- Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis
-
Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclinical investigation of 29d, a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments.
- Klug, Dana M.,Mavrogiannaki, Eftychia M.,Forbes, Katherine C.,Silva, Lisseth,Diaz-Gonzalez, Rosario,Pérez-Moreno, Guiomar,Ceballos-Pérez, Gloria,Garcia-Hernández, Raquel,Bosch-Navarrete, Cristina,Cordón-Obras, Carlos,Gómez-Li?án, Claudia,Saura, Andreu,Momper, Jeremiah D.,Martinez-Martinez, Maria Santos,Manzano, Pilar,Syed, Ali,El-Sakkary, Nelly,Caffrey, Conor R.,Gamarro, Francisco,Ruiz-Perez, Luis Miguel,Gonzalez Pacanowska, Dolores,Ferrins, Lori,Navarro, Miguel,Pollastri, Michael P.
-
supporting information
p. 9404 - 9430
(2021/07/25)
-
- DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis
-
Visceral leishmaniasis (VL) is a parasitic disease endemic across multiple regions of the world and is fatal if untreated. Current therapies are unsuitable, and there is an urgent need for safe, short-course, and low-cost oral treatments to combat this ne
- Bello, Davide,Braillard, Stéphanie,Caljon, Guy,Carvalho, Sandra,Corpas-Lopez, Victoriano,Freund, Yvonne,Gilbert, Ian H.,Glossop, Paul A.,Jacobs, Robert T.,Lukac, Iva,Maes, Louis,Mowbray, Charles E.,Nare, Bakela,Pandi, Bharathi,Patterson, Stephen,Speake, Jason,Van Den Kerkhof, Magali,Wall, Richard J.,Whitlock, Gavin A.,Wyllie, Susan,Yardley, Vanessa,Zuccotto, Fabio
-
supporting information
p. 16159 - 16176
(2021/11/16)
-
- AZAINDOLE DERIVATIVE AND USE THEREOF AS FGFR AND C-MET INHIBITOR
-
A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0125; 0130
(2021/05/29)
-
- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
-
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
- -
-
Paragraph 0269; 0270
(2021/11/13)
-
- PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
-
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
- -
-
-
- Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis
-
Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo
- Janetka, James W.,Hopper, Allen T.,Yang, Ziping,Barks, Jennifer,Dhason, Mary Savari,Wang, Qiuling,Sibley, L. David
-
supporting information
p. 6144 - 6163
(2020/07/10)
-
- PYRROLOTRIAZINE DERIVATIVES FOR TREATING KIT- AND PDGFRA-MEDIATED DISEASES
-
The present disclosure provides compounds of Formula I, pharmaceutical salts thereof, and/or solvates of any of the foregoing which are useful for treating diseases and conditions related to mutant KIT and PDGFRa and present an advantageously non-brain pe
- -
-
Paragraph 00236-00237
(2020/10/21)
-
- Quinoline Derivatives and Their Use as ALK and ALK L1196M Inhibitors
-
The present invention relates to quinoline derivatives and a use thereof as inhibitors of ALK and mutated ALK. A pharmaceutical composition containing quinoline derivatives of chemical formula 1 or each of pharmaceutically acceptable salt thereof, has an effect of preventing or treating diseases associated with ALK and ALK L1196M, in other words, proliferative diseases caused by abnormal cell growth and function or behavior thereof.COPYRIGHT KIPO 2019
- -
-
Paragraph 0243-0244; 0280-0281; 0287
(2019/05/04)
-
- TAM KINASE INHIBITORS
-
Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat diseases, such as cancer.
- -
-
Paragraph 0165
(2019/02/02)
-
- Novel heterocyclic derivative capable of being used as SHP2 inhibitor
-
The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.
- -
-
Paragraph 0329
(2019/08/30)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
-
The present disclosure is directed to compounds of Formula (I) and methods of their use and preparation, as well as compositions comprising compounds of Formula (I).
- -
-
Page/Page column 102; 111
(2018/06/30)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
-
Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').
- -
-
Page/Page column 162
(2018/06/30)
-
- Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists
-
CXCR2 has emerged as a therapeutic target for not only peripheral inflammatory diseases but also neurological abnormalities in the central nervous system (CNS). Herein, we describe the discovery of a novel 1-cyclopentenyl-3-phenylurea series as potent and CNS penetrant CXCR2 antagonists. Extensive SAR studies, wherein molecules' property forecast index (PFI) was carefully optimized for overall balanced developability profiles, led to the discovery of the advanced lead compound 68 with a desirable PFI. Compound 68 demonstrated good in vitro pharmacology with excellent selectivity over CXCR1 and other chemokine receptors. Rat and dog pharmacokinetics (PK) revealed good oral bioavailability, high oral exposure, and desirable elimination half-life of the compound in both species. In addition, the compound demonstrated dose-dependent efficacy in the in vivo pharmacology neutrophil infiltration "air pouch" model in rodents after oral administration. Further, compound 68 is a CNS penetrant molecule with high unbound fraction in brain tissue.
- Lu, Hongfu,Yang, Ting,Xu, Zhongmiao,Lin, Xichen,Ding, Qian,Zhang, Yueting,Cai, Xin,Dong, Kelly,Gong, Sophie,Zhang, Wei,Patel, Metul,Copley, Royston C. B.,Xiang, Jianing,Guan, Xiaoming,Wren, Paul,Ren, Feng
-
supporting information
p. 2518 - 2532
(2018/03/26)
-
- NOVEL PHENYL PROPIONIC ACID DERIVATIVES AND USES THEREOF
-
The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of meta
- -
-
Paragraph 247-248; 249-251
(2018/07/05)
-
- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
-
This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
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-
Page/Page column 70
(2018/10/19)
-
- PYRAZOLOPYRIMIDINE DERIVATIVES AS BTK INHIBITORS FOR THE TREATMENT OF CANCER
-
This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of t
- -
-
Paragraph 00220
(2017/05/02)
-
- POLYCYCLIC COMPOUNDS AS INHIBITORS OF BRUTON'S TYROSINE KINASE
-
The present disclosure is directed to compounds of Formula (I) as Bruton's kinase inhibitors and their preparation, as well as compositions comprising compounds of Formula (I).
- -
-
Page/Page column 103; 112
(2017/07/06)
-
- INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
-
The present disclosure is directed to compounds of formula I and methods of their use and preparation, as well as compositions comprising compounds of formula I.
- -
-
Page/Page column 162
(2017/09/02)
-
- PYRAZOLOPYRIDINE DERIVATIVES FOR THE TREATMENT OF CANCER
-
The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders such as cancer, inflammatory disorders and autoimmune diseases.
- -
-
Page/Page column 90
(2017/12/29)
-
- FUSED RING HETEROARYL COMPOUNDS AND THEIR USE AS TRK INHIBITORS
-
The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases. In some compounds of Formula I, Q is —CH═CR3C(O)NR4R5, —C≡CC(O)NR4R5, or
- -
-
Paragraph 0503; 0504
(2016/07/05)
-
- HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
-
The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
- -
-
Paragraph 00674
(2016/01/25)
-
- 4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS
-
The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
- -
-
Page/Page column 147; 148; 668; 669
(2016/06/14)
-
- FLOURO-NAPHTHYL DERIVATIVES
-
The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five- or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
- -
-
Paragraph 0094
(2016/11/28)
-
- SUBSTITUTED PYRIDINES AND METHOD OF USE
-
The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
- -
-
Paragraph 00301
(2016/12/22)
-
- SUBSTITUTED IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS TROPOMYOSIN RECEPTOR KINASE A (TrkA) INHIBITORS
-
The present application relates to a series of substituted imidazo[1,2-a]pyridine compounds of formula (I), pharmaceutically acceptable salts, pharmaceutically acceptable solvates or stereoisomers thereof, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
- -
-
Paragraph 0651; 0652
(2016/01/15)
-
- INDOL AND INDAZOL DERIVATIVES
-
The present invention relates to indole and indazole derivatives of the following formula (I) wherein A is (AA) and the remaining variables are as defined in the specification. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
- -
-
Page/Page column 74
(2015/04/15)
-
- AMINOPYRIDINE DERIVATIVES AS TAM FAMILY KINASE INHIBITORS
-
Provided herein are aminopyridine derivatives and pharmaceutical compositions that are useful as TAM family kinase inhibitors.
- -
-
Page/Page column 84
(2015/06/11)
-
- FLUORO-NAPHTHYL DERIVATIVES
-
The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five-or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
- -
-
Page/Page column 18
(2015/08/06)
-
- 1 -(CYCLOPENT-2-EN-1 -YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS
-
The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
- -
-
Page/Page column 72
(2015/12/18)
-
- PYRAZINE DERIVATIVES AS FGFR INHIBITORS
-
The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
- -
-
Paragraph 0245; 0246
(2014/03/21)
-
- HISTONE DEMETHYLASE INHIBITORS
-
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like
- -
-
Paragraph 00187
(2014/10/04)
-
- CXCR7 ANTAGONISTS
-
Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.
- -
-
Paragraph 0457; 0458
(2014/06/23)
-
- SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS
-
The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, L, m, p and W are as defined in the specification.
- -
-
Page/Page column 43
(2014/06/24)
-
- ALKENYL COMPOUNDS AND METHODS OF USE
-
The present invention provides novel substituted alkenyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
- -
-
Paragraph 0256
(2014/12/12)
-
- NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
-
The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof
- -
-
Paragraph 0727
(2013/03/26)
-
- NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
-
The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
- -
-
Paragraph 0449
(2013/10/07)
-
- NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS
-
The present invention relates to compounds of general formula I, (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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-
Page/Page column 79
(2013/10/21)
-
- NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS
-
The present invention relates to compounds of general formula (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
- -
-
Page/Page column 120; 121
(2013/10/21)
-
- Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors
-
A series of 2-amino-N-benzylpyridine-3-carboxnamides, 2-amino-N- benzylpyridine-3-sulfonamides and 2-amino-3-benzylthiopyridines against c-Met were designed by means of bioisosteric replacement and docking analysis. Optimization of the 2-amino-3-benzylthiopyridine scaffold led to the identification of compound (R)-10b displaying c-Met inhibition with an IC 50 up to 7.7 nM. In the cytotoxic evaluation, compound (R)-10b effectively inhibited the proliferation of c-Met addictive human cancer cell lines (IC50 from 0.19 to 0.71 μM) and c-Met activation-mediated cell metastasis. At a dose of 100 mg/Kg, (R)-10b evidently inhibited tumor growth (45%) in NIH-3T3/TPR-Met xenograft model. Of note, (R)-10b could overcome c-Met-activation mediated gefitinib-resistance, which indicated its potential use for drug combination. Taken together, 2-amino-3-benzylthiopyridine scaffold was first disclosed and exhibited promising pharmacological profiles against c-Met, which left room for further exploration.
- Zhang, Dengyou,Zhang, Xiaowei,Ai, Jing,Zhai, Yun,Liang, Zhongjie,Wang, Ying,Chen, Yi,Li, Chunpu,Zhao, Fei,Jiang, Hualiang,Geng, Meiyu,Luo, Cheng,Liu, Hong
-
p. 6804 - 6820
(2013/10/22)
-
- Substituted Cyclic Carboxamide and Urea Derivatives as Ligands of the Vanilloid Receptor
-
Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and/or inhibition of pain and other conditions mediated by the vanilloid receptor 1.
- -
-
-
- GAMMA SECRETASE INHIBITORS
-
Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing t
- -
-
Page/Page column 34
(2012/10/18)
-
- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
-
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
- -
-
Page/Page column 25
(2012/10/08)
-
- Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors
-
A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the sca
- Zhang, Dengyou,Ai, Jing,Liang, Zhongjie,Li, Chunpu,Peng, Xia,Ji, Yinchun,Jiang, Hualiang,Geng, Meiyu,Luo, Cheng,Liu, Hong
-
supporting information
p. 5169 - 5180
(2012/11/07)
-
- Compounds Which Selectively Modulate The CB2 Receptor
-
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
- -
-
-
- TETRAZOLE COMPOUNDS WHICH SELECTIVELY MODULATE THE CB2 RECEPTOR
-
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally usefu
- -
-
-
- SPIROINDOLINONE PYRROLIDINES
-
There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
- -
-
Page/Page column 69
(2011/06/23)
-
- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
-
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
- -
-
Page/Page column 40
(2011/07/30)
-
- 5, 7-SUBSTITUTED-IMIDAZO [1, 2-C] PYRIMIDINES AS INHIBITORS OF JAK KINASES
-
Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
- -
-
Page/Page column 81
(2011/11/01)
-
- Spiroindolinone Derivatives
-
There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents
- -
-
Page/Page column 7-8
(2010/08/22)
-
- NEW COMPOUNDS II
-
The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates t
- -
-
Page/Page column 23-24
(2010/04/25)
-