AR037736A1 - Derivados de pirimidina como moduladores o inhibidores de la actividad del factor de crecimiento insulinico tipo 1 (igf-1r) - Google Patents
Derivados de pirimidina como moduladores o inhibidores de la actividad del factor de crecimiento insulinico tipo 1 (igf-1r)Info
- Publication number
- AR037736A1 AR037736A1 ARP020104747A ARP020104747A AR037736A1 AR 037736 A1 AR037736 A1 AR 037736A1 AR P020104747 A ARP020104747 A AR P020104747A AR P020104747 A ARP020104747 A AR P020104747A AR 037736 A1 AR037736 A1 AR 037736A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- saturated
- atom
- independently represent
- Prior art date
Links
- 239000003102 growth factor Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 9
- 229920006395 saturated elastomer Polymers 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 amino, hydroxyl Chemical group 0.000 abstract 3
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 2
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 abstract 1
- 235000015107 ale Nutrition 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se provee compuestos de la fórmula (1), procesos para su preparación, composiciones farmacéuticas que las contienen, un proceso para preparar las composiciones farmacéuticas y su uso en terapias para enfermedades proliferativas e hiperproliferativas. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1), donde: R1 representa un anillo heteroaromático de 5 o 6 miembros que comprende al menos un heteroátomo en el anillo seleccionado entre N, O, y S, estando el anillo opcionalmente sustituido por al menos un sustituyente seleccionado entre C1-6 alquilo, C1-6 alcoxi (cada uno de los cuales puede ser opcionalmente sustituido por al menos un sustituyente seleccionado entre halógeno, amino, hidroxilo y trifluorometilo), halógeno, nitro, ciano, -NR5R6, carboxilo, hidroxilo, C2-6 alquenilo, C3-6 cicloalquilo, C1-6 alcoxicarbonilo, C1-6 alquilcarbonilo, C1-6 alquilcarbonilamino, fenilcarbonilo, -S(O)mC1-6 alquilo, -C(O)NR7R8, -SO2NR7aRa, y un anillo insaturado de 5 a 6 miembros que puede comprender al menos un heteroátomo en el anillo seleccionado entre N, O, y S, estando el anillo en sí mismo opcionalmente sustituido por al menos un sustituyente seleccionado entre C1-6 alquilo, C1-6 alcoxi (cada uno de los cuales puede ser opcionalmente sustituido por al menos un sustituyente seleccionado entre halógeno, amino, hidroxilo y trifluorometilo), halógeno, nitro, ciano, -NR9R10, carboxilo, hidroxilo, C2-6 alquenilo, C3-6 cicloalquilo, C1-6 alcoxicarbonilo, C1-6 alquilcarbonilo, C1-6 alquilcarbonilamino, fenilcarbonilo, -S(O)nC1-6 alquilo, -C(O)NR11R12 y -SO2NR11aR12a; m es 0, 1 ó 2; n es 0, 1 ó 2; R2 representa un grupo C1-4 alquilo opcionalmente sustituido por al menos un sustituyente seleccionado entre halógeno, hidroxilo y C1-3 alcoxi; R3 representa H, halógeno o trifluorometilo; R4 representa un anillo heteroaromático de 5 miembros que comprende al menos un heteroátomo en el anillo seleccionado entre N, O, y S, estando el anillo opcionalmente sustituido por al menos un sustituyente seleccionado entre C1-6 alquilo, C1-6 alcoxi (cada uno de los cuales puede ser opcionalmente sustituido por al menos un sustituyente seleccionado entre halógeno, amino, hidroxilo y trifuorometilo), halógeno, nitro, ciano, -NR13R14, carboxilo, hidroxilo, C2-6 alquenilo, C3-6 cicloalquilo, C1-4 alcoxicarbonilo, C1-4 alquilcarbonilo, C1-4 alquilcarbonilamino, fenilcarbonilo, -S(O)pC1-4 alquilo, -C(O)NR15R16 y -SO2NR15aR16a, p es 0, 1 ó 2; R5 y R6 representan cada uno independientemente H, C1-4 alquilo, o C3-6 cicloalquilo, o R5 y R6 junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R7 y R8 representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R7 y R8 junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R7a y R8a representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R7a y R8a junto al átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R9 y R10 representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R9 y R10 junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R11 y R12 representan cada uno independientemente H, C1-4 alquilo, o C3-6 cicloalquilo, o R11 y R12 junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R11a y R12a representan cada uno independientemente H, C1-4 alquilo, o C3-6 cicloalquilo, o R11a y R12a junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R13 y R14 representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R13 y R14 junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; R15 y R16 representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R15 y R16 junto al átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; y R15a y R16a representan cada uno independientemente H, C1-4 alquilo o C3-6 cicloalquilo, o R15a y R16a junto con el átomo de N al cual están unidos forman un heterociclo saturado de 4 a 6 miembros; o una sal aceptable para uso farmacéutico o solvato el mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0104140A SE0104140D0 (sv) | 2001-12-07 | 2001-12-07 | Novel Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037736A1 true AR037736A1 (es) | 2004-12-01 |
Family
ID=20286257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104747A AR037736A1 (es) | 2001-12-07 | 2002-12-06 | Derivados de pirimidina como moduladores o inhibidores de la actividad del factor de crecimiento insulinico tipo 1 (igf-1r) |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US7521453B2 (es) |
| EP (1) | EP1456182B1 (es) |
| JP (1) | JP4347051B2 (es) |
| KR (1) | KR100930558B1 (es) |
| CN (1) | CN1289486C (es) |
| AR (1) | AR037736A1 (es) |
| AT (1) | ATE425150T1 (es) |
| AU (1) | AU2002365864B2 (es) |
| BR (1) | BR0214605A (es) |
| CA (1) | CA2467838C (es) |
| CO (1) | CO5590919A2 (es) |
| CY (1) | CY1109101T1 (es) |
| DE (1) | DE60231542D1 (es) |
| DK (1) | DK1456182T3 (es) |
| EG (1) | EG24930A (es) |
| ES (1) | ES2323125T3 (es) |
| HU (1) | HUP0401855A3 (es) |
| IL (2) | IL162376A0 (es) |
| IS (1) | IS7294A (es) |
| MX (1) | MXPA04005347A (es) |
| MY (1) | MY135705A (es) |
| NO (1) | NO327502B1 (es) |
| NZ (1) | NZ533130A (es) |
| PL (1) | PL369528A1 (es) |
| PT (1) | PT1456182E (es) |
| RU (1) | RU2317291C2 (es) |
| SE (1) | SE0104140D0 (es) |
| SI (1) | SI1456182T1 (es) |
| TW (1) | TWI324152B (es) |
| UA (1) | UA78259C2 (es) |
| WO (1) | WO2003048133A1 (es) |
| ZA (1) | ZA200404223B (es) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| MXPA05001096A (es) | 2002-07-29 | 2005-11-23 | Rigel Pharmaceuticals Inc | Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina. |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| US7442698B2 (en) | 2003-07-24 | 2008-10-28 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| AU2004265288A1 (en) | 2003-07-30 | 2005-02-24 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| US20050113398A1 (en) * | 2003-08-07 | 2005-05-26 | Ankush Argade | 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents |
| BRPI0415395A (pt) * | 2003-10-15 | 2006-12-12 | Osi Pharm Inc | composto, métodos para inibir a atividade da proteìna quinase e para tratar um paciente que tenha uma condição que seja mediada pela atividade da proteìna quinase, e, composição |
| JP2007510626A (ja) | 2003-10-17 | 2007-04-26 | アストラゼネカ アクチボラグ | 癌の治療に使用の4−(ピラゾール−3−イルアミノ)ピリミジン誘導体 |
| MY141220A (en) * | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| ES2299825T3 (es) | 2004-03-12 | 2008-06-01 | Analytecon S.A. | Derivados de tetrahidroisoquinoleino y de tetrahidrobenzazepina utilizados como inhibidores de igf-1r. |
| AU2005230847B2 (en) * | 2004-03-31 | 2012-11-08 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| EP2305682A1 (en) | 2004-04-02 | 2011-04-06 | OSI Pharmaceuticals, Inc. | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
| DE102004022897A1 (de) * | 2004-05-10 | 2005-12-08 | Bayer Cropscience Ag | Azinyl-imidazoazine |
| AR053090A1 (es) | 2004-07-20 | 2007-04-25 | Osi Pharm Inc | Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos |
| US7557207B2 (en) | 2004-11-24 | 2009-07-07 | Rigel Pharmaceuticals, Inc. | Spiro 2,4-pyrimidinediamine compounds and their uses |
| WO2006074057A2 (en) * | 2004-12-30 | 2006-07-13 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| CN101115761B (zh) | 2005-01-19 | 2012-07-18 | 里格尔药品股份有限公司 | 2,4-嘧啶二胺化合物的前药及其应用 |
| SI1846394T1 (sl) | 2005-02-04 | 2012-06-29 | Astrazeneca Ab | Pirazolilaminopiridinski derivati uporabni kot kinazni inhibitorji |
| RU2415852C2 (ru) * | 2005-02-04 | 2011-04-10 | Астразенека Аб | Производные пиразолиламинопиридина, пригодные в качестве ингибиторов киназы |
| BRPI0607455A2 (pt) * | 2005-02-16 | 2009-09-01 | Astrazeneca Ab | composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica |
| GB0507347D0 (en) * | 2005-04-12 | 2005-05-18 | Astrazeneca Ab | Chemical compounds |
| CN101208093A (zh) * | 2005-04-27 | 2008-06-25 | 阿斯利康(瑞典)有限公司 | 吡唑-嘧啶衍生物在治疗疼痛中的用途 |
| JP2008540622A (ja) * | 2005-05-16 | 2008-11-20 | アストラゼネカ アクチボラグ | 化合物 |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| NZ563454A (en) | 2005-06-08 | 2011-03-31 | Rigel Pharmaceuticals Inc | 2,4-diaminopyrimidine derivatives for inhibition of the JAK pathway |
| US7566721B2 (en) * | 2005-08-08 | 2009-07-28 | Osi Pharmaceuticals, Inc. | Substituted thienol[2,3-d]pyrimidines as kinase inhibitors |
| AR056471A1 (es) | 2005-08-24 | 2007-10-10 | Wyeth Corp | Formulaciones de acetato de bazedoxifeno |
| DK1926996T3 (da) | 2005-09-20 | 2012-01-23 | Osi Pharmaceuticals Llc | Biologiske markører, som er prædiktive for anti-cancer-reaktion på insulinlignende vækstfaktor-1-receptorkinasehæmmere |
| EP1945631B8 (en) | 2005-10-28 | 2013-01-02 | AstraZeneca AB | 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer |
| AR057960A1 (es) | 2005-12-02 | 2007-12-26 | Osi Pharm Inc | Inhibidores de proteina quinasa biciclicos |
| US8575164B2 (en) * | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
| MX2008015726A (es) * | 2006-06-09 | 2008-12-19 | Novartis Ag | Polipeptidos de factor de crecimiento de tipo insulina estabilizada. |
| KR20090023698A (ko) * | 2006-06-15 | 2009-03-05 | 베링거 인겔하임 인터내셔날 게엠베하 | 2-아닐리노-4-아미노알킬렌아미노피리미딘 |
| UY30444A1 (es) * | 2006-06-30 | 2008-01-31 | Astrazeneca Ab | Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos. |
