AR037821A1 - 2-guanidin-4-heterociclilquinazolinas - Google Patents
2-guanidin-4-heterociclilquinazolinasInfo
- Publication number
- AR037821A1 AR037821A1 ARP020104838A ARP020104838A AR037821A1 AR 037821 A1 AR037821 A1 AR 037821A1 AR P020104838 A ARP020104838 A AR P020104838A AR P020104838 A ARP020104838 A AR P020104838A AR 037821 A1 AR037821 A1 AR 037821A1
- Authority
- AR
- Argentina
- Prior art keywords
- hal
- polysubstituted
- monosubstituted
- compounds
- nha
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 aromatic heterocyclic radical Chemical class 0.000 abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 abstract 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 206010020852 Hypertonia Diseases 0.000 abstract 1
- 108091006649 SLC9A3 Proteins 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 102000046061 Sodium-Hydrogen Exchanger 3 Human genes 0.000 abstract 1
- 230000002253 anti-ischaemic effect Effects 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 239000002934 diuretic Substances 0.000 abstract 1
- 229940030606 diuretics Drugs 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
- C07D213/50—Ketonic radicals
-
- 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
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos 2-guanidin-4-heterociclilquinazolinas. Uso para preparar medicamentos inhibidores de NHE-3, preparación farmacéutica, proceso para obtenerlas, medicamento, kit, proceso para preparar los compuestos e intermediarios. Utiles para tratar hipertonía, como diuréticos, anti-isquémicos. Reivindicación 1: Compuestos, caracterizados porque son de la fórmula (1), donde: Y es un compuestos seleccionado de las fórmulas (2) ó (3); Het es un radical heterocíclico saturado, insaturado o aromático que no está sustituido o que está monosustituido o polisustituido con R3 y/o R4; R1, R2, R3 y R4 son cada uno, independientemente entre sí, H, A, OA, Hal, CF3, CH2CONH2, CH2CO2H, CH2CO2A, CH2NH2, CH2NA2, CH2NHA, CH2OH, CH2OA, OH, NO2, NH2, NHA, NA2, NHCO-A, NH-CO-Ph, SA, SO-A, SO2-A, SO2-Ph, CN, OCF3, CO-A, CO2H, CO2A, CO-NH2, CO-NHA, CO-NA2, SO2NH2, SO2NHA, SO2NA2, CHO, o son fenilo, bencilo o ciclohexilmetilo, cada uno de los cuales puede no estar sustituido o estar monosustituido o polisustituido con A, OH, OA, Hal, CN o CF3, o es un radical heterocíclico que está monosustituido o polisustituido con A, OH, OA, Hal, CN o CF3; A es un alquilo C1-6; Hal es un F, Cl, Br o I; R5, R6, R7 y R8 son cada uno, independientemente entre sí, H, bencilo, alilo u otro grupo aminoprotector, A, o fenilo, que no está sustituido o que está monosustituido o polisustituido con A, OA, CN, Hal o CF3, donde R5 y R7, R5 y R6 y R7 y R8 pueden formar anillos de 5 a 7 miembros, y las sales, los solvatos y estereoisómeros de los mismos, incluyendo mezclas de los mismos en cualquier proporción, y derivados de utilidad farmacéutica de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10161767A DE10161767A1 (de) | 2001-12-15 | 2001-12-15 | 2-Guanidino-4-heterocyclyl-chinazoline |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037821A1 true AR037821A1 (es) | 2004-12-09 |
Family
ID=7709413
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104838A AR037821A1 (es) | 2001-12-15 | 2002-12-13 | 2-guanidin-4-heterociclilquinazolinas |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20050113396A1 (es) |
| EP (1) | EP1453823A1 (es) |
| KR (1) | KR20040065233A (es) |
| AR (1) | AR037821A1 (es) |
| AU (1) | AU2002342918A1 (es) |
| BR (1) | BR0214875A (es) |
| CA (1) | CA2470030A1 (es) |
| DE (1) | DE10161767A1 (es) |
| MX (1) | MXPA04005692A (es) |
| PL (1) | PL370174A1 (es) |
| WO (1) | WO2003051866A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7241775B2 (en) | 2003-03-24 | 2007-07-10 | Sanofi-Aventis Deutschland Gmbh | Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines |
| DE10312963A1 (de) * | 2003-03-24 | 2004-10-07 | Aventis Pharma Deutschland Gmbh | Substituierte 4-Phenyltetrahydroisochinoline, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, sowie sie enthaltendes Medikament |
| BRPI0918502A2 (pt) | 2008-09-02 | 2015-12-01 | Sanofi Aventis | aminoindanos substituídos e análogos dos mesmos, e o uso farmacêutico dos mesmos |
| WO2018129556A1 (en) | 2017-01-09 | 2018-07-12 | Ardelyx, Inc. | Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders |
| SI2384318T1 (en) | 2008-12-31 | 2018-03-30 | Ardelyx, Inc. | MEASURES AND PROCEDURES FOR THE INHIBITION OF ANTIPORT INHIBITED BY NHE IN THE TREATMENT OF DISEASES RELATED TO STRENGTH OF FLAMMABILITY OR TRADEMARITY WITH SOLO, AND THE EMISSION OF GASTROINTESTINAL TREATMENT |
| US10376481B2 (en) | 2012-08-21 | 2019-08-13 | Ardelyx, Inc. | Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders |
| RU2015107019A (ru) | 2012-08-21 | 2016-10-10 | Эрделикс Инк. | Соединения и способы для ингибирования nhe-опосредованного антипорта в лечении расстройств, ассоциированных с задержкой жидкости или солевой перегрузкой и заболеваний желудочно-кишечного тракта |
| MX382203B (es) | 2013-04-12 | 2025-03-11 | Ardelyx Inc | Compuestos de union a nhe3 (intercambiador de sodio-hidrogeno 3) y metodos para inhibir transporte de fosfato. |
| KR102386666B1 (ko) | 2014-07-25 | 2022-04-15 | 다이쇼 세이야꾸 가부시끼가이샤 | 헤테로아릴로 치환된 페닐테트라히드로이소퀴놀린 화합물 |
| UA126283C2 (uk) | 2017-01-09 | 2022-09-14 | Арделікс, Інк. | Сполуки, придатні для лікування розладів шлунково-кишкового тракту |
| JP2020505333A (ja) | 2017-01-09 | 2020-02-20 | アルデリックス， インコーポレイテッド | Ｎｈｅ媒介性アンチポートの阻害薬 |
| KR20240144491A (ko) | 2017-08-04 | 2024-10-02 | 알데릭스, 인코포레이티드 | 고칼륨혈증 치료를 위한 글리시레틴산 유도체 |
| EP4234016B1 (en) | 2019-02-07 | 2025-06-18 | Ardelyx, Inc. | Glycyrrhetinic acid derivatives for use in treating hyperkalemia |
| WO2020237096A1 (en) | 2019-05-21 | 2020-11-26 | Ardelyx, Inc. | Combination for lowering serum phosphate in a patient |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US395526A (en) * | 1889-01-01 | Tenoning-ivjachine | ||
| US396495A (en) * | 1889-01-22 | Ink-bottle and attachment therefor | ||
| NL122319C (es) * | 1961-06-20 | |||
| NL292083A (es) * | 1962-09-18 | |||
| US3950526A (en) * | 1970-04-20 | 1976-04-13 | Sumitomo Chemical Company, Limited | Quinazoline derivatives in pharmaceutical compositions for treating pain and inflammation |
| BE795970A (fr) * | 1972-02-29 | 1973-08-27 | Pfizer | Nouveaux derives de quinoleine, quinoxaline et quinazoline er composition pharmaceutiques les contenant |
| US3900476A (en) * | 1973-05-17 | 1975-08-19 | Upjohn Co | 2(2'-pyrimidylamino)quinazolines and their preparation |
| US3956495A (en) * | 1973-10-30 | 1976-05-11 | Eli Lilly And Company | 2,4-Diaminoquinazolines as antithrombotic agents |
| IL102764A0 (en) * | 1991-08-16 | 1993-01-31 | Merck & Co Inc | Quinazoline derivatives,and pharmaceutical compositions containing them |
| DE19633966A1 (de) * | 1996-08-22 | 1998-02-26 | Hoechst Ag | Phenylsubstituierte Alkenylcarbonsäure-guanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament |
| DE10019062A1 (de) * | 2000-04-18 | 2001-10-25 | Merck Patent Gmbh | 2-Guanidino-4-aryl-chinazoline als NHE-3 Inhibitoren |
| KR100383080B1 (ko) * | 2000-09-05 | 2003-05-12 | 주식회사 포스코 | 조절된 아민기 밀도와 공간을 제공하는 분자층을 표면에포함하는 기질 및 이의 제조방법 |
| US20030139431A1 (en) * | 2001-09-24 | 2003-07-24 | Kawakami Joel K. | Guanidines which are agonist/antagonist ligands for neuropeptide FF (NPFF) receptors |
-
2001
- 2001-12-15 DE DE10161767A patent/DE10161767A1/de not_active Withdrawn
-
2002
- 2002-11-21 WO PCT/EP2002/013061 patent/WO2003051866A1/de not_active Ceased
- 2002-11-21 US US10/498,806 patent/US20050113396A1/en not_active Abandoned
- 2002-11-21 CA CA002470030A patent/CA2470030A1/en not_active Abandoned
- 2002-11-21 AU AU2002342918A patent/AU2002342918A1/en not_active Abandoned
- 2002-11-21 PL PL02370174A patent/PL370174A1/xx unknown
- 2002-11-21 MX MXPA04005692A patent/MXPA04005692A/es unknown
- 2002-11-21 BR BR0214875-7A patent/BR0214875A/pt not_active Application Discontinuation
- 2002-11-21 EP EP02779568A patent/EP1453823A1/de not_active Withdrawn
- 2002-11-21 KR KR10-2004-7008399A patent/KR20040065233A/ko not_active Withdrawn
- 2002-12-13 AR ARP020104838A patent/AR037821A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2470030A1 (en) | 2003-06-26 |
| AU2002342918A1 (en) | 2003-06-30 |
| PL370174A1 (en) | 2005-05-16 |
| WO2003051866A1 (de) | 2003-06-26 |
| MXPA04005692A (es) | 2004-12-06 |
| KR20040065233A (ko) | 2004-07-21 |
| BR0214875A (pt) | 2004-12-28 |
| US20050113396A1 (en) | 2005-05-26 |
| EP1453823A1 (de) | 2004-09-08 |
| DE10161767A1 (de) | 2003-06-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |