IL113599A - 5-aryl pyrimidines, their preparation and pharmaceutical compositions containing them - Google Patents
5-aryl pyrimidines, their preparation and pharmaceutical compositions containing themInfo
- Publication number
- IL113599A IL113599A IL113599A IL11359995A IL113599A IL 113599 A IL113599 A IL 113599A IL 113599 A IL113599 A IL 113599A IL 11359995 A IL11359995 A IL 11359995A IL 113599 A IL113599 A IL 113599A
- Authority
- IL
- Israel
- Prior art keywords
- hydrogen
- halo
- alkyl
- preparation
- pharmaceutical compositions
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000001257 hydrogen Substances 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 125000005843 halogen group Chemical group 0.000 abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 125000004849 alkoxymethyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 229930195712 glutamate Natural products 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 239000002858 neurotransmitter agent Substances 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- -1 nitro, amino Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- 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
- C07D239/48—Two nitrogen atoms
- C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
-
- 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
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Liquid Crystal Substances (AREA)
- Paper (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB909012316A GB9012316D0 (en) | 1990-06-01 | 1990-06-01 | Pharmacologically active cns compounds |
| IL9833091A IL98330A (en) | 1990-06-01 | 1991-05-31 | 4-Amino-2-(4-n- propylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl) pyrimidine and acid addition salts thereof their preparation and pharmaceutical compositions containing them |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL113599A0 IL113599A0 (en) | 1995-08-31 |
| IL113599A true IL113599A (en) | 1997-09-30 |
Family
ID=10676964
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL113599A IL113599A (en) | 1990-06-01 | 1991-05-31 | 5-aryl pyrimidines, their preparation and pharmaceutical compositions containing them |
| IL9833091A IL98330A (en) | 1990-06-01 | 1991-05-31 | 4-Amino-2-(4-n- propylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl) pyrimidine and acid addition salts thereof their preparation and pharmaceutical compositions containing them |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL9833091A IL98330A (en) | 1990-06-01 | 1991-05-31 | 4-Amino-2-(4-n- propylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl) pyrimidine and acid addition salts thereof their preparation and pharmaceutical compositions containing them |
Country Status (25)
| Country | Link |
|---|---|
| EP (2) | EP0679645A1 (enExample) |
| JP (1) | JPH06340634A (enExample) |
| KR (1) | KR920000733A (enExample) |
| AT (1) | ATE141263T1 (enExample) |
| AU (2) | AU652753B2 (enExample) |
| CA (1) | CA2043640A1 (enExample) |
| CZ (1) | CZ281070B6 (enExample) |
| DE (1) | DE69121317T2 (enExample) |
| DK (1) | DK0459819T3 (enExample) |
| ES (1) | ES2093078T3 (enExample) |
| FI (1) | FI912623A7 (enExample) |
| GB (1) | GB9012316D0 (enExample) |
| GR (1) | GR3021237T3 (enExample) |
| HU (2) | HUT58707A (enExample) |
| IE (1) | IE911861A1 (enExample) |
| IL (2) | IL113599A (enExample) |
| MY (2) | MY109958A (enExample) |
| NO (1) | NO180375C (enExample) |
| NZ (3) | NZ238360A (enExample) |
| PL (2) | PL170373B1 (enExample) |
| PT (1) | PT97827B (enExample) |
| RU (1) | RU2091374C1 (enExample) |
| SK (1) | SK278444B6 (enExample) |
| TW (1) | TW224460B (enExample) |
| ZA (1) | ZA914165B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI895821A7 (fi) * | 1988-12-07 | 1990-06-08 | The Wellcome Foundation Ltd | Farmaseuttisesti aktivisia CNS-yhdisteitä |
| US5629016A (en) * | 1991-01-30 | 1997-05-13 | Glaxo Wellcome Inc. | Water-dispersible tablets |
| CH685978A5 (fr) * | 1991-01-30 | 1995-11-30 | Wellcome Found | Comprimes dispersables dans l'eau. |
| GB9215908D0 (en) * | 1992-07-27 | 1992-09-09 | Wellcome Found | Water dispersible tablets |
| JPH08504798A (ja) * | 1992-12-18 | 1996-05-21 | ザ ウエルカム ファウンデーション リミテッド | 酵素阻害薬としての,ピリミジン,ピリジン,プテリジノンおよびインダゾール誘導体 |
| GB9226377D0 (en) * | 1992-12-18 | 1993-02-10 | Babbedge Rachel C | Pharmaceutical compositions |
| US5698226A (en) * | 1993-07-13 | 1997-12-16 | Glaxo Wellcome Inc. | Water-dispersible tablets |
| GB9319341D0 (en) * | 1993-09-17 | 1993-11-03 | Wellcome Found | Novel process |
| FR2741879A1 (fr) * | 1995-12-05 | 1997-06-06 | Esteve Labor Dr | Derives de fluorophenyl-triazines et pyrimidines, leur preparation et leur application en tant que medicament |
| US6440965B1 (en) * | 1997-10-15 | 2002-08-27 | Krenitsky Pharmaceuticals, Inc. | Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system |
| DE19751949A1 (de) * | 1997-11-24 | 1999-05-27 | Bayer Ag | Verwendung von substituierten Aminomethyl-Chromanen zur Verhinderung der neuronalen Degeneration und zur Förderung der neuronalen Regeneration |
| GB9726987D0 (en) | 1997-12-22 | 1998-02-18 | Glaxo Group Ltd | Compounds |
| US6583148B1 (en) | 1999-04-08 | 2003-06-24 | Krenitsky Pharmaceuticals, Inc. | Neurotrophic substituted pyrimidines |
| DE19918325A1 (de) | 1999-04-22 | 2000-10-26 | Euro Celtique Sa | Verfahren zur Herstellung von Arzneiformen mit regulierter Wirkstofffreisetzung mittels Extrusion |
| MY123528A (en) | 1999-09-16 | 2006-05-31 | Mitsubihsi Tanabe Pharma Corp | Aromatic nitrogen-containing 6-membered cyclic compounds. |
| WO2001062233A2 (en) * | 2000-02-25 | 2001-08-30 | F. Hoffmann La Roche Ag | Adenosine receptor modulators |
| US7273868B2 (en) | 2000-04-28 | 2007-09-25 | Tanabe Seiyaku Co., Ltd. | Pyrazine derivatives |
| MXPA02010693A (es) | 2000-04-28 | 2003-03-10 | Tanabe Seiyaku Co | Compuestos ciclicos. |
| WO2002008205A1 (en) * | 2000-07-24 | 2002-01-31 | Krenitsky Pharmaceuticals, Inc. | Substituted 5-alkynyl pyrimidines having neurotrophic activity |
| MXPA03007623A (es) | 2001-02-26 | 2003-12-04 | Tanabe Seiyaku Co | Derivado de piridopirimidina o naftiridina. |
| PL372390A1 (en) * | 2002-02-05 | 2005-07-25 | Novo Nordisk A/S | Novel aryl- and heteroarylpiperazines |
| TW200637556A (en) * | 2005-01-31 | 2006-11-01 | Basf Ag | Substituted 5-phenyl pyrimidines I in therapy |
| EP1902028A2 (en) | 2005-07-04 | 2008-03-26 | Novo Nordisk A/S | Histamine h3 receptor antagonists |
| CA2653062A1 (en) | 2006-05-23 | 2007-11-29 | Transtech Pharma, Inc. | 6- (4-cyclopropylpiperazin-1-yl) -2 ' -methyl- [3, 4 ' ] -bipyridine and its use as a medicament |
