Korea Research Institute of Chemical Technology

Korea Institute of Science and Technology

Korea Research Institute of Bioscience and Biotechnology

Handok Inc.

Ubix Therapeutics, Inc.

Sung Yun Cho

Jae Du Ha

Chi Hoon Park

Chong Ock Lee

Jong Yeon Hwang

Hyoung Rae Kim

Hee Jung Jung

Chang Soo Yun

Sunjoo Ahn

Chong Hak Chae

Pilho Kim

Dae Chul Park

Sang Un Choi

Kwangho Lee

Pil Ho Kim

Chang Hoon Lee

Hwan Mook Kim

Sung Soo Kim

Kwang Ho Lee

Hwan Geun Choi

Kyung Ho Yoo

Tae Bo Sim

Chang Hyun Oh

Jung Beom Son

Young Jin Ham

Hyun Jin Kim

Dong Cho Han

Jung Mi Hah

Yong Ki Min

Byoung Mog Kwon

Seung Kyu Kang

So Ha Lee

Joo Youn Lee

Song Hee Lee

Dong Sik Park

Joong Kwon Choi

Ji Youn Park

Je Ho Ryu

Ho Hyun Lee

Jung Min Ahn

Woo S Chang

Eul Kyun Yum

Sun Joo Ahn

Jong Kook Lee

Ye Seul Lim

Hee Jung Moon

Beom Seon Suh

Sun Mi Yoo

Han Wool Kim

The present invention relates to a novel heterocyclic compound and a composition, for preventing or treating a cancer, an autoimmune disease, and an inflammatory disease, comprising same. The novel heterocyclic compound of the present invention is a bifunctional compound having a Bruton's tyrosine kinase (BTK) degradation function via a ubiquitin proteasome pathway, and may be utilized as a composition for preventing or treating a cancer, an autoimmune disease, and Parkinson's disease.

Bifunctional heterocyclic compound having BTK degradation function via ubiquitin proteasome pathway, and use thereof

The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.

Piperidine-2,6-dione derivative and use thereof

The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.

Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient

A pyrimidine derivative compound of Chemical Formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the same as an active ingredient. The pyrimidine derivative compound of Chemical Formula 1, the optical isomer thereof, or the pharmaceutically acceptable salt thereof has an excellent selective inhibitory effect especially against TYRO 3 among TAM receptor inhibitory effects, and thus can be used as an excellent composition of preventing or treating cancer without adverse effects resulting from the inhibition of Axl and Mer. 

Pyrimidine derivative compound, optical isomer thereof, or pharmaceutically acceptable salt thereof, and composition for preventing or treating Tyro 3 related disease comprising same as active ingredient

The present invention relates to a 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

4-(2-amino-tetrahydronaphthalenyl)pyrimidine derivative, preparation method therefor, and pharmaceutical composition for preventing or treating cancer, containing same as active ingredient

The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

N2-(2-methoxyphenyl)pyrimidine derivative, method for preparing same, and pharmaceutical composition for cancer prevention or treatment containing same as active ingredient

The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according to the present invention has the good effect of inhibiting anaplastic lymphoma kinase (ALK) activity, whereby a therapeutic effect on cancer cells having an anaplastic lymphoma kinase (ALK) fusion protein such as EML4-ALK, NPM-ALK, etc. can be enhanced and it is expected that a recurrence of cancer will be effectively inhibited. As such, the compound can be effectively used in a pharmaceutical composition for prevention or treatment of cancer.

Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient

The present invention relates to a novel triazolopyrazine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating hyper proliferative disorder. The present invention can be useful as a therapeutic agent for various hyper proliferative disorders associated with excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy, by efficiently inhibiting c-Met tyrosine kinase activity.

Triazolopyrazine derivative and use thereof

Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.

N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer

Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.

Indazole derivatives or pharmaceutically acceptable salts thereof as protein kinase inhibitors for proliferative diseases treatment, and a pharmaceutical composition containing the same as an active ingredient

Process for preparing 1-aryl-4-oxopyrrolo �3,2-c! quinoline derivatives

The present invention relates to a process for preparing a catalyst useful in producing ethylidene diacetate and to a process for producing ethylidene diacetate by a continuous process using the catalyst prepared. In the preparation of ethylidene diacetate from carbon monoxide and hydrogen, the conventional preparation method using a homogeneous catalyst system comprising a transition metal catalyst is hampered by difficulty in separating the catalyst from the reaction product after completion of the reaction. The catalyst of the present invention is separated easily from the reaction product. The heterogeneous catalyst of the present invention is prepared by adding a compound of a group VIII metal, preferably rhodium or palladium, to a carrier, preferably .alpha.-alumina, kieselguhr or silica, together with an accelerator containing phosphorus or nitrogen, preferably triphenylphosphine. Using the improved catalyst of the present invention also resulted in increased yield of product over conventional methods. The ethylidene diacetate produced using the present method is useful as a starting material for the production of vinyl acetate monomer.

Methods for preparing ethylidene diacetate

The present invention relates to the field of catalyst technology, and more particularly to the preparation of a supported catalyst and a method of producing ethylidene diacetate using that supported catalyst. The catalyst is represented by the formula M.sub.a X. Compound M includes a group VIII transition metal which catalyzes the formation of ethylidene diacetate, preferably a compound of rhodium or palladium. Carrier X is an organic carrier, preferably selected from the divinylbenzene-polystyrene copolymers, most preferably copolymers having about 1-20% crosslinking. The weight percent of metal M contained in the catalyst is represented by the latter a. The supported heterogenized catalyst results from covalent bonding of the transition metal compound to the organic polymer carrier. Ethylidene diacetate was produced by reacting methyl acetate, iodomethane, carbon monoxide and hydrogen in the presence of this supported catalyst and an accelerator at elevated temperature and pressure. According to the present invention, the reaction product, ethylidene diacetate, is easily separated from the catalyst. The produced ethylidene diacetate may be used as a starting material for preparing vinyl acetate monomer.

Methods for producing ethylidene diacetate using catalysts supported on

The present invention relates to a catalyst, a process for preparing the catalyst and a process for using the catalyst to produce ethylidene diacetate. The conventional preparation methods of ethylidene diacetate suffer from difficulty in separating the catalyst from the product after completion of the reaction. The catalyst of the present invention is simply separated from the product by mere filtration following the completion of reaction. This is a result of using a heterogenized catalyst which is obtained by supporting a homogeneous catalyst in an inorganic carder. The catalyst of the present invention is of the general formula M.sub.a X where M is a compound of a group VIII transition metal, most preferably RhCl.sub.3 .multidot.xH.sub.2 O, and X is an inorganic carrier, preferably selected from the group consisting of kieselguhr, .gamma.-alumina, silica, TiO.sub.2, MgO, ZnO and activated charcoal. Ethylidene diacetate produced using the present method is useful as an intermediate for producing precision chemical articles or as a starting material for the production of vinyl acetate monomer.

Catalysts on inorganic carriers for producing ethylidene diacetate

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Daejeon, South Korea

Sung Yun Cho