Methods of treating cancer by targeting tumor-associated macrophages
US-2024415921-A1 · Dec 19, 2024 · US
IAP antagonists
US9603889B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9603889-B2 |
| Application number | US-201314432517-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 1, 2013 |
| Priority date | Oct 2, 2012 |
| Publication date | Mar 28, 2017 |
| Grant date | Mar 28, 2017 |
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- Title
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- Abstract
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- Assignees and inventors
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- Key dates
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- First independent claim
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Abstract
Official abstract text for this publication.
There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
First claim
Opening claim text (preview).
What is claimed is: 1. A compound selected from the following (S)-N-(4-(((3S,5S)-1-((S)-3,3-Dimethyl-2-((R)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-((R)-1-(2-fluorophenyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-phenethyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(3-methoxyphenyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(4-fluorophenyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-N-((R)-1-(2-Chlorophenyl)ethyl)-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-N-((R)-1-(2,3-Difluorophenyl)ethyl)-2-((S)-3,3-dimethyl-2)-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S))-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-phenylbutyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-2-methoxy-1-phenylethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-N-(2,3-Dichlorobenzyl)-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen- 1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-(2-(naphthalen-2-yl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-N-Benzyl-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-(naphthalen-2-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(naphthalen-2-yl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-phenethyl-1,2,3,4-tetrahydroisoquinoline-1-carboxamide, (S)-N-((S)-1-(3-Chlorophenyl)ethyl)-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(2-fluorophenyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)- 1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-phenylpropyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1,1-diphenylpropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((S)-1,2,3,4-tetrahydronaphthalen-1-yl)-1,2, 3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-phenylethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(2-methoxyphenyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(2-fluorophenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (3S)-N-(1-(2-Chlorophenyl)ethyl)-2-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(2-fluorophenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-1-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)carbamoyl)benzyl)-N-((R)-1-(o-tolyl)ethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-N-(4-(((3S,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carba
Assignees
Inventors
Classifications
the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala · CPC title
having 5 to 11 amino acids · CPC title
Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title
- A61K38/08Primary
Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)} · CPC title
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US9603889B2 cover?
- There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
- Who is the assignee on this patent?
- Bristol Myers Squibb Co
- What technology area does this patent fall under?
- Primary CPC classification A61K38/08. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Mar 28 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).