- CEREBLON BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
-
Provided herein are piperidine dione compounds having the following structure: wherein R1, R2, R3, R4, L, V, X, A, A′, a and m are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
- -
-
-
- HETEROBICYCLIC AMIDES AS INHIBITORS OF CD38
-
The present invention relates to heterobicyclic amides and related compounds which are inhibitors of CD38 and are useful in the treatment of cancer.
- -
-
Paragraph 0429
(2021/02/05)
-
- CEREBLON BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
-
Provided herein are piperidine dione compounds having the following structure: wherein RN, R1, R2, R3, R4, RN, L, V, X, a, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
- -
-
-
- CEREBLON BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
-
Provided herein are piperidine dione compounds having the following structure: wherein R1, R2, R3, R4, L, V, X, a and m are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
- -
-
-
- CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
-
This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
- -
-
Page/Page column 172; 198
(2021/11/26)
-
- Discovery of the c-Jun N-Terminal Kinase Inhibitor CC-90001
-
As a result of emerging biological data suggesting that within the c-Jun N-terminal kinase (JNK) family, JNK1 and not JNK2 or JNK3 may be primarily responsible for fibrosis pathology, we sought to identify JNK inhibitors with an increased JNK1 bias relative to our previous clinical compound tanzisertib (CC-930). This manuscript reports the synthesis and structure-activity relationship (SAR) studies for a novel series of JNK inhibitors demonstrating an increased JNK1 bias. SAR optimization on a series of 2,4-dialkylamino-pyrimidine-5-carboxamides resulted in the identification of compounds possessing low nanomolar JNK inhibitory potency, overall kinome selectivity, and the ability to inhibit cellular phosphorylation of the direct JNK substrate c-Jun. Optimization of physicochemical properties in this series resulted in compounds that demonstrated excellent systemic exposure following oral dosing, enabling in vivo efficacy studies and the selection of a candidate for clinical development, CC-90001, which is currently in clinical trials (Phase II) in patients with idiopathic pulmonary fibrosis (NCT03142191).
- Apuy, Julius,Bahmanyar, Sogole,Benish, Brent,Bennett, Brydon L.,Blease, Kate,Canan, Stacie S.,Condroski, Kevin,Delgado, Mercedes,Elsner, Jan,Erdman, Paul,Haelewyn, Jason,Hilgraf, Robert,Khambatta, Godrej,Lebrun, Laurie,McCarrick, Meg,Moghaddam, Mehran F.,Mortensen, Deborah S.,Nagy, Mark A.,Norris, Stephen,Paisner, David,Romanow, William J.,Satoh, Yoshitaka,Tikhe, Jayashree,Xu, Li,Yoon, Won
-
p. 18193 - 18208
(2021/12/27)
-
- TREATMENT OF CDK4/6 INHIBITOR RESISTANT NEOPLASTIC DISORDERS
-
This invention is to methods for treating disorders involving abnormal cellular proliferation that have developed resistance to a selective CDK4/6 inhibitor.
- -
-
Page/Page column 79-80
(2020/10/19)
-
- CRYSTALLINE SUBSTITUTED CYCLOHEXYL PYRAZOLO[1,5-A]PYRIMIDINYL CARBOXAMIDE COMPOUND AND THERAPEUTIC USES THEREOF
-
The invention provides crystalline 5,7-dimethyl-N-((1S*,4S)-4-(pentyloxy)cyclohexyl) pyrazolo[1,5-a]pyrimidine-3-carboxamide, compositions containing the crystalline compound, methods for making the crystalline compound, medical kits, and methods for usin
- -
-
Paragraph 00225; 00230
(2019/07/14)
-
- HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELLULAR PROLIFERATION
-
This invention is in the area of heterocyclic-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
- -
-
Page/Page column 163
(2019/07/20)
-
- 1,3 DI-SUBSTITUTED CYCLOBUTANE OR AZETIDINE DERIVATIVES AS HEMATOPOIETIC PROSTAGLANDIN D SYNTHASE INHIBITORS
-
A compound of formula (I), wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
- -
-
Page/Page column 110
(2018/04/27)
-
- MDM2-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
-
The description relates to MDM2 binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the MDM2 E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
- -
-
Paragraph 0435
(2017/01/31)
-
- Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors
-
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasm
- Haffner, Curt D.,Becherer, J. David,Boros, Eric E.,Cadilla, Rodolfo,Carpenter, Tiffany,Cowan, David,Deaton, David N.,Guo, Yu,Harrington, Wallace,Henke, Brad R.,Jeune, Michael R.,Kaldor, Istvan,Milliken, Naphtali,Petrov, Kim G.,Preugschat, Frank,Schulte, Christie,Shearer, Barry G.,Shearer, Todd,Smalley, Terrence L.,Stewart, Eugene L.,Stuart, J. Darren,Ulrich, John C.
-
supporting information
p. 3548 - 3571
(2015/05/05)
-
- Synthesis of dibenzylamino-1-methylcyclohexanol and dibenzylamino-1-trifluoromethylcyclohexanol isomers
-
The isomers of dibenzylamino-1-methylcyclohexan-1-ol and dibenzylamino-1-trifluoromethylcyclohexan-1-ol have been prepared. The stereochemistry of these compounds was unequivocally assigned through a combination of NMR spectroscopy and single crystal X-ra
- Jones, D. Heulyn,Bresciani, Stefano,Tellam, James P.,Wojno, Justyna,Cooper, Anthony W. J.,Kennedy, Alan R.,Tomkinson, Nicholas C. O.
-
p. 172 - 182
(2015/12/30)
-
- PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
-
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
- -
-
Paragraph 0288
(2014/03/26)
-
- DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
-
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
- -
-
Page/Page column 40
(2012/08/08)
-
- TRI-SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS
-
The present invention provides a tri-substituted pyrimidine compound having an excellent PDE10 inhibitory activity. The present invention relates to a tri-substituted pyrimidine compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compound for PDE10 inhibitor, and a pharmaceutical composition comprising said compounds as an active ingredient: wherein: either one of X1 and X2 is N, and the other of X1 and X2 is CH; A is *-CH═CH—, *-C(Alk)=CH—, *-CH2—CH2— or *-O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted quinoxalinyl or an optionally substituted quinolyl; Y0 is mono- or di-substituted amino group, or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 27-28
(2011/07/08)
-
- Pyrimido?5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
-
The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula STR1 in which Ra to Rc are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.
- -
-
-
- Cyclic imino derivatives and pharmaceutical compositions containing them
-
The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
- -
-
-
- A simple method of preparation of 7-alkyl-7-azabicyclo[2.2.1] heptanes
-
Action of triphenylphosphine - carbon tetrachloride on the trans-4-alkylaminocyclohexanols leads to 7-alkyl-7-azabicyclo[2.2.1]heptanes in the good yields. The starting aminoalcohols are easily available from the monoethylene ketal of 1,4-cyclohexanedione and primary amines in a four step process without isolation of intermediates.
- Hassner, Alfred,Belostotskii, Anatoly M.
-
p. 1709 - 1712
(2007/10/02)
-