http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-106241-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_945ae1209056dcb497edf108d69159da |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 |
| filingDate | 2016-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8d96b440f42da09ddb7f26e8a0c80819 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7c96d8e33be6b33ff9cb714ae8ab3a5f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d2a8fda9f1d7c336fbc848e0b34dc05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1f49f417a12f5800adadb2620d440501 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d89e0d645f86ea900a7c4e75b523704 |
| publicationDate | 2017-12-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-106241-A1 |
| titleOfInvention | HUMAN PLASMATIC CALICREIN INHIBITORS |
| abstract | Claim 1: A compound represented by the formula (1), or a pharmaceutically acceptable salt thereof, wherein, independently for each case: R¹ represents -OH, -ORᶜ, -NH₂, -NHRᶜ, -NRᶜRᵈ , alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, halo, haloalkyl, cycloalkyl, (cycloalkyl) alkyl, -C (O) Rᶜ, -C (O) OH, -C (O) ORᶜ, -OC (O) Rᶜ, -C (O) NH₂, -C (O) NHRᶜ, -C (O) NRᶜRᵈ, -NHC (O) Rᶜ or -NRᶜC (O) Rᵈ; or two geminal cases of R¹ taken together with the carbon to which they are attached represent -C (O) -; or two neighboring or geminal cases of R¹ taken together form an optionally substituted fused carbocyclic or heterocyclic ring; W is a bond, -C (O) NH-, -C (O) N (Rᶜ) -, -C (O) O-, -CH₂- or -C (O) -; R² represents aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, (cycloalkyl) alkyl) or (heterocycloalkyl) optionally substituted alkyl; V represents optionally substituted aryl or heteroaryl; Z is absent or represents one or more substituents independently selected from the group consisting of halo, haloalkyl, -NO₂, -CN, -C (O) Rᶜ, -C (O) OH, -C (O) ORᶜ, -OC ( O) Rᶜ, -C (O) NH₂, -C (O) NHRᶜ, -C (O) NRᶜRᵈ, -NHC (O) Rᶜ, -N (Rᶜ) C (O) Rᵈ, -OS (O) ₚ ( Rᶜ), -NHS (O) ₚ (Rᶜ) and -NRᶜS (O) ₚ (Rᶜ); X represents -C (NH₂) -, -C (NH (Rᶜ)) -, -C (NRᶜRᵈ) -, -C (NHS (O) ₚRᶜ) -, -C (NHC (O) Rᶜ) -, -C (NHC (O) NH₂) -, C (NHC (O) NHRᶜ) -, -C (NHC (O) NRᶜRᵈ) -, -C (OH) -, -C (O (alkyl)) -, -C ( N₃) -, -C (CN) -, -C (NO₂) -, -C (S (O) ₙRᵃ) -, -C [-C (= O) Rᶜ] -, C [-C (= O) NRᶜRᵈ] -, -C [-C (= O) SRᶜ] -, -C [-S (O) Rᶜ] -, -C [-S (O) ₂Rᶜ] -, -C [S (O) (ORᶜ )] -, -C [-S (O) ₂ (ORᶜ)] -, -C [-SO₂NRᶜRᵈ] -, -C (halogen) -, -C (alkyl), -C ((cycloalkyl) alkyl), - C (alkenyl) -, -C (alkynyl) - or -C (aralkyl) -; R³ represents optionally substituted aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R³ᵃ is absent or represents one or more substituents independently selected from the group consisting of halo, hydroxy, alkyl, -CF₃, -OCF₃, alkoxy, aryl, heteroaryl, aryloxy, amino, aminoalkyl, -C (O) NH₂, cyano, - NHC (O) alkyl, -SO₂-alkyl, -SO₂NH₂, cycloalkyl, - (CH₂) ʳORᵃ, -NO₂, - (CH₂) ʳNRᵃRᵇ, - (CH₂) ʳC (O) Rᵃ, -NRᵃC (O) Rᵇ, -C (O) NRᶜRᵈ, -NRᵃC (O) NRᶜRᵈ, -C (= NRᵃ) NRᶜRᵈ, -NHC (= NRᵃ) NRᶜRᵈ, -NRᵃRᵇ, -SO₂NRᶜRᵈ, -NRᵃSO₂NRᶜRᵈ, -NRᵃSO₂-alkyl, -NRᵃSO₂Rᵃ, -S (O) ₚRᵃ, - (CF₂) ʳCF₃, -NHCH₂Rᵃ, -OCH₂Rᵃ, -SCH₂Rᵃ, -NH (CH₂) ₂ (CH₂) ʳRᵃ, -O (CH₂) ₂ (CH₂) ʳRᵃ or -S (CH₂) ₂ (CH₂) ʳRᵃ; And represents a link; or -Y-R⁴ represents -alkylene-R⁴, -CH₂C (O) -R⁴, -CH₂NH-R⁴, -CH₂N (alkyl) -R⁴, -CRᵃRᵇ-R⁴, -NH-R⁴, -NHCH₂-R⁴, -NHC ( O) -R⁴, -N (alkyl) -R⁴, -N (alkyl) CH₂-R⁴, -N ((CH₂) ₂OH) -R⁴, -N ((cycloalkyl) alkyl) R⁴, -heterocyclyl-R⁴, -OR⁴ , -OCH₂-R⁴, -OC (O) -R⁴, -OC (O) NRᵃRᵇ, -SCH₂R⁴ or -SR⁴ optionally substituted; R⁴ represents hydrogen, hydroxy, alkyl, cycloalkyl, (heterocycloalkyl) alkyl, (cycloalkyl) alkyl, -CH₂OH, -CH (alkyl) OH, -CH (NH₂) CH (alkyl) ₂, aryl, aralkyl, heteroaryl, heteroaralkyl, - CH₂S (alkyl), amino or cyano optionally substituted; or - (CRᵃRᵇ) ʳ (CRᵃRᵇ) ₚ- fused to position 4 of the ring having Z to form a 5- to 7-membered heterocyclic ring with optional substituents; or when R³ is phenyl, R⁴ can represent -NRᵃ-fused to the ortho position to X in that phenyl; each Rᵃ and Rᵇ is independently H alkyl, alkenyl, alkynyl, aralkyl, (cycloalkyl) alkyl, -C (= O) Rᶜ, -C (= O) ORᶜ, -C (= O) NRᶜRᵈ, -C (= O) SRᶜ, -S (O) Rᶜ, -S (O) ₂Rᶜ, -S (O) (ORᶜ) or -SO₂NRᶜRᵈ; Rᶜ and Rᵈ represent, independently in each case, alkyl, alkenyl, alkynyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, (cycloalkyl) alkyl, heterocycloalkyl, (heterocycloalkyl) alkyl, -C (O) alkyl or -S ( O) ₚ (alkyl) optionally substituted; or Rᶜ and Rᵈ can be taken together to form an optionally substituted heterocyclic ring; the remainder of formula (2) may represent a compound of the group of formulas (3); r is 0, 1, 2 or 3; n is an integer from 0 to 6; p is 0, 1 or 2. |
| priorityDate | 2015-10-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 49.