| WO2008005538A2 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| WO2008129255A1 (en) * | 2007-04-18 | 2008-10-30 | Astrazeneca Ab | 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer |
| UA99459C2 (en) * | 2007-05-04 | 2012-08-27 | Астразенека Аб | 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer |
| CN101687863B (zh) * | 2007-05-04 | 2012-09-12 | 阿斯利康(瑞典)有限公司 | 氨基-噻唑基-嘧啶衍生物及其治疗癌症的用途 |
| US8178091B2 (en) | 2007-05-21 | 2012-05-15 | University Of Washington | Compositions and methods for the treatment of respiratory disorders |
| WO2009019518A1 (en) * | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
| JP2011510018A (ja) * | 2008-01-18 | 2011-03-31 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 癌治療のためのイミダゾピラジノール誘導体 |
| EP2283020B8 (en) * | 2008-05-19 | 2012-12-12 | OSI Pharmaceuticals, LLC | Substituted imidazopyr-and imidazotri-azines |
| TW201006830A (en) * | 2008-06-11 | 2010-02-16 | Astrazeneca Ab | Chemical compounds |
| DE102008041214A1 (de) | 2008-08-13 | 2010-02-18 | Bayer Cropscience Ag | N-substituierte Azinylakyl-azincarboxamide und deren Analoge |
| MX2011003447A (es) * | 2008-09-30 | 2011-07-29 | Astrazeneca Ab | Inhibidores heterociclicos de jak quinasa. |
| EP2400985A2 (en) | 2009-02-25 | 2012-01-04 | OSI Pharmaceuticals, LLC | Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor |
| EP2400990A2 (en) | 2009-02-26 | 2012-01-04 | OSI Pharmaceuticals, LLC | In situ methods for monitoring the emt status of tumor cells in vivo |
| US8465912B2 (en) | 2009-02-27 | 2013-06-18 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2010099138A2 (en) | 2009-02-27 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2010099363A1 (en) | 2009-02-27 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| EP2421837A1 (en) | 2009-04-20 | 2012-02-29 | OSI Pharmaceuticals, LLC | Preparation of c-pyrazine-methylamines |
| JP2012526138A (ja) * | 2009-05-07 | 2012-10-25 | オーエスアイ・ファーマシューティカルズ,エルエルシー | 副腎皮質癌を治療するためのosi−906の使用 |
| WO2010146059A2 (en) | 2009-06-16 | 2010-12-23 | F. Hoffmann-La Roche Ag | Biomarkers for igf-1r inhibitor therapy |
| US20110275644A1 (en) | 2010-03-03 | 2011-11-10 | Buck Elizabeth A | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors |
| CA2783665A1 (en) | 2010-03-03 | 2011-09-09 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors |
| WO2011112666A1 (en) | 2010-03-09 | 2011-09-15 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| CN102970867A (zh) | 2010-03-18 | 2013-03-13 | 拜耳知识产权有限责任公司 | 作为活性剂对抗非生物植物应激的芳基和杂芳基磺酰胺 |
| MX2012013274A (es) | 2010-05-21 | 2013-05-28 | Chemilia Ab | Novedosos derivados de la pirimidina. |
| UY33817A (es) * | 2010-12-21 | 2012-07-31 | Boehringer Ingelheim Int | ?nuevas oxindolpirimidinas bencílicas?. |
| US20140037642A1 (en) | 2011-02-02 | 2014-02-06 | Amgen Inc. | Methods and compositions relating to inhibition of igf-1r |
| US20120214830A1 (en) | 2011-02-22 | 2012-08-23 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma |
| JP5886411B2 (ja) | 2011-03-24 | 2016-03-16 | ノビガ・リサーチ・エービーNoviga Research AB | 新規のピリミジン誘導体 |
| US9975967B2 (en) | 2011-04-13 | 2018-05-22 | Eastman Chemical Company | Cellulose ester optical films |
| WO2012149014A1 (en) | 2011-04-25 | 2012-11-01 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
| JP6268097B2 (ja) | 2011-11-11 | 2018-01-24 | デューク・ユニヴァーシティ | 固形腫瘍治療のための併用薬物療法 |
| WO2013152252A1 (en) | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| US8980259B2 (en) | 2012-07-20 | 2015-03-17 | Novartis Ag | Combination therapy |
