AR043057A1 - Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa - Google Patents
Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasaInfo
- Publication number
- AR043057A1 AR043057A1 ARP030103973A ARP030103973A AR043057A1 AR 043057 A1 AR043057 A1 AR 043057A1 AR P030103973 A ARP030103973 A AR P030103973A AR P030103973 A ARP030103973 A AR P030103973A AR 043057 A1 AR043057 A1 AR 043057A1
- Authority
- AR
- Argentina
- Prior art keywords
- phenyl
- hydrogen
- och3
- unsubstituted
- optionally substituted
- Prior art date
Links
Classifications
-
- 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
- C07D417/14—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
-
- 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
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
-
- 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
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
- A61P37/02—Immunomodulators
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
Abstract
La presente se refiere a compuestos útiles como inhibidores de las proteínas quinasa, además, provee composiciones farmacéuticamente aceptables que comprenden dichos a compuestos, y métodos para la utilización de las composiciones para el tratamiento de varias enfermedades, condiciones o trastornos proliferativos, inflamatorios, autoinminológicos, neurodegenerativos y usos de los mismos como quimioterapéuticos. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque B es una de las estructuras (2), (3), (4), R1 es halógeno, CN, NO2, o VmR; Z1 y Z3 son cada uno independientemente N o CRZ, y Z2 es N o CR1, con la condición de que provided that Z1, Z2 y Z3 no sean simultaneamente N; cada vez que RZ está presente, es independientemente halógeno, CN, NO2, o UnR'; R2 es UnR'; X1 y X2 son cada uno independientemente CR4 o N; cada vez que R4 está presente, es independientemente halógeno, CN, NO2, o VmR; cada vez que está presente, U o V es independientemente una cadena alquilideno C1-6 opcionalmente substituida, donde hasta dos unidades de metileno de la cadena están opcional e independientemente reemplazadas por -NR-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR-, -NRCO-, -NRCO2-, -NRCO2-, -SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2NR-, -PO-, -PO2- o -POR-; m y n son cada uno independientemente 0 o 1; cada vez que está presente, R es independientemente hidrógeno o un grupo alifático C1-6 opcionalmente substituido; y cada vez que está presente R' es independientemente hidrógeno o un grupo alifático C1-6 opcionalmente substituido, un anillo arilo C1-6 opcionalmente substituido, un anillo heteroarilo opcionalmente substituido que tiene de 5-10 átomos en el anillo, o un anillo heterociclilo opcionalmente substituido, que tiene de 3-10 átomos en el anillo; o R y R', dos R presentes; o dos R' presentes se toman junto con el/los átomo/s a los cuales están unidos para formar un anillo opcionalmente substituido de 3-8 miembros saturado, parcialmente insaturado, o completamente insaturado que tiene 0-4 heteroátomos seleccionados de manera independiente entre nitrógeno, oxígeno, o azufre; Q1 es -CO-, -SO2-, -CONR-, o -SO2NR-; R3 es Q2-Ar, o R2 y Q1-R3, tomados junto con el átomo de nitrógeno, forman el grupo cíclico (5): donde s es 1 o 2, cada vez que está presente Y es independientemente, según la valencia y estabilidad lo permitan, -CO-, -CS-, -SO2-, -O-, -S-, -NR5 -, o -C(R5)2-, y R5 es UnR'; Q2 y Q3 son cada uno independientemente un enlace o una cadena alquilideno C1-6, donde hasta dos unidades de metileno de la cadena son opcional e independientemente reemplazadas por -NR'-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR'-, -NR'CO-, -NR'CO2-, -SO2NR'-, -NR'SO2-, -CONR'NR'-, -NR'CONR'-, -OCONR'-, -NR'NR'-, -NR'SO2NR'-, -SO-, -SO2-, -PO-, -PO2-, o -POR'-; y donde cada átomo de carbono en una o más unidades metileno está opcionalmente substituido con una o R6 presentes, donde cada vez que está presente R6 es independientemente halógeno, CN, NO2, o UnR', o dos R6 presentes, o R' y R6, tomados junto con los átomos a los cuales están unidos, forman un anillo opcionalmente substituido de 3 6 miembros, cicloalquilo, heterociclilo, arilo o heteroarilo; y Ar1 y Ar2 son independientemente un anillo monocíclico que tiene de 5-6 miembros saturado, parcialmente insaturado, o completamente insaturado que tiene de 0-3 heteroátomos seleccionados de manera independiente entre nitrógeno, oxígeno, o azufre, o un sistema de anillo bicíclico que tiene de 8-10 miembros saturado, parcialmente insaturado, o completamente insaturado que tiene de 0-5 heteroátomos seleccionados de manera independiente entre nitrógeno, oxígeno, o azufre; donde Ar1 y Ar2 están cada uno opcionalmente substituido con 0-5 TR7 presentes independientes; donde T es un enlace o es una cadena C1-C6 alquilideno donde hasta dos unidades metileno de T están opcionalmente reemplazadas por -NR-, -S-, -O-, -CS-, -CO2-, -OCO-,-CO-, -COCO-, -CONR-, -NRCO-, -NRCO2-, -SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; y cada vez que aparece R7 es independientemente R', halógeno, NO2, o CN; con la condición de que: I) Para los compuestos descriptos donde B es de la estructura (2) se aplican una o más de, o todas las siguientes condiciones: A) para los compuestos que tienen la estructura (6): i) cuando R1 es Cl, y R2 es -CH(CH3)COOCH3 o hidrógeno, entonces Q1-R3 no es -CO(fenilo no substituido), -CO(2-furilo no substituido), o -COCH2(fenilo no substituido); ii) cuando R1 es hidrógeno, R2 es hidrógeno, y Q1 es -CO-, entonces R3 no es: a) fenilo substituido con 4-O(CH2)4-7CH3 o 4-(CH2)4-7CH3; b) fenilo substituido con 2-Cl, 4-NO2, 4-Cl, 2-Br, 3-Br, 3-I, 3-CH3, 4-OCH3, 3-NO2, o 4-I; c) 2,6-OCH3-fenilo d) (5-Cl, 3-CH3, 1-fenil)-pirazol-4-ilo; o e) 4-OnBu-fenilo, -CH2O(2-F-fenilo), -(CH2)2fenilo, furan-2-ilo, tiofen-2-ilo, 4-CH3-fenilo, -CH2O(2-CH3-fenilo), 3-OCH3-fenilo, 2-(2,5-dimetoxilfenil)quinolin-4-ilo, -NH-(4-Cl-fenilo), -NH-(3,4-diclorofenilo), (2-CO2H, 3-NO2)-fenilo, 3,5-dimetil-isoxazol-4-ilo, -CH=CH-fenilo, 4-F-fenilo, C(CH3)2O-(4-Cl-fenilo), -NH(3-Cl-fenilo), -NHfenilo, fenilo no substituido, 3,4,5-OCH3-fenilo, 4-NO2-fenilo, 4-ciclopentoxi-fenilo, -(CH2)3fenilo, -(triciclo[3.3.1.13,7]decan-1-ilo, -CH2O-(3-CH3-fenilo), 3-NO2-fenilo, -ciclopropil-(4-tert-butil-fenilo), 2,3-OCH3-fenilo, 1,3-benzodioxo-5-ilo, -CH2-O-(4-F-fenilo), o 3-Br-fenilo; iii) cuando R1 es hidrógeno, R2 es hidrógeno, y Q1 es -CSNH-, entonces R3 no es 2,3,4,6-tetra-O-acetil-beta-D-glucopiranosilo; iv) cuando R1 es hidrógeno, R2 es hidrógeno, y Q1 es SO2, entonces R3 no es fenilo no substituido, bencilo no substituido, naftilo no substituido, fenilo substituido con para-NHCOCH3, para-NH2, o para-CH3; y v) cuando R1 es hidrógeno, R2 es -CH2CH-CH2, y Q1 es CO, entonces R3 no es 4-OCH3-fenilo, naftilo no substituido, -NH-(4-OCH3-fenilo), 3,5-OCH3-fenilo, CH2Ofenilo, -CH2-tiofen-2-ilo, o -CH(fenilo)(CH2CH3); y vi) cuando R1 es hidrógeno, R2 es CH2CH3, y Q1 es CO, entonces R3 no es 2,4-Cl-fenilo; y B) para los compuestos que tienen la estructura (7): cuando R2 es hidrógeno o CH3, y Q1 es -CO-, entonces R3 no es -OCH2CH2OCH2fenilo; II) Para los compuestos descriptos, donde B es de fórmula (3) se aplican una o más de, o todas las siguientes condiciones: A) para los compuestos que tienen la estructura (8); i) cuando R3 es Q2-Ar1, y Q2 es