EP1654237A1 - Derives de 2-aminopyrimidine - Google Patents
Derives de 2-aminopyrimidineInfo
- Publication number
- EP1654237A1 EP1654237A1 EP04763418A EP04763418A EP1654237A1 EP 1654237 A1 EP1654237 A1 EP 1654237A1 EP 04763418 A EP04763418 A EP 04763418A EP 04763418 A EP04763418 A EP 04763418A EP 1654237 A1 EP1654237 A1 EP 1654237A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- amino
- alkyl
- halogen
- phenyl
- hydroxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- 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]
-
- 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
Definitions
- Rb 2 is halogen, alkyl, OH, (un)substituted heteroaryl, (un)substituted heterocyclyl, etc;
- WOOl/062233 discloses pyrimidine derivatives represented by the general formula:
- R 11 and R 12 independently represent hydrogen or C 1-6 alkyl optionally substituted by halogen, cyano, hydroxy, carboxy, amino, Ci- ⁇ alkylamino, N,N-di(C ⁇ - 6 alkyl)arnino, Ci. 6 alkylthio, C ⁇ -6 alkoxy, or C 3-8 cycloalkyl; and
- the compound of the formula (I) of the present invention can be, but not limited to be, prepared by combining various known methods.
- one or more of the substituents, such as amino group, carboxyl group, and hydroxyl group of the compounds used as starting materials or intermediates are advantageously protected by a protecting group known to those skilled in the art. Examples of the protecting groups are described in "Protective Groups in Organic Synthesis (3rd Edition)" by Greene and Wuts, John Wiley and Sons, New York 1999.
- the compound of the formula (I) of the present invention can be, but not limited to be, prepared by the Method [A] and [B] below.
- compound of formula (XIII) (wherein R 2 is the same as defined above) can be prepared by the oxidation of sulfur atom of compound of formula (XII) (wherein R 2 is the same as defined above) .
- the carrier may be a finely divided solid which is in admixture with the finely divided active ingredient.
- the active ingredient may be mixed with a carrier having binding properties in suitable proportions and compacted in the shape and size desired to produce tablets.
- the powders and tablets preferably contain from about 1 to about 99 weight percent of the active ingredient which is the novel composition of the present invention.
- Suitable solid carriers are magnesium carboxymethyl cellulose, low melting waxes, and cocoa butter.
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04763418A EP1654237A1 (fr) | 2003-08-05 | 2004-07-23 | Derives de 2-aminopyrimidine |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03017810A EP1505064A1 (fr) | 2003-08-05 | 2003-08-05 | Dérivés de 2-aminopyrimidine |
EP04763418A EP1654237A1 (fr) | 2003-08-05 | 2004-07-23 | Derives de 2-aminopyrimidine |
PCT/EP2004/008225 WO2005014556A1 (fr) | 2003-08-05 | 2004-07-23 | Derives de 2-aminopyrimidine |
Publications (1)
Publication Number | Publication Date |
---|---|
EP1654237A1 true EP1654237A1 (fr) | 2006-05-10 |
Family
ID=33547634
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP03017810A Withdrawn EP1505064A1 (fr) | 2003-08-05 | 2003-08-05 | Dérivés de 2-aminopyrimidine |
EP04763418A Withdrawn EP1654237A1 (fr) | 2003-08-05 | 2004-07-23 | Derives de 2-aminopyrimidine |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP03017810A Withdrawn EP1505064A1 (fr) | 2003-08-05 | 2003-08-05 | Dérivés de 2-aminopyrimidine |
Country Status (2)
Country | Link |
---|---|
EP (2) | EP1505064A1 (fr) |
WO (1) | WO2005014556A1 (fr) |
Families Citing this family (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1942463A (zh) * | 2004-04-15 | 2007-04-04 | 安斯泰来制药株式会社 | 2-氨基嘧啶衍生物 |
WO2007031529A1 (fr) * | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | Dérivés de 2-aminopyrimidine en tant que modulateurs de l'activité du récepteur h4 de l'histamine |
EP1767537A1 (fr) * | 2005-09-21 | 2007-03-28 | Cellzome (UK) Ltd. | Dérivés de pyrimidine pour le traitement de troubles inflammatoires |
GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
NL2000323C2 (nl) * | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
WO2007090854A1 (fr) * | 2006-02-10 | 2007-08-16 | Cellzome (Uk) Ltd. | Composés d'amino pyrimidine d'azétidine destinés à traiter des troubles inflammatoires |
EP1860108A1 (fr) * | 2006-05-24 | 2007-11-28 | Cellzome (UK) Ltd. | Enantiomères d'aminopyrimidines utilisés dans le traitement de maladies inflammatoires. |
WO2007090853A1 (fr) * | 2006-02-10 | 2007-08-16 | Cellzome (Uk) Ltd. | Enantiomères de composes d'amino pyrimidine destinés à traiter des troubles inflammatoires |
EP1860109A1 (fr) * | 2006-05-24 | 2007-11-28 | Cellzome (UK) Ltd. | Composés d'amino pyrimidine substitués avec une azetidine pour traiter les maladies inflammatoires |
WO2007117401A2 (fr) | 2006-04-07 | 2007-10-18 | Janssen Pharmaceutica N.V. | Indoles et benzoimidazoles modulateurs du récepteur de l'histamine h4 |
US20100035863A1 (en) * | 2006-09-12 | 2010-02-11 | 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 |
WO2008122378A1 (fr) * | 2007-04-04 | 2008-10-16 | Ucb Pharma, S.A. | Nouveaux derives de pyridine, procedes de preparation et compositions pharmaceutiques associes |
CA2705719C (fr) | 2007-09-14 | 2016-10-11 | Janssen Pharmaceutica N.V. | Modulateurs du recepteur d'histamine h<sb>4</sb> de types thieno- et furo-pyrimidine |
EP2209775A1 (fr) * | 2007-10-09 | 2010-07-28 | UCB Pharma, S.A. | Composés hétérobicycliques utiles comme antagonistes du récepteur h4 de l'histamine |
PE20091035A1 (es) * | 2007-11-30 | 2009-07-16 | Palau Pharma Sa | Derivados de 2-aminopirimidina |
PE20091524A1 (es) * | 2007-12-19 | 2009-09-25 | Palau Pharma Sa | Derivados de 2-aminopirimidina |
RU2489430C2 (ru) * | 2007-12-21 | 2013-08-10 | Палау Фарма, С.А. | Производные 4-аминопиримидина |
US8436005B2 (en) * | 2008-04-03 | 2013-05-07 | Abbott Laboratories | Macrocyclic pyrimidine derivatives |
EA018198B1 (ru) | 2008-06-12 | 2013-06-28 | Янссен Фармацевтика Нв | Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h |
US8436008B2 (en) | 2008-12-22 | 2013-05-07 | Incyte Corporation | Substituted heterocyclic compounds |
EP2201982A1 (fr) | 2008-12-24 | 2010-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antagonistes du récepteur H4 de l'histamine pour le traitement de troubles vestibulaires |
US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
WO2010108059A1 (fr) * | 2009-03-20 | 2010-09-23 | Incyte Corporation | Dérivés substitués de pyrimidine en tant qu'antagonistes du récepteur histaminique h4 |
TWI478714B (zh) | 2009-10-29 | 2015-04-01 | Vectura Ltd | 作為Janus激酶3(JAK3)抑制劑之含氮雜芳基衍生物類 |
US8901146B2 (en) * | 2009-12-23 | 2014-12-02 | Medicis Pharmaceutical Corporation | Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists |
WO2011082268A2 (fr) | 2009-12-30 | 2011-07-07 | Arqule Inc. | Composés naphthalényl-pyrimidine substitués |
WO2011092293A2 (fr) | 2010-02-01 | 2011-08-04 | Novartis Ag | Dérivés de cyclohexylamide utilisés en tant qu'antagonistes du récepteur du crf |
US20120295942A1 (en) | 2010-02-01 | 2012-11-22 | Nicholas James Devereux | Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists |
US8835444B2 (en) | 2010-02-02 | 2014-09-16 | Novartis Ag | Cyclohexyl amide derivatives as CRF receptor antagonists |
UY34094A (es) | 2011-05-27 | 2013-01-03 | Novartis Ag | Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina |
EP2852591A1 (fr) | 2012-05-03 | 2015-04-01 | Novartis AG | Sel de l-malate de dérivés de 2,7-diaza-spiro[4.5]déc-7-yle et ses formes cristallines à titre d'agonistes des récepteurs de ghreline |
JP6185574B2 (ja) | 2012-06-08 | 2017-08-23 | センソリオン | 耳鳴りを治療するためのh4受容体阻害剤 |
US20190047966A1 (en) * | 2016-01-29 | 2019-02-14 | Meiji Seika Pharma Co., Ltd. | Novel compound and pharmacologically acceptable salt thereof |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5256659A (en) * | 1989-01-09 | 1993-10-26 | Janssen Pharmaceutica N.V. | 2-aminopyrimidinone derivatives |
GB9012311D0 (en) * | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
WO2001062233A2 (fr) * | 2000-02-25 | 2001-08-30 | F. Hoffmann La Roche Ag | Modulateurs de recepteurs de l'adenosine |
WO2002096867A2 (fr) * | 2001-05-30 | 2002-12-05 | Lg Biomedical Institute | Inhibiteurs de la proteine kinase destines au traitement d'une maladie |
-
2003
- 2003-08-05 EP EP03017810A patent/EP1505064A1/fr not_active Withdrawn
-
2004
- 2004-07-23 EP EP04763418A patent/EP1654237A1/fr not_active Withdrawn
- 2004-07-23 WO PCT/EP2004/008225 patent/WO2005014556A1/fr not_active Application Discontinuation
Non-Patent Citations (1)
Title |
---|
See references of WO2005014556A1 * |
Also Published As
Publication number | Publication date |
---|---|
WO2005014556A1 (fr) | 2005-02-17 |
EP1505064A1 (fr) | 2005-02-09 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
17P | Request for examination filed |
Effective date: 20060306 |
|
AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): DE ES FR GB IT |
|
RIN1 | Information on inventor provided before grant (corrected) |
Inventor name: SAKAI, KATSUYA Inventor name: SATO, HIROKI Inventor name: URBAHNS, KLAUS Inventor name: FUKUSHIMA, KEIKO Inventor name: GANTNER, FLORIAN Inventor name: SHIMAZAKI, MAKOTO Inventor name: BACON, KEVIN C/O ACTIMIS PHARMACEUTICALS |
|
DAX | Request for extension of the european patent (deleted) | ||
RBV | Designated contracting states (corrected) |
Designated state(s): DE ES FR GB IT |
|
RIN1 | Information on inventor provided before grant (corrected) |
Inventor name: SAKAI, KATSUYA Inventor name: SHIMAZAKI, MAKOTO Inventor name: BACON, KEVIN C/O ACTIMIS PHARMACEUTICALS Inventor name: FUKUSHIMA, KEIKO Inventor name: SATO, HIROKI Inventor name: URBAHNS, KLAUS Inventor name: GANTNER, FLORIAN |
|
17Q | First examination report despatched |
Effective date: 20070205 |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
|
18D | Application deemed to be withdrawn |
Effective date: 20070616 |