PE20091035A1 - DERIVATIVES OF 2-AMINOPYRIMIDINE - Google Patents
DERIVATIVES OF 2-AMINOPYRIMIDINEInfo
- Publication number
- PE20091035A1 PE20091035A1 PE2008001971A PE2008001971A PE20091035A1 PE 20091035 A1 PE20091035 A1 PE 20091035A1 PE 2008001971 A PE2008001971 A PE 2008001971A PE 2008001971 A PE2008001971 A PE 2008001971A PE 20091035 A1 PE20091035 A1 PE 20091035A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidin
- amine
- atoms
- alkyl
- aminopyrimidine
- Prior art date
Links
- 150000005006 2-aminopyrimidines Chemical class 0.000 title 1
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 abstract 4
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000004624 Dermatitis Diseases 0.000 abstract 1
- 102000004187 Histamine H4 receptors Human genes 0.000 abstract 1
- 108090000796 Histamine H4 receptors Proteins 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010039085 Rhinitis allergic Diseases 0.000 abstract 1
- 208000024780 Urticaria Diseases 0.000 abstract 1
- 201000010105 allergic rhinitis Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- XSGHLZBESSREDT-UHFFFAOYSA-N methylenecyclopropane Chemical group C=C1CC1 XSGHLZBESSREDT-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE 2-AMINOPIRIMIDINA DE FORMULA (I) DONDE R1 ES ALQUILO(C2-C8) O CICLOALQUILO(C3-C7)-ALQUILO(C0-C4) OPCIONALMENTE SUSTITUIDO CON ALQUILO(C1-C4), FENILO O FLUOR; R2 Y R3 FORMAN JUNTO EL ATOMO DE N AL CUAL ESTAN UNIDOS UN HETEROCICLICO MONOCICLICO DE 4 A 7 ATOMOS, BICICLICO DE 7 A 8 ATOMOS O BICICLICO FUSIONADO DE 8 A 12 ATOMOS. SON COMPUESTOS PREFERIDOS: 4-(CICLOPROPILMETIL)-6-((3R)-3-(METILAMINO)PIRROLIDIN-1-IL)PIRIMIDIN-2-AMINA, 4-CICLOPROPILMETIL-6-(3-(METILAMINO)AZETIDIN-1-IL)PIRIMIDIN-2-AMINA, 4-CICLOPROPILMETIL-6-((3R)-3-AMINOPIRROLIDIN-1-IL)PIRIMIDIN-2-AMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE HISTAMINA H4 SIENDO UTILES EN EL TRATAMIENTO DE ASMA, RINITIS ALERGICA, DERMATITIS, PSORIASIS, URTICARIAREFERS TO COMPOUNDS DERIVED FROM 2-AMINOPYRIMIDINE FROM FORMULA (I) WHERE R1 IS ALKYL (C2-C8) OR CYCLALKYL (C3-C7) -ALKYL (C0-C4) OPTIONALLY SUBSTITUTED WITH ALKYL (C1-C4), FENYL ; R2 AND R3 TOGETHER FORM THE ATOM OF N TO WHICH THEY ARE UNITED A MONOCYCLIC HETEROCYCLIC OF 4 TO 7 ATOMS, BICYCLE OF 7 TO 8 ATOMS OR FUSED BICYCLE OF 8 TO 12 ATOMS. PREFERRED COMPOUNDS ARE: 4- (CYCLOPROPylmethyl) -6 - ((3R) -3- (METHYLAMINE) PYRROLIDIN-1-IL) PYRIMIDIN-2-AMINE, 4-CYCLOPROPYLMEthyl-6- (3- (METHYLAMINE) AZETIDIN-1- IL) PYRIMIDIN-2-AMINE, 4-CYCLOPROPYLMETIL-6 - ((3R) -3-AMINOPYRROLIDIN-1-IL) PYRIMIDIN-2-AMINE, AMONG OTHERS. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION. SAID COMPOUNDS ARE ANTAGONISTS OF THE HISTAMINE H4 RECEPTOR, BEING USEFUL IN THE TREATMENT OF ASTHMA, ALLERGIC RHINITIS, DERMATITIS, PSORIASIS, URTICARIA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07381074 | 2007-11-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091035A1 true PE20091035A1 (en) | 2009-07-16 |
Family
ID=39197144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001971A PE20091035A1 (en) | 2007-11-30 | 2008-11-25 | DERIVATIVES OF 2-AMINOPYRIMIDINE |
Country Status (5)
| Country | Link |
|---|---|
| AR (1) | AR069480A1 (en) |
| CL (1) | CL2008003537A1 (en) |
| PE (1) | PE20091035A1 (en) |
| TW (1) | TW200936570A (en) |
| WO (1) | WO2009068512A1 (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602007008545D1 (en) | 2006-03-31 | 2010-09-30 | Janssen Pharmaceutica Nv | BENZOIMIDAZOLE-2-YL PYRIDINES AND PYRAZINES AS HISTAMINE H4 RECEPTOR MODULATORS |
| CN101511190A (en) | 2006-07-11 | 2009-08-19 | 詹森药业有限公司 | Pressure sensor fault detection |
| TW200904437A (en) | 2007-02-14 | 2009-02-01 | Janssen Pharmaceutica Nv | 2-aminopyrimidine modulators of the histamine H4 receptor |
| TW200924781A (en) | 2007-09-14 | 2009-06-16 | Janssen Pharmaceutica Nv | Thieno- and furo-pyrimidine modulators of the histamine H4 receptor |
| US8841287B2 (en) | 2008-06-12 | 2014-09-23 | Janssen Pharmaceutica N.V. | Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
| EP2201982A1 (en) | 2008-12-24 | 2010-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Histamine H4 receptor antagonists for the treatment of vestibular disorders |
| EP2493895B1 (en) | 2009-10-29 | 2017-04-26 | Vectura Limited | N-containing heteroaryl derivatives as jak3 kinase inhibitors |
| US8901146B2 (en) * | 2009-12-23 | 2014-12-02 | Medicis Pharmaceutical Corporation | Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists |
| BR112014003496B1 (en) | 2011-08-18 | 2022-02-22 | Nippon Shinyaku Co., Ltd | Heterocyclic derivative, uses thereof and pharmaceutical composition |
| WO2013182711A1 (en) | 2012-06-08 | 2013-12-12 | Sensorion | H4 receptor inhibitors for treating tinnitus |
| WO2014010748A1 (en) * | 2012-07-10 | 2014-01-16 | Shionogi & Co., Ltd. | Cyclopropane derivative having bace1 inhibiting activity |
| PL2964229T3 (en) | 2013-03-06 | 2020-05-18 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
| WO2017160922A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| WO2017160925A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| GB201817047D0 (en) | 2018-10-19 | 2018-12-05 | Heptares Therapeutics Ltd | H4 antagonist compounds |
| GB202005858D0 (en) * | 2020-04-22 | 2020-06-03 | Heptares Therapeutics Ltd | H4 Antagonist compounds |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1505064A1 (en) * | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| WO2005054239A1 (en) * | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| RU2008114378A (en) * | 2005-09-13 | 2009-10-20 | Палау Фарма, С.А. (Es) | 2-AMINOPYRIMIDINE DERIVATIVES AS ACTIVITY MODULATORS OF THE H4-HISTAMIN RECEPTOR |
| NL2000323C2 (en) * | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine derivatives. |
| EP2066645A2 (en) * | 2006-09-12 | 2009-06-10 | UCB Pharma S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| US7985745B2 (en) * | 2006-10-02 | 2011-07-26 | Abbott Laboratories | Method for pain treatment |
| TW200904437A (en) * | 2007-02-14 | 2009-02-01 | Janssen Pharmaceutica Nv | 2-aminopyrimidine modulators of the histamine H4 receptor |
-
2008
- 2008-11-25 WO PCT/EP2008/066110 patent/WO2009068512A1/en not_active Ceased
- 2008-11-25 AR ARP080105118A patent/AR069480A1/en unknown
- 2008-11-25 PE PE2008001971A patent/PE20091035A1/en not_active Application Discontinuation
- 2008-11-26 TW TW097145757A patent/TW200936570A/en unknown
- 2008-11-27 CL CL2008003537A patent/CL2008003537A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2008003537A1 (en) | 2009-03-06 |
| TW200936570A (en) | 2009-09-01 |
| WO2009068512A1 (en) | 2009-06-04 |
| AR069480A1 (en) | 2010-01-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |