Dana-farber-cancer Institute Inc.

Korea Institute of Science and Technology

The General Hospital Corporation

The Broad Institute, Inc.

Korea Research Institute of Bioscience and Biotechnology

Hanmi Science Co., Ltd.

Lg Chem, Ltd

Harvard College

Korea Research Institute of Chemical Technology

University of Miami

Daegu Gyeongbuk Institute of Science and Technology

National Cancer Center

Hanmi Pharm. Co., Ltd.

Samsung Life Public Welfare Foundation

Catholic University Industry Academic Cooperation Foundation

Hwan Geun Choi

Nathanael Schiander Gray

Tae Bo Sim

Jung Beom Son

Yanke Liang

Young Jin Ham

Yi Kyung Ko

Pasi Antero Janne

Nam Doo Kim

Jaebong Jang

Jung Mi Hah

So Young Kim

Jianming Zhang

Seock Yong Kang

Hwan Mook Kim

Ramnik Xavier

Alykhan Shamji

Ho Jong Yoon

Thomas Sundberg

Eun Hwa Ko

Eunhwa Ko

Jin-Hee Park

Seungyeon Lee

Tinghu Zhang

Guang Yang

Xianming Deng

Kyung Ho Yoo

Sara Jean Buhrlage

Chang Hyun Oh

David E Fisher

Steven P Treon

Li Tan

Woo Young Hur

Hwan Oh Kim

Nisma Mujahid

Youn Ho Lee

Sun-Hwa Lee

Yuan Xiong

Jae Hyun Bae

Ju Hee Kang

Se In Kang

Dayea Kim

Sun Joo Lee

Sang Bum Kim

Young Gil Ahn

John M Hatcher

Kwok-kin Wong

Jae Won Chang

Maeng Sup Kim

Wenjun Zhou

Taebo Sim

Philip Cohen

Jean Zhao

Michael Eck

Seung Hyun Jung

Hai-Tsang Huang

Young Hee Jung

Chi Man Song

Han Na Cho

Yubao Wang

Suk Kyoon Yoon

Ellen Weisberg

Hee Yoon Ryu

Yun Ju Nam

Eunmi Hong

Kristopher Clark

Dong-sik Park

Eun Jin Jun

Seung Min Lee

Stuart L Schreiber

Dong-wook Kim

Jae Chul Lee

Matthew Meyerson

Eun Young Kim

Henry M Kronenberg

Ji Yeon Song

Seung Hoon Lee

Sung Yun Cho

Nathanael S Gray

Young Kwan Kim

Do-Hyun Nam

Jae Du Ha

Dong Cho Han

Jae Yul Choi

Jong Bae Park

Byoung Mog Kwon

Hyun Kyoung Kim

Izidore Lossos

Mi Kyoung Lee

Kenneth Dale Westover

So Ha Lee

Sang Min Lim

Sungchan Cho

Ryo Murakami

Seung Hye Choi

Marc Wein

Kyu-Sun Lee

The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

Pyrimidines as EGFR-inhibitors and methods of treating disorders

The present invention relates to a 6-(isooxazolidin-2-yl)-N-phenylpyrimidin-4-amine derivative, and a pharmaceutical composition for preventing or treating cancer comprising the compound as an effective component. The compound exhibits high inhibitory activity against an epidermal growth factor receptor (EGFR) variant, or wild-type or variants of one or more of ERBB2 and ERBB4, and thus may be usefully used in the treatment of cancers in which same are expressed. In particular, the compound exhibits excellent inhibitory activity on proliferation of lung cancer cell lines, and thus can be usefully used in the treatment of lung cancer.

Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component

The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Type II raf kinase inhibitors

The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

Bicyclic urea kinase inhibitors and uses thereof

Pyrimidines as EGFR inhibitors and methods of treating disorders

The present invention relates to a novel compound exhibiting enteropeptidase-inhibiting activity, a pharmaceutically acceptable salt thereof, a pharmaceutical composition for preventing and treating metabolic diseases such as obesity, diabetes mellitus or hyperlipidemia, etc. comprising the compound or pharmaceutically acceptable salt, and a method for preventing or treating metabolic disease using the above novel compound. The compound of the present invention has excellent inhibitory activity against enteropeptidase, and thus is not absorbed into the body, but are excreted outside the body. However, since not only fat but also protein are discharged together, it has few side effects such as fat stools and acts only in the gastrointestinal tract, so it has few side effects such as depression, and is very useful as a therapeutic or prophylactic drug for various metabolic diseases such as obesity, diabetes mellitus, and hyperlipidemia.

Compound exhibiting enteropeptidase inhibitory activity

The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein. 

Uses of pyrimidopyrimidinones as SIK inhibitors

The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI). 

Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis

The present invention relates to a novel pyrrolo-pyrimidine derivative compound, a preparation method therefor, and a pharmaceutical composition comprising the same compound as an effective ingredient for preventing or treating a protein kinase-related disease. The compound represented by Chemical Formula 1 according to the present invention, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an effective ingredient has outstanding inhibitory activity against LRRK2 kinase and against phosphorylation in the NIH-3T3 cell line, which is an LRRK2-expressing cell line, and NCC01 and 448T cell lines, which are both derived from patients with brain tumors. Verified to have inhibitory activity against various protein kinases in addition to LRRK2, the compound can find effective applications in the treatment or prevention of protein kinase-related diseases. 

Pyrrolo-pyrimidine derivative compound, preparation method therefor, and pharmaceutical composition comprising same compound as effective ingredient for preventing or treating protein kinase-related disease

The present invention relates to a pyrrolo-pyridine derivative compound, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for the prevention or treatment of protein kinase-related diseases. A compound represented by chemical formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, according to the present invention, has excellent inhibitory activity against various protein kinases including DYRK1A, and therefore, the pharmaceutical composition containing the same as an active ingredient can be favorably used in the treatment or prevention of protein kinase-related diseases. Particularly, the pharmaceutical composition can be effectively used in the prevention, treatment, or alleviation of Alzheimer's disease, dementia, or Alzheimer's dementia.

Pyrrolo-pyridine derivative compound, method for preparing same, and pharmaceutical composition containing same as active ingredient for prevention or treatment of protein kinase-related diseases

The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein. 

Imidazolyl kinase inhibitors and uses thereof

The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein. 

Compounds having the formula I, II, or III: are provided. Compounds of the present disclosure are useful for the treatment of neurodegenerative diseases, such as Parkinson's Disease.

LRRK2 inhibitors and methods of making and using the same

Growing community of inventors

Seoul, South Korea

Hwan Geun Choi