cas 170011-57-1, 4-P-AMINOPHENYL-1-BOC-PIPERIDINE

Articles about 170011-57-1Total 29 be found

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WEE1 inhibitors as well as preparation and application thereof
The invention relates to WEE1 inhibitors as well as preparation and application thereof. The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates, polymorphs or isomers thereof, and their use in the preparation of medicaments for the treatment of diseases associated with WEE1 activity.
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(2020/10/14)

POSITRON EMISSION TOMOGRAPHY (PET) RADIOTRACERS FOR IMAGING MACROPHAGE COLONY-STIMULATING FACTOR 1 RECEPTOR (CSF1R) IN NEUROINFLAMMATION
Positron emission tomography (PET) radiotracers for imaging macrophage colony stimulating factor-1 receptors in a subject afflicted with or suspected of being afflicted with a neuroinflammatory or neurodegenerative disease or disorder are disclosed.
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(2020/01/24)

HETEROCYCLIC COMPOUNDS AND USES THEREOF
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
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(2019/04/25)

N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
Provided herein are certain substituted N-aryl and N-heteroaryl piperidine compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R 6 are as defined. The said novel compounds, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory disease and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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(2018/04/27)

PHARMACEUTICAL COMPOUND
Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.
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(2017/01/26)

Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character
The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.
Campbell, Peter S.,Jamieson, Craig,Simpson, Iain,Watson, Allan J. B.
p. 46 - 49
(2017/12/27)

Imidazole derivatives, its pharmaceutical composition and use thereof
Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
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Paragraph 0544-0546

(2017/02/24)

PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS
The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.
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(2015/07/07)

FLT3 INHIBITORS AND USES THEREOF
The present invention provides methods of using compounds of formula I: or compositions thereof for the inhibition of FLT3, and the treatment of FLT3-mediated disorders.
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(2014/12/12)

CDK8 INHIBITORS AND USES THEREOF
The present invention provides methods of using compounds of formula I: and compositions thereof for the inhibition of CDK8, and the treatment of CDK8-mediated disorders.
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(2014/12/12)

IRAK INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 0374

(2014/07/22)

FAK AND FLT3 INHIBITORS
The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
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(2014/03/22)

IMIDAZOPYRAZINE SYK INHIBITORS
Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suf-fering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or dis-order are provided.
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(2014/01/08)

8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER
Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.
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Paragraph 00532

(2013/04/10)

FAK INHIBITORS
A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
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(2012/09/10)

Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N -[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1 H -imidazole-2-carboxamide (JNJ-28312141)
A class of potent inhibitors of colony-stimulating factor-1 receptor (CSF-1R or FMS), as exemplified by 8 and 21, was optimized to improve pharmacokinetic and pharmacodynamic properties and potential toxicological liabilities. Early stage absorption, distribution, metabolism, and excretion assays were employed to ensure the incorporation of druglike properties resulting in the selection of several compounds with good activity in a pharmacodynamic screening assay in mice. Further investigation, utilizing the type II collagen-induced arthritis model in mice, culminated in the selection of anti-inflammatory development candidate JNJ-28312141 (23, FMS IC50 = 0.69 nM, cell assay IC50 = 2.6 nM). Compound 23 also demonstrated efficacy in rat adjuvant and streptococcal cell wall-induced models of arthritis and has entered phase I clinical trials.
Illig, Carl R.,Manthey, Carl L.,Wall, Mark J.,Meegalla, Sanath K.,Chen, Jinsheng,Wilson, Kenneth J.,Ballentine, Shelley K.,Desjarlais, Renee L.,Schubert, Carsten,Crysler, Carl S.,Chen, Yanmin,Molloy, Christopher J.,Chaikin, Margery A.,Donatelli, Robert R.,Yurkow, Edward,Zhou, Zhao,Player, Mark R.,Tomczuk, Bruce E.
p. 7860 - 7883
(2012/01/05)

PYRAZOLE DERIVATIVES AS ANTI-PLATELET AND ANTI-THROMBOTIC AGENTS
This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.
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Page/Page column 59-60

(2010/11/30)

METHOD OF INHIBITING C-KIT KINASE
A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
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Page/Page column 41

(2008/06/13)

5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, R101 and R200 are described in the specification.
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Page/Page column 90

(2008/12/05)

Structure-based optimization of a potent class of arylamide FMS inhibitors
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based modeling provided the framework to efficiently effect this transformation and restore potencies to previous levels. This optimization removed a risk factor for potential idiosyncratic drug reactions.
Meegalla, Sanath K.,Wall, Mark J.,Chen, Jinsheng,Wilson, Kenneth J.,Ballentine, Shelley K.,DesJarlais, Renee L.,Schubert, Carsten,Crysler, Carl S.,Chen, Yanmin,Molloy, Christopher J.,Chaikin, Margery A.,Manthey, Carl L.,Player, Mark R.,Tomczuk, Bruce E.,Illig, Carl R.
scheme or table
p. 3632 - 3637
(2009/04/06)

UREA DERIVATIVE
The present invention relates to a urea derivative or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect. A urea derivative having the formula: [wherein R 1 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; R 2 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; E is a group having the formula (II) or the formula (III) (wherein R 3 is a hydrogen atom or others; R 4 and R 5 , which are the same or different, are a hydrogen atom or others; X and U, which are the same or different, are a group represented by the formula CH or others; m and n, which are the same or different, are 1 or another number) or others; and A is a group represented by the formula -NH-C(=O)- or others], or a pharmacologically acceptable salt thereof.
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Page/Page column 87; 165

(2010/11/26)

THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].
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Page/Page column 27

(2008/06/13)

5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.
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Page/Page column 53

(2010/11/26)

METHOD OF INHIBITING FLT3 KINASE
A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
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Page/Page column 76

(2010/11/27)

BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES
The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.
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Page/Page column 189

(2008/06/13)

INHIBITORS OF C-FMS KINASE
The invention is directed to compounds of Formula (I): wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
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Page/Page column 58-59

(2008/06/13)

SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR
The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
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Page/Page column 55

(2008/06/13)

QUINOLINE- AND ISOQUINOLINE-BASED COMPOUNDS EXHIBITING ATP-UTILIZING ENZYME INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF
Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.
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Page/Page column 74

(2008/06/13)

Oxazolidinone derivatives
The present invention relates to compounds of the formula: STR1 wherein R is H or alkyl; Y1 is --CH= or --N=; and Y2 --CH=, --C(OH)=, --C(NO2)=, --C(NH2)=, --C(Hal)=, --N=; X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, optionally substituted by phenyl-2-oxo-5 -methoxymethyl-oxazolidinyl; bicyclo[2.2.1]-hept-5 -en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally substituted by amino, alkyl, --CN, oxo hydroxyimino, ethylenedioxy or by --OR1, R1 is --CH(C6 H5)2, --(CH2)n C6 H5, alkyl, H, --(CH2)n NHCOCH3, --(CH2)n NH2, --(CH2)n CN, --(CH2)n SCH3 --(CH2)n SO2 CH3, --CO-lower-alkyl, --COC6 H5, optionally substituted by oxazolidine; or by =CR2 R3, R2 is alkyl R3 is H, --CN, alkyl, phenyl or COO-alkyl; or by --(CH2)n R4 R4 is --CN, amino, --NHCOCH3, --COC6 H5 Hal, phenyl or hydroxy; or by --COR5, R5 is alkyl, --CH=CH--C6 H5, --C6 H5, --C6 H5 CF3 or --O-alkyl; or by --NR6 R7, R6 is or --COCH3 ; R7 is --COCH3, benzyl or --(CH2)n NHCOC6 H4 Hal; and n is 1-3; These can be used for the prevention or control of depressive, panic and anxiety states, and treatment of certain cognitive disorders and neurodegenerative diseases.
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(2008/06/13)