PE20121480A1 - Aminopirimidinas como inhibidores de syk - Google Patents
Aminopirimidinas como inhibidores de sykInfo
- Publication number
- PE20121480A1 PE20121480A1 PE2012000838A PE2012000838A PE20121480A1 PE 20121480 A1 PE20121480 A1 PE 20121480A1 PE 2012000838 A PE2012000838 A PE 2012000838A PE 2012000838 A PE2012000838 A PE 2012000838A PE 20121480 A1 PE20121480 A1 PE 20121480A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidin
- cycloalkyl
- hydroxy
- phenyl
- alkyl
- Prior art date
Links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
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- 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
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- 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
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- 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
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
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- C07D495/04—Ortho-condensed systems
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE AMINOPIRIMIDINAS DE FORMULA (I) DONDE p ES DE 0 A 4; q ES DE 0 A 2; Cy ES CICLOALQUILO(C4-C7), OXETANILO, PIRROLIDINILO, PIPERIDINILO, ENTRE OTROS; R1 ES H, ALQUILO(C1-C4), HALOALQUILO(C1-C4), CICLOALQUILO(C3-C6), ENTRE OTROS; R4 ES H, ALQUILO(C1-C4) O CICLOALQUILO(C3-C4); Ry(a) ES AMINOMETILO, OH, OCH3, F, ENTRE OTROS; Rz(a) ES FLUOROALQUILO(C1-C3), HALOGENO, CN, ALQUILO(C1-C4), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO (1R,4S)-4-[5-(3-CICLOPROPIL-5-{[4-(TRIFLUOROMETIL)PIRIMIDIN-2-IL]AMINO}FENIL)-1,3-TIAZOL-2-IL]-4-HIDROXI-2,2-DIMETILCICLOHEXANOCARBOXILICO; ACIDO (1S,4R)-4-HIDROXI-2,2-DIMETIL-4-{5-[3-METIL-5-(4-METIL-PIRIMIDIN-2-ILAMINO)-FENIL]-TIAZOL-2-IL}-CICLOHEXANOCARBOXILICO; 5-HIDROXI-5-[5-(3-METIL-5-{[4-(TRIFLUOROMETIL)PIRIMIDIN-2-IL]AMINO}FENIL)-1,3-TIAZOL-2-IL]AZEPAN-2-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TIROSINA QUINASA DEL BAZO (SYK) SIENDO UTILES EN EL TRATAMIENTO DE ASMA, COLITIS ULCERATIVA, DERMATITIS, PSORIASIS
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US28726709P | 2009-12-17 | 2009-12-17 |
Publications (1)
Publication Number | Publication Date |
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PE20121480A1 true PE20121480A1 (es) | 2012-11-10 |
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ID=43502894
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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PE2012000838A PE20121480A1 (es) | 2009-12-17 | 2010-12-15 | Aminopirimidinas como inhibidores de syk |
Country Status (27)
Country | Link |
---|---|
US (3) | US8551984B2 (es) |
EP (1) | EP2513098B1 (es) |
JP (2) | JP5242857B2 (es) |
KR (1) | KR101445012B1 (es) |
CN (1) | CN102858767B (es) |
AR (1) | AR080672A1 (es) |
AU (1) | AU2010331927B2 (es) |
BR (1) | BR112012014703B1 (es) |
CA (1) | CA2782889C (es) |
CL (1) | CL2012001627A1 (es) |
CO (1) | CO6551728A2 (es) |
CR (1) | CR20120331A (es) |
DO (1) | DOP2012000166A (es) |
EA (1) | EA022790B1 (es) |
EC (1) | ECSP12011982A (es) |
ES (1) | ES2609040T3 (es) |
GE (1) | GEP20146125B (es) |
GT (1) | GT201200202A (es) |
MA (1) | MA33926B1 (es) |
MX (1) | MX2012007154A (es) |
NI (1) | NI201200108A (es) |
NZ (1) | NZ600673A (es) |
PE (1) | PE20121480A1 (es) |
SG (1) | SG181803A1 (es) |
TN (1) | TN2012000288A1 (es) |
TW (1) | TW201132637A (es) |
WO (2) | WO2011075515A1 (es) |
Families Citing this family (79)
Publication number | Priority date | Publication date | Assignee | Title |
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CN102858767B (zh) * | 2009-12-17 | 2015-08-19 | 默沙东公司 | 作为syk抑制剂的氨基嘧啶 |
US8735417B2 (en) | 2009-12-17 | 2014-05-27 | Merck Sharp & Dohme Corp. | Aminopyrimidines as Syk inhibitors |
MX2012007402A (es) | 2009-12-23 | 2012-08-23 | Takeda Pharmaceutical | Pirrolidinonas heteroaromaticas fusionadas como inhibidores de tirosina cinasa esplenica (syk). |
US8962665B2 (en) | 2010-01-12 | 2015-02-24 | Ab Science | Thiazole and oxazole kinase inhibitors |
US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
KR20140025500A (ko) * | 2011-05-04 | 2014-03-04 | 머크 샤프 앤드 돔 코포레이션 | 아미노-피리딘-함유 비장 티로신 키나제 (Syk) 억제제 |
US9145391B2 (en) | 2011-05-10 | 2015-09-29 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as Syk inhibitors |
JP2014513687A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Syk阻害薬としてのピリジルアミノピリジン |
BR112013028900A2 (pt) | 2011-05-10 | 2017-01-03 | Merck Sharp & Dohe Corp | Composto, composição farmacêutica, e, método para o tratamento ou a prevenção de doenças |
JP2014159375A (ja) * | 2011-06-15 | 2014-09-04 | Takeda Chem Ind Ltd | アゼパン化合物 |
WO2012177714A1 (en) | 2011-06-22 | 2012-12-27 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
ES2638144T3 (es) * | 2011-12-21 | 2017-10-18 | Bayer Intellectual Property Gmbh | Bencilpirazoles sustituidos |
US8906889B2 (en) | 2012-02-15 | 2014-12-09 | Bristol-Myers Squibb Company | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
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