| WO2014134202A1 (en) | 2013-02-26 | 2014-09-04 | Triact Therapeutics, Inc. | Cancer therapy |
| CA2923667A1 (en) | 2013-09-09 | 2015-03-12 | Triact Therapeutics, Inc. | Cancer therapy |
| WO2017129763A1 (en) | 2016-01-28 | 2017-08-03 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of signet ring cell gastric cancer |
| CN115124475B (zh) * | 2022-07-11 | 2023-11-10 | 贵阳学院 | 一种嘧啶衍生物及其制备方法和用途 |
| WO2024153237A1 (zh) * | 2023-01-19 | 2024-07-25 | 北京普祺医药科技股份有限公司 | 一种igf-1r酪氨酸激酶抑制剂、药物组合物及其用途 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1417402A (en) * | 1972-03-30 | 1975-12-10 | Boots Co Ltd | Pharmacologically active anilinobenzothiazoles |
| DE2426180A1 (de) | 1974-05-29 | 1975-12-18 | Bayer Ag | Verfahren zum faerben von polyurethankunststoffen |
| US4485284A (en) * | 1982-01-11 | 1984-11-27 | Advanced Moisture Technology, Inc. | Apparatus and process for microwave moisture analysis |
| HU206337B (en) | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| CA2104053C (en) * | 1992-08-31 | 1999-04-13 | Miguel A. Cacho | Automated fluid bed process |
| US5935966A (en) | 1995-09-01 | 1999-08-10 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| WO1997009325A1 (en) | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| WO1998044341A1 (de) * | 1997-03-27 | 1998-10-08 | Glatt Gmbh | Verfahren zum überwachen und/oder steuern und regeln eines granulations-, agglomerations-, instantisierungs-, coating- und trocknungsprozesses in einer wirbelschicht oder einer bewegten schüttung durch bestimmung der produktfeuchte sowie lufttechnischer apparat zur durchführung des verfahrens |
| US6247246B1 (en) * | 1998-05-27 | 2001-06-19 | Denver Instrument Company | Microwave moisture analyzer: apparatus and method |
| ATE342892T1 (de) | 1998-08-29 | 2006-11-15 | Astrazeneca Ab | Pyrimidine verbindungen |
| KR100658489B1 (ko) | 1998-11-10 | 2006-12-18 | 얀센 파마슈티카 엔.브이. | Hiv 복제를 억제하는 피리미딘 |
| WO2000035455A1 (en) | 1998-12-15 | 2000-06-22 | Telik, Inc. | Heteroaryl-aryl ureas as igf-1 receptor antagonists |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| DE19917785A1 (de) * | 1999-04-20 | 2000-10-26 | Bayer Ag | 2,4-Diamino-pyrimidin-Derivate |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| US6399780B1 (en) * | 1999-08-20 | 2002-06-04 | Cephalon, Inc. | Isomeric fused pyrrolocarbazoles and isoindolones |
| CZ300712B6 (cs) * | 1999-09-24 | 2009-07-22 | Janssen Pharmaceutica N. V. | Cásticová farmaceutická kompozice, pevná disperze a farmaceutická dávková forma, zpusoby jejich prípravy a použití a obchodní balení s jejich obsahem |
| US6455525B1 (en) * | 1999-11-04 | 2002-09-24 | Cephalon, Inc. | Heterocyclic substituted pyrazolones |
| AU2001237041B9 (en) | 2000-02-17 | 2005-07-28 | Amgen Inc. | Kinase inhibitors |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| DK1282607T3 (en) | 2000-05-08 | 2016-02-01 | Janssen Pharmaceutica Nv | Prodrugs of HIV replication inhibiting pyrimidines |
| US6610677B2 (en) * | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1317450B1 (en) * | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6613776B2 (en) * | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) * | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CA2432222C (en) * | 2000-12-21 | 2008-07-29 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| AU2002321910A1 (en) * | 2001-08-03 | 2003-02-17 | Vertex Pharmaceuticals Incorporated | Pyrazole-derived kinase inhibitors and uses thereof |
