Patent classifications
C07D213/61
COMPOUNDS FOR INHIBITION OF ALPHA 4 BETA 7 INTEGRIN
- Peter A. Blomgren ,
- Taryn Campbell ,
- Jayaraman Chandrasekhar ,
- Christopher T. Clark ,
- Julian A. Codelli ,
- Kevin S. Currie ,
- Jeffrey E. Kropf ,
- Yasamin Moazami ,
- Nicole Nava ,
- Leena Patel ,
- Stephane Perreault ,
- Jason K. Perry ,
- Kassandra F. Sedillo ,
- Natalie Seeger ,
- Kirk L. Stevens ,
- Jennifer Anne Treiberg ,
- Suet C. Yeung ,
- Zhongdong Zhao
The present disclosure provides a compound of Formula (I):
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or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
STAT INIHIBITORY COMPOUNDS AND COMPOSITIONS
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for the inhibition of Signal Transducer and Activator of Transcription 5a and 5b (STAT5). Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as, for example, breast cancer, hematological cancer, and pancreatic cancer.
Inhibitors and their uses
The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##
Inhibitors and their uses
The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.3a, R.sup.5a, X.sup.a and Y.sup.a are as defined herein. ##STR00001##
NOVEL SYNTHETIC OPTIONS TOWARDS THE MANUFACTURE OF (6R,10S)-10-{4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL)PHENYL]-6-OXO-1(6H)-PYRIMIDINYL}- 1-(DIFLUOROMETHYL)-6-METHYL-1,4,7,8,9,10-HEXAHYDRO-11,15-(METHENO)PYRAZOLO[4,3-B][1,7]DIAZACYCLOTETRADECIN-5(6H)-ONE
Highly efficient methods are provided for preparing key intermediates in the synthesis of Compound (I), which are broadly applicable and can provide selected components having a variety of substituents groups.
##STR00001##
NOVEL SYNTHETIC OPTIONS TOWARDS THE MANUFACTURE OF (6R,10S)-10-{4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL)PHENYL]-6-OXO-1(6H)-PYRIMIDINYL}- 1-(DIFLUOROMETHYL)-6-METHYL-1,4,7,8,9,10-HEXAHYDRO-11,15-(METHENO)PYRAZOLO[4,3-B][1,7]DIAZACYCLOTETRADECIN-5(6H)-ONE
Highly efficient methods are provided for preparing key intermediates in the synthesis of Compound (I), which are broadly applicable and can provide selected components having a variety of substituents groups.
##STR00001##
METHOD FOR PREPARING AROMATIC AMINO ACID DERIVATIVE
The present invention provides methods of efficiently producing various optically active aromatic amino acid derivatives by reacting, using an additive, a specific ester compound with an aromatic halide and zinc in the presence of a catalyst. The present invention also provides amino acid derivatives that can be produced by the methods.
SARS-CoV-2 inhibitors for treating coronavirus infections
Provided herein are compounds, pharmaceutical compositions, and methods for treating a SARS-CoV-2 infection.
NOVEL AMINO ACID DERIVATIVES
- Naoki OKADA ,
- Kyosuke UEDA ,
- Masatoshi TAKUWA ,
- Shunichi NAKANO ,
- Kotaro TOKUMOTO ,
- Tomoko ASHIZAWA ,
- Shuhei YAMAKOSHI ,
- Yutaka KOBAYASHI ,
- Katsuma MATSUI ,
- Ayumu MATSUDA ,
- Masatoshi MATSUMOTO ,
- Keiichi MASUYA ,
- Atsushi YOSHIZAWA ,
- Masahiko KINEBUCHI ,
- Takeru EHARA ,
- Masami YAMADA ,
- Kouki MORIMOTO ,
- Yoshihide MIZUKOSHI ,
- Haruaki KURASAKI ,
- Motoki MURAI ,
- Kentarou FUKUMOTO ,
- Douglas Robert CARY
A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve solubility of polypeptides comprising the derivative therein.
PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS
Compounds of the formula (I) wherein the substituents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling animal pests, including arthropods and in particular insects, nematodes, molluscs or representatives of the order Acarina.
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