- Catalytic enantioselective synthesis of 20(S)-camptothecin: A practical application of the sharpless asymmetric dihydroxylation reaction
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The first catalytic asymmetric route to 20(S)-camptothecin was achieved, using as the key steps a tandem intramolecular Heck reaction/olefin isomerization process and a Sharpless asymmetric dihydroxylation (AD) reaction.
- Fang,Xie,Lowery
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- INHIBITORS OF BETA SECRETASE
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The present invention relates to tricyclic inhibitors of beta-secretase having the structure shown in Formula (I) and (II) (I) and (II) wherein the radicals are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.
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Page/Page column 28; 29
(2018/09/28)
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- INHIBITORS OF BETA SECRETASE
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The present invention relates to tricyclic inhibitors of beta-secretase having the structure shown in Formula (I) and (II) (I) and (II) and the tautomers and the stereoisomeric forms thereof, wherein the radicals are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.
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Page/Page column 25; 26
(2018/09/28)
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- PYRROLO PYRIMIDINE DERIVATIVE
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The compound represented by general formula (I) has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolo pyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease.
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Paragraph 0375
(2016/09/26)
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- PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
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Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Formula (I). Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
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Paragraph 0105
(2014/09/29)
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- PYRIDONEAMIDE DERIVATIVES AS FOCAL ADHESION KINASE (FAK) INHIBITORS AND THEIR USE FOR THE TREATMENT OF CANCER
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Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufact
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Page/Page column 27
(2009/04/25)
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- PYRIDINONE COMPOUNDS
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The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as ca
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Page/Page column 7
(2008/12/05)
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- PROCESS FOR PRODUCING TRICYCLIC KETONE
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In order to efficiently supply CPT, which is a starting compound of irinotecan hydrochloride and a variety of camptothecin derivatives, by a practical total synthesis, the invention provides a means of efficiently preparing a tricyclic ketone that corresp
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Page/Page column 14-15
(2008/06/13)
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- Imidazole based kinase inhibitors
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The present invention provides compounds having Formula I and their use for the treatment of cancer.
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Page/Page column 11
(2008/06/13)
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- NOVEL TYROSINE KINASE INHIBITORS
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The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents.
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- Novel tyrosine kinase inhibitors
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.
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- Asymmetric total synthesis of (20R)-homocamptothecin, substituted homocamptothecins and homosilatecans
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An efficient asymmetric synthesis of a key DE lactone pyridone intermediate in the synthesis of homocamptothecin is reported. The synthesis is scalable and features a Stille coupling and a Sharpless asymmetric epoxidation as the key steps. The key intermediate has been parleyed into homocamptothecin and an assortment of fluorinated homocamptothecins and homosilatecans (7-silylhomocamptothecins), thereby providing the first asymmetric entry to this important new class of antitumor agents.
- Gabarda, Ana E,Du, Wu,Isarno, Thomas,Tangirala, Raghuram S,Curran, Dennis P
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p. 6329 - 6341
(2007/10/03)
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- Preparation of a camptothecin derivative by intramolecular cyclisation
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PCT No. PCT/US95/05427 Sec. 371 Date Nov. 1, 1996 Sec. 102(e) Date Nov. 1, 1996 PCT Filed May 2, 1995 PCT Pub. No. WO95/29919 PCT Pub. Date Nov. 9, 1995The present invention relates to a method for the preparation of camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I') known by the chemical name "7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin", which comprises cyclising the compound of formula (II'), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I') is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer, and/or if desired, converting the resulting compound of formula (I') or a salt thereof into a physiologically acceptable salt or solvate thereof.
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- Intermediates in pharmaceutical camptothecin preparation
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A process of providing novel compounds of Formula (I) below, which are useful as intermediates in the preparation of camptothecin and camptothecin-like compounds, STR1 wherein: R1 represents alkyl, particularly methyl, R2 represents H or alkyl, particularly methyl, R3 represents H or alkyl, particularly H; Q represents triflate or halo particularly bromo and iodo more particularly iodo and Y represents H, chloro or OR4, wherein R4 represents alkyl or triflate, or particularly H.
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