AR043885A1 - Derivados de pirimidina - Google Patents
Derivados de pirimidinaInfo
- Publication number
- AR043885A1 AR043885A1 ARP040101311A ARP040101311A AR043885A1 AR 043885 A1 AR043885 A1 AR 043885A1 AR P040101311 A ARP040101311 A AR P040101311A AR P040101311 A ARP040101311 A AR P040101311A AR 043885 A1 AR043885 A1 AR 043885A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halogen
- alkylcarbamoyl
- tri
- Prior art date
Links
Classifications
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- 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D239/30—Halogen atoms or nitro radicals
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Otolaryngology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a un derivado de pirimidina y a las sales del mismo que es útil como ingrediente activo de preparaciones farmacéuticas. El derivado de pirimidina de la presente tiene una actividad antagonista de CRTH2 excelente (un receptor quimioatrayente acoplado a proteína G, expresado en células Th2) y se puede usar para la profilaxis y el tratamiento de enfermedades relacionadas con la actividad de CRTH2, en particular para el tratamiento de enfermedades alérgicas, tales como asma, rinitis alérgica, dermatitis atópica y conjuntivitis alérgica; enfermedades relacionadas con eosinófilos, tales como el síndrome de Churg-Strauss y sinusitis; enfermedades relacionadas con basófilos, tales como leucemia basófila, urticaria crónica y leucocitosis basófila en seres humanos y otros mamíferos; y enfermedades inflamatorias caracterizadas por linfocitos T e infiltrados abundantes de leucocitos tales como psoriasis, eccema, enfermedad inflamatoria del intestino, colitis ulcerosa, enfermedad de Crohn, COPD (trastorno pulmonar obstructivo crónico) y artritis. Reivindicación 1: Un derivado de pirimidina de fórmula (1), su forma tautomérica o su forma estereoisomérica, o una sal, éster o profármaco del mismo en la que R1 representa H, uno de los compuestos del grupo de fórmulas (2) en las que n representa un entero de 0 a 6; -Q1- representa -NH-, -N(alquilo C1-6)-, u -O-; Y representa H, alquilo C1-6, cicloalquilo C3-8 opcionalmente sustituido con alquilo C1-6, cicloalquilo C3-8 condensado con benceno, arilo o heteroarilo, en el que dicho arilo y heteroarilo están opcionalmente sustituidos en una posición sustituible con uno o más sustituyentes seleccionados entre el grupo compuesto por ciano, halógeno, nitro, guanidino, pirrolilo, sulfamoilo, alquilaminosulfonilo C1-6, feniloxi, fenilo, amino, alquilamino C1-6, dialquilamino C1-6, alcoxicarbonilo C1-6, alcanoilo C1-6, alcanoilamino C1-6, carbamoilo, alquilcarbamoilo C1-6, dialquilcarbamoilo C1-6, alquilsulfonilo C1-6, alquilo C1-6 opcionalmente sustituido con mono-, di-, o tri-halógeno, alcoxi c1-6 opcionalmente sustituido con mono-, di-, o tri-halógeno y alquiltio C1-6 opcionalmente sustituido con mono-, di-, o tri-halógeno, o arilo condensado con 1,3-dioxolano; R2 representa H o alquilo C1-6; R3 representa halógeno, alcoxi C1-6 opcionalmente sustituido con mono-, di-, o tri-halógeno, o como se muestra en el grupo de fórmula (3) en las que R3a y R3b representan, independientemente, cicloalquilo C3-8 o alquilo C1-6, dicho alquilo C1-6 está opcionalmente sustituido con hidroxi, carboxi, cicloalquilo C3-8, carbamoilo, alquilcarbamoilo C1-6, alquilcarbamoilo C1-6 sustituido con arilo, alquilcarbamoilo C1-6, dialquilcarbamoilo C1-6, cicloalquilcarbamoilo C3-8, heterociclocarbonilo C3-8, alquilamino C1-6, dialquilamino C1-6 o alcoxi C1-6, q representa un entero de 1 a 3; R3c representa H, hidroxi, carboxi o alquilo C1-6 opcionalmente sustituido con hidroxi, carboxi o (alquilo C1-6 sustituido con fenilo)carbamoilo; Xa representa -O-, -S- o -N(R3d)-, en el que R3d representa h, halógeno, alcoxi C1-6, dialquilamino C1-6 o alquilo C1-6 opcionalmente sustituido con alcoxi C1-6 o mono-, di-, o tri-halógeno; R5 representa H o alquilo C1-6; y R6 representa carboxi, carboxamida, nitrilo o tetrazolilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03009384A EP1471057B1 (en) | 2003-04-25 | 2003-04-25 | Pyrimidinylacetic acid derivatives useful for the treatment of diseases mediated by CRTH2 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR043885A1 true AR043885A1 (es) | 2005-08-17 |
Family
ID=32946880
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040101311A AR043885A1 (es) | 2003-04-25 | 2004-04-19 | Derivados de pirimidina |
Country Status (33)
Country | Link |
---|---|
US (2) | US7812160B2 (es) |
EP (2) | EP1471057B1 (es) |
JP (2) | JP4671955B2 (es) |
KR (1) | KR101110491B1 (es) |
CN (2) | CN1809539B (es) |
AR (1) | AR043885A1 (es) |
AT (2) | ATE316077T1 (es) |
AU (1) | AU2004233966B2 (es) |
BR (1) | BRPI0409733A (es) |
CA (1) | CA2523439C (es) |
CL (1) | CL43596B (es) |
CY (1) | CY1111295T1 (es) |
DE (2) | DE60303238T2 (es) |
DK (2) | DK1471057T3 (es) |
DO (1) | DOP2004000875A (es) |
ES (2) | ES2257616T3 (es) |
GT (1) | GT200400079A (es) |
HK (1) | HK1095320A1 (es) |
HN (1) | HN2004000129A (es) |
IL (1) | IL171566A (es) |
MX (1) | MXPA05011399A (es) |
MY (1) | MY147984A (es) |
NO (1) | NO20055588L (es) |
NZ (1) | NZ543693A (es) |
PE (1) | PE20050143A1 (es) |
PL (1) | PL1633726T3 (es) |
PT (2) | PT1471057E (es) |
RU (1) | RU2361865C2 (es) |
SI (1) | SI1633726T1 (es) |
TW (1) | TWI353980B (es) |
UY (1) | UY28286A1 (es) |
WO (1) | WO2004096777A1 (es) |
ZA (1) | ZA200508722B (es) |
Families Citing this family (59)
Publication number | Priority date | Publication date | Assignee | Title |
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SE0301010D0 (sv) | 2003-04-07 | 2003-04-07 | Astrazeneca Ab | Novel compounds |
DE60303238T2 (de) | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
SA04250253B1 (ar) | 2003-08-21 | 2009-11-10 | استرازينيكا ايه بي | احماض فينوكسي اسيتيك مستبدلة باعتبارها مركبات صيدلانية لعلاج الامراض التنفسية مثل الربو ومرض الانسداد الرئوي المزمن |
EP1703893B1 (en) * | 2003-12-23 | 2012-04-11 | Genentech, Inc. | Novel anti-il 13 antibodies and uses thereof |
RU2373208C2 (ru) | 2004-01-31 | 2009-11-20 | Актимис Фармасьютикалз, Инк. | Производные имидазо[1,2-c]пиримидинилуксусной кислоты |
DK1725553T3 (da) | 2004-03-11 | 2008-08-18 | Actelion Pharmaceuticals Ltd | Tetrahydropyridoindolderivater |
GB0415320D0 (en) | 2004-07-08 | 2004-08-11 | Astrazeneca Ab | Novel compounds |
GB0418830D0 (en) | 2004-08-24 | 2004-09-22 | Astrazeneca Ab | Novel compounds |
ATE517085T1 (de) | 2004-11-23 | 2011-08-15 | Astrazeneca Ab | Zur behandlung von atemwegserkrankungen geeignete phenoxyessigsäurederivate |
US8796280B2 (en) | 2005-04-21 | 2014-08-05 | Merck Serono, S.A. | 2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors |
WO2006125784A1 (en) | 2005-05-24 | 2006-11-30 | Laboratoires Serono S.A. | Tricyclic spiro derivatives as crth2 modulators |
PE20110118A1 (es) | 2005-10-04 | 2011-03-08 | Aventis Pharma Inc | Compuestos de pirimidina amida como inhibidores de pgds |
TW200745003A (en) | 2005-10-06 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
JP5155171B2 (ja) * | 2005-10-06 | 2013-02-27 | アストラゼネカ・アクチエボラーグ | 新規化合物 |
WO2007062677A1 (en) * | 2005-11-30 | 2007-06-07 | 7Tm Pharma A/S | Thiazolyl- and pyrimidinyl-acetic acids and their use as crth2 receptor ligands |
EP2044044A2 (en) * | 2006-06-09 | 2009-04-08 | Icos Corporation | Substituted phenyl acetic acids as dp-2 antagonists |
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JP2011512359A (ja) | 2008-02-14 | 2011-04-21 | アミラ ファーマシューティカルズ,インク. | プロスタグランジンd2受容体のアンタゴニストとしての環式ジアリールエーテル化合物 |
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MX2014007239A (es) | 2011-12-16 | 2014-08-08 | Atopix Therapeutics Ltd | Combinacion de un antagonista crth2 y un inhibidor de bomba de proton para el tratamiento de esofagitis eosinofilica. |
RU2014129613A (ru) | 2011-12-21 | 2016-02-10 | Актелион Фармасьютиклз Лтд | Гетероциклильные производные и их применение в качестве модуляторов рецептора простагландина d2 |
CN104428305A (zh) | 2012-07-05 | 2015-03-18 | 埃科特莱茵药品有限公司 | 1-苯基-取代的杂环衍生物及其作为前列腺素d2受体调节剂的用途 |
US20140148470A1 (en) * | 2012-11-23 | 2014-05-29 | Boehringer Ingelheim International Gmbh | Pyrimidine compounds for treating hairloss |
TWI695831B (zh) | 2014-09-13 | 2020-06-11 | 香港商南北兄弟藥業投資有限公司 | Crth2拮抗劑化合物及其用途 |
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BE790679A (fr) | 1971-11-03 | 1973-04-27 | Ici Ltd | Derives de l'indole |
JPH03112985A (ja) * | 1989-09-28 | 1991-05-14 | Morishita Pharmaceut Co Ltd | N―(1h―テトラゾール―5―イル)―2―フェニル―5―ピリミジンカルボキシアミド類及びその合成用中間体 |
GB9125842D0 (en) * | 1991-12-04 | 1992-02-05 | Ici Plc | Heterocyclic derivatives |
US6326368B1 (en) * | 1996-03-27 | 2001-12-04 | Dupont Pharmaceuticals Company | Aryloxy- and arylthiosubstituted pyrimidines and triazines and derivatives thereof |
JP2001302667A (ja) | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
CA2408727A1 (en) * | 2000-05-22 | 2001-11-29 | Leo Pharma A/S | Benzophenones as inhibitors of il-1.beta. and tnf-.alpha. |
US6878522B2 (en) * | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
SE0200411D0 (sv) | 2002-02-05 | 2002-02-05 | Astrazeneca Ab | Novel use |
EP1413306A1 (en) * | 2002-10-21 | 2004-04-28 | Warner-Lambert Company LLC | Tetrahydroquinoline derivatives as CRTH2 antagonists |
ES2401079T3 (es) | 2002-12-20 | 2013-04-16 | Amgen Inc. | Moduladores del asma y de la inflamación alérgica |
DE60303238T2 (de) | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
US8278310B2 (en) | 2007-06-21 | 2012-10-02 | Actimis Pharmaceuticals, Inc. | Amine salts of a CRTH2 antagonist |
JP2010530425A (ja) | 2007-06-21 | 2010-09-09 | アクチミス ファーマシューティカルズ インコーポレーテッド | Crth2アンタゴニストの粒子 |
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