- BENZENESULFONAMIDE DERIVATIVES AND USES THEREOF
-
Provided herein are benzenesulfonamide derivatives having Formula (III), pharmaceutical compositions comprising said compounds, and method for using said compounds for disrupting proteins/polypeptides, protein/polypeptide function, and for the treatment of diseases through the disruption of proteins or polypeptides involved in the etiology of the disease. Said compounds comprise fluorinated benzene sulfonamide structures.
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Paragraph 00210
(2021/02/12)
-
- Preparation of key intermediate (by machine translation)
-
The invention belongs to the field of chemistry and relates to a preparation method of a key intermediate. The preparation method is simple in preparation steps, cheap and accessible in raw materials, free of precious metal reagents, and beneficial to industrial production. (by machine translation)
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Paragraph 0020-0021
(2020/09/12)
-
- Preparation method of precursor of ibrutinib
-
The invention relates to the pharmaceutical industry, in particular to a preparation method of a drug intermediate, and specifically discloses a preparation method of a precursor of ibrutinib. The preparation method comprises the following steps: (1) reacting a compound (III) with triphenylphosphine and azodicarbonic acid diester to obtain an intermediate (III-B); (2) reacting the intermediate (III-B) with a compound (IV) under the action of a catalyst to obtain an intermediate (V-C); and (3) reacting the intermediate (V-C) under the action of hydrochloric acid to obtain (R)-3-(4-phenoxy phenyl)-1-(piperidine-3-yl)-1H-pyrazolo [3, 4-d] pyrimidine-4-amine (I). The method has the advantages of high yield, high purity, convenience in purification, simplicity and convenience in operation and the like, is suitable for industrial production, and contributes to reducing the cost to a certain extent.
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Paragraph 0035; 0047-0049
(2020/04/22)
-
- 4 - Phenoxyphenyl pyrazolo pyrimidine amide derivatives and preparation method and application thereof (by machine translation)
-
The invention provides a preparation method and application of 4 -phenoxyphenyl pyrazolo pyrimidine amide derivatives. The compound has the structure shown in the formula (I). Wherein X and Y are two linking groups, X is selected from benzyl, substituted benzyl, piperidinyl and C. 1 -6 Straight-chain or branched alkyl; Y is-(CH)2 )n - N is any integer selected from 0-4; R is selected from hydroxyl, hydroxyl and phthalo; the structure of formula (I) contains its racemates and stereoisomers. The compound has BTK K K K/HDAC double-target inhibition effect and growth inhibitory activity on T-cell leukemia cells and cell lymphoma cells, and is used for preparing antitumor drugs. (by machine translation)
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Paragraph 0068; 0117; 0118
(2020/06/17)
-
- A PROCESS FOR PREPARATION OF 1H-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVES
-
The present invention relates to an efficient and industrially advantageous process for the preparation of 1H-pyrazolo[3,4-d] pyrimidine derivatives. In particular the present invention provides a process for the preparation of 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidine and tert-butyl (R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidin-1-yl)piperidine-1-carboxylate. Said compounds are important intermediates in the synthesis of ibrutinib. The method provided for preparing intermediates of ibrutinib has the advantages of a simple operation, high yield and low costs.
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Page/Page column 13-14
(2020/07/05)
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- Synthesis method of imatinib intermediate (by machine translation)
-
The invention provides a preparation method of (I) an imatinib intermediate body, namely 4 - the (II) preparation 3 - 3 - (4 -) - 4 - method of the imatinib intermediate body [3 comprises 4 the [3 d] following (III) steps: replacing-4-(I) amino-1H-pyrazolopyr-pyrazol 4 - d]. The synthesis route is novel, operation is simple, raw materials are cheap and easy to obtain, and large-scale amplification and industrial production are facilitated. (by machine translation)
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Paragraph 0036-0037
(2019/12/09)
-
- 1, 3-di-substituted-4-amino pyrazolopyrimidine compound, preparation method thereof and application of compound
-
The invention relates to a 1, 3-di-substituted-4-amino pyrazolopyrimidine compound, a preparation method thereof and an application of the compound. The compound is provided with a structure as shownin a formula I. The invention further relates to a preparation method of the compound with the structure as shown in the formula I and a medicine composition. The invention further provides an application of the compound and pharmaceutically acceptable salt thereof to preparation of MCL (mantle cell lymphoma) resistance medicines.
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Paragraph 0103; 0122-0123
(2019/03/08)
-
- Preparation of ibrutinib intermediate
-
The invention relates to preparation of an ibrutinib intermediate, in particular to preparation of 3-(4-phenoxyphenyl)-4-amino-1H-pyrazole[3,4-d]pyrimidine. According to the method, the reaction stepsare few and use of expensive reagents is avoided.
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Paragraph 0017-0018
(2019/01/23)
-
- Synthetic process of 3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine-4-amine
-
The invention discloses a synthetic process of 3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine-4-amine and belongs to the technical field of chemical synthesis of medicine. The synthetic process is characterized by including the steps of adding iodine, hydrogen peroxide, 4-aminopyrazolo[3,4-d]pyrimidine and a solid superacid gradually into acetic anhydride solution, and allowing reacting to obtain 3-iodo-4-aminopyrazolo[3,4-d]pyrimidine; dissolving the 3-iodo-4-aminopyrazolo[3,4-d]pyrimidine, 4-phenoxyphenylboronic acid and potassium phosphate in a mixed liquid of 1,4-dioxane and water, adding tetrakis(triphenylphosphine)palladium under argon protection, and allowing reacting to obtain 3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine-4-amine. The synthetic process has the advantages of mild reaction conditions, good operational convenience, controllable cost and high yield.
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Paragraph 0038; 0039
(2019/01/23)
-
- 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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- 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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- 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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- The compounds of structure containing conjugated zincon, its pharmaceutical composition and use thereof (by machine translation)
-
The present invention relates to compounds having a structure containing conjugated zincon, its pharmaceutical composition and use, and in particular relates to the general formula (I) or a salt thereof to the compound represented by the, pharmaceutical compositions thereof, and its as BTK inhibitors and/or B cell activation inhibitor, for the prevention or treatment B cell activity with abnormal and/or the use of the BTK-related diseases. The compounds of lymphoma, breast cancer, liver cancer, colon cancer, gastric cancer, such as lung cancer and cervical cancer cell has better lethal effect, note has potential for the treatment of cancer and self-immune diseases related to potential. (by machine translation)
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Paragraph 0231; 0234-0235
(2018/03/24)
-
- 1,2-DITHIOLANE COMPOUNDS USEFUL IN NEUROPROTECTION, AUTOIMMUNE AND CANCER DISEASES AND CONDITIONS
-
This invention provides confounds of the formula (I): wherein Y1, Y2 Z, X1, X2, and W are defined in the specification. These compounds are useful in the treatment of tyrosine kinases, MAPK signaling pathway kinases and Ρ13K/ΑΚΤ/mTor signaling pathway kinases-mediated diseases; or conditions, such as neurodegeneration, neuroprotection, cancer, autoimmune as well as other diseases and conditions associated with the modulation of tyrosine kinases selected from FYN, FYN Y531F, FLT3, FLT3 -ITD, BRK, ITK, FRK, BTK, BMX, SRC, FGR, YES1, LCK, HCK, RET, CSK, LYN, and ROSI; MAPK pathway kinases selected from ARAF, BRAE CRAP, ERK1 /2, MEK1, MEK2, MEK3, MEK4, MEK5. MEK6, and MEK7; and P13K/AKT/mTor pathway kinases: selected from mTor, P13K a, Ρ13Κ β, P13Kγ, and P13K δ.
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-
-
- Preparation method of Ibrutinib intermediate 4-amino-3-(4-phenoxy) phenyl-1H-pyrazol [3,4-d] pyrimidine
-
The invention relates to a preparation method of an Ibrutinib intermediate 4-amino-3-(4-phenoxy) phenyl-1H-pyrazol [3,4-d] pyrimidine. The method is characterized in that 4-phenoxybenzaldehyde is adopted as the original raw material; 4-phenoxybenzaldehyde and malononitrile achieve dehydration condensation, and 2-cyano-3-(4-phenoxy) phenyl acrylonitrile (II) is generated; 2-cyano-3-(4-phenoxy) phenyl acrylonitrile (II) and hydrazine hydrate achieve cyclization, and 5-amino-3-(4-phenoxy) phenyl-4-cyano-2,3-2h-pyrazole (III) is obtained; the compound III is subjected to formamide condensation and then is subjected to oxidation, and 4-amino-3-(4-phenoxy) phenyl-1H-pyrazol [3,4-d] pyrimidine (I) is obtained; or the compound III is firstly subjected to oxidation and then is subjected to formamide condensation, and the object compound is obtained. According to the preparation method, the utilized raw materials are low in price and easy to obtain, the one-pot method is adopted, reaction conditions are moderate, and the method is easy to operate, safe and environment-friendly in technology, good in reaction selectivity, high in product purity, low in cost, and suitable for industrial production.
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Paragraph 0056; 0057
(2017/05/16)
-
- 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 18; 19
(2017/10/13)
-
- 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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- Ibrutinib preparation method, ibrutinib intermediate, and ibrutinib intermediate preparation method
-
The present invention provides an ibrutinib preparation method, which comprises that (a) a compound (3) reacts with diethyl sulfate to obtain a compound (4); (b) the compound (4) reacts with a hydrazine dihydrochloride to obtain a compound (5); (c) the compound (5) reacts with formamide to obtain a compound (6); (d) after the compound (6) reacts with (R)-1-Boc-3-hydroxypiperidine, an acid is added to make a compound (7) be subjected to a deprotection reaction to obtain a compound (8); and (e) the compound (8) reacts with acryloyl chloride to obtain a compound (9) ibrutinib. The present invention further provides an ibrutinib intermediate represented by a formula (4) and a preparation method of the intermediate compound (8). According to the present invention, the method has advantages of low cost, good safety and high yield, and is suitable for large-scale production. The reaction route is defined in the specification.
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- 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:
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-
-
- Preparation method for ibrutinib
-
The invention discloses a preparation method for ibrutinib and belongs to the technical field of drug synthesis. The preparation method specifically includes the steps that 3-amino-4-cyano pyrazol and formamidine acetate serve as initial raw materials, and ibrutinib is obtained through a cyclization reaction, a halogenating reaction, a nucleophilic substitution reaction, a Mitsunobu reaction and an amidation reaction. According to the method, the raw materials are easy to obtain, conditions are mild, the process operability and controllability are high, cost is low, the yield is high, fewer side products are generated, purification is easy, and the high-quality product is obtained.
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Paragraph 0053
(2016/10/10)
-
- Method for synthesizing ibrutinib
-
The invention provides a method for synthesizing ibrutinib. The method takes 4,6-dihydroxypyrimidine as an initial raw material, the material is subjected to formylation and chlorination to obtain a compound in a formula 3; the compound in the formula 3 and a compound in a formula 4 are subjected to a reaction to obtain a compound in a formula 5; the compound in the formula 5 is subjected to oxidation to obtain a compound in a formula 6; the compound in the formula 6 is subjected to ammonification to obtain a compound in a formula 7; the compound in the formula 7 and hydrazine hydrate are subjected to a reaction for closing pyrazole ring to obtain a compound in a formula 8; the compound in the formula 8 and a compound in a formula 9 are subjected to an alkylation reaction to obtain a compound in a formula 10; the compound in the formula 10 is subjected to acid deprotection to obtain a compound in a formula 11; and the compound in the formula 11 and acryloyl chloride are subjected to the reaction to obtain ibrutinib. The invention also discloses an ibrutinib intermediate. The raw materials have the advantages of low cost and easy acquisition, no dangerous highly-toxic product, mild reaction condition, no requirement of cryogenic cooling and high temperature, and simple operation, and is suitable for industrial production.
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-
- SYNTHESIS OF SUBSTITUTED 1H-PYRAZOLO[3,4-D]PYRIMIDINES
-
The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H- pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-l-yl)prop-2-en-l-one(ibrutinib) and its synthesis intermediates.
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- IBRUTINIB INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
-
The present invention relates to the technical field of ibrutinib, particularly to the technical field of ibrutinib intermediate compounds and preparation methods thereof. The intermediate compounds are represented by formula (A), wherein, the dotted line represents a double bond or a single bond between carbon and oxygen.
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- BTK inhibitor and uses thereof
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The present invention provides a BTK inhibitor compound (having s structure represented by a formula (I)) and uses of the BTK inhibitor compound in medicines. According to the present invention, the compound and the pharmaceutical composition can be used for treatment of diffuse large B-cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. The formula (I) is defined in the specification.
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- Double-site non-reversible brewton tyrosine kinase inhibitors
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The invention provides a double-site irreversible Brutons tyrosine kinase inhibitor, a drug combination containing the same and application thereof to the anti-tumor field. The compound provided by the invention has an anti-proliferation inhibiting effect to tumor cell stains such as A549, SGC7901, MCF-7, PC-9 and HL-60, and can be applied to drugs for treating solid tumors or blood cancers related to human or animal cell proliferation; the compound provided by the invention has a better pharmacokinetic property and can be applied to treating solid tumors or blood cancers related to human or animal cell proliferation or autoimmune diseases through oral taking; the compound provided by the invention has a double-site response characteristic.
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Paragraph 0046; 0047; 0048; 0049
(2016/11/24)
-
- 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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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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Described herein are compounds and their applications with Bruton's tyrosine kinase inhibitory activity. The described compounds comprise at least a compound of Formula (I), or pharmaceutically acceptable salts thereof. Also described herein are methods for synthesizing such compounds, and their applications in the treatment of diseases: autoimmune diseases or conditions associated with aberrant B-cell proliferation such as rheumatoid arthritis, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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-
- Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: A comparative study
-
Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) and has been approved for the treatment of haematological malignancies, such as chronic lymphocytic leukaemia, mantle cell lymphoma and Waldenstr?m's macroglobulinemia. The covalent and irreversible nature of its molecular mode of action allows identification and monitoring of its target in an activity-based protein profiling (ABPP) setting. Fluorescent and biotinylated ibrutinib derivatives have appeared in the literature in recent years to monitor BTK in vitro and in situ. The work described here complements this existing methodology and pertains a comparative study on the efficacy of direct and two-step bioorthogonal ABPP of BTK.
- Liu, Nora,Hoogendoorn, Sascha,Van De Kar, Bas,Kaptein, Allard,Barf, Tjeerd,Driessen, Christoph,Filippov, Dmitri V.,Van Der Marel, Gijsbert A.,Van Der Stelt, Mario,Overkleeft, Herman S.
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p. 5147 - 5157
(2015/05/13)
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- Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia
-
FLT3-ITD mutant has been observed in about 30% of AML patients and extensively studied as a drug discovery target. On the basis of the structure of PCI-32765 (ibrutinib), a BTK kinase inhibitor that was recently reported to bear FLT3 kinase activity through a structure-guided drug design approach, we have discovered compound 18 (CHMFL-FLT3-122), which displayed an IC50 of 40 nM against FLT3 kinase and achieved selectivity over BTK kinase (over 10-fold). It significantly inhibited the proliferation of FLT3-ITD positive AML cancer cell lines MV4-11 (GI50 = 22 nM), MOLM13/14 (GI50 = 21 nM/42 nM). More importantly, 18 demonstrated 170-fold selectivity between FLT3 kinase and c-KIT kinase (GI50 = 11 nM versus 1900 nM) in the TEL-fusion isogenic BaF3 cells indicating a potential to avoid the FLT3/c-KIT dual inhibition induced myelosuppression toxicity. In the cellular context it strongly affected FLT3-ITD mediated signaling pathways and induced apoptosis by arresting the cell cycle into the G0/G1 phase. In the in vivo studies 18 demonstrated a good bioavailability (30%) and significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model (50 mg/kg) without exhibiting obvious toxicity. Compound 18 might be a potential drug candidate for FLT3-ITD positive AML.
- Li, Xixiang,Wang, Aoli,Yu, Kailin,Qi, Ziping,Chen, Cheng,Wang, Wenchao,Hu, Chen,Wu, Hong,Wu, Jiaxin,Zhao, Zheng,Liu, Juan,Zou, Fengming,Wang, Li,Wang, Beilei,Wang, Wei,Zhang, Shanchun,Liu, Jing,Liu, Qingsong
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p. 9625 - 9638
(2016/01/12)
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- DEUTERATED IBRUTINIB
-
The present invention in one embodiment provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula (I) are as defined in the specification.
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- HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS
-
The present invention encompasses compounds of the formula (I) wherein the groups X and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
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- INHIBITORS OF THE IRE-1/XBP-1 PATHWAY AND METHODS OF USING THEREOF
-
Disclosed are XBP-1/IRE-1 inhibitors having formula disclosed herein. Methods of making and using these inhibitors for the treatment of cancer, in particular B cell cancers, are also disclosed. Also disclosed is a genetic XBP-1 -knockout cancer mouse model. In still further aspects, the disclosed subject matter relates to methods for treating oncological and inflammatory disorders in a patient. For example, disclosed herein are methods whereby an effective amount of a compound or composition disclosed herein is administered to a patient having an oncological disorder, for example B-cell chronic lymphocytic leukemia (CLL), and who is in need of treatment thereof. XBP-1 deficiency causes leukemic cells to acquire phenotypes that are disadvantageous for their survival, such as compromised BCR signaling capability and increased surface expression of S1 P1.
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- 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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- 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.
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- CYCLIC MOLECULES AS BRUTON'S TYROSINE KINASE INHIBITORS
-
The present document describes novel molecules having protein tyrosine kinase inhibitory activity, and methods of synthesizing and using such compounds. More specifically, the present document describes compound of Formula (A): (Formula (A)) or a pharmaceutically acceptable salt, hydrate or solvate thereof, and methods of synthesizing and using such compounds.
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Paragraph 00128; 00129
(2013/08/15)
-
- PROTEIN KINASE INHIBITORS AND METHODS OF TREATMENT
-
The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
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- Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
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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 11-12
(2008/12/08)
-
- Kinase antagonists
-
The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.
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Page/Page column 25
(2008/06/13)
-