HUP0202646A2 - 5,6-Szubsztituált pirimidin-gyűrűt tartalmazó új karbonsavszármazékok, előállításuk, alkalmazásuk endotelin receptor antagonista gyógyszerkészítmények előállítására és a vegyületeket tartalmazó gyógyszerkészítmények - Google Patents
5,6-Szubsztituált pirimidin-gyűrűt tartalmazó új karbonsavszármazékok, előállításuk, alkalmazásuk endotelin receptor antagonista gyógyszerkészítmények előállítására és a vegyületeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0202646A2 HUP0202646A2 HU0202646A HUP0202646A HUP0202646A2 HU P0202646 A2 HUP0202646 A2 HU P0202646A2 HU 0202646 A HU0202646 A HU 0202646A HU P0202646 A HUP0202646 A HU P0202646A HU P0202646 A2 HUP0202646 A2 HU P0202646A2
- Authority
- HU
- Hungary
- Prior art keywords
- optionally substituted
- group
- alkyl
- alkenyl
- alkynyl
- Prior art date
Links
- 150000001732 carboxylic acid derivatives Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 229940118365 Endothelin receptor antagonist Drugs 0.000 title 1
- 239000002308 endothelin receptor antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000714 pyrimidinyl group Chemical group 0.000 title 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 125000000304 alkynyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 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
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- -1 phenyl- Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical class [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 abstract 1
- 102000002045 Endothelin Human genes 0.000 abstract 1
- 108050009340 Endothelin Proteins 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001768 cations Chemical class 0.000 abstract 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 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000002184 metal Chemical group 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
-
- 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
- A61P9/04—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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
A találmány tárgyát az általános képletű karbonsavszármazékok - amelyekben R1 tetrazolilcsoport vagy csoport, amelyben R a) - OR7 általános képletű csoport, ebben R7 hidrogénatom, fém kation, cikloalkil-, alkil-, adott esetben szubsztituált ammóniumion, -CH2-fenil-, fenil-, alkenil-, alkinilcsoport, b) adott esetben szubsztituált heteroaromás rendszer; c) általános képletű csoport, amelyben k 0-2, p 1-4, és R8 1-4 alkil-, cikloalkil-, alkenil-, alkinil- vagy adott esetben szubsztituált fenilcsoport; d) csoport, amelyben R9 adott esetben szubsztituált alkil-, alkenil-, alkinil-, cikloalkilcsoport; R2 hidroxi-, adott esetben szubsztituált amino-, alkil-, alkenil-, alkinil-, alkoxi-, alkil-tio- csoport vagy CR2 a CR3 -mal együtt egy adott esetben szubsztituált alkilén- vagy alkeniléngyűrűt képez; R3 halogénatom, hidroxi-, adott esetben szubsztituált amino-, alkil-, alkenil-, alkinil-, alkenil-oxi, alkil-karbonil-, alkoxi-karbonil-, -NH-O-alkil-, alkil-tio-csoport, vagy CR3 CR2 -vel gyűrűt képez; R4 és R5 cikloalkil- vagy adott esetben szubsztituált és adott esetben összekapcsolt fenil- vagy naftilcsoport; R6 hidrogénatom, adott esetben szubsztituált alkil-, alkenil-, alkinil-, cikloalkil-, fenil-, naftilcsoport vagy heteroaromás gyűrű; és Z kén vagy oxigénatom és endotelin-antagonistákként gyógyszerkészítmények előállítására való alkalmazásuk képezik. A találmány kiterjed az (I) általános képletű vegyületeket tartalmazó gyógyszerkészítményekre is. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19933164A DE19933164A1 (de) | 1999-07-20 | 1999-07-20 | Neue Carbonsäurederivate mit 5,6 substituiertem Pyrimidinring, ihre Herstellung und Verwendung als Endothelin Rezeptorantagonisten |
| PCT/EP2000/006293 WO2001005771A1 (de) | 1999-07-20 | 2000-07-05 | Neue carbonsäurederivate mit 5,6 substituiertem pyrimidinring, ihre herstellung und verwendung als endothelin rezeptorantagonisten |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0202646A2 true HUP0202646A2 (hu) | 2003-02-28 |
| HUP0202646A3 HUP0202646A3 (en) | 2003-03-28 |
Family
ID=7914884
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0202646A HUP0202646A3 (en) | 1999-07-20 | 2000-07-05 | Novel carboxylic acid derivatives with 5,6 substituted pyrimidine ring, the production and utilization thereof for producing endothelin receptor antagonists and pharmaceutical compositions containing the compounds |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1196394A1 (hu) |
| JP (1) | JP2003505377A (hu) |
| KR (1) | KR20020019550A (hu) |
| CN (1) | CN1367778A (hu) |
| AR (1) | AR030026A1 (hu) |
| AU (1) | AU6561500A (hu) |
| BG (1) | BG106321A (hu) |
| BR (1) | BR0012592A (hu) |
| CA (1) | CA2379545A1 (hu) |
| CZ (1) | CZ2002190A3 (hu) |
| DE (1) | DE19933164A1 (hu) |
| HU (1) | HUP0202646A3 (hu) |
| IL (1) | IL147666A0 (hu) |
| MX (1) | MXPA02000616A (hu) |
| NO (1) | NO20020254L (hu) |
| PL (1) | PL353165A1 (hu) |
| SK (1) | SK772002A3 (hu) |
| TR (1) | TR200200622T2 (hu) |
| TW (1) | TW555749B (hu) |
| WO (1) | WO2001005771A1 (hu) |
| ZA (1) | ZA200200333B (hu) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011004402A2 (en) * | 2009-07-10 | 2011-01-13 | Cadila Healthcare Limited | Improved process for the preparation of ambrisentan and novel intermediates thereof |
| US20130060031A1 (en) | 2010-03-15 | 2013-03-07 | Natco Pharma Limited | Process for the preparation of highly pure ambrisentan |
Family Cites Families (2)
| 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 |
| WO1999023078A2 (de) * | 1997-10-31 | 1999-05-14 | Basf Aktiengesellschaft | Neue carbonsäurederivate, die amidseitenketten tragen, ihre herstellung und verwendung als endothelin-rezeptorantagonisten |
-
1999
- 1999-07-20 DE DE19933164A patent/DE19933164A1/de not_active Withdrawn
-
2000
- 2000-07-05 CN CN00810533A patent/CN1367778A/zh active Pending
- 2000-07-05 JP JP2001511432A patent/JP2003505377A/ja not_active Abandoned
- 2000-07-05 IL IL14766600A patent/IL147666A0/xx unknown
- 2000-07-05 AU AU65615/00A patent/AU6561500A/en not_active Abandoned
- 2000-07-05 KR KR1020027000815A patent/KR20020019550A/ko not_active Application Discontinuation
- 2000-07-05 HU HU0202646A patent/HUP0202646A3/hu unknown
- 2000-07-05 WO PCT/EP2000/006293 patent/WO2001005771A1/de not_active Application Discontinuation
- 2000-07-05 SK SK77-2002A patent/SK772002A3/sk unknown
- 2000-07-05 MX MXPA02000616A patent/MXPA02000616A/es unknown
- 2000-07-05 PL PL00353165A patent/PL353165A1/xx not_active Application Discontinuation
- 2000-07-05 CA CA002379545A patent/CA2379545A1/en not_active Abandoned
- 2000-07-05 BR BR0012592-0A patent/BR0012592A/pt not_active IP Right Cessation
- 2000-07-05 TR TR2002/00622T patent/TR200200622T2/xx unknown
- 2000-07-05 EP EP00953009A patent/EP1196394A1/de not_active Withdrawn
- 2000-07-05 CZ CZ2002190A patent/CZ2002190A3/cs unknown
- 2000-07-13 TW TW089113992A patent/TW555749B/zh active
- 2000-07-17 AR ARP000103661A patent/AR030026A1/es unknown
-
2002
- 2002-01-15 ZA ZA200200333A patent/ZA200200333B/en unknown
- 2002-01-17 NO NO20020254A patent/NO20020254L/no not_active Application Discontinuation
- 2002-01-18 BG BG106321A patent/BG106321A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0202646A3 (en) | 2003-03-28 |
| CZ2002190A3 (cs) | 2003-08-13 |
| SK772002A3 (en) | 2003-01-09 |
| CN1367778A (zh) | 2002-09-04 |
| NO20020254L (no) | 2002-02-20 |
| BG106321A (en) | 2002-08-30 |
| WO2001005771A1 (de) | 2001-01-25 |
| TW555749B (en) | 2003-10-01 |
| TR200200622T2 (hu) | 2002-06-21 |
| AR030026A1 (es) | 2003-08-13 |
| AU6561500A (en) | 2001-02-05 |
| MXPA02000616A (es) | 2002-08-30 |
| JP2003505377A (ja) | 2003-02-12 |
| PL353165A1 (en) | 2003-10-20 |
| DE19933164A1 (de) | 2001-01-25 |
| EP1196394A1 (de) | 2002-04-17 |
| BR0012592A (pt) | 2002-05-28 |
| CA2379545A1 (en) | 2001-01-25 |
| ZA200200333B (en) | 2003-04-30 |
| IL147666A0 (en) | 2002-08-14 |
| KR20020019550A (ko) | 2002-03-12 |
| NO20020254D0 (no) | 2002-01-17 |
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