Northwestern University

Other

Warner-lambert Company

Cambria Pharmaceuticals, Inc.

University of California

The General Hospital Corporation

Hadasit Medical Research Services and Development Ltd.

Chapman University

University of Chicago

Albert Einstein College of Medicine

Brookhaven Science Associates, Lcc

Bial - R&d Investments, S.a.

Lysosomal Therapeutics Inc.

Catalyst Pharmaceutical Partners, Inc.

Richard B Silverman

Ryszard Andruszkiewicz

Po-wai Yuen

Denis Martin Sobieray

Lloyd Charles Franklin

Mark Alan Schwindt

Dimitri Krainc

Fengtian Xue

Jianbin Zheng

Qing Jing

Hoang V Le

Haitao Ji

He Huang

Richard I Morimoto

Dustin D Hawker

Anthony C Arvanites

Radhia Benmohamed

Donald R Kirsch

Sun Yang

Yaron Ilan

Aleksey G Kazantsev

Thomas E Adrian

Gerald A Soff

Wei Zhang

Soosung Kang

Shouxin Liu

Wenxin Gu

Maris A Cinelli

Jose Juncosa

Yinan Zhang

Hua Wang

Mohammad Khanfar

Andrew Charles Good

Renato T Skerlj

Peter T Lansbury

Elyse Marie Josee Bourque

Kenji Takaya

Rima McLeod

Hejun Lu

Frank L Meyskens

Jung-Mi Hah

Dalton James Surmeier, Jr

Thomas L Poulos

Dennis H Flint

Matthew J Moschitto

Heng-Yen Wang

Soo Sung Kang

Yue Pan

Jose Antonio Gomez Vidal

Garry Cooper

Paramita Mukherjee

Ehud Zigmond

Hien M Nguyen

Anthony V Pensa

Stephen L Dewey

Henry Q Zhang

Herbert Estreicher

Graham Richard Lawton

Mizuki Watanabe

Sida Shen

Steven Miller

Hui Huang

Matthew Moschitto

Ha T Do

Pathum Manjula Weerawarna

Guoyao Xia

Chi-Li Ni

Thomas S Leyh

Younghee Lee

Yajuan Qin

Fengwei Zou

Fengtlan Xue

Takashi Kudoh

Erik Erdal

Tian Chen

James M Kraus

Provided herein are processes, compounds and compositions for making (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid. Also provided herein a pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid.

Process for the synthesis of (s) 3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid

Disclosed are new small molecules having a substituted pyrimidine or substituted fused pyrimidine core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including Gaucher's disease and neurological diseases and disorders such as genetic and sporadic synucleinopathies, including Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy associated with aberrant glucocerebrosidase activity. The small molecules may contain a fluorophore or may be conjugated to a fluorophore in order to prepare a fluorescent probe for use in high throughput screening methods to identify new modulators of glucocerebrosidase activity via fluorescence polarization.

Substituted fused pyrimidine compounds and uses thereof

Disclosed are 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase (NOS). In particular, the field of the invention relates to 2-aminopyridine derivative compounds for use as inhibitors of neuronal nitric oxide synthase (nNOS), which are formulated as pharmaceutical compositions for treating diseases and disorders associated with nNOS such as Alzheimer's, Parkinson's, and Huntington's diseases, and amyotrophic lateral sclerosis, cerebral palsy, stroke/ischemic brain damage, and migraine headaches.

Potent and selective human neuronal nitric oxide synthase inhibitors

Disclosed are substituted aminoquinoline and aminopyridine compounds and their use as bacterial nitric oxide synthase (bNOS) inhibitors. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject having or at risk for developing a disease or disorder that is associated with bNOS activity.

Bacterial nitric oxide synthase inhibitors

Disclosed herein are methods and compositions for administering immunotherapy to a subject in need thereof and for treating a subject in need thereof, where in the methods the subject is administered an effective amount of an inhibitor of nNOS for inducing an immunotherapeutic response in the subject and for treating the subject. The disclosed methods and composition may be utilized for treating a subject having a cell proliferative disease or disorder such as melanoma.

