 | Fujisawa Pharmaceutical Co. Ltd. | Peptide compound and its preparation |
| CA2043741C (en) * | 1990-06-07 | 2003-04-01 | Kiyofumi Ishikawa | Endothelin antagonistic peptide derivatives |
| GB9123967D0 (en) * | 1991-11-12 | 1992-01-02 | Fujisawa Pharmaceutical Co | New compound and its preparation |
-
1992
- 1992-11-25 TW TW081109457A patent/TW217417B/zh not_active IP Right Cessation
- 1992-11-26 DE DE69231546T patent/DE69231546T2/de not_active Expired - Lifetime
- 1992-11-26 AT AT92120225T patent/ATE197305T1/de not_active IP Right Cessation
- 1992-11-26 EP EP92120225A patent/EP0555537B1/en not_active Expired - Lifetime
- 1992-11-30 CA CA002084163A patent/CA2084163C/en not_active Expired - Lifetime
- 1992-12-02 AU AU29838/92A patent/AU657585B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| EP0555537A3 (en) | 1994-11-02 |
| EP0555537A2 (en) | 1993-08-18 |
| DE69231546D1 (de) | 2000-12-07 |
| DE69231546T2 (de) | 2001-05-31 |
| AU657585B2 (en) | 1995-03-16 |
| CA2084163C (en) | 2004-06-29 |
| CA2084163A1 (en) | 1993-06-05 |
| EP0555537B1 (en) | 2000-11-02 |
| AU2983892A (en) | 1993-06-10 |
| TW217417B (https=) | 1993-12-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |