- A synthetic method of ibutinib
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The present invention provides a preparation method of ibutinib and its application, by optimizing the feeding ratio and reaction conditions, increasing the purification step of the intermediate, and the use of inorganic alkali instead of organic base as an acid binding agent, significantly reducing the impurity content of ibutinib synthetic intermediates and final products, especially the content of isomer impurities, to ensure the quality of drugs and clinical drug safety provides a strong guarantee.
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- Preparation method of ibrutinib intermediate
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The invention relates to a preparation method of ibrutinib and an intermediate thereof, belonging to the field of medicinal chemistry. According to the preparation method, ibrutinib can be obtained through condensation, cyclization, substitution, Suzuki reaction and acylation reaction by taking a low-cost material flow as a starting material. The method is low in cost, free of light delay reaction, high in yield, good in selectivity, short in route, few in generated three wastes and suitable for industrial large-scale production.
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Paragraph 0097-0099
(2021/08/06)
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- A Cleavable C2-Symmetric trans-Cyclooctene Enables Fast and Complete Bioorthogonal Disassembly of Molecular Probes
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Bioorthogonal chemistry is bridging the divide between static chemical connectivity and the dynamic physiologic regulation of molecular state, enabling in situ transformations that drive multiple technologies. In spite of maturing mechanistic understanding and new bioorthogonal bond-cleavage reactions, the broader goal of molecular ON/OFF control has been limited by the inability of existing systems to achieve both fast (i.e., seconds to minutes, not hours) and complete (i.e., >99%) cleavage. To attain the stringent performance characteristics needed for high fidelity molecular inactivation, we have designed and synthesized a new C2-symmetric trans-cyclooctene linker (C2TCO) that exhibits excellent biological stability and can be rapidly and completely cleaved with functionalized alkyl-, aryl-, and H-tetrazines, irrespective of click orientation. By incorporation of C2TCO into fluorescent molecular probes, we demonstrate highly efficient extracellular and intracellular bioorthogonal disassembly via omnidirectional tetrazine-triggered cleavage.
- Carlson, Jonathan C. T.,Haider, Maximilian,Herrmann, Barbara,Klubnick, Jenna,Mikula, Hannes,Sohr, Barbara,Weissleder, Ralph,Wilkovitsch, Martin
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supporting information
p. 19132 - 19141
(2020/11/13)
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- PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR
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Disclosed is a process for the preparation of certain intermediates, e.g. a process for preparing a compound of formula (I) wherein, R1, R2 and X1 are as defined in the description, and which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
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Page/Page column 20; 22
(2020/12/07)
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- Preparation method of precursor of ibrutinib
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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 0037; 0039-0043
(2020/04/22)
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- PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR
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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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- Heteroaryl compound having pharmaceutical activity
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The present invention provides a class of new compounds having Btk selective inhibition activity, wherein the new compounds have good metabolic stability and the like.
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Paragraph 0140; 0141; 0142
(2019/01/10)
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- Method for using zinc chloride to separate and purify ibrutinib intermediate
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The invention discloses a method for using zinc chloride to separate and purify an ibrutinib intermediate, and particularly relates to a separation and purification method of the ibrutinib intermediate (3R)-4-amido-3-(4-phenoxy phenyl)-1-(1-tert-butoxy carbonyl piperidine-3-yl)-1H-pyrazolo[3,4-d]pyrimidine. After Mitsunobu reaction for preparing the intermediate is terminated, zinc chloride is added into a mixture, heated and cooled, composition sediment of zinc chloride and triphenylphosphine oxide is removed by filtering, and the intermediate with good purity is obtained. The process omits column chromatography, and is an efficient and low-cost separation and purification method.
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Paragraph 0014
(2019/02/04)
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- PROCESS FOR PREPARING IBRUTINIB
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The present application relates to a method for preparing Ibutinib as shown by the following synthetic route and the intermediate compounds involved therein.
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Paragraph 0107; 0108
(2018/03/25)
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- A synthetic method for ibrutinib
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A synthetic method for ibrutinib (I) is provided. Nano-magnetic material-loaded triphenylphosphine (PPh3@NMM) is adopted and subjected to a Mitsunobu reaction, efficient preparation of an intermediateIV and efficient separation of a by-product triphenylphosphine oxide are achieved, and an intermediate IV is further acrylated to obtain ibrutinib. The whole route has the advantages of simple operation, a low cost, a high yield, obvious reduction of three wastes, and the like, and the method is suitable for industrial scale-up production.
