AR050622A1 - Derivados de pirimidinilpirazoles como inhibidores de la via de senalizacion por tgfbeta y composiciones farmaceuticas que los contienen. - Google Patents
Derivados de pirimidinilpirazoles como inhibidores de la via de senalizacion por tgfbeta y composiciones farmaceuticas que los contienen.Info
- Publication number
- AR050622A1 AR050622A1 ARP050103635A ARP050103635A AR050622A1 AR 050622 A1 AR050622 A1 AR 050622A1 AR P050103635 A ARP050103635 A AR P050103635A AR P050103635 A ARP050103635 A AR P050103635A AR 050622 A1 AR050622 A1 AR 050622A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocycloalkyl
- heteroaryl
- alkynyl
- cycloalkyl
- Prior art date
Links
Classifications
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- 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
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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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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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
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D405/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Estos compuestos de formula (1) tienen una afinidad elevada por Alk 5 y/o Alk 4, y pueden ser utiles como antagonistas de éstos para la prevencion y/o tratamiento de numerosas enfermedades, incluyendo los trastornos fibroticos. Y composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de formula (1) o un N-oxido o una sal farmacéuticamente aceptable de dicho compuesto en donde: cada Ra, independientemente, es alquilo, alquenilo, alquinilo, alcoxilo, acilo, halogeno, hidroxilo, -NH2, -NH(alquilo no sustituido), -N(alquilo no sustituido)2, nitro, oxo, tioxo, ciano, guanadino, amidino, carboxilo, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, arilcarbonilamino, heteroarilcarbonilamino, alquilsulfonilamino, arilsulfonilamino, heteroarilsulfonilamino, alcoxicarbonilo, alquilcarboniloxilo, urea, tiourea, sulfamoílo, sulfamida, carbamoílo, cicloalquilo, cicloalquiloxilo, cicloalquilsulfanilo, cicloalquilcarbonilo, heterocicloalquilo, heterocicloalquiloxilo, heterocicloalquilsulfanilo, heterocicloalquilcarbonilo, ariloxilo, arilsulfanilo, aroílo, heteroarilo, heteroariloxilo, heteroarilsulfanilo, o heteroaroilo; R1 es un enlace, alquileno, alquenileno, alquinileno, o -(CH2)r1-O-(CH2)r2-, en donde cada r1 y r2, independientemente, es 2 o 3; R2 es cicloalquileno, heterocicloalquileno, cicloalquenileno, heterocicloalquenileno, arileno, heteroarileno, o un enlace; R3 es -C(O)-, -C(O)-O-, -O-C(O)-, -S(O)p-O-, -O-S(O)p-, -C(O)-N(Rb)-, -N(Rb)-C(O)-, -O-C(O)-N(Rb)-, -N(Rb)-C(O)-O-, -C(O)-N(Rb)-O-, -O-N(Rb)-C(O)-, -O-S(O)p-N(Rb)-, -N(Rb)-, S(O)p-O-, -S(O)p-N(Rb)-O-, -O-N(Rb)-S(O)p-, -N(Rb)-C(O)-N(Rc)-, -N(Rb)- S(O)p-N(Rc)-, -C(O)-N(Rb)-S(O)p-, -S(O)p-N(Rb)-C(O)-, -C(O)-N(Rb)-S(O)p-N(Rc)-, -C(O)-O-S(O)p-N(Rb)-, -N(Rb)-S(O)p-N(Rc)-C(O)-, -N(Rb)-S(O)p-O-C(O)-, -S(O)p-N(Rb)-, -N(Rb)-S(O)p-, -N(Rb)-, -S(O)p-, -O-, -S-, -(C(Rb)(Rc))q-, o un enlace; en donde cada Rb y Rc es independientemente H, hidroxilo, alquilo, arilo, arilalquilo, heterocicloalquilo, heteroarilo, o heteroarilalquilo; p es 1 o 2; y q es 1-4; R4 es H, alquilo, alquenilo, alquinilo, cicloalquilo, (cicloalquil)alquilo, heterocicloalquilo, (heterocicloalquil)alquilo, cicloalquenilo, (cicloalquenil)alquilo, heterocicloalquenilo, (heterocicloalquenil)alquilo, arilo, arilalquilo, heteroarilo, o heteroarilalquilo; R5 es H, alquilo no sustituido, alquilo sustituido con halogeno, alcoxilo, alquilsulfinilo, amino, alquenilo, alquinilo, cicloalcoxilo, cicloalquilsulfinilo, heterocicloalcoxilo, heterocicloalquilsulfinilo, ariloxilo, arilsulfinilo, heteroariloxilo, o heteroarilsulfinilo; R6 es un heterociclilo monocíclico de 5 a 6 miembros o un heteroarilo bicíclico de 8 a 11 miembros; estando cada uno opcionalmente sustituido con alquilo, alquenilo, alquinilo, alcoxilo, acilo, halogeno, hidroxilo, amino, nitro, oxo, tioxo, ciano, guanadino, amidino, carboxilo, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, arilcarbonilamino, heteroarilcarbonilamino, alquilsulfonilamino, arilsulfonilamino, heteroarilsulfonilamino, alcoxicarbonilo, alquilcarboniloxilo, urea, tiourea, sulfamoílo, sulfamida, carbamoílo, cicloalquilo, cicloalquiloxilo, cicloalquilsulfanilo, heterocicloalquilo, heterocicloalquiloxilo, heterocicloalquilsulfanilo, cicloalquilcarbonilo, heterocicloalquilcarbonilo, arilo, ariloxilo, arilsulfanilo, aroílo, heteroarilo, heteroariloxilo, heteroarilsulfanilo, o heteroaroilo; y m es 0-3; siempre que cuando m >igual2, dos grupos Ra adyacentes pueden unirse para formar un grupo cíclico de 4 a 8 miembros opcionalmente sustituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60604604P | 2004-08-31 | 2004-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050622A1 true AR050622A1 (es) | 2006-11-08 |
Family
ID=35432389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103635A AR050622A1 (es) | 2004-08-31 | 2005-08-30 | Derivados de pirimidinilpirazoles como inhibidores de la via de senalizacion por tgfbeta y composiciones farmaceuticas que los contienen. |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20080171755A1 (es) |
| EP (1) | EP1786803A1 (es) |
| JP (1) | JP2008511630A (es) |
| AR (1) | AR050622A1 (es) |
| AU (1) | AU2005280167A1 (es) |
| CA (1) | CA2578628A1 (es) |
| TW (1) | TW200621752A (es) |
| WO (1) | WO2006026305A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2584248A1 (en) * | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| SI1928454T1 (sl) | 2005-05-10 | 2015-01-30 | Intermune, Inc. | Piridonski derivati za moduliranje s stresom aktiviranega protein kinaznega sistema |
| US8642034B2 (en) | 2006-10-03 | 2014-02-04 | Genzyme Corporation | Use of TGF-β antagonists to treat infants at risk of developing bronchopulmonary dysplasia |
| ES2559521T3 (es) | 2006-10-16 | 2016-02-12 | Thesan Pharmaceuticals, Inc. | Pirazolil tienopiridinas terapéuticas |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| JP5627574B2 (ja) | 2008-06-03 | 2014-11-19 | インターミューン， インコーポレイテッド | 炎症性および線維性疾患を治療するための化合物および方法 |
| JP5886212B2 (ja) | 2010-12-27 | 2016-03-16 | Ｌｓｉｐファンド運営合同会社 | ｉＰＳ細胞とその製造法 |
| WO2013014262A1 (en) | 2011-07-27 | 2013-01-31 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating myhre syndrome |
| IN2014DN03049A (es) | 2011-10-26 | 2015-05-15 | Seattle Childrens Res Inst | |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
| PT3470409T (pt) * | 2016-06-13 | 2020-05-11 | Genfleet Therapeutics Shanghai Inc | Composto de amida alfa e beta insaturada derivado de benzotriazol utilizado como inibidor de tgf-beta ri |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| CN114105975A (zh) * | 2021-02-25 | 2022-03-01 | 无锡海伦生物科技有限公司 | 一种[1,2,4]三氮唑[1,5-a]吡啶-6-甲醛的合成方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002062787A1 (en) * | 2001-02-02 | 2002-08-15 | Glaxo Group Limited | Pyrazoles as tgf inhibitors |
| WO2004026306A2 (en) * | 2002-09-18 | 2004-04-01 | Pfizer Products Inc. | Pyrazole derivatives as transforming growth factor (tgf) inhibitors |
| CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
-
2005
- 2005-08-24 US US11/661,531 patent/US20080171755A1/en not_active Abandoned
- 2005-08-24 JP JP2007530092A patent/JP2008511630A/ja not_active Withdrawn
- 2005-08-24 WO PCT/US2005/030132 patent/WO2006026305A1/en active Application Filing
- 2005-08-24 CA CA002578628A patent/CA2578628A1/en not_active Abandoned
- 2005-08-24 EP EP05789976A patent/EP1786803A1/en not_active Withdrawn
- 2005-08-24 AU AU2005280167A patent/AU2005280167A1/en not_active Abandoned
- 2005-08-30 AR ARP050103635A patent/AR050622A1/es unknown
- 2005-08-31 TW TW094129851A patent/TW200621752A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20080171755A1 (en) | 2008-07-17 |
| JP2008511630A (ja) | 2008-04-17 |
| CA2578628A1 (en) | 2006-03-09 |
| EP1786803A1 (en) | 2007-05-23 |
| AU2005280167A1 (en) | 2006-03-09 |
| TW200621752A (en) | 2006-07-01 |
| WO2006026305A1 (en) | 2006-03-09 |
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