un enlace entonces Ar1 no es uno ni más de uno de los siguientes: fenilo no substituido o fenilo substituido con 2-Br; 2-Cl; 2-I; 2,6-F; 3,5-OCH3; 3,4,5-OCH3; 2,4-OCH3; 3,4-CH3; 2,5-Cl; 3,4,-OCH3; 2-Cl, 5-NO2; 3,5-Cl; 3-O(CH2)4CH3, 3-O-n-butilo, 3-CF3, 3-OCH3, 3-Br; 3-NO2; 3-CH3; 3-O-fenilo; 3-Cl; 4-N(CH3)2; 4-N(CH2CH3)2; 4-SO2N(R')2; 4-CN; 4-COOCH3; 4-C(O)fenilo; 4-fenilo; 4-tert-butilo, 4-O-fenilo; 4-O-isopropilo; 4-OCH3; 4-OCH2CH3; 4-O-n-butilo; 4-Cl; 4-Br; 4-F; 4-CH3; 4-NO2; 4-Cl; 3-NO2, 4-morfolino; 3-NO2, 2,5-dioxopirrolidinilo, o 4-piperidinilo; y ii) R3 no es uno ni más de uno de los siguientes grupos: fórmula (9), fórmula (10), -CH-CH(tiofen-2-ilo), -CH-CH-fenilo no substituido, -CH2(3-NHCOPh-fenilo), -6-bromo-2-(4-etilfenil)-4-quinolinilo, -CH2-pirrolidina, ciclohexilo no substituido, bencilo no substituido, furan-2-ilo no substituido, -CH-CH(3-NO2fenilo), -CH-CH(4-NO2-fenilo), -CH2-naftilo, naftilo no substituido, tiofeno no substituido, ciclopropilo no substituido, 1,4-benzodioxin, 2-oxo-1-benzopirano, 4-oxo-1-benzopirano, 2-tienil-quinolin-4-ilo, 3-cloro-benzo[b]tiofen-2-ilo, 5-Br-(tiofen-2-ilo), 5-Cl-(tiofen-2-ilo), 5-NO2(tiofen-2-ilo), 5-NO2(furan2-ilo), 2,5-Cl-(tiofen-3-ilo), -CH-CH-(5-NO2-tiofen-2-ilo), 5-NO2-(benzotiofen-2-ilo), 3-OCH3-(naft-2-ilo), -CH2O(2,4-Cl-fenilo), -(CH2)2S-fenilo, 2-fenil-quinolin-4-ilo, -CH2O(4-Cl-fenilo), -CH2CH2-3-(4-Cl-fenil)-1-fenil-1-fenil-1-H-pirazol-4ilo, o -CH2(1,3-dioxoisoindol); y B) para los compuestos que tienen la estructura (11): i) cuando R1 es Cl, y X1 es C-Cl, entonces R3 no es NHSO2-(2-CF3-fenilo) o -NHSO2-(2,6-dimetoxi-fenilo); ii) cuando R1 es CH3, y X1 es C-CH3, entonces R3 no es un indol opcionalmente substituido o dihidroindol opcionalmente substituido; y C) para compuestos de la fórmula general (1), cuando Z1, Z2 y Z3 son, cada uno, CH, R1 es H, X1 es CH y X2 es C-COOCH3, entonces R3 no es 2-(4-etil-fenil)-6-bromo-quinolin-4-ilo; y III. Para los compuestos descriptos anteriormente, donde B es de fórmula (4) se aplican una o más de, o todas las siguientes condiciones: A) cuando Z1, Z2 y Z3 son cada uno CH, X2 es N, X1 is CH, Q1 es -CONR-, y R2 es hidrógeno o -CH3, entonces R3 no es piridilo opcionalmente substituido, tiazol-4-ilo opcionalmente substituido, -CH2piridilo, benzimidazol-4-ilo, quinolin-2-ilo, 1-bromo-isoquinolin-3-ilo, benzotiazol-2-ilo, 5,6,7,8-tetrahidro-naftiridin-2-ilo opcionalmente substituido, o fenilo substituido con -CH2piperidinilo; y B) cuando Z1, Z2 y Z3 son cada uno CH, X2 es N, X1 es CH, Q1 es SO2, y R2 es hidrógeno, entonces R3 no es fenilo substituido con la estructura (12) donde R'' es hidrógeno o -COCH3; C) cuando Z1, Z2 y Z3 son cada uno CH, X1 es C-CO2H, X2 es CH, R2 es hidrógeno, y Q1 es SO2, entonces R3 no es 2-CH3-fenilo; y D) cuando Z1, Z2 y Z3 son cada uno CH, X1 es CH, X2 es N, R2 es hidrógeno, y Q1 es CO, entonces R3 no es 5-metoxi-6-trifluorometil-1H-indol.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US42244102P | 2002-10-30 | 2002-10-30 | |
US47669103P | 2003-06-06 | 2003-06-06 | |
US47643303P | 2003-06-06 | 2003-06-06 | |
US47990303P | 2003-06-19 | 2003-06-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR043057A1 true AR043057A1 (es) | 2005-07-13 |
Family
ID=32314959
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030103973A AR043057A1 (es) | 2002-10-30 | 2003-10-30 | Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa |
Country Status (14)
Country | Link |
---|---|
US (1) | US20040122016A1 (es) |
EP (1) | EP1558607B1 (es) |
JP (1) | JP2006514684A (es) |
KR (1) | KR20050088283A (es) |
AR (1) | AR043057A1 (es) |
AT (1) | ATE466855T1 (es) |
AU (1) | AU2003288956A1 (es) |
CA (1) | CA2504320A1 (es) |
DE (1) | DE60332475D1 (es) |
MX (1) | MXPA05004689A (es) |
NO (1) | NO20052595L (es) |
NZ (1) | NZ540161A (es) |
TW (1) | TW200416221A (es) |
WO (1) | WO2004041813A1 (es) |
Families Citing this family (112)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7196106B2 (en) * | 2002-11-05 | 2007-03-27 | Merck & Co., Inc | Cyanothiophene derivatives, compositions containing such compounds and methods of use |
AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
WO2005019190A2 (en) * | 2003-08-20 | 2005-03-03 | Vertex Pharmaceuticals Incorporated | (4 -amino -1,2, 5-oxadiazol-4-yl) -hetξroaromatic compounds useful as protein kinase inhibitors |
WO2005026137A2 (en) * | 2003-09-06 | 2005-03-24 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
US20050085531A1 (en) * | 2003-10-03 | 2005-04-21 | Hodge Carl N. | Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof |
SI1700856T1 (sl) * | 2003-12-26 | 2016-02-29 | Kyowa Hakko Kirin Co., Ltd., | Tiazolni derivat |
EP3219709B1 (en) * | 2004-01-30 | 2020-03-18 | Vertex Pharmaceuticals Incorporated | Intermediate compound of modulators of atp-binding cassette transporters |
US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
WO2005095386A1 (en) * | 2004-03-30 | 2005-10-13 | Chiron Corporation | Substituted thiophene derivatives as anti-cancer agents |
ATE464303T1 (de) * | 2004-04-28 | 2010-04-15 | Vertex Pharma | Als inhibitoren von rock und anderen proteinkinasen geeignete zusammensetzungen |
WO2005113548A1 (en) * | 2004-05-20 | 2005-12-01 | Sugen, Inc. | Thiophene heteroaryl amines |
CA2575466A1 (en) | 2004-08-13 | 2006-02-23 | Genentech, Inc. | Thiazole based inhibitors of atp-utilizing enzymes |
EA012181B1 (ru) * | 2004-10-18 | 2009-08-28 | Амген, Инк. | Соединения тиадиазола и их применение |
WO2006058074A1 (en) * | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases |
EP1824835A1 (en) * | 2004-12-03 | 2007-08-29 | Novo Nordisk A/S | Heteroaromatic glucokinase activators |
EP1894930A4 (en) | 2005-06-23 | 2010-06-23 | Kyowa Hakko Kirin Co Ltd | THIAZOLE DERIVATIVE |
WO2007037543A1 (ja) * | 2005-09-29 | 2007-04-05 | Banyu Pharmaceutical Co., Ltd. | ビアリールアミド誘導体 |
JP2009513711A (ja) * | 2005-11-01 | 2009-04-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | グルコキナーゼのアロステリックモジュレーターとしての置換ピロロン |
EP1960385A1 (en) * | 2005-11-01 | 2008-08-27 | Janssen Pharmaceutica N.V. | Substituted dihydroisoindolones as allosteric modulators of glucokinase |
EP1951706A1 (en) * | 2005-11-01 | 2008-08-06 | Janssen Pharmaceutica N.V. | Dihydroisoindolones as allosteric modulators of glucokinase |
CA2627910A1 (en) * | 2005-11-01 | 2007-05-10 | Janssen Pharmaceutica N.V. | Substituted cycloalkylpyrrolones as allosteric modulators of glucokinase |
CA2636077C (en) * | 2006-01-18 | 2012-01-03 | Amgen Inc. | Thiazole compounds as protein kinase b (pkb) inhibitors |
US8211925B2 (en) | 2006-04-28 | 2012-07-03 | Transtech Pharma, Inc. | Benzamide glucokinase activators |
KR20090017589A (ko) * | 2006-05-12 | 2009-02-18 | 버텍스 파마슈티칼스 인코포레이티드 | Rock 단백질 키나아제의 선택적 억제제 및 이의 용도 |
WO2008014199A2 (en) * | 2006-07-28 | 2008-01-31 | Boehringer Ingelheim International Gmbh | Sulfonyl compounds which modulate the cb2 receptor |
US20080045560A1 (en) * | 2006-08-15 | 2008-02-21 | Wyeth | Pyrrolidine and related derivatives useful as PR modulators |
BRPI0718509A2 (pt) * | 2006-09-22 | 2015-09-29 | Novartis Ag | compostos orgânicos heterocíclicos |
WO2008050600A1 (fr) * | 2006-10-25 | 2008-05-02 | Neugen Pharma Inc. | Agent thérapeutique ou préventif pour des maladies réfractaires, basé sur la mort cellulaire induite par le stress oxydatif en tant que contexte moléculaire |
