TW200936570A - 2-aminopyrimidine derivatives - Google Patents

2-aminopyrimidine derivatives Download PDF

Info

Publication number: TW200936570A
Authority: TW; Taiwan
Prior art keywords: group; amine; compound; methylamino; formula
Prior art date: 2007-11-30

Application number

TW097145757A

Other languages

English (en)

Chinese (zh)

Inventor

Gonzalez Elena Carceller

Fuentes Eva Maria Medina

Via Josep Marti

Bernado Marina Virgili

Original Assignee

Palau Pharma Sa

Priority date (The priority date 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 date listed.)

2007-11-30

Filing date

2008-11-26

Publication date

2009-09-01

2008-11-26 Application filed by Palau Pharma Sa filed Critical Palau Pharma Sa

2009-09-01 Publication of TW200936570A publication Critical patent/TW200936570A/zh

Links

150000005006 2-aminopyrimidines Chemical class 0.000 title abstract description 3
150000001875 compounds Chemical class 0.000 claims abstract description 369
OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 217
125000000217 alkyl group Chemical group 0.000 claims description 193
125000000623 heterocyclic group Chemical group 0.000 claims description 178
125000004433 nitrogen atom Chemical group N* 0.000 claims description 139
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 112
-1 4-cyclopropylmethyl-6-(3-(methylamino)azol-1-yl)pyrimidine-2-amine Chemical compound 0.000 claims description 87
LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims description 83
238000000034 method Methods 0.000 claims description 62
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 57
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 54
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 49
229910003827 NRaRb Inorganic materials 0.000 claims description 48
125000002619 bicyclic group Chemical group 0.000 claims description 46
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 45
150000003839 salts Chemical class 0.000 claims description 44
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 40
125000005842 heteroatom Chemical group 0.000 claims description 33
125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 31
125000001424 substituent group Chemical group 0.000 claims description 29
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208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
208000026278 immune system disease Diseases 0.000 claims description 23
208000027866 inflammatory disease Diseases 0.000 claims description 23
125000002950 monocyclic group Chemical group 0.000 claims description 23
150000001412 amines Chemical class 0.000 claims description 20
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 20
125000004429 atom Chemical group 0.000 claims description 18
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 17
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 16
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 15
KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical group [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims description 15
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125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
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108010002059 Histamine Receptors Proteins 0.000 claims description 9
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 9
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LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 8
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125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims description 5
125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 5
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125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
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239000003638 chemical reducing agent Substances 0.000 claims description 2
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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

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Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
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TW097145757A 2007-11-30 2008-11-26 2-aminopyrimidine derivatives TW200936570A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
EP07381074		2007-11-30

Publications (1)

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TW200936570A true TW200936570A (en)	2009-09-01

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TW097145757A TW200936570A (en)	2007-11-30	2008-11-26	2-aminopyrimidine derivatives

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AR (1)	AR069480A1 (es)
CL (1)	CL2008003537A1 (es)
PE (1)	PE20091035A1 (es)
TW (1)	TW200936570A (es)
WO (1)	WO2009068512A1 (es)

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KR20090028819A (ko)	2006-07-11	2009-03-19	얀센 파마슈티카 엔.브이.	히스타민 ｈ４ 수용체의 벤조푸로- 및 벤조티에노피리미딘 조절제
CL2008000467A1 (es)	2007-02-14	2008-08-22	Janssen Pharmaceutica Nv	Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
CA2705719C (en)	2007-09-14	2016-10-11	Janssen Pharmaceutica N.V.	Thieno-and furo-pyrimidine modulators of the histamine h4 receptor
MX2010013726A (es)	2008-06-12	2011-01-14	Janssen Pharmaceutica Nv	Moduladores de diamino-piridina, pirimidina, y piridazina del receptor h4 de histamina.
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
ES2629006T3 (es)	2009-10-29	2017-08-07	Vectura Limited	Derivados que contienen N-heteroarilo como inhibidores de la quinasa jak3
WO2011076878A1 (en) *	2009-12-23	2011-06-30	Palau Pharma, S.A.	Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists
PH12014500326B1 (en)	2011-08-18	2018-01-10	Nippon Shinyaku Co Ltd	Heterocyclic derivative and pharmaceutical drug
HUE039713T2 (hu)	2012-06-08	2019-02-28	Sensorion	H4 receptor inhibitorok tinnitus kezelésére
WO2014010748A1 (en) *	2012-07-10	2014-01-16	Shionogi & Co., Ltd.	Cyclopropane derivative having bace1 inhibiting activity
SMT202000084T1 (it)	2013-03-06	2020-03-13	Janssen Pharmaceutica Nv	Modulatori benzoimidazol-2-il pirimidinici del recettore h4 dell'istamina
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

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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
CA2622372A1 (en) *	2005-09-13	2007-03-22	Palau Pharma, S.A.	2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity
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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
CL2008000467A1 (es) *	2007-02-14	2008-08-22	Janssen Pharmaceutica Nv	Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma

2008
- 2008-11-25 WO PCT/EP2008/066110 patent/WO2009068512A1/en not_active Ceased
- 2008-11-25 PE PE2008001971A patent/PE20091035A1/es not_active Application Discontinuation
- 2008-11-25 AR ARP080105118A patent/AR069480A1/es unknown
- 2008-11-26 TW TW097145757A patent/TW200936570A/zh unknown
- 2008-11-27 CL CL2008003537A patent/CL2008003537A1/es unknown

Also Published As

Publication number	Publication date
WO2009068512A1 (en)	2009-06-04
CL2008003537A1 (es)	2009-03-06
PE20091035A1 (es)	2009-07-16
AR069480A1 (es)	2010-01-27

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TW200936570A (en)	2009-09-01	2-aminopyrimidine derivatives
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