- PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR
-
Disclosed is a process for the preparation of certain intermediates, e.g. process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof, in an enantioenriched form, which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
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Page/Page column 23; 24
(2020/12/07)
-
- Catalytic Azido-Hydrazination of Alkenes Enabled by Visible Light: Mechanistic Studies and Synthetic Applications
-
A visible-light-enabled catalytic intermolecular azido-hydrazination method for unactivated alkenes is developed via an orderly radical addition sequence. This transformation features metal-free and redox-neutral conditions and is applicable to a wide range of alkenes with commercially available reagents. Mechanistic and kinetic studies reveal that the efficient generation of azide radical enabled by fluorenone under visible-light is critical to this methodology. The β-azido alkyl hydrazines prepared with this reaction can be conveniently derived to valuable synthetic building blocks, and one of the products has been successfully applied in the total synthesis of (±)-ibrutinib, which is used to treat B cell cancers. (Figure presented.).
- Wang, Peng,Luo, Yunxuan,Zhu, Songsong,Lu, Dengfu,Gong, Yuefa
-
supporting information
p. 5565 - 5575
(2019/11/14)
-
- TREATMENT OF INDOLENT OR AGGRESSIVE B-CELL LYMPHOMAS USING A COMBINATION COMPRISING BTK INHIBITORS
-
Disclosed herein is a method for the prevention, delay of progression or treatment of indolent or aggressive B-cell lymphomas in an individual in need thereof, comprising administering a Btk inhibitor (in particularly (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof) in combination with an anti-PD-1 antibody. The potent and selective BTK inhibitor in combination with the anti-PD-1 antibody have a manageable toxicity profile in patients with indolent and aggressive lymphomas.
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Paragraph 0106
(2019/06/17)
-
- Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor
-
Therapeutic combinations of a proteasome inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a proteasome inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
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Paragraph 0465-0467
(2019/07/23)
-
- A according to lu tini and its key intermediate for the preparation of the new method (by machine translation)
-
The invention relates to a according to lu tini and its key intermediate for the preparation of the new method, the existing synthetic process avoids the more stringent reaction conditions, and the expensive starting material and reagent. The oxide by a one-pot reaction synthesis of key intermediate, simplified post-processing operation is relatively complex, and the cost is reduced. The obtained intermediate purity of 99% or more, the yield is higher, the operation is simple, and is suitable for industrial production. (by machine translation)
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Paragraph 0014
(2018/03/26)
-
- Method for preparing ibrutinib
-
The invention discloses a method for preparing ibrutinib. The method includes the following steps of 1, preparation of IB-A, 2, preparation of IB-B, 3, preparation of IB-C, 4, preparation of IB-D, 5,preparation of IB-E, 6, preparation of IB-F, 7, preparation of IB-G, 8, preparation of IB-H, and 9, preparation of IB-J. The method has the advantages that the process is mature and stable, the quality of the product is stable, the production process is safe and reliable, and the ibrutinib is suitable for industrial production.
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-
Paragraph 0049-0052; 0090; 0128
(2018/03/26)
-
- Ibrutinib intermediate and preparation method thereof
-
The invention discloses an ibrutinib intermediate and a preparation method thereof. The structure of the ibrutinib intermediate provided by the invention is shown as a formula I; the definition of R is shown as a specification and a claim. The ibrutinib intermediate can be used for preparing an ibrutinib key intermediate of 3-(4-phenoxyl phenyl)-1H-parazole[3,4-d]pyrimidine-4-amine; the preparation method comprises the steps of preparing an active intermediate of a compound shown as a formula II from a compound shown as a formula I under the effect of active nucleophilic reagents; cyclizing the compound shown as the formula II to obtain a compound 3-amino-5-(4-phenoxyl phenyl)-4-cyan-1H-parazole shown as a formula 4; performing ring closing on the compound shown as the formula 4 to obtainthe ibrutinib key intermediate. The method has the advantages that the raw materials are cheap and can be easily obtained; the use of dangerous reagents is not needed; the reaction conditions are mild; the operation is simple; the method is suitable for industrial production. (The formulas are shown in the description.).
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-
Paragraph 0092; 0111-0113
(2018/11/22)
-
- USE OF A COMBINATION COMPRISING A BTK INHIBITOR FOR TREATING CANCERS
-
A method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent. A pharmaceutical combination comprising a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent.
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Paragraph 0100
(2018/03/09)
-
- CRYSTALLINE FORM OF (S)-7-(1-ACRYLOYLPIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF
-
The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
- -
-
Paragraph 0055; 0091; 0092
(2018/08/19)
-
- CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF
-
The present invention relates to a crystalline form of (S) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahydropyrazolo [1, 5-a] pyri midine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
- -
-
Paragraph 00133; 00134
(2018/09/08)
-
- Methods of Using BTK Inhibitors to Treat Dermatoses
-
In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat dermatoses, such as psoriasis, atopic dermatitis, contact dermatitis, scleroderma, and cutaneous lupus erythematosus. In other embodiments, the methods of the invention further comprise the step of administering a therapeutically effective dose of an anti-inflammatory agent.
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Paragraph 0421-0423
(2018/11/26)
-
- PROCESS FOR THE SYNTHESIS OF STABLE AMORPHOUS IBRUTINIB
-
Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.
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Page/Page column 16
(2017/09/05)
-
- INHIBITOR OF BRUTON'S TYROSINE KINASE
-
Provided are a compound represented by formula (III) or pharmaceutically acceptable salts, solvates, active metabolites, polymorphs, esters, tautomers or prodrugs thereof, pharmaceutical compositions containing the compound represented by formula (III), and the application of the pharmaceutical compositions as selective inreversible inhibitor of Bruton's tyrosine kinase for the prevention and treatment of inflammation, autoimmune diseases (such as rheumatoid arthritis) associated with aberrant B cell proliferation and cancers.
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-
Paragraph 027; 0128; 0129
(2017/03/28)
-
- PROCESS FOR PREPARING PURE LH-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVE
-
The present invention relates to an efficient and industrially advantageous process for the preparation of pure lH-pyrazolo[3,4-d] pyrimidine derivative. In particular the present invention provides a process for the preparation of pure 4-amino-3-(4- phenoxyphenyl)-lH-pyrazolo[3,4-d] pyrimidine, a key intermediate of ibrutinib. Particularly, the present invention provides a process for the preparation of 3-amino-4-cyano-5-(4-phenoxy phenyl)pyrazole, wherein none of the intermediates have been isolated, an important precursor for the preparation of 4-amino-3-(4-phenoxyphenyl)- lH-pyrazolo[3,4-d] pyrimidine.
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Page/Page column 16
(2017/10/13)
-
- FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.
- -
-
Paragraph 0169; 0170; 0171
(2018/06/26)
-
- THERAPEUTIC COMBINATIONS OF A CD19 INHIBITOR AND A BTK INHIBITOR
-
Therapeutic combinations of a CD 19 inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a CD 19 inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer, such as a hematological malignancy. A combination of a BTK inhibitor and a CD 19 inhibitor, such as a CD19-targeted antibody or a CD19-targeted chimeric antigen receptor expressing T cell or NK cell, and compositions and uses thereof are disclosed. Combinations of a BTK inhibitor and a CD 19 inhibitor with a programmed death- 1 (PD-1) or PD-1 ligand (PD-L1) inhibitor and compositions and uses thereof are also disclosed.
- -
-
Paragraph 00409-00411
(2017/04/08)
-
- Therapeutic Combinations of an IRAK4 Inhibitor and a BTK Inhibitor
-
Therapeutic combinations of an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of an IRAK4 inhibitor and a BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
- -
-
Paragraph 0538; 0539; 0540
(2017/06/12)
-
- BTK INHIBITORS TO TREAT SOLID TUMORS THROUGH MODULATION OF THE TUMOR MICROENVIRONMENT
-
In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.
- -
-
Paragraph 00261
(2016/02/29)
-
- THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR AND/OR A CDK 4/6 INHIBITOR
-
Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms (PI3K-γ,δ, PI3K-γ, and PI3K-δ, a Janus kinase-2 (JAK-2) inhibitor, a cyclin-dependent kinase- 4/6 (CDK4/6) inhibitor, and/or a Bruton's tyrosine kinase (BTK) inhibitor are described. In certain embodiments, the invention includes therapeutic combinations of a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor and a BTK inhibitor, a PI3K-δ inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a JAK-2, PI3K-δ, and BTK inhibitor.
- -
-
Paragraph 00558
(2016/02/29)
-
- THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR, A JAK-2 INHIBITOR, AND/OR A BCL-2 INHIBITOR
-
Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms (PI3K-γ,δ, PI3K-γ, and PI3K-δ), a Janus kinase-2 (JAK-2) inhibitor, a Bruton's tyrosine kinase (BTK) inhibitor, and/or a B-cell lymphoma-2 (BCL-2) inhibitor are described. In some embodiments, the invention provides therapeutic combinations of a PI3K-δ inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a BCL-2 and BTK inhibitor.
- -
-
Paragraph 00527
(2016/02/29)
-
- METHODS OF TREATING CANCERS, IMMUNE AND AUTOIMMUNE DISEASES, AND INFLAMMATORY DISEASES BASED ON BTK OCCUPANCY AND BTK RESYNTHESIS RATE
-
In an embodiment, therapeutic methods and use of a Bruton's Tyrosine Kinase (BTK) inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described. In an embodiment, dosing regimens for a BTK inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described.
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Page/Page column 00222-00224
(2016/04/20)
-
- PROCESS FOR THE PREPARATION OF 1-[(3R)-3-[4-AMINO-3-(4-PHENOXYPHENVL)-1H- PVRAZOLO[3,4-D]PYRINIIDIN-1-Y1]-1-PIPERIDINVL]-2-PROPEN-1-ONE AND ITS POLYMORPHS THEREOF
-
The present invention relates to an improved process for the preparation of 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)- 1 H-pyrazolo[3,4-d]pyrimidin- 1 -yl]- 1 -piperidin yl]-2-propen-1-one compound of formula- 1 and its polymorphs thereof, which is represented by the following structural formula:
- -
-
Page/Page column 29; 30
(2016/11/14)
-
- Protein Kinase Inhibitors and Uses Thereof
-
The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
- -
-
Paragraph 0128; 0129; 0130
(2015/02/05)
-
- Inhibitors of Bruton'S tyrosine kinase for the treatment of solid tumors
-
Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.
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-
Page/Page column 111-112
(2015/09/22)
-
- METHODS OF BLOCKING THE CXCR-4/SDF-1 SIGNALING PATHWAY WITH INHIBITORS OF BRUTON'S TYROSINE KINASE
-
In some embodiments, the present invention relates to novel small molecule inhibitors that block the CXCR4-SDF-1 signaling pathway by directly inhibiting members of the Tec family of kinases, namely Bruton's tyrosine kinase (BTK), and their use in treating diseases in which pathogenesis is mediated by the CXCR4/SDF-1 signaling pathway.
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Page/Page column 00159; 00161
(2015/12/18)
-
- METHODS OF BLOCKING THE CXCR-4/SDF-1 SIGNALING PATHWAY WITH INHIBITORS OF BONE MARROW X KINASE
-
In some embodiments, the present invention relates to novel small molecule inhibitors that block the CXCR4-SDF-1 signaling pathway by directly inhibiting members of the Tec family of kinases, namely bone marrow X kinase (BMX) (also known as epithelial and endothelial tyrosine kinase (ETK)), and their use in treating diseases in which pathogenesis is mediated by the CXCR4/SDF-1 signaling pathway.
- -
-
Paragraph 00160
(2015/12/30)
-
- THERAPEUTIC COMBINATIONS OF A BTK INHIBITOR, A PI3K INHIBITOR AND/OR A JAK-2 INHIBITOR
-
Therapeutic combinations of a Janus kinase-2 (JAK-2) inhibitor, a Bruton's tyrosine kinase (BTK) inhibitor, and/or a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms, are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of (1) a ΡΙ3Κ-δ inhibitor and a BTK inhibitor, (2) a JAK-2 inhibitor and a BTK inhibitor, or (3) a JAK-2 inhibitor, ΡΙ3Κ-δ inhibitor, and BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
- -
-
Paragraph 00453-00454
(2016/04/26)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE
-
The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans. Formula (IV)
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-
Paragraph 0379; 0385
(2014/06/23)
-
- BRUTON'S TYROSINE KINASE INHIBITORS
-
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
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Page/Page column 74
(2014/05/24)
-
- FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
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-
Paragraph 0167-0171
(2014/11/13)
-
- Methods and Compositions for Inhibition of Bone Resorption
-
Disclosed herein are methods and compounds for inhibiting bone and/or cartilage resorption in an individual. The methods comprise administering to the individual a composition comprising a therapeutically effective amount of a compound that is an irreversible inhibitor of a Bruton's tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. Also described are irreversible inhibitors of Btk and methods for the preparation of the compounds. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the inhibition of cancer metastasis, and for inhibition of bone or cartilage resorption in cancer patients.
- -
-
Paragraph 0549
(2013/07/19)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE
-
Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
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-
Paragraph 00363
(2013/03/26)
-
- Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR
-
We have described the synthesis, enzyme inhibitory activity, structure-activity relationships, and proposed binding mode of a novel series of pyrrole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC50s 10 nM) for Lck kinase inhibition.
- Takayama, Tetsuo,Umemiya, Hiroki,Amada, Hideaki,Yabuuchi, Tetsuya,Shiozawa, Fumiyasu,Katakai, Hironori,Takaoka, Akiko,Yamaguchi, Akie,Endo, Mayumi,Sato, Masakazu
-
scheme or table
p. 108 - 111
(2010/03/30)
-
- Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR
-
We have identified a novel series of ring-fused pyrazole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC50s 50s 1 nM).
- Takayama, Tetsuo,Umemiya, Hiroki,Amada, Hideaki,Yabuuchi, Tetsuya,Koami, Takeshi,Shiozawa, Fumiyasu,Oka, Yusuke,Takaoka, Akiko,Yamaguchi, Akie,Endo, Mayumi,Sato, Masakazu
-
scheme or table
p. 112 - 116
(2010/04/02)
-
- Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
-
Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
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-
Page/Page column 37
(2010/06/11)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE
-
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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-
Page/Page column 58
(2008/06/13)
-
- BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING
-
Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.
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Page/Page column 11
(2008/12/08)
-
- Pyrazolopyrimidines as therapeutic agents
-
The present invention is directed to pyrazolopyrimidine derivatives of formula (I) wherein the substituents are defined herein, which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.
- -
-
-
- Pyrazolopyrimidines as therapeutic agents
-
The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
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-
-