- PYRAZOLOPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR USE IN PREVENTING OR TREATING CANCER, AUTOIMMUNE DISEASE AND BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.
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Paragraph 258-262
(2018/12/02)
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- PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
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Paragraph 0109
(2017/07/29)
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- Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)
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Page/Page column 57
(2017/07/31)
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- QUATERNARY AMMONIUM SALT COMPOUNDS
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[Problem] The object of the present invention is to provide a novel compound having 132 adrenergic receptor agonist activity and muscarinic receptor antagonist activity. [Means for Solving the Problem] The present invention is a quaternary ammonium salt compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, with superior β32 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.
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Page/Page column 62; 63
(2012/03/10)
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- HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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Page/Page column 112
(2010/08/18)
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- Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 34
(2008/06/13)
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- HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF
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The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.
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Page/Page column 51
(2008/12/06)
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- Orally active factor Xa inhibitors: Investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy
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A series of novel and potent 3-amidinophenylsulfonamide derivatives of factor Xa inhibitors were designed and synthesized using an amidoxime prodrug strategy. We focused on systemic clearance of parent compounds in rats, and performed in vivo pharmacokinetic screening. Incorporation of a carboxymethoxy group markedly improved systemic clearance (compound 43), and the related amidoxime 44 showed sufficient prodrug conversion. Compound 45, the double prodrug of 43, exhibited practicable bioavailability after oral administration in rats. Among the various compounds under investigation, KFA-1982 was selected for clinical development.
- Uchida, Masahiko,Okazaki, Kosuke,Mukaiyama, Harunobu,Isawa, Hidetoshi,Kobayashi, Hiroaki,Shiohara, Hiroaki,Muranaka, Hideyuki,Kai, Yuichiro,Kikuchi, Norihiko,Takeuchi, Hideki,Yokoyama, Kenji,Tsuji, Eiichi,Ozawa, Tomonaga,Hoyano, Yuji,Koizumi, Takashi,Misawa, Keiko,Hara, Kiyoto,Nakano, Shigeru,Murakami, Yasuoki,Okuno, Hiroaki
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scheme or table
p. 4682 - 4687
(2009/04/08)
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- 1,2,3,4-Tetrahydropyrazin-2-yl acetamides and methods of use
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Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and
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Page/Page column 44
(2010/02/15)
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- HETEROCYCLIC CYCLOPENTYL TETRAHYDROISOQUINOLINE AND TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- INDOLE ACETAMIDES AS INHIBITORS OF THE HEPATITIS C VIRUS NS5B POLYMERASE
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The present invention relates to indole and azaindole compounds of formula (I): wherein X1, X2, X3, X4, A1, Ar1, R1, R2 and n are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
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- 5-AMIDINO-N-(2-AMINOPHENETHYL)-HYDROXYBENZENESULFONAMIDE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND INTERMEDIATE THEREFOR
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The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom, an opti
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- CB 1/CB 2 RECEPTOR LIGANDS AND THEIR USE IN THE TREATMENT OF PAIN
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Compounds of formula (I) or pharmaceutically acceptable salts thereof wherein Ar?1?, Ar?2?, R?1?, R?2?, n and X are as defined in the specificationas well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in th
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- Preparation of 1,2,3,4-tetrahydroisoquinolines lacking electron donating groups - An intramolecular cyclization complementary to the Pictet-Spengler reaction
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The synthesis of 1,2,3,4-tetrahydroisoquinolines via an intramolecular cyclization of N-trifluoroacylated phenethylamines devoid of electron donating groups, with paraformaldehyde mediated by acetic/sulfuric acid milieu is described.
- Stokker
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p. 5453 - 5456
(2007/10/03)
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