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1.
ACS Med Chem Lett ; 15(6): 763-765, 2024 Jun 13.
Article in English | MEDLINE | ID: mdl-38894907

ABSTRACT

The invention in this patent application relates to thiazolo[5,4-b]pyridine derivatives represented generally by formula 1. These compounds are inhibitors of the activity of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT-1) protease and may potentially be useful in the treatment of some forms of cancer, particularly ABC-DLBCL.

2.
ACS Med Chem Lett ; 15(6): 766-768, 2024 Jun 13.
Article in English | MEDLINE | ID: mdl-38894906

ABSTRACT

The invention in this patent application relates to N-(pyrrolidine-3-yl or piperidin-4-yl)acetamide derivatives represented generally by formula 1. These compounds possess activities as somatostatin receptor 4 (SSTR4) agonists and may potentially be beneficial in the treatment of diseases or disorders, associated with SSTR4 such as Alzheimer's disease (AD) and other CNS disorders such as epilepsy and depression.

3.
ACS Med Chem Lett ; 15(1): 9-11, 2024 Jan 11.
Article in English | MEDLINE | ID: mdl-38229747

ABSTRACT

The invention in this patent application relates to 1-aminophthalazine derivatives represented generally by formula 1. These compounds are inhibitors of the interaction of the catalytic site of SOS1 with RAS-family proteins which are involved in controlling cell proliferation. They may potentially be used as a treatment for RAS mutant cancers such as pancreatic, lung, and colorectal cancers, cholangiocarcinoma, multiple myeloma, melanoma, and thyroid cancer.

4.
ACS Med Chem Lett ; 15(1): 6-8, 2024 Jan 11.
Article in English | MEDLINE | ID: mdl-38229741

ABSTRACT

The invention in this patent application relates to spirocyclopropane-2-carboxamide derivatives represented generally by formula 1. These compounds are positive allosteric modulators of α7 nAChR and may be useful in preventing, treating, or ameliorating central nervous system diseases and disorders such as cognitive impairments in Alzheimer's disease, Parkinson's disease, schizophrenia, and L-DOPA-induced dyskinesia as well as inflammation and cough.

5.
ACS Med Chem Lett ; 14(10): 1323-1325, 2023 Oct 12.
Article in English | MEDLINE | ID: mdl-37849533

ABSTRACT

The invention in this patent application relates to 4-aminopyridazin-6-one derivatives represented generally by formula 1. These compounds are inhibitors of the NOD-like receptor protein 3 (NLRP3) inflammasome pathway and may potentially provide a useful treatment for one or more of the diseases and disorders mediated by NLRP3, including but not limited to immune diseases, inflammatory diseases, autoimmune diseases, autoinflammatory fever syndromes, cryopyrin-associated periodic syndrome, chronic liver disease, kidney-related disease, hyperoxaluria, lupus nephritis, Type I and Type II diabetes, nephropathy, neurodegenerative diseases, Alzheimer's disease, cardiovascular diseases, metabolic diseases and many more.

6.
ACS Med Chem Lett ; 14(10): 1320-1322, 2023 Oct 12.
Article in English | MEDLINE | ID: mdl-37849546

ABSTRACT

The invention in this patent application relates to 1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[2,3-b][1,4]oxazepine derivatives represented generally by Formula 1. These compounds are Bcl-2 inhibitors and may be useful for the treatment of chronic lymphocytic leukemia, small lymphocytic lymphoma, and/or acute lymphocytic lymphoma.

7.
ACS Med Chem Lett ; 14(2): 127-128, 2023 Feb 09.
Article in English | MEDLINE | ID: mdl-36793430

ABSTRACT

The invention in this patent application relates to piperazine-2,3-dione derivatives represented generally by formula 1. These compounds show activities as selective interleukin 4 induced protein 1 (IL4I1) inhibitors and may potentially be useful in preventing and treating IL4Il-related diseases, such as endometrial, ovarian, and triple negative breast cancers.

8.
ACS Med Chem Lett ; 14(2): 129-130, 2023 Feb 09.
Article in English | MEDLINE | ID: mdl-36793429

ABSTRACT

The invention in this patent application relates to (S)-spiro[benzo[d][1,3]oxazine-4,3'-pyrrolidin]-2(1H)-one derivatives, represented generally by formula 1. These compounds are selective plasma kallikrein inhibitors and may potentially be beneficial in the treatment of several diseases and disorders, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy, and retinal vein occlusion.

15.
ACS Med Chem Lett ; 12(12): 1892-1893, 2021 Dec 09.
Article in English | MEDLINE | ID: mdl-34917249
16.
ACS Med Chem Lett ; 12(8): 1191-1192, 2021 Aug 12.
Article in English | MEDLINE | ID: mdl-34413937
20.
ACS Med Chem Lett ; 12(3): 334-336, 2021 Mar 11.
Article in English | MEDLINE | ID: mdl-33738058
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