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Paragraph 0043; 0044
(2018/10/27)
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- A according to lu tini and its key intermediate for the preparation of the new method (by machine translation)
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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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- Refined preparing method of ibrutinib
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The invention discloses a refined preparing method of ibrutinib. According to the method, a compound with a formula 1 is used as a raw material, and the compound with the formula 1 and a compound with a formula 2 are reacted in the presence of a mitsunobu reaction reagent to generate a compound with a formula 3, and a protecting group of the compound with the formula 3 is removed in the presence of acid to generate a compound with a formula 4; the compound with the formula 4 and a compound with a formula 5 are subjected to a Suzuki coupling reaction in the presence of alkali and a catalyst to generate a compound with a formula 6; the compound with the formula 6 and acryloyl chloride are reacted in the presence of alkali to generate ibrutinib. Finally column chromatography separation is conducted, macroporous adsorption resin is adopted as filler, the eluent is ethyl acetate or petroleum ether, and a high-purity material is obtained. According to the refined preparing method of ibrutinib, the yield is high in every step, the product is convenient to purify, the purity is high, and the industrialized production prospect is good.
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- PROCESS FOR THE SYNTHESIS OF STABLE AMORPHOUS IBRUTINIB
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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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- PROCESS FOR PREPARING PURE LH-PYRAZOLO[3,4-D] PYRIMIDINE DERIVATIVE
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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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- PROCESS FOR THE PREPARATION OF IBRUTINIB
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The present invention relates to a process for the preparation of 1-[(3R)-3 -[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl] -1-piperidinyl]-2-propen-1-one or Ibrutinib of Formula (I). The present invention further relates to a process for the preparation highly pure 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1 H-pyrazolo[3,4-d]pyrimidin-1-yl] -1-piperidinyl]-2-propen-l-one or Ibrutinib.
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- A METHOD FOR PREPARATION OF IBRUTINIB PRECURSOR
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A method for the preparation of ibrutinib's precursor, 3-(4-phenoxyphenyl)-1-((3R)-piperidin-3-il)-1H-pyrazolof [3,4-d]|pyrimidin-4-amine, involving arylation of N-protected 1-(piperidin-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine in the presence of palladium catalyst, nitrogen-containing ligand, and base, with subsequent removal of the protecting groups by known methods, is reported. (Formula (II))
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Page/Page column 7; 8
(2017/03/28)
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- According to lu tini synthesis method
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The invention discloses a synthesis method of ibrutinib. The method uses Suzuki coupling reaction and Kumada coupling reaction, does not need to separate the intermediate, obtains the intermediate (9) at high yield by a one-pot process, and uses mixed anhydrides instead of acryloyl chloride. The technique utilizes cheap 4-halodianisole as the initial raw material, adopts Suzuki coupling reaction and Kumada coupling reaction, and uses the one-pot process. The whole route is disclosed in the specification. The method can obtain the intermediate (9) (the chemical purity and optical purity are greater than or equal to 99%) at high yield without separating and purifying the intermediate, and avoids microwave, high temperature/high pressure and other specific reaction conditions; and the acrylic acid and mixed anhydrides generated by acyl chloride and sulfonyl chloride are used instead of the acryloyl chloride in the last step to avoid the amidation reaction of the intermediate (10) in multiple sites and reduce the generation of the byproduct, thereby obtaining the high-purity ibrutinib at high yield. The method has the advantages of short process route and lower cost, and is beneficial to the environment and suitable for industrialized scale-up production.
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Paragraph 0070; 0071; 0072; 0074; 0075
(2017/08/31)
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- High-efficiency preparation method for ibrutinib
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The invention discloses a high-efficiency preparation method for ibrutinib, which belongs to the technical field of organic synthesis. A concrete synthetic route is shown in a specification. The method has the advantages of mild reaction condition, simple operation, low cost, convenient purifying, friendly environment, and high product optical purity, and is suitable for industrial production.
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- PROCESS FOR PREPARING IBRUTINIB AND ITS INTERMEDIATES
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The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.