WO2008124000A2 (en) * | 2007-04-02 | 2008-10-16 | Ligand Pharmaceuticals Incorporated | Thiazole derivatives as androgen receptor modulator compounds |
WO2009011871A2 (en) | 2007-07-17 | 2009-01-22 | Amgen Inc. | Thiadiazole modulators of pkb |
WO2009011880A2 (en) | 2007-07-17 | 2009-01-22 | Amgen Inc. | Heterocyclic modulators of pkb |
EP2178865B1 (en) | 2007-07-19 | 2015-08-19 | Lundbeck, H., A/S | 5-membered heterocyclic amides and related compounds |
CA2699157A1 (en) | 2007-09-10 | 2009-03-19 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
JP2011507851A (ja) * | 2007-12-19 | 2011-03-10 | ザ スクリプス リサーチ インスティチュート | Rhoキナーゼインヒビターとしてのベンゾイミダゾールおよびアナログ |
PA8809001A1 (es) | 2007-12-20 | 2009-07-23 | Novartis Ag | Compuestos organicos |
CA2709918A1 (en) * | 2007-12-21 | 2009-06-25 | The Scripps Research Institute | Benzopyrans and analogs as rho kinase inhibitors |
JP2011507850A (ja) * | 2007-12-21 | 2011-03-10 | ザ スクリプス リサーチ インスティチュート | Rhoキナーゼインヒビターとしてのアニリドおよびアナログ |
EP2303852A4 (en) * | 2008-06-26 | 2011-12-28 | Glaxosmithkline Llc | ACTIVITY INHIBITORS AKT |
WO2009158373A1 (en) * | 2008-06-26 | 2009-12-30 | Smithkline Beecham Corporation | Inhibitors of akt activity |
GB0812648D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
DE102008035552A1 (de) * | 2008-07-30 | 2010-02-04 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Pyridine und ihre Verwendung |
AU2009288245B2 (en) | 2008-08-27 | 2012-12-20 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
US8524763B2 (en) | 2008-09-22 | 2013-09-03 | Calcimedica, Inc. | Inhibitors of store operated calcium release |
US20110263647A1 (en) | 2009-01-15 | 2011-10-27 | Amgen Inc. | Fluoroisoquinoline substituted thiazole compounds and methods of use |
CN102365277B (zh) | 2009-02-06 | 2015-11-25 | 伊兰药品公司 | Jun n-末端激酶抑制剂 |
US8785468B2 (en) | 2009-02-13 | 2014-07-22 | Amgen Inc. | Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions |
SG174398A1 (en) * | 2009-03-23 | 2011-10-28 | Glenmark Pharmaceuticals Sa | Furopyrimidinedione derivatives as trpa1 modulators |
UA107791C2 (en) | 2009-05-05 | 2015-02-25 | Dow Agrosciences Llc | Pesticidal compositions |
WO2010150927A1 (en) * | 2009-06-25 | 2010-12-29 | Sk Holdings Co., Ltd. | Pharmaceutical composition for prevention and treatment of cancer diseases comprising benzamide derivatives |
US8293753B2 (en) * | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
EP2477982A4 (en) | 2009-09-16 | 2013-04-03 | Calcimedica Inc | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM |
DE102009058280A1 (de) * | 2009-12-14 | 2011-06-16 | Merck Patent Gmbh | Thiazolderivate |
WO2011076732A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating gastrointestinal disorders |
WO2011076734A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases |
MX2012011784A (es) | 2010-04-16 | 2013-03-21 | Bayer Ip Gmbh | Nuevos compuestos heterociclicos como pesticidas. |
US9221808B2 (en) | 2010-04-16 | 2015-12-29 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinase (ROCK) and methods of use |
US9079891B2 (en) | 2010-08-27 | 2015-07-14 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
JP5990170B2 (ja) * | 2010-09-01 | 2016-09-07 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 除草活性を有するケトスルタム類及びジケトピリジン類 |
CN103619171B (zh) | 2010-11-03 | 2015-11-25 | 陶氏益农公司 | 杀虫组合物和与其相关的方法 |
CN104010505B (zh) | 2011-10-26 | 2017-03-15 | 陶氏益农公司 | 杀虫组合物和与其相关的方法 |
US9282739B2 (en) | 2012-04-27 | 2016-03-15 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
NZ700595A (en) | 2012-04-27 | 2016-04-29 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
US9708288B2 (en) | 2012-04-27 | 2017-07-18 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
US9512116B2 (en) | 2012-10-12 | 2016-12-06 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
WO2014060381A1 (de) * | 2012-10-18 | 2014-04-24 | Bayer Cropscience Ag | Heterocyclische verbindungen als schädlingsbekämpfungsmittel |
EP3016951B1 (en) | 2013-07-02 | 2017-05-31 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
EP3016950B1 (en) | 2013-07-02 | 2017-06-07 | Bristol-Myers Squibb Company | Tricyclic pyrido-carboxamide derivatives as rock inhibitors |
CN105636446B (zh) | 2013-10-17 | 2018-07-13 | 美国陶氏益农公司 | 制备杀虫化合物的方法 |
JP2016539092A (ja) | 2013-10-17 | 2016-12-15 | ダウ アグロサイエンシィズ エルエルシー | 有害生物防除性化合物の製造方法 |
KR20160074540A (ko) | 2013-10-17 | 2016-06-28 | 다우 아그로사이언시즈 엘엘씨 | 살충성 화합물의 제조 방법 |
MX2016004940A (es) | 2013-10-17 | 2016-06-28 | Dow Agrosciences Llc | Proceso para la preparacion de compuestos plaguicidas. |
CA2925914A1 (en) | 2013-10-17 | 2015-04-23 | Dow Agrosciences Llc | Processes for the preparation of pesticidal compounds |
MX2016004945A (es) | 2013-10-17 | 2016-06-28 | Dow Agrosciences Llc | Procesos para la preparacion de compuestos plaguicidas. |
CN105636440A (zh) | 2013-10-17 | 2016-06-01 | 美国陶氏益农公司 | 制备杀虫化合物的方法 |
EP3060051A4 (en) | 2013-10-22 | 2017-04-05 | Dow AgroSciences LLC | Synergistic pesticidal compositions and related methods |
AR098090A1 (es) | 2013-10-22 | 2016-05-04 | Dow Agrosciences Llc | Composiciones plaguicidas sinérgicas y métodos relacionados |
EP3060045A4 (en) | 2013-10-22 | 2017-04-05 | Dow AgroSciences LLC | Synergistic pesticidal compositions and related methods |
RU2016119360A (ru) | 2013-10-22 | 2017-11-28 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | Синергетические пестицидные композиции и связанные с ними способы |
WO2015061155A1 (en) | 2013-10-22 | 2015-04-30 | Dow Agrosciences Llc | Pesticidal compositions and related methods |
NZ719759A (en) | 2013-10-22 | 2017-05-26 | Dow Agrosciences Llc | Pesticidal compositions and related methods |
RU2016119560A (ru) | 2013-10-22 | 2017-11-28 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | Синергетические пестицидные композиции и относящиеся к ним способы |
CN108812681B (zh) | 2013-10-22 | 2021-02-26 | 美国陶氏益农公司 | 杀虫组合物和与其相关的方法 |
CA2926438A1 (en) | 2013-10-22 | 2015-04-30 | Dow Agrosciences Llc | Pesticidal compositions and related methods |
US9788545B2 (en) | 2013-10-22 | 2017-10-17 | Dow Agrosciences Llc | Synergistic pesticidal compositions and related methods |
RU2016119553A (ru) | 2013-10-22 | 2017-12-04 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | Синергетические пестицидные композиции и связанные с ними способы |
US9155304B2 (en) | 2013-10-22 | 2015-10-13 | Dow Agrosciences Llc | Synergistic pesticidal compositions and related methods |
TW201519777A (zh) | 2013-10-22 | 2015-06-01 | Dow Agrosciences Llc | 協同性殺蟲組成物及相關方法(九) |
CA2927206A1 (en) | 2013-10-22 | 2015-04-30 | Dow Agrosciences Llc | Synergistic pesticidal compositions and related methods |
RU2656391C2 (ru) | 2013-10-22 | 2018-06-05 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | Пестицидные композиции и связанные с ними способы |
RU2658995C2 (ru) | 2013-10-22 | 2018-06-26 | ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи | Пестицидные композиции и связанные с ними способы |
TW201519776A (zh) | 2013-10-22 | 2015-06-01 | Dow Agrosciences Llc | 協同性殺蟲組成物及相關方法(八) |
WO2015106272A1 (en) * | 2014-01-13 | 2015-07-16 | Harki Daniel A | Small molecule inhibitors of apobec3g and apobec3b |
GB201409624D0 (en) * | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
EP3174856A4 (en) | 2014-07-31 | 2018-01-10 | Dow AgroSciences LLC | Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine |
EP3186229A4 (en) | 2014-07-31 | 2018-01-10 | Dow AgroSciences LLC | Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine |
US9249122B1 (en) | 2014-07-31 | 2016-02-02 | Dow Agrosciences Llc | Process for the preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine |
BR112017002735A2 (pt) | 2014-08-19 | 2017-12-19 | Dow Agrosciences Llc | processo para a preparação de 3-(3-cloro-1h-pirazol-1-il)piridina |
CA2960985A1 (en) | 2014-09-12 | 2016-03-17 | Dow Agrosciences Llc | Process for the preparation of 3-(3-chloro-1h-pyrazol-1-yl)pyridine |
KR101726819B1 (ko) | 2014-10-27 | 2017-04-13 | 동아에스티 주식회사 | Gpr119 작용 활성을 갖는 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약제학적 조성물 |
EP3034500A1 (en) * | 2014-12-17 | 2016-06-22 | Genkyotex Sa | Amido thiazole derivatives as NADPH oxidase inhibitors |
WO2017023684A2 (en) * | 2015-07-31 | 2017-02-09 | Progenra, Inc. | Covalent irreversible inhibitors of usp7 as anti-cancer agents |
AU2017221707B2 (en) | 2016-02-16 | 2019-10-03 | Daegu-Gyeongbuk Medical Innovation Foundation | Novel 2,3,5-substituted thiophene compound as protein kinase inhibitor |
US10233155B2 (en) | 2016-12-29 | 2019-03-19 | Dow Agrosciences Llc | Processes for the preparation of pesticide compounds |
CN110139853B (zh) | 2016-12-29 | 2023-06-16 | 美国陶氏益农公司 | 用于制备杀有害生物化合物的方法 |
US11273154B2 (en) | 2017-03-03 | 2022-03-15 | Progenra, Inc. | Azole compounds as ubiquitin-specific protease USP7 inhibitors |
WO2018167103A1 (en) * | 2017-03-13 | 2018-09-20 | Genfit | Pharmaceutical compositions for combination therapy |
CN111032653A (zh) * | 2017-06-14 | 2020-04-17 | 欧洲分子生物学实验室 | 用于疗法的双环杂芳族酰胺化合物 |
EP3652164B1 (en) | 2017-07-12 | 2023-06-21 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
US11174253B2 (en) | 2017-08-02 | 2021-11-16 | Alphala Co., Ltd. | Compound and pharmaceutical composition containing the same |
IL291985A (en) | 2019-10-07 | 2022-06-01 | Kallyope Inc | gpr119 agonists |
MX2022008395A (es) * | 2020-01-07 | 2022-09-26 | Disarm Therapeutics Inc | Inhibidores de sarm1. |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9823871D0 (en) * | 1998-10-30 | 1998-12-23 | Pharmacia & Upjohn Spa | 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents |
GB9823873D0 (en) | 1998-10-30 | 1998-12-30 | Pharmacia & Upjohn Spa | 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents |
AU6471300A (en) * | 1999-08-06 | 2001-03-05 | Takeda Chemical Industries Ltd. | P38map kinase inhibitors |
SK4772002A3 (en) * | 1999-09-10 | 2002-11-06 | Merck & Co Inc | Tyrosine kinase inhibitors, pharmaceutical composition containing the same and their use |
JP2002053566A (ja) | 2000-08-11 | 2002-02-19 | Japan Tobacco Inc | チアゾール化合物及びその医薬用途 |
US20020173507A1 (en) * | 2000-08-15 | 2002-11-21 | Vincent Santora | Urea compounds and methods of uses |
ES2254611T3 (es) * | 2001-05-11 | 2006-06-16 | Pfizer Products Inc. | Derivados de tiazol. |
ES2274035T3 (es) * | 2001-06-01 | 2007-05-16 | Vertex Pharmaceuticals Incorporated | Compuestos de tiazol utiles como inhibidores de proteina quinasas. |
AR040123A1 (es) * | 2002-05-31 | 2005-03-16 | Upjohn Co | Compuestos tiofeno, antihelminticos e insecticidas |
-
2003
- 2003-10-30 AR ARP030103973A patent/AR043057A1/es unknown
- 2003-10-30 DE DE60332475T patent/DE60332475D1/de not_active Expired - Lifetime
- 2003-10-30 TW TW092130255A patent/TW200416221A/zh unknown
- 2003-10-30 MX MXPA05004689A patent/MXPA05004689A/es unknown
- 2003-10-30 EP EP03781448A patent/EP1558607B1/en not_active Expired - Lifetime
- 2003-10-30 WO PCT/US2003/034319 patent/WO2004041813A1/en active Application Filing
- 2003-10-30 AT AT03781448T patent/ATE466855T1/de not_active IP Right Cessation
- 2003-10-30 JP JP2005502202A patent/JP2006514684A/ja not_active Withdrawn
- 2003-10-30 US US10/696,862 patent/US20040122016A1/en not_active Abandoned
- 2003-10-30 NZ NZ540161A patent/NZ540161A/en unknown
- 2003-10-30 CA CA002504320A patent/CA2504320A1/en not_active Abandoned
- 2003-10-30 AU AU2003288956A patent/AU2003288956A1/en not_active Abandoned
- 2003-10-30 KR KR1020057007702A patent/KR20050088283A/ko not_active Application Discontinuation
-
2005
- 2005-05-30 NO NO20052595A patent/NO20052595L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
DE60332475D1 (de) | 2010-06-17 |
NO20052595D0 (no) | 2005-05-30 |
NO20052595L (no) | 2005-06-27 |
ATE466855T1 (de) | 2010-05-15 |
EP1558607A1 (en) | 2005-08-03 |
CA2504320A1 (en) | 2004-05-21 |
NZ540161A (en) | 2008-03-28 |
MXPA05004689A (es) | 2005-12-05 |
KR20050088283A (ko) | 2005-09-05 |
US20040122016A1 (en) | 2004-06-24 |
EP1558607B1 (en) | 2010-05-05 |
AU2003288956A1 (en) | 2004-06-07 |
JP2006514684A (ja) | 2006-05-11 |
WO2004041813A1 (en) | 2004-05-21 |
TW200416221A (en) | 2004-09-01 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR043057A1 (es) | Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa | |
AR040351A1 (es) | Derivados de quinuclidina-amida, composicion farmaceutica, procedimiento de preparacion del compuesto y su uso para fabricar medicamentos | |
RU2336275C2 (ru) | Пиримидопроизводные, характеризующиеся антипролиферативной активностью, и фармацевтическая композиция | |
AR119698A2 (es) | Compuesto amida n-urea sustituida derivado de aminoácido | |
AR040870A1 (es) | Compuestos inhibidores de proteinquinasas y composicion farmaceutica que los comprende | |
AR082152A1 (es) | Derivados de n-(metilsulfonil)benzamida, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de nav1.7 | |
AR055592A1 (es) | Derivados de 2-amino-5-cicloalquil-hidantoina como moduladores y/o inhibidores de la beta-secretasa(bace) | |
AR052943A1 (es) | Derivados de 2-(4-oxo-4h-quinazolin-3-il)acetamida | |
AR062270A1 (es) | Compuestos de heteroarilo inhibidores de enzimas de activacion e1, composiciones farmaceuticas que los contienen y usos en desordenes asociados a proliferacion celular,tales como canceres y trastornos inflamatorios. | |
AR050692A1 (es) | Derivados de triazolopiridinilsulfanilo como inhibidores de quinasa map p38; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por tnf o por p38 | |
AR083876A1 (es) | 5-halogenopirazolcarboxamidas | |
AR034264A1 (es) | Derivados azepino(4,5-b)indol sustituidos y composiciones farmaceuticas | |
AR050188A1 (es) | Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen | |
CO6290658A2 (es) | Derivados de azetidina y ciclobutano como inhibidores de jack | |
RU2008152180A (ru) | ПРОИЗВОДНЫЕ ПИРРОЛА, МОДУЛИРУЮЩИЕ АКТИВНОСТЬ CRTh2 РЕЦЕПТОРА | |
BRPI0512533A (pt) | carboxamidas indazol e seu uso | |
AR059428A1 (es) | Pirazoles para el tratamiento de enfermedades mediadas por la modulacion de los receptores de histamina h3 y una composicion farmaceutica que los comprende. | |
AR069045A1 (es) | Derivados de amina que tienen una actividad antagonista del receptor npy y5, y sus usos | |
AR100810A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
AR057525A1 (es) | Compuestos inhibidores selectivos de gsk3 y un proceso para su preparacion | |
AR055698A1 (es) | Tiazolidinonas metasustituidas, su preparacion y su uso como medicamento | |
RU2010101067A (ru) | Производное морфолина | |
AR087211A1 (es) | ANTAGONISTAS DE CRTh2 | |
EA202191040A1 (ru) | Производные флаваглина для ингибирования активации онкогена kras | |
AR089297A1 (es) | Uso de derivados de diamida antranilicos con sustituyentes heteroaromaticos y heterociclicos en combinacion con un agente de control biologico |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |