AR022047A1 - Nuevos derivados de acidos carboxilicos con heterociclos de nitrogeno aril-sustituidos, su preparacion y utilizacion como antagonistas de los receptores deendotelina - Google Patents
Nuevos derivados de acidos carboxilicos con heterociclos de nitrogeno aril-sustituidos, su preparacion y utilizacion como antagonistas de los receptores deendotelinaInfo
- Publication number
- AR022047A1 AR022047A1 ARP000102660A ARP000102660A AR022047A1 AR 022047 A1 AR022047 A1 AR 022047A1 AR P000102660 A ARP000102660 A AR P000102660A AR P000102660 A ARP000102660 A AR P000102660A AR 022047 A1 AR022047 A1 AR 022047A1
- Authority
- AR
- Argentina
- Prior art keywords
- endothelin
- alkyl
- receptors
- halogen atoms
- carry
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
- C07D251/30—Only oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La endotelina es un péptido formado por 21 aminoácidos, que es sintetizado y liberado por el endotelio vascular. La endotelina existe en tres isoformas,ET-1, ET-2 y ET-3. La endotelina es un potente vasoconstrictor y tiene un fuerte efecto sobre elt ono vascular. Se sabe que esa vasoconstriccion es provocadapor la ligadura de endotelina a su receptor. La liberacion aumentada o anormal de endotelina provoca una contraccion vascular continua en los vasos sanguíneosperiféricos, renales ycerebrales , lo que puede llevar a enfermedades. Por lo menos dos subtipos de receptores de endotelina, los receptores ETA y ETB han sidodescriptos hasta ahora en la bibliografía y las sustancias que inhiben la ligadura de endotelina a uno o a ambosreceptores, antagonizan los efectosfisiologicos de endotelina y por lo tanto representan fármacos valiosos. Por lo tanto, se proveen antagonistas de los receptores de endotelina adicionales conpropiedades farmacologicas valiosas. Un derivado deácidos carboxíli cos de la Formula (1), en donde R1 es tetrazolilo o un grupo O=C-R en donde R tiene elsiguiente significado: a) un radical OR6, en donde R6 es: hidrogeno, el cation de un metal alcalino, el cation de un metal alcalinotérreo, un ionamonioorgánico fis iologicamente tolerable, como alquilamonio C1-4 terciario o el ion amonio; cicloalquilo C3-8, alquilo C1-8, CH2-fenilo que puede estar sustituidopor uno o varios de los siguientes radicales: halogeno, nitro, ciano, alquilo C1-4,haloalquilo C1-4, hid roxilo, alcoxi C1-4, mercapto, alquiltio C1-4, amino,NH(alquilo C1-4), N(alquilo C1-4)2; un grupo alquenilo C2-6 o alquinilo C3-6, pudiendo llevar estos grupos a su vez 1 a 5 átomos de halogeno; R6 puede serademás un radicalfenilo, que puede llevar 1 a 5 átomos de halogeno y/o 1 a 3 de los siguientes radicales: nitro, ciano, alquilo C1-4, haloalquilo C1-4,hidroxilo, alcoxi C1-4, mercapto, alquiltio C1-4, amino, NH(alquilo C1-4), N(alquilo C1-4)2; b) un sistemaheteroaromático de 5 miembros, lig ado a través de unátomo de nitrogeno, tal como pirrolilo, pirazolilo, imidazolilo y triazolilo, que puede llevar 1 a 2 átomos de halogeno, o 1 a 2 grupos alquilo C1-4 o 1 a 2
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19924892A DE19924892A1 (de) | 1999-06-01 | 1999-06-01 | Neue Carbonsäurederivate mit arylsubstituierten Stickstoffheterocyclen, ihre Herstellung und Verwendung als Endothelin Rezeptorantagonisten |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR022047A1 true AR022047A1 (es) | 2002-09-04 |
Family
ID=7909761
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000102660A AR022047A1 (es) | 1999-06-01 | 2000-05-30 | Nuevos derivados de acidos carboxilicos con heterociclos de nitrogeno aril-sustituidos, su preparacion y utilizacion como antagonistas de los receptores deendotelina |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1181281A2 (es) |
| JP (1) | JP2003500476A (es) |
| KR (1) | KR20020006049A (es) |
| CN (1) | CN1359376A (es) |
| AR (1) | AR022047A1 (es) |
| AU (1) | AU765345B2 (es) |
| BG (1) | BG106154A (es) |
| BR (1) | BR0011105A (es) |
| CA (1) | CA2375666A1 (es) |
| CZ (1) | CZ20014312A3 (es) |
| DE (1) | DE19924892A1 (es) |
| HK (1) | HK1047102A1 (es) |
| HU (1) | HUP0201387A3 (es) |
| IL (1) | IL146800A0 (es) |
| MX (1) | MXPA01012284A (es) |
| NO (1) | NO20015762L (es) |
| PL (1) | PL355112A1 (es) |
| SK (1) | SK17552001A3 (es) |
| TR (1) | TR200103475T2 (es) |
| WO (1) | WO2000073276A2 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120035196A1 (en) * | 2009-04-22 | 2012-02-09 | Kenji Negoro | Carboxylic acid compound |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR199901416T2 (xx) * | 1996-12-18 | 1999-08-23 | Basf Aktiengesellschaft | Heterosiklik karbonikasit t�revleri. |
| DE19726146A1 (de) * | 1997-06-19 | 1998-12-24 | Basf Ag | Neue ß-Amino und ß-Azidopcarbonsäurederivate, ihre Herstellung und Verwendung als Endothelinrezeptorantagonisten |
| BR9811631A (pt) * | 1997-09-04 | 2000-09-26 | Basf Ag | Derivado de ácido carboxìlico e uso do mesmo |
| DE19806438A1 (de) * | 1998-02-17 | 1999-08-19 | Basf Ag | Neue Carbonsäurederivate mit 5-substituiertem Pyrimidinring, ihre Herstellung und Verwendung |
| DE19809144A1 (de) * | 1998-03-04 | 1999-09-09 | Basf Ag | Neue unsymmetrisch substituierte Carbonsäurederivate, ihre Herstellung und Verwendung als gemischte ET¶LAMBDA¶/ET¶B¶-Rezeptorantagonisten |
| DE19836044A1 (de) * | 1998-08-10 | 2000-02-17 | Basf Ag | Neue Carbonsäurederivate, die Ketoseitenketten tragen, ihre Herstellung und Verwendung als Endothelin-Rezeptorantagonisten |
-
1999
- 1999-06-01 DE DE19924892A patent/DE19924892A1/de not_active Withdrawn
-
2000
- 2000-05-19 EP EP00938660A patent/EP1181281A2/de not_active Withdrawn
- 2000-05-19 CZ CZ20014312A patent/CZ20014312A3/cs unknown
- 2000-05-19 WO PCT/EP2000/004571 patent/WO2000073276A2/de not_active Application Discontinuation
- 2000-05-19 CA CA002375666A patent/CA2375666A1/en not_active Abandoned
- 2000-05-19 CN CN00809738A patent/CN1359376A/zh active Pending
- 2000-05-19 BR BR0011105-8A patent/BR0011105A/pt not_active IP Right Cessation
- 2000-05-19 MX MXPA01012284A patent/MXPA01012284A/es unknown
- 2000-05-19 PL PL00355112A patent/PL355112A1/xx not_active Application Discontinuation
- 2000-05-19 JP JP2000621342A patent/JP2003500476A/ja active Pending
- 2000-05-19 AU AU53959/00A patent/AU765345B2/en not_active Ceased
- 2000-05-19 IL IL14680000A patent/IL146800A0/xx unknown
- 2000-05-19 KR KR1020017015482A patent/KR20020006049A/ko not_active Application Discontinuation
- 2000-05-19 TR TR2001/03475T patent/TR200103475T2/xx unknown
- 2000-05-19 SK SK1755-2001A patent/SK17552001A3/sk unknown
- 2000-05-19 HU HU0201387A patent/HUP0201387A3/hu unknown
- 2000-05-30 AR ARP000102660A patent/AR022047A1/es unknown
-
2001
- 2001-11-26 NO NO20015762A patent/NO20015762L/no not_active Application Discontinuation
- 2001-11-27 BG BG106154A patent/BG106154A/xx unknown
-
2002
- 2002-11-29 HK HK02108677.1A patent/HK1047102A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL146800A0 (en) | 2002-07-25 |
| HK1047102A1 (zh) | 2003-02-07 |
| SK17552001A3 (sk) | 2002-08-06 |
| AU5395900A (en) | 2000-12-18 |
| EP1181281A2 (de) | 2002-02-27 |
| BR0011105A (pt) | 2002-03-05 |
| CA2375666A1 (en) | 2000-12-07 |
| MXPA01012284A (es) | 2002-07-30 |
| CN1359376A (zh) | 2002-07-17 |
| DE19924892A1 (de) | 2000-12-07 |
| HUP0201387A3 (en) | 2004-12-28 |
| NO20015762L (no) | 2001-12-13 |
| CZ20014312A3 (cs) | 2003-02-12 |
| WO2000073276A2 (de) | 2000-12-07 |
| WO2000073276A3 (de) | 2001-05-10 |
| TR200103475T2 (tr) | 2002-04-22 |
| JP2003500476A (ja) | 2003-01-07 |
| AU765345B2 (en) | 2003-09-18 |
| NO20015762D0 (no) | 2001-11-26 |
| HUP0201387A2 (en) | 2002-08-28 |
| PL355112A1 (en) | 2004-04-05 |
| KR20020006049A (ko) | 2002-01-18 |
| BG106154A (en) | 2002-08-30 |
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