- HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
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Paragraph 00162
(2016/10/31)
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- NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS
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The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.
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Paragraph 1615-1618
(2013/10/22)
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- Development of an efficient, scalable route for the preparation of a novel insulin-like growth factor-1 receptor modulator
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A chromatography-free and efficient synthesis of insulin-like growth factor-1 receptor (IGF-1R) modulator is reported. Herein we describe an improved synthesis for the target compound, which features facile introduction of a novel pyrrolidinyl-pyrimidyl isoxazole 8, via in situ sulfone displacement by fluorine. The overall process consists of six chemical steps and five isolations, with introduction of the expensive triheterocyclic unit 8 towards the end of the synthesis.
- Kumar, C.H. Vinod,Kavitake, Santosh,Kumar, Sythana Suresh,Cornwall, Philip,Ashok, Mithun,Bhagat, Sagar,Manjunatha, Sulur G.,Nambiar, Sudhir
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p. 1416 - 1421
(2012/10/29)
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- Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors
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Thiazol-2-yl amine was identified as an isosteric replacement for pyrazol-3-yl amine during our efforts to identify potent and selective JAK2 inhibitors. The rationale, synthesis and biological evaluation of several analogs is reported, along with the in vivo evaluation of the lead compounds.
- Ioannidis, Stephanos,Lamb, Michelle L.,Almeida, Lynsie,Guan, Huiping,Peng, Bo,Bebernitz, Geraldine,Bell, Kirsten,Alimzhanov, Marat,Zinda, Michael
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scheme or table
p. 1669 - 1673
(2010/08/20)
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- AMINO-THIAZOLYL- PYRIMIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
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The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 57-58
(2009/01/20)
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- S-6-METH0XY-2- (2- (3- (PYRIMID-2-YL) IS0XAZ0L-5-YL) PYRROLIDIN-1-YL) -4- (5-METHYL-IH-PYRAZOL-S-YLAMINO) PYRIMIDINE AND POLYMORPHIC FORMS THEREOF AS MODULATORS OF THE INSULIN-LIKE GROWTH
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There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salsts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 29
(2008/12/04)
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- PYRIMIDINE DERIVATIVES FOR THE INHIBITION OF IGF-IR TYROSINE KINASE ACTIVITY
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A compound of formula (I) wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
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Page/Page column 96
(2008/06/13)
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- 4-(PYRID-2-YL) AMINO SUBSTITUTED PYRIMIDINE AS PROTEIN KINASE INHIBITORS
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A compound of formula (I): wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm-blooded animal such as man.
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Page/Page column 97
(2008/06/13)
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- Amines useful in producing pharmaceutically active CNS compounds
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Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- Amines useful in producing pharmaceutically active CNS compounds
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Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- Pharmaceutically active amines
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The aromatic amines (I), alkyl amines (II), bicyclic amines (III). STR1 cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
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- Amino-9,10-secosteroids useful for treating head injury, spinal cord trauma or stroke
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The amino-9,10-secosteroids STR1 of the present invention contain an amino group attached to the terminal carbon atom of the C17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
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