| US6875789B2 (en) * | 2001-08-03 | 2005-04-05 | Vertex Pharmaceuticals Incorporated | Pyrazole-derived kinase inhibitors and uses thereof |
| US6747461B2 (en) * | 2001-10-25 | 2004-06-08 | Pioneer Hi-Bred International, Inc. | Apparatus and method for monitoring drying of an agricultural porous medium such as grain or seed |
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| MY141220A (en) * | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| WO2006052913A1 (en) * | 2004-11-04 | 2006-05-18 | Vertex Pharmaceuticals Incorporated | PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES |
| BRPI0607455A2 (pt) * | 2005-02-16 | 2009-09-01 | Astrazeneca Ab | composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica |
| SG166827A1 (en) * | 2005-11-03 | 2010-12-29 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| UY30444A1 (es) * | 2006-06-30 | 2008-01-31 | Astrazeneca Ab | Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos. |
| TW200823196A (en) * | 2006-11-01 | 2008-06-01 | Astrazeneca Ab | New use |
| TW200826937A (en) * | 2006-11-01 | 2008-07-01 | Astrazeneca Ab | New use |
-
2001
- 2001-12-07 SE SE0104140A patent/SE0104140D0/xx unknown
-
2002
- 2002-03-12 UA UA20040705367A patent/UA78259C2/uk unknown
- 2002-12-02 TW TW091134937A patent/TWI324152B/zh not_active IP Right Cessation
- 2002-12-03 WO PCT/SE2002/002221 patent/WO2003048133A1/en not_active Ceased
- 2002-12-03 MX MXPA04005347A patent/MXPA04005347A/es active IP Right Grant
- 2002-12-03 ES ES02791165T patent/ES2323125T3/es not_active Expired - Lifetime
- 2002-12-03 EP EP02791165A patent/EP1456182B1/en not_active Expired - Lifetime
- 2002-12-03 CA CA2467838A patent/CA2467838C/en not_active Expired - Fee Related
- 2002-12-03 CN CNB02827802XA patent/CN1289486C/zh not_active Expired - Fee Related
- 2002-12-03 DK DK02791165T patent/DK1456182T3/da active
- 2002-12-03 US US10/497,744 patent/US7521453B2/en not_active Expired - Fee Related
- 2002-12-03 KR KR1020047008612A patent/KR100930558B1/ko not_active Expired - Fee Related
- 2002-12-03 AU AU2002365864A patent/AU2002365864B2/en not_active Ceased
- 2002-12-03 JP JP2003549325A patent/JP4347051B2/ja not_active Expired - Fee Related
- 2002-12-03 IL IL16237602A patent/IL162376A0/xx unknown
- 2002-12-03 RU RU2004121029/04A patent/RU2317291C2/ru not_active IP Right Cessation
- 2002-12-03 BR BR0214605-3A patent/BR0214605A/pt not_active IP Right Cessation
- 2002-12-03 DE DE60231542T patent/DE60231542D1/de not_active Expired - Lifetime
- 2002-12-03 AT AT02791165T patent/ATE425150T1/de active
- 2002-12-03 PL PL02369528A patent/PL369528A1/xx not_active Application Discontinuation
- 2002-12-03 HU HU0401855A patent/HUP0401855A3/hu unknown
- 2002-12-03 SI SI200230824T patent/SI1456182T1/sl unknown
- 2002-12-03 NZ NZ533130A patent/NZ533130A/en not_active IP Right Cessation
- 2002-12-03 PT PT02791165T patent/PT1456182E/pt unknown
- 2002-12-04 MY MYPI20024549A patent/MY135705A/en unknown
- 2002-12-06 AR ARP020104747A patent/AR037736A1/es unknown
-
2004
- 2004-05-28 ZA ZA200404223A patent/ZA200404223B/en unknown
- 2004-06-03 IS IS7294A patent/IS7294A/is unknown
- 2004-06-03 CO CO04052141A patent/CO5590919A2/es not_active Application Discontinuation
- 2004-06-06 EG EGNA2004000039 patent/EG24930A/xx active
- 2004-06-06 IL IL162376A patent/IL162376A/en not_active IP Right Cessation
