HUP9800273A2 - Endotelin antagonista hatású benzotiazin-dioxid-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények - Google Patents
Endotelin antagonista hatású benzotiazin-dioxid-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP9800273A2 HUP9800273A2 HU9800273A HUP9800273A HUP9800273A2 HU P9800273 A2 HUP9800273 A2 HU P9800273A2 HU 9800273 A HU9800273 A HU 9800273A HU P9800273 A HUP9800273 A HU P9800273A HU P9800273 A2 HUP9800273 A2 HU P9800273A2
- Authority
- HU
- Hungary
- Prior art keywords
- powder
- general formula
- alkyl
- pco2r
- por
- Prior art date
Links
- GHNLJDPNIAIWOQ-UHFFFAOYSA-N 2h-1$l^{6},2-benzothiazine 1,1-dioxide Chemical class C1=CC=C2S(=O)(=O)NC=CC2=C1 GHNLJDPNIAIWOQ-UHFFFAOYSA-N 0.000 title 1
- 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
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000843 powder Substances 0.000 abstract 8
- -1 phenyl- Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001540 azides Chemical class 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
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- ZHXTWWCDMUWMDI-UHFFFAOYSA-N dihydroxyboron Chemical compound O[B]O ZHXTWWCDMUWMDI-UHFFFAOYSA-N 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229940126601 medicinal product Drugs 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Dental Preparations (AREA)
- Polyesters Or Polycarbonates (AREA)
Abstract
A találmány tárgyai új, (I) általánős képletű vegyületek, ahől az (I)általánős képletben R2 hidrőgénatőm, alkilcsőpőrt, (b) általánősképletű vagy (CH2)n-ciklőalkil-csőpőrt; Ra, Rb és Rc mindegyike 1-5vagy 1-4 szűbsztitűens, éspedig a következők közül: hidrőgén- vagyhalőgénatőm, alkil-, alkenil-, alkinil-, ciklőalkil-, fenil-, C(O)-fenil-, metilén-diőxi-, etilén-diőxi-, nitrő-, azidőcsőpőrt, -CN, -CF3, -CF2CF3, -CHO vagy -B(OH)2 képletű csőpőrt, -OR, -NRR1, -SR1, -COR, -CO2R, -CONRR1, -SO2NRR1, -SO2R, -OCOR, -NH(CH2)pCO2R, -S(CH2)pCO2R, -O(CH2)pCO2R, -O(CH2)pOR, -NH(CH2)pOR vagy -S(CH2)pORáltalánős képletű csőpőrt, amelyekben R és R1 egymástól függetlenülhidrőgénatőm, alkil-, alkenil- alkinil-, ciklőalkil- vagy adőttesetben szűbsztitűált fenil- vagy benzilcsőpőrt; Rd hidrőgénatőm, PO4Hvagy B(OH)2 képletű csőpőrt, -CO2R, -CO3R, -CONRR1, -SO2NRR1, -C(O)NHSO2R1, (c) vagy (d) általánős képletű csőpőrt, n 0-2, p 1-4, -egyes vagy kettős kötés; és X őxigénatőm, -(CH2)n-, -NR- vagy -S(O)n-általánős képletű csőpőrt. Az (I) általánős képletű vegyületekettartalmazó gyógyszerkészítmény a megemelkedett endőtelinszintkezelésére használhatók. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/393,143 US5599811A (en) | 1995-02-21 | 1995-02-21 | Benzothiazine dioxides as endothelin antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9800273A2 true HUP9800273A2 (hu) | 1999-07-28 |
| HUP9800273A3 HUP9800273A3 (en) | 1999-09-28 |
Family
ID=23553452
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9800273A HUP9800273A3 (en) | 1995-02-21 | 1996-01-26 | Benzothiazine dioxides as endothelin antagonists, process for their production and pharmaceutical compositions containing the same |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US5599811A (hu) |
| EP (1) | EP0811001B1 (hu) |
| JP (1) | JPH11501013A (hu) |
| KR (1) | KR19980702358A (hu) |
| CN (1) | CN1071327C (hu) |
| AT (1) | ATE207911T1 (hu) |
| AU (1) | AU720036B2 (hu) |
| BG (1) | BG62613B1 (hu) |
| CA (1) | CA2211027A1 (hu) |
| CZ (1) | CZ294412B6 (hu) |
| DE (1) | DE69616515T2 (hu) |
| DK (1) | DK0811001T3 (hu) |
| EE (1) | EE03564B1 (hu) |
| ES (1) | ES2167544T3 (hu) |
| FI (1) | FI973380A (hu) |
| GE (1) | GEP20001969B (hu) |
| HU (1) | HUP9800273A3 (hu) |
| NO (1) | NO308897B1 (hu) |
| NZ (1) | NZ302116A (hu) |
| PL (1) | PL321866A1 (hu) |
| PT (1) | PT811001E (hu) |
| RO (1) | RO116898B1 (hu) |
| RU (1) | RU2164225C2 (hu) |
| SK (1) | SK284275B6 (hu) |
| UA (1) | UA47424C2 (hu) |
| WO (1) | WO1996026195A1 (hu) |
| ZA (1) | ZA961342B (hu) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5962490A (en) * | 1987-09-25 | 1999-10-05 | Texas Biotechnology Corporation | Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin |
| US6342610B2 (en) | 1993-05-20 | 2002-01-29 | Texas Biotechnology Corp. | N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin |
| US6030991A (en) * | 1993-05-20 | 2000-02-29 | Texas Biotechnology Corp. | Benzenesulfonamides and the use thereof to modulate the activity of endothelin |
| US6376523B1 (en) | 1994-05-20 | 2002-04-23 | Texas Biotechnology Corporation | Benzenesulfonamides and the use thereof to modulate the activity of endothelin |
| US6541498B2 (en) | 1993-05-20 | 2003-04-01 | Texas Biotechnology | Benzenesulfonamides and the use thereof to modulate the activity of endothelin |
| US6613804B2 (en) | 1993-05-20 | 2003-09-02 | Encysive Pharmaceuticals, Inc. | Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin |
| US5945448A (en) * | 1995-06-02 | 1999-08-31 | Shionogi & Co., Ltd. | Brain edema inhibitor |
| US5804585A (en) | 1996-04-15 | 1998-09-08 | Texas Biotechnology Corporation | Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin |
| US5783705A (en) * | 1997-04-28 | 1998-07-21 | Texas Biotechnology Corporation | Process of preparing alkali metal salys of hydrophobic sulfonamides |
| EE04156B1 (et) | 1997-04-28 | 2003-10-15 | Texas Biotechnology Corporation | Sulfoonamiidid endoteliini vahendatud haiguste ravimiseks |
| BR9810456A (pt) | 1997-06-27 | 2001-09-25 | Fujisawa Pharmaceutical Co | Composto de sulfonamida, método para sua obtenção e seu uso farmacêutico |
| AU759169B2 (en) | 1997-09-05 | 2003-04-10 | Warner-Lambert Company | Certain benzothiazine dioxide endothelin antagonists and processes for their preparation |
| GB2337048B (en) * | 1998-05-05 | 2000-06-28 | Warner Lambert Co | 2,1,3-Benzothiadiazole containing endothelin antagonists |
| EP1289558A2 (en) * | 2000-05-31 | 2003-03-12 | Warner-Lambert Company Llc | Combinations of an endothelin receptor antagonist and an antiepileptic compound having pain alleviating properties or analgesic |
| US20020115661A1 (en) * | 2000-12-07 | 2002-08-22 | Keller Laurence Harvey | Method for treating chronic obstructive pulmonary disease |
| RU2435585C2 (ru) * | 2006-04-13 | 2011-12-10 | Актелион Фармасьютиклз Лтд | Антагонисты рецептора эндотелина, предназначенные для ранней стадии идиопатического фиброза легких |
| FR2942797B1 (fr) * | 2009-03-03 | 2011-04-29 | Pf Medicament | Derives de benzothiazines, leur preparation et leur application a titre de medicaments |
| EP3509588B1 (en) * | 2016-09-12 | 2023-06-07 | Integral Health,Inc. | Bicyclic compounds useful as gpr120 modulators |
| CN112521384B (zh) * | 2021-01-13 | 2021-11-02 | 湖北大学 | 溶剂热一锅法合成苯并噻嗪并环戊二烯衍生物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3237473A1 (de) * | 1982-10-09 | 1984-04-12 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue 4-hydroxy-2h-1,2-benzothiazin-3-carboxamid-1,1-dioxide, verfahren zu ihrer herstellung, ihre verwendung und diese verbindungen enthaltende arzneimittel |
| CA2032559C (en) * | 1989-12-28 | 2001-11-06 | Kiyofumi Ishikawa | Endothelin antagonistic cyclic pentapeptides |
| JPH0441483A (ja) * | 1990-06-07 | 1992-02-12 | Tanabe Seiyaku Co Ltd | ベンゾチアジン誘導体及びその製法 |
| CZ287406B6 (cs) * | 1991-11-05 | 2000-11-15 | Smithkline Beecham Corporation | Indanové a indenové deriváty, způsob jejich výroby a farmaceutické prostředky s jejich obsahem |
| US5389620A (en) * | 1993-08-18 | 1995-02-14 | Banyu Pharmaceutical Co., Ltd. | Endothelin antagonistic heteroaromatic ring-fused cyclopentene derivatives |
-
1995
- 1995-02-21 US US08/393,143 patent/US5599811A/en not_active Expired - Fee Related
-
1996
- 1996-01-26 ES ES96903708T patent/ES2167544T3/es not_active Expired - Lifetime
- 1996-01-26 CA CA002211027A patent/CA2211027A1/en not_active Abandoned
- 1996-01-26 SK SK1146-97A patent/SK284275B6/sk unknown
- 1996-01-26 KR KR1019970705755A patent/KR19980702358A/ko not_active Application Discontinuation
- 1996-01-26 RU RU97116154/04A patent/RU2164225C2/ru not_active IP Right Cessation
- 1996-01-26 JP JP8525692A patent/JPH11501013A/ja not_active Abandoned
- 1996-01-26 PT PT96903708T patent/PT811001E/pt unknown
- 1996-01-26 EP EP96903708A patent/EP0811001B1/en not_active Expired - Lifetime
- 1996-01-26 CZ CZ19972607A patent/CZ294412B6/cs not_active IP Right Cessation
- 1996-01-26 CN CN96192042A patent/CN1071327C/zh not_active Expired - Fee Related
- 1996-01-26 AT AT96903708T patent/ATE207911T1/de not_active IP Right Cessation
- 1996-01-26 EE EE9700147A patent/EE03564B1/xx not_active IP Right Cessation
- 1996-01-26 AU AU47703/96A patent/AU720036B2/en not_active Ceased
- 1996-01-26 WO PCT/US1996/001093 patent/WO1996026195A1/en active IP Right Grant
- 1996-01-26 DK DK96903708T patent/DK0811001T3/da active
- 1996-01-26 GE GEAP19963855A patent/GEP20001969B/en unknown
- 1996-01-26 PL PL96321866A patent/PL321866A1/xx unknown
- 1996-01-26 UA UA97094674A patent/UA47424C2/uk unknown
- 1996-01-26 RO RO97-01580A patent/RO116898B1/ro unknown
- 1996-01-26 HU HU9800273A patent/HUP9800273A3/hu unknown
- 1996-01-26 DE DE69616515T patent/DE69616515T2/de not_active Expired - Fee Related
- 1996-02-20 ZA ZA961342A patent/ZA961342B/xx unknown
-
1997
- 1997-08-18 FI FI973380A patent/FI973380A/fi unknown
- 1997-08-20 NO NO973822A patent/NO308897B1/no not_active IP Right Cessation
- 1997-08-21 NZ NZ302116A patent/NZ302116A/en unknown
- 1997-09-01 BG BG101867A patent/BG62613B1/bg unknown
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