http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-108657-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dcce39a20bef16c3f04497659caba40f |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J71-00 |
| filingDate | 2017-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c585cdafbddbf2a741e311bae60ea76b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c1eb6c0118748f3ceb93a4d3cd4606dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ee958afc3a6d610e614569f4f6518f8c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5c218b6cface9158ba1644a830e3a35e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29163bd2299b5afb44776d6d06780536 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d4a5e0dd1929d1171d3660f0d0b3d445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a1d97993e78b4534a7aea3dbaf71bae7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d58bc7ef4677618df7785a93b408a12f |
| publicationDate | 2018-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-108657-A1 |
| titleOfInvention | GLUCOCORTICOID AND IMMUNOCONJUGATE RECEPTOR AGONIST OF THE SAME |
| abstract | Immunoconjugates of glucocorticoid receptor agonists, glucocorticoid receptor agonists, and methods for using them, for example, to treat autoimmune and inflammatory diseases are provided herein. Claim 1: A compound characterized in that it has the formula (1a): (SM-L-Q) ₙ-A¹ (1a) wherein: A¹ is an anti-tumor necrosis factor (TNF) protein a; L is a connector; Q is a heterobifunctional group or a heterotrifunctional group; or Q is absent; n is a number between 1 and 10; and SM is a monovalent radical of a glucocorticosteroid. Claim 2: A compound characterized in that it has the formula (1b): (SM-L-Q) ₙ-A² (1b) wherein: A² is a protein; L is a connector; Q is a heterobifunctional group or a heterotrifunctional group; or Q is absent; n is a number between 1 and 10; and SM is a radical of a glucocorticosteroid represented by formula (2) or formula (3), wherein: R¹ is selected from the group consisting of hydrogen and halo; R² is selected from the group consisting of hydrogen, halo, and hydroxyl; R³ is selected from the group consisting of -CH₂OH, -CH₂SH, -CH₂Cl, -SCH₂Cl, -SCH₂F, -SCH₂CF₃, hydroxyl, -OCH₂CN, -OCH₂Cl, -OCH₂F, -OCH₃, -OCH₂CH₃, -SCH₂CN, or a remainder group of formulas (4); R³ᵃ is selected from the group consisting of hydrogen and C₁₋₄ alkyl; R³ᵇ is selected from the group consisting of C₁₋₄ alkyl and C₁₋₄ alkoxy; R³ᶜ is selected from the group consisting of hydrogen, C₁₋₄ alkyl, CH₂OH, and C₁₋₄ alkoxy; R³ᵈ and R³ᵉ are independently selected from hydrogen and C₁₋₄ alkyl; R⁶ᵃ, R⁶ᵇ, R⁶ᶜ, R⁶ᵈ, and R⁶ᵉ are each independently selected from the group consisting of hydrogen, halo, C₁₋₄ alkyl, C₁₋₄ haloalkyl, cyano, hydroxyl, thiol, amino, alkylthio, and alkoxy; X is selected from the group consisting of - (CR⁴ᵃR⁴ᵇ) ₜ-, -O-, -S-, -S (= O) -, -S (= O) ₂-, -NR⁵-, -CH₂S-, -CH₂O -, -N (H) C (R⁸ᵃ) (R⁸ᵇ) ₜ-, -CR⁴ᶜ = CR⁴ᵈ-, and -C ° C; or X is absent; Y² is selected from the group consisting of -O-, -S-, and -N (R⁷ᵃ) -; or Y² is absent; t is 1 or 2; Z is selected from the group consisting of = CR¹¹ᵃ- y = N-; each R⁴ᵃ and R⁴ᵇ is independently selected from the group consisting of hydrogen and C₁₋₄ alkyl; or R⁴ᵃ and R⁴ᵇ taken together with the carbon atom to which they are attached form a cycloalkyl of between 3 and 6 members; R⁴ᶜ and R⁴ᵈ are independently selected from the group consisting of hydrogen and C₁₋₄ alkyl; R⁵ is selected from the group consisting of hydrogen and C₁₋₄ alkyl; R⁷ᵃ is selected from the group consisting of hydrogen and C₁₋₄ alkyl; R⁸ᵃ and R⁸ᵇ are independently selected from the group consisting of hydrogen and C₁₋₄ alkyl; R⁹ᶠ is selected from the group consisting of hydrogen and C₁₋₄ alkyl; R¹¹ᵃ and R¹¹ᵇ are independently selected from the group consisting of hydrogen, halo, C₁₋₄ alkyl, C₁₋₄ haloalkyl, cyano, hydroxyl, thiol, amino, alkylthio, and alkoxy; and ⁻ ⁻ ⁻ ⁻ represents a single link or a double link. |
| priorityDate | 2016-06-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 27.