- Medicine composition for treating myocardial damage and preparation method and use thereof
-
The invention discloses a medical composition for treating myocardial damage, and belongs to the technical field of medicines. The medical composition comprises active components having the structureas shown in the description, one or more of a pharmaceutic adjuvant, a diluent or a carrier. The invention further relates to a preparation method and application of the medical composition. The medical composition has the effect of protecting cardiac muscle cell structures and functions, in addition, can also alleviate ischemia reperfusion injury, is notable in effect, and can be used as a medicine used by patients suffering from myocardium damage.
- -
-
Paragraph 0023; 0025; 0026; 0027; 0028
(2018/09/26)
-
- 1-SUBSTITUTED 1,2,3,4-TETRAHYDRO-1,7-NAPHTHYRIDIN-8-AMINE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR ANTAGONISTS
-
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.
- -
-
Paragraph 0250
(2017/02/09)
-
- INHIBITORS OF HIF PROLYL HYDROXYLASE
-
The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
- -
-
Page/Page column 108
(2016/04/20)
-
- Discovery of imigliptin, a novel selective DPP-4 inhibitor for the treatment of type 2 diabetes
-
We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.
- Shu, Chutian,Ge, Hu,Song, Michael,Chen, Jyun-Hong,Zhou, Huimin,Qi, Qu,Wang, Feng,Ma, Xifeng,Yang, Xiaolei,Zhang, Genyan,Ding, Yanwei,Zhou, Dapeng,Peng, Peng,Shih, Cheng-Kon,Xu, Jun,Wu, Frank
-
supporting information
p. 921 - 926
(2014/09/17)
-
- Process Development and Multikilogram-Scale Synthesis of a TRPV1 Antagonist
-
The process development and multikilogram preparation of a TRPV1 antagonist, 1, is described. Pyrido[2,3-b]pyrazine 1 was prepared in a convergent manner by the coupling of two key fragments, glyoxal 2 and diamine 3. Glyoxal 2 was synthesized in six chemical steps in 20% overall yield, the key step being a challenging Grignard reaction to install the glyoxalate moiety. Diamine 3 was also prepared in six chemical steps in 46% overall yield, exploiting a regioselective nucleophilic aromatic substitution to obtain the key nitrodiamine intermediate 19.
- Cleator, Ed,Scott, Jeremy P.,Avalle, Paulo,Bio, Matthew M.,Brewer, Sarah E.,Davies, Antony J.,Gibb, Andrew D.,Sheen, Faye J.,Stewart, Gavin W.,Wallace, Debra J.,Wilson., Robert D.
-
p. 1561 - 1567
(2014/01/06)
-
- Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin- 3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists
-
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
- Dzierba, Carolyn D.,Sielecki, Thais M.,Arvanitis, Argyrios G.,Galka, Amy,Johnson, Tricia L.,Takvorian, Amy G.,Rafalski, Maria,Kasireddy-Polam, Padmaja,Vig, Shikha,Dasgupta, Bireshwar,Zhang, Ge,Molski, Thaddeus F.,Wong, Harvey,Zaczek, Robert C.,Lodge, Nicholas J.,Combs, Andrew P.,Gilligan, Paul J.,Trainor, George L.,Bronson, Joanne J.,MacOr, John E.
-
scheme or table
p. 4986 - 4989
(2012/08/28)
-
- FUSED PYRIDINE DERIVATIVES
-
Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
- -
-
Page/Page column 29
(2012/12/13)
-
- FUSED PYRIDINE DERIVATIVES
-
Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
- -
-
Page/Page column 32
(2012/12/13)
-
- HETEROCYCLIC DERIVATIVES
-
The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.
- -
-
Page/Page column 53
(2011/02/25)
-
- PROCESS FOR PREPARATION OF NITROPYRIDINE DERIVATIVES
-
Disclosed here is a process for the preparation of nitropyridine derivatives of Formula (I) and its salt and precursors such as halogenated amino pyridines; Wherein; R1 is selected from amino group, hydroxyl group, acyl group, alkyl amino group, halogen atom, -NH - C (O) - R3; Where R3 is branched or linear alkyl group having 1 - 6 carbon atoms, or cycloalkyl group having 3 - 6 carbon atoms; R2 is selected from hydroxyl group, halogen atom, alkoxy group,
- -
-
Page/Page column 15
(2010/08/18)
-
- Compounds for the Treatment of Neurodegeneration and Stroke
-
Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP.
- -
-
Page/Page column 27
(2008/06/13)
-
- 9-AZABICYCLO [3 . 3 . 1] NONANE DERIVATIVES AS MONOAMINE REUPTAKE INHIBITORS
-
The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula (I), wherein R1 is H or C1-5alkyl; X is O or NR2, wherein R2 is H, C1-5alkyl or C2-5acyl and Ar is C6-10aryl or a 5-10 membered heteroaryl ring system, both being optionally substituted with one to three of R3-R5 independently selected from halogen, C1-5alkyl, C1-5alkoxy, C3-6cycloalkyl, C2-5alkenyl, C2-5alkynyl, CN, NO2, hydroxy, phenyl, phenoxy and phenylC1-2alkoxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein said phenyl, phenoxy and phenylC1-2alkoxy are optionally substituted with one to three substituents independently selected from halogen and methyl or two of R3-R5 at adjacent positions together form a methylenedioxy or propylene unit, with the proviso that the compounds exo-9-methyl-3-phenoxy-9-azabicyclo[3.3.1]nonane and N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H indazole-5-amine are excluded, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.
- -
-
Page/Page column 24
(2010/11/26)
-
- Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
-
A series of high affinity CRF receptor ligands with an imidazo[4,5-b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmacokinetic model to assess plasma levels at 1mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3mg/kg (po). The structure-activity relationships for good receptor binding affinity are described herein.
- Arvanitis, Argyrios G,Rescinito, Joseph T,Arnold, Charles R,Wilde, Richard G,Cain, Gary A,Sun, Jung Hui,Yan, Jia-Sheng,Teleha, Christopher A,Fitzgerald, Lawrence W,McElroy, John,Zaczek, Robert,Hartig, Paul R,Grossman, Scott,Arneric, Stephen P,Gilligan, Paul J,Olson, Richard E,Robertson, David W
-
p. 125 - 128
(2007/10/03)
-
- MONOCYCLIC OR BICYCLIC CARBOCYCLES AND HETEROCYCLES AS FACTOR XA INHIBITORS
-
The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
- -
-
-
- Imidazopyridines for the treatment of neurological disorders
-
Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
- -
-
-
- Preparation of [1S-[1A,2B,3B,4A(S*)]]-4-[7-[[1-(3-chloro-2-thienyl)methyl propyl]amino]-3H-imidazo[4,5-B]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide
-
This invention is directed to methods for the preparation of [1S-[1a,2b,3b,4a(S*)]]-4-[7-[[1-(3-chloro-2-thienyl) methyl]propyl]amino]-3H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide, methods for the preparation of intermediates thereto, and to said intermediates themselves.
- -
-
-
- Thrombin inhibitors
-
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:
- -
-
-