Use of neuronal nitric oxide synthase inhibitors for immunotherapy in melanoma patients

Disclosed are cyclopentene compounds for use as inhibitors of aminotransferases such as gamma-aminobutyric acid (GABA) aminotransferase (AT) and/or ornithine aminotransferase (OAT). The disclosed cyclopentene compounds include 3-amino-4-halocyclopente carboxylic acid compounds which may be formulated in pharmaceutical composition for treating diseases and disorders associated with GABA-AT and/or OAT activity, including epilepsy, addiction, hepatocellular carcinoma (HCC), and non-small cell lung cancer (NSCLC).

3-amino-4-halocyclopentene carboxylic acids as inactivators of aminotransferases

The invention provides substituted pyrrolo[1,2-a]pyrimidines and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidines compounds described herein include substituted 2,4-dimethyl-N-phenylpyrrolo[1,2-a]pyrimidine-8-carboxamide compounds and variants thereof.

Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders

Disclosed are methods, compounds, and compositions for treating infection by an Apicomplexan parasite that include administering a compound that selectively inactivates ornithine aminotransferase of the Apicomplexan parasite. Specifically, the methods, compounds, compounds may be utilized for treating infection byand toxoplasmosis and for treating infection byand malaria. The compounds disclosed herein are observed to selectively inactivateornithine aminotransferase (TgOAT) relative to human OAT and relative to human &#x3b3;-aminobutyric aminotransferase (GABA-AT).

Inactivators of toxoplasma gondii ornithine aminotransferase for treating toxoplasmosis and malaria

Disclosed are compound and methods of using the compounds for modulating ornithine aminotransferase (OAT) activity. The disclosed compound are characterized as analogs of 3-amino-4-(propan-2-ylidene)cyclopentane-1-carboxylic acid which may be formulated as therapeutic agents for treating diseases and disorders associated with ornithine aminotransferase (OAT) activity such as hepatocellular carcinoma and other cancers.

Analogs of 3-amino-4-(propan-2-ylidene)cyclopentane-1-carboxylic acid and uses thereof for treating diseases and disorders associated with ornithine aminotransferase activity

Disclosed are enantiomerically pure cyclopentane-based compounds that are prepared by a multiple-step synthesis process. The disclosed compounds have been designed to inhibit gamma-aminobutyric acid-amino transferase (GABA-AT) activity and ornithine aminotransferase (OAT) activity. Some of the enantiomerically pure compounds inhibit OAT activity more potently than the racemic compound. The disclosed compounds may be used to selectively inhibit OAT activity, for example, to treat hepatocellular carcinoma and/or used to selected inhibit GABA-AT activity, for example, to treat neurological diseases and disorders.

2-difluoro substituted 4-aminocyclopentanecarboxylic acids as inhibitors of gamma-aminobutyric acid aminotransferase and human ornithine aminotransferase

Disclosed are new small molecules having a substituted quinazoline core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules or activated glucocerebrosidase conjugated to the small molecules, which compositions may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurological diseases and disorders such as Gaucher's disease and Parkinson's disease.

Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity

Disclosed are new small molecules having a pyrrolopyrimidine core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurological diseases and disorders such as Gaucher's disease and Parkinson's disease. The small molecules may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase thusly generated can be administered in enzyme replacement therapy and/or utilized in screening assays for new small molecules that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase.

Pyrrolopyrimidine compounds and uses thereof for modulating glucocerebrosidase activity

Disclosed are cyclopentene compounds for use as inhibitors of gamma-aminobutyric acid (GABA) aminotransferase (AT) and/or ornithine aminotransferase (OAT). The disclosed cyclopentene compounds include 3-carbon substituted 4-aminocyclopent-1-ene-carboxylic acid compounds which may be formulated in pharmaceutical composition for treating diseases and disorders associated with GABA-AT and/or OAT activity, including epilepsy, addiction, and hepatocellular carcinoma (HCC).

3-carbon substituted 4-aminocyclopent-1-ene-1-carboxylic acid compounds as inhibitors of gamma-aminobutyric acid (GABA) aminotransferase

Growing community of inventors

Winnetka, IL, United States of America

Richard B Silverman