AR013153A1 - Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n. - Google Patents
Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n.Info
- Publication number
- AR013153A1 AR013153A1 ARP980103175A ARP980103175A AR013153A1 AR 013153 A1 AR013153 A1 AR 013153A1 AR P980103175 A ARP980103175 A AR P980103175A AR P980103175 A ARP980103175 A AR P980103175A AR 013153 A1 AR013153 A1 AR 013153A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- derivatives
- ring
- alkoxy
- substituted
- Prior art date
Links
- 108090000312 Calcium Channels Proteins 0.000 title abstract 2
- 102000003922 Calcium Channels Human genes 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 230000001537 neural effect Effects 0.000 title abstract 2
- 239000003446 ligand Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- -1 amino, hydroxy Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 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
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- OKGNMRKOGWTADH-UHFFFAOYSA-N 1,4-dihydropyrimidine Chemical compound C1C=CNC=N1 OKGNMRKOGWTADH-UHFFFAOYSA-N 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P9/10—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
-
- 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
- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Derivados de 2-arildihidropirimidina, que comprende la formula I incluyendo su forma tautomérica 3,4-dihidropirimidina en la cual: R1 representa un anillomonocíclico aromático que optativamente incorpora una o tres heteroátomos que pueden ser iguales o diferentes y que son elegidos entre N, O o S, anillo quepuede ser optativamente sustituido con halogeno, alquilo C1 a 6, alcoxi C1 a 6 trifluorometilo; R2 represena alquilo C1 a 6 o alquilo C2 a 6, optativamenteincluyendo O, o bien S, y que está sustituido con un anillo de fenilo o heteroarilo monocíclico, anillo aromático que está sustituido con uno o mássustituyentes seleccionados entre halogeno, alquilo C1 a 6 o alcoxi C1 a 6; R3 representa un anillo monocíclico o bicíclico optativamente incorpora un átomoseleccionado entre N, O o S, optativamente sustituido con uno o más sustituyentes independientemenete seleccionados entre, alquilo C1 a 6, alcoxiC1 a 6, ciano, trifluorometilo, amino, hidroxi, nitro o carbometoxi; R4 y R5 representan independientemente hidrogeno, alquilo C1 a 6 o bencilo; o el grupoNR4R5 junto representa piperidinilo, morfolinilo, 3,4-deshidropiperidinilo, tiomorfolinilo, perhidroazepinilo, pirrolidinilo, piperazinilo o piperaziniloque también esta sustituido en N-4 por alquilo C1 a 6; R6 y R7 representan independientemente alquilo C1 a 6 o cicloalquilo C3 a 6, o bencilo,optativamente sustituido en el anillo fenilo por alquilo C1 a 6 alcoxi C1 a 6 o halogeno; X representaO, S o NR6; R8 representa hidrogeno o alquilo C1 a 6; yn representa un entero de 2 a 4; y los isomeros opticos y racematos de los mismos, así como las sales farmacéuticamente aceptables; de los mismos,procesos para su preparacion, composicionesque los contienen y su uso como antagonistas de los canales de calcio neuronales tipo N que sirven para el
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE9702564A SE9702564D0 (sv) | 1997-07-02 | 1997-07-02 | New compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR013153A1 true AR013153A1 (es) | 2000-12-13 |
Family
ID=20407620
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980103175A AR013153A1 (es) | 1997-07-02 | 1998-06-30 | Derivados de 2-arildihidropirimidina, proceso para su preparacion, composiciones farmaceuticas que contienen dichos derivados, y el uso de dichosderivados y composiciones como ligandos para canales de calcio neuronales de tipo n. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6218538B1 (es) |
| EP (1) | EP0993450A1 (es) |
| JP (1) | JP2002508780A (es) |
| AR (1) | AR013153A1 (es) |
| AU (1) | AU8249998A (es) |
| CA (1) | CA2294746A1 (es) |
| SE (1) | SE9702564D0 (es) |
| WO (1) | WO1999001438A1 (es) |
| ZA (1) | ZA985323B (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19817264A1 (de) * | 1998-04-18 | 1999-10-21 | Bayer Ag | Neue Dihydropyrimidine |
| DE19817265A1 (de) * | 1998-04-18 | 1999-10-21 | Bayer Ag | Verwendung von Dihydropyrimidinen als Arzneimittel und neue Stoffe |
| US20040259866A1 (en) * | 1998-06-30 | 2004-12-23 | Snutch Terrance P. | Calcium channel blockers comprising two benzhydril moieties |
| AU4289100A (en) * | 1999-03-25 | 2000-10-16 | Bayer Aktiengesellschaft | Dihydropyrimidines and their use in the treatment of hepatitis |
| AU5568400A (en) | 1999-06-23 | 2001-01-09 | Ajinomoto Co., Inc. | Novel dihydropyrimidine derivatives |
| DE10012824A1 (de) * | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10012823A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013126A1 (de) * | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| JP4623354B2 (ja) | 2000-09-14 | 2011-02-02 | 味の素株式会社 | 新規ピリミジン誘導体及び新規ピリジン誘導体 |
| TW200418814A (en) * | 2003-01-02 | 2004-10-01 | Ardent Pharmaceuticals Inc | Cardioprotective delta opioid receptor agonists and methods of using same |
| US7314880B2 (en) * | 2003-01-02 | 2008-01-01 | Mount Cook Biosciences, Inc. | Cardioprotective delta opioid receptor agonists and methods of using same |
| CN100582889C (zh) * | 2004-06-23 | 2010-01-20 | 夏普株式会社 | 液晶显示器及其制造方法 |
| JP2008534630A (ja) * | 2005-04-08 | 2008-08-28 | ニューロメッド ファーマシューティカルズ リミテッド | 疼痛の軽減のためのｎ型カルシウムチャネルブロッカーを含む組み合わせ治療の方法 |
| WO2007133481A2 (en) * | 2006-05-11 | 2007-11-22 | Neuromed Pharmaceuticals Ltd. | Method for increasing the bioavailability of benzhydryl piperazine containing compounds |
| CN101225084A (zh) * | 2007-01-16 | 2008-07-23 | 北京摩力克科技有限公司 | 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途 |
| MX2013010306A (es) | 2011-03-08 | 2013-12-09 | Zalicus Pharmaceuticals Ltd | Formulaciones de dispersion solida y metodos de uso de las mismas. |
| US8409560B2 (en) | 2011-03-08 | 2013-04-02 | Zalicus Pharmaceuticals Ltd. | Solid dispersion formulations and methods of use thereof |
| RU2014142598A (ru) * | 2012-03-31 | 2016-05-27 | Ф. Хоффманн-Ля Рош Аг | Новые 4-метилдигидропиримидины для лечения и профилактики инфекции вируса гепатита в |
| US20130267517A1 (en) | 2012-03-31 | 2013-10-10 | Hoffmann-La Roche Inc. | Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| CA2876690C (en) | 2012-08-24 | 2020-06-09 | Sunshine Lake Pharma Co., Ltd. | Dihydropyrimidine compounds and their application in pharmaceuticals |
| EP2892893B2 (en) * | 2012-09-10 | 2019-10-16 | F.Hoffmann-La Roche Ag | 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| MX2016006564A (es) | 2013-11-19 | 2017-09-12 | Sunshine Lake Pharma Co Ltd | Compuestos dihidropirimidina y su aplicacion en productos farmaceuticos. |
| RU2688193C1 (ru) | 2013-11-27 | 2019-05-21 | Саншайн Лейк Фарма Ко., Лтд. | Процессы приготовления производных дигидропиримидина и их промежуточных соединений |
| EP3122747B1 (en) | 2014-03-28 | 2020-05-20 | North & South Brother Pharmacy Investment Company Limited | Dihydropyrimidine compounds and their application in pharmaceuticals |
| US10098889B2 (en) | 2015-02-07 | 2018-10-16 | Sunshine Lake Pharma Co., Ltd. | Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3234684A1 (de) | 1982-09-18 | 1984-03-22 | Bayer Ag, 5090 Leverkusen | Neue dihydropyrimidine, verfahren zu ihrer herstellung sowie ihre verwendung in arzneimitteln |
| JPS61271278A (ja) | 1985-05-20 | 1986-12-01 | イ− ア−ル スクイブ アンド サンズ インコ−ポレ−テツド | ２−置換チオまたはオキソ−４−アリ−ルまたはヘテロシクロ−５−カルボキシ−１，４−ジヒドロピリミジン |
| DE69500377T2 (de) | 1994-08-19 | 1997-10-09 | Mitsui Toatsu Chemicals | Pyrimidin-Dion-Derivate und diese enthaltende antiarrhythmische Zusammensetzungen |
-
1997
- 1997-07-02 SE SE9702564A patent/SE9702564D0/xx unknown
-
1998
- 1998-06-18 ZA ZA985323A patent/ZA985323B/xx unknown
- 1998-06-22 WO PCT/SE1998/001208 patent/WO1999001438A1/en not_active Ceased
- 1998-06-22 JP JP50700899A patent/JP2002508780A/ja active Pending
- 1998-06-22 EP EP98932675A patent/EP0993450A1/en not_active Ceased
- 1998-06-22 AU AU82499/98A patent/AU8249998A/en not_active Abandoned
- 1998-06-22 US US09/171,174 patent/US6218538B1/en not_active Expired - Fee Related
- 1998-06-22 CA CA002294746A patent/CA2294746A1/en not_active Abandoned
- 1998-06-30 AR ARP980103175A patent/AR013153A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2294746A1 (en) | 1999-01-14 |
| WO1999001438A1 (en) | 1999-01-14 |
| JP2002508780A (ja) | 2002-03-19 |
| ZA985323B (en) | 1999-01-11 |
| EP0993450A1 (en) | 2000-04-19 |
| AU8249998A (en) | 1999-01-25 |
| SE9702564D0 (sv) | 1997-07-02 |
| US6218538B1 (en) | 2001-04-17 |
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