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Paragraph 0126; 0132
(2017/06/23)
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- Method for synthesizing ibrutinib
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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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- 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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- Ibrutinib preparation method, ibrutinib intermediate, and ibrutinib intermediate preparation method
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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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- Preparation method of ibrutinib
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The invention relates to the technical field of medicine, in particular to a preparation method of ibrutinib. The preparation method of ibrutinib comprises the following steps that 4-amino-3-(4-phenoxy phenyl)-1H-pyrazol[3,4-d]pyrimidine and S-1-tert-butyloxycarbonyl-3-hydroxyl piperidine are prepared into a compound shown in the formula IV (please see the formula in the description) through a Mitsunobu reaction, and a Boc protecting group of the compound shown in the formula IV is removed to prepare a compound shown in the formula V (please see the formula in the description); the compound shown in the formula V and acrylic ester are prepared into a compound shown in the formula I (please see the formula in the description) in the presence of a catalyst and an activating agent. According to the preparation method, the reaction process is mild in condition, few reaction steps are needed, high temperature and copious cooling are not needed, no high-toxicity reagent is adopted, and the whole synthesizing process is stable and controllable; ibrutinib prepared through the method is high in yield and quality and has the advantages of being good in stability, high in purity, convenient to store and the like.
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- Pyrazolopyrimidine derivative, preparation method, pharmaceutical composition and application
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The invention discloses a pyrazolopyrimidine derivative, a preparation method, a pharmaceutical composition and application. The invention provides the pyrazolopyrimidine derivative as shown in a formula I and stereoisomer or solvate or pharmaceutically acceptable salts or active metabolite or prodrug thereof. The pyrazolopyrimidine derivative as shown in the formula I has good inhibitory activity on Bruton's tyrosine kinase (Btk) and particularly has good in vitro and in vivo inhibitory activity on growth of tumor cells, and a good marketization prospect is achieved. Please see the formula I in the description.
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Paragraph 0153; 0154; 0155
(2017/07/19)
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- Preparation method for ibrutinib
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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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- Preparation method of ibrutinib
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The invention belongs to the field of drug synthesis and relates to preparation of a crude drug and an intermediate, in particular to a preparation method of ibrutinib 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one. The method is characterized in that (1) 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (SM1) and (S)-1-Boc-3-hydroxypiperidine (SM2) are adopted as starting materials and subjected to a Mitsunobu reaction, and an intermediate (-1): (R)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine is obtained and condensed with acrylic anhydride for an amidation reaction, and the finished product ibrutinib is prepared through recrystallization.
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Paragraph 0062; 0063
(2017/01/02)
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- Preparation method of Ibrutinib drug impurity
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The invention belongs to the field of pharmaceutical synthesis, and relates to an impurity in the bulk pharmaceutical chemical production process and a preparation method of the impurity, in particular to a process impurity of Ibrutinib 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1Hpyrazole [3,4-d]pyrimidine-1-yl]-1-piperidyl]-2-propylene-1-ketone and a preparation method of the process impurity.
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Paragraph 0066; 0067
(2017/10/03)
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- Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: A comparative study
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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
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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
-
p. 9625 - 9638
(2016/01/12)
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- PROCESSES AND INTERMEDIATES FOR PREPARING A MEDICAMENT
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Disclosed is a process for the preparation of the following compounds: (I), (II) where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.
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Page/Page column 19; 25
(2014/09/29)
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- TREATMENT OF DRY EYE
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The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.
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Page/Page column 50
(2014/02/16)
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- Tyrosine kinase inhibitors
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The present disclosure provides compounds such as pyrazolpyrimidine compounds, and pharmaceutically acceptable salts thereof, that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 201
(2014/03/26)
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- INHIBITORS OF THE IRE-1/XBP-1 PATHWAY AND METHODS OF USING THEREOF
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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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Page/Page column 66
(2014/11/13)
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- REVERSIBLE COVALENT PYRROLO- OR PYRAZOLOPYRIMIDINES USEFUL FOR THE TREATMENT CANCER AND AUTOIMMUNE DISEASES
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Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production, and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.
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Page/Page column 157
(2014/01/09)
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- PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
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Page/Page column 77
(2012/12/13)
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- BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING
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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 12
(2008/12/08)
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