| ATE538116T1 (de) | 2006-05-29 | 2012-01-15 | High Point Pharmaceuticals Llc | 3-(1,3-benyodioxol-5-yl)-6- (4- cyclopropylpiperazin-1-yl)-pyridazin, dessen salze und solvate und dessen verwendung als histamin-h3-rezeptorantagonist |
| EP2014656A3 (en) | 2007-06-11 | 2011-08-24 | High Point Pharmaceuticals, LLC | New heteocyclic h3 antagonists |
| US9073947B2 (en) | 2011-06-10 | 2015-07-07 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| WO2015107493A1 (en) * | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| CA3023216A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| RU2769132C2 (ru) | 2017-01-10 | 2022-03-28 | Новартис Аг | Фармацевтическая комбинация, содержащая ингибитор alk и ингибитор shp2 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE518622A (enExample) * | ||||
| FI895821A7 (fi) * | 1988-12-07 | 1990-06-08 | The Wellcome Foundation Ltd | Farmaseuttisesti aktivisia CNS-yhdisteitä |
| US5136080A (en) * | 1989-12-04 | 1992-08-04 | Burroughs Wellcome Co. | Nitrile compounds |
-
1990
- 1990-06-01 GB GB909012316A patent/GB9012316D0/en active Pending
-
1991
- 1991-05-30 ZA ZA914165A patent/ZA914165B/xx unknown
- 1991-05-31 PL PL91305331A patent/PL170373B1/pl unknown
- 1991-05-31 PT PT97827A patent/PT97827B/pt not_active IP Right Cessation
- 1991-05-31 NO NO912100A patent/NO180375C/no unknown
- 1991-05-31 KR KR1019910009010A patent/KR920000733A/ko not_active Ceased
- 1991-05-31 EP EP95111314A patent/EP0679645A1/en not_active Withdrawn
- 1991-05-31 FI FI912623A patent/FI912623A7/fi not_active Application Discontinuation
- 1991-05-31 EP EP91304935A patent/EP0459819B1/en not_active Expired - Lifetime
- 1991-05-31 IL IL113599A patent/IL113599A/xx not_active IP Right Cessation
- 1991-05-31 NZ NZ238360A patent/NZ238360A/en unknown
- 1991-05-31 MY MYPI91000962A patent/MY109958A/en unknown
- 1991-05-31 JP JP3235334A patent/JPH06340634A/ja active Pending
- 1991-05-31 NZ NZ272001A patent/NZ272001A/en unknown
- 1991-05-31 PL PL91290496A patent/PL166656B1/pl unknown
- 1991-05-31 AT AT91304935T patent/ATE141263T1/de not_active IP Right Cessation
- 1991-05-31 CA CA002043640A patent/CA2043640A1/en not_active Abandoned
- 1991-05-31 SK SK1643-91A patent/SK278444B6/sk unknown
- 1991-05-31 RU SU914895583A patent/RU2091374C1/ru active
- 1991-05-31 NZ NZ248501A patent/NZ248501A/en unknown
- 1991-05-31 HU HU911826A patent/HUT58707A/hu unknown
- 1991-05-31 IE IE186191A patent/IE911861A1/en unknown
- 1991-05-31 IL IL9833091A patent/IL98330A/en active IP Right Grant
- 1991-05-31 MY MYPI95001459A patent/MY136248A/en unknown
- 1991-05-31 TW TW080104285A patent/TW224460B/zh active
- 1991-05-31 AU AU78097/91A patent/AU652753B2/en not_active Ceased
- 1991-05-31 DE DE69121317T patent/DE69121317T2/de not_active Expired - Fee Related
- 1991-05-31 DK DK91304935.9T patent/DK0459819T3/da active
- 1991-05-31 ES ES91304935T patent/ES2093078T3/es not_active Expired - Lifetime
- 1991-05-31 CZ CS911643A patent/CZ281070B6/cs unknown
-
1994
- 1994-07-13 AU AU67455/94A patent/AU680252B2/en not_active Expired - Fee Related
-
1995
- 1995-06-30 HU HU95P/P00669P patent/HU211649A9/hu unknown
-
1996
- 1996-10-03 GR GR960402585T patent/GR3021237T3/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| EXP | Patent expired | ||
| RH | Patent void |