- 2004-07-06 NO NO20042872A patent/NO327502B1/no not_active IP Right Cessation
-
2009
- 2009-01-26 US US12/359,541 patent/US20090131463A1/en not_active Abandoned
- 2009-05-25 CY CY20091100558T patent/CY1109101T1/el unknown
-
2011
- 2011-12-07 US US13/313,097 patent/US20120095011A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR037736A1 (es) | Derivados de pirimidina como moduladores o inhibidores de la actividad del factor de crecimiento insulinico tipo 1 (igf-1r) | |
| AR120855A1 (es) | Derivados de pirazolilo útiles como agentes anticancerígenos | |
| PE20231312A1 (es) | Derivados triciclicos de carboxamida como inhibidores de la prmt5 | |
| AR127309A2 (es) | Derivados de piridazinona | |
| AR046711A1 (es) | 5-7-diaminopirazolo[4,3d]pirimidinas como inhibidores de la pde-5,composiciones farmaceuticas que las contienen y usos en el tratamiento de hipertensiones | |
| ES2328820T3 (es) | Derivados de 4-(pirazol-3-ilamino)pirimidina para uso en el tratamiento de cancer. | |
| AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
| AR078786A1 (es) | Derivados de la cromenona | |
| AR054799A1 (es) | Derivados de oxindol | |
| AR079205A1 (es) | Morfolinotiazoles como moduladores alostericos positivos alfa 7 | |
| AR046779A1 (es) | Derivados de pirazol, metodos para su preparacion y usos de los mismos en la fabricacion de composiciones farmaceuticas y medicamentos que los contienen con actividad inhibitoria de trk para el tratamiento o profilaxis del cancer. | |
| AR045595A1 (es) | Composiciones utiles como inhibidores de proteinas quinasas | |
| AR041066A1 (es) | 2,5-dioxoimidazolidin-4-il-acetamidas y analogos como inhibidores de la metaloproteinasa mmp12 | |
| AR067757A1 (es) | Derivados de imidazo[4,5-c]piridin-2-ona, composiciones farmaceuticas que los contienen, procedimiento para su preparacion y uso de los mismos como agentes antivirales. | |
| AR049092A1 (es) | Derivados de tetrahidronaftiridina como ligandos del receptor h3 de histamina | |
| AR065719A1 (es) | Imidazo y triazolopirimidinas, un procedimiento para su preparacion y su uso en la elaboracion de un medicamento para el tratamiento de trastornos hematologicos. | |
| AR083367A1 (es) | Compuestos de tipo quinazolinona como antagonistas de crth | |
| AR045691A1 (es) | Derivados de heteroarilamida como receptores antagonistas p2x7 y sus usos | |
| AR065133A1 (es) | Derivados de tetrahidroisoquinolina, composiciones farmaceuticas que los contienen y usos de los mismos para tratar o prevenir enfermedades o trastornos asociados a la actividad de gpr119, tales como diabetes, obesidad y trastornos cardiovasculares, entre otros. | |
| AR088029A1 (es) | Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central | |
| ECSP105253A (es) | Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa | |
| AR060287A1 (es) | Compuesto de 5,6 dihidro-3h-pirrolo[1,2,3-de]quinoxalini-3-ona, su uso para preparar un medicamento, composicion farmaceutica que lo comprende y compuesto intermediario util para su preparacion | |
| AR055303A1 (es) | Derivados de triazol sustituidos como antagonistas de oxitocina, composicion farmaceutica y uso del compuesto para preparar un medicamento | |
| AR056511A1 (es) | Derivados de 2-aminopirimidinas, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por el receptor de histamina h4 | |
| AR046992A1 (es) | Derivados de espiro-dihidrobenzofuranos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |