http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-088328-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dcce39a20bef16c3f04497659caba40f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2012-10-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_383bb5bd16c2bcb3a1bb1ff7387cedea http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dba4e7b342adf534d1970883442fe43f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_276714053f5fce7cb8e7a4b50f34a232 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b31c2f389893c576d4ab58f077fb3e2f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a42f5e1507fe690c44327c7aa617fb1f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5715b73e2f3b62b161de17c3c006087 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d8ed0801efc11f054b2287950168df58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e41cfe83ffeba2de7530c270b5a2178 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0149e3d4c11582b96d99818de7dc2809 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9077877a190acdbc4d4483ff08a97ab7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3ef36bad2e31846d9491ff4b5891e6b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_da3d5277845247b8b691201a66077b25 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_791f3541ed1fa7d21160e009bcaae366 |
| publicationDate | 2014-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-088328-A1 |
| titleOfInvention | APOPTOSIS INDUCTIVE AGENTS THAT CAN BE USED TO TREAT CANCER AND IMMUNE AND AUTOIMMUNE DISEASES |
| abstract | Compounds that inhibit the activity of Bcl-xL antiapoptotic proteins, compositions containing said compounds and methods for treating diseases in which Bcl-xL antiapoptotic proteins are expressed. Claim 1: A compound characterized in that it is of the formula (1) or an acceptable salt for therapy thereof, or an acceptable salt for therapy thereof, wherein X is heteroaryl; wherein the heteroaryl represented by X is optionally substituted with one, two, three, or four R⁴; Y¹ is phenylene, or C₅₋₆ heteroarylene; optionally fused with one or two rings selected from the group consisting of C₃₋₈ cycloalkane, C₃₋₈ cycloalkene, benzene, C₅₋₆ heteroarene, C₃₋₈ heterocycloalkane, and C₃₋₈ heterocycloalkene; where Y¹ is optionally substituted with one, two, three, or four substituents independently selected from the group consisting of R⁵, OR⁵, SR⁵, S (O) R⁵, SO₂R⁵, C (O) R⁵, CO (O) R⁵ , OC (O) R⁵, OC (O) OR⁵, NH₂, NHR⁵, N (R⁵) ₂, NHC (O) R⁵, NR⁵C (O) R⁵, NHS (O) ₂R⁵, NR⁵S (O) ₂R⁵, NHC (O ) OR⁵, NR⁵C (O) OR⁵, NHC (O) NH₂, NHC (O) NHR⁵, NHC (O) N (R⁵) ₂, NR⁵C (O) NHR⁵, NR⁵C (O) N (R⁵) ₂, C (O ) NH₂, C (O) NHR⁵, C (O) N (R⁵) ₂, C (O) NHOH, C (O) NHOR⁵, C (O) NHSO₂R⁵, C (O) NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N (R⁵ ) ₂, CO (O) H, C (O) H, OH, CN, N₃, NO₂, F, Cl, Br and I; L¹ is selected from the group consisting of (CR⁶R⁷) q, (CR⁶R⁷) ₛ-O- (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-C (O) - (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-S- (CR⁶R⁷ ) ʳ, (CR⁶R⁷) ₛ-S (O) ₂- (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-NR⁶AC (O) - (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-C (O) NR⁶A- (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-NR⁶A- (CR⁶R⁷) ʳ, (CR⁶R⁷) ₛ-S (O) ₂NR⁶A- (CR⁶R⁷) ʳ, and (CR⁶R⁷) ₛ-NR⁶AS (O) ₂- (CR⁶R⁷) ʳ; and Y² is selected from the group consisting of C₃₋₁₁ alkyl, branched chain, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, phenyl, and C₃₋₇ heterocyclyl; wherein C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, phenyl, and C₃₋₇ heterocyclyl are optionally fused with one or two rings selected from the group consisting of C₃₋₈ cycloalkane, C₃₋₈ cycloalkene, benzene, C₅₋₆ heteroarene, C₃₋₈ heterocycloalkane, and C₃₋₈ heterocycloalkene; where Y² is optionally substituted with one, two, three, four, or five substituents independently selected from the group consisting of R⁸, OR⁸, SR⁸, S (O) R⁸, SO₂R⁸, C (O) R⁸, CO (O ) R⁸, OC (O) R⁸, OC (O) OR⁸, NH₂, NHR⁸, N (R⁸) ₂, NHC (O) R⁸, NR⁸C (O) R⁸, NHS (O) ₂R⁸, NR⁸S (O) ₂R⁸, NHC (O) OR⁸, NR⁸C (O) OR⁸, NHC (O) NH₂, NHC (O) NHR⁸, NHC (O) N (R⁸) ₂, NR⁸C (O) NHR⁸, NR⁸C (O) N (R⁸) ₂, C (O) NH₂, C (O) NHR⁸, C (O) N (R⁸) ₂, C (O) NHOH, C (O) NHOR⁸, C (O) NHSO₂R⁸, C (O) NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N (R⁸) ₂, CO (O) H, C (O) H, OH, CN, N₃, NO₂, F, Cl, Br and I; or L¹ is a link; and Y² is selected from the group consisting of C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, phenyl, and C₃₋₇ heterocyclyl; wherein C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, phenyl, and C₃₋₇ heterocyclyl represented by Y² are optionally fused with one or two rings selected from the group consisting of C₃₋₈ cycloalkane, C₃₋₈ cycloalkene, benzene, C₅ heteroarene ₋₆, C₃₋₈ heterocycloalkane, and C₃₋₈ heterocycloalkene; where each Y² and each ring fused with Y² are optionally substituted with one, two, three, four, or five substituents independently selected from the group consisting of R⁸, OR⁸, SR⁸, S (O) R⁸, SO₂R⁸, C ( O) R⁸, CO (O) R⁸, OC (O) R⁸, OC (O) OR⁸, NH₂, NHR⁸, N (R⁸) ₂, NHC (O) R⁸, NR⁸C (O) R⁸, NHS (O) ₂R⁸, NR⁸S (O) ₂R⁸, NHC (O) OR⁸, NR⁸C (O) OR⁸, NHC (O) NH₂, NHC (O) NHR⁸, NHC (O) N (R⁸) ₂, NR⁸C (O) NHR⁸, NR⁸C (O) N (R⁸) ₂, C (O) NH₂, C (O) NHR⁸, C (O) N (R⁸) ₂, C (O) NHOH, C (O) NHOR⁸, C (O) NHSO₂R⁸, C (O) NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N (R⁸) ₂, CO (O) H, C (O) H, OH, CN, N₃, NO₂, F, Cl, Br and I; Z¹ is selected from the group consisting of C (O) OR⁹, C (O) NR¹⁰R¹¹, C (O) R¹¹, NR¹⁰C (O) R¹¹, NR¹⁰C (O) NR¹⁰R¹¹, OC (O) NR¹⁰R¹¹, NR¹⁰C (O) OR⁹ , C (= NOR¹⁰) NR¹⁰R¹¹, NR¹⁰C (= NCN) NR¹⁰R¹¹, NR¹⁰S (O) ₂NR¹⁰R¹¹, S (O) ₂R⁹, S (O) ₂NR¹⁰R¹¹, N (R¹⁰) S (O) ₂R¹¹, NR¹⁰C (= NR¹¹) NR¹⁰R¹¹, C (= S) NR¹⁰R¹¹, C (= NR¹⁰) NR¹⁰R¹¹, halogen, NO₂, and CN; or Z¹ is selected from the group consisting of the group of formulas (2); R¹, in each instance, is independently selected from the group consisting of halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and C₁₋₆ haloalkyl; R², in each instance, is independently selected from the group consisting of deuterium, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and C₁₋₆ haloalkyl; two R² that bind to the same carbon atom, together with said carbon atom, optionally form a ring selected from the group consisting of heterocycloalkyl, heterocycloalkenyl, cycloalkyl, and cycloalkenyl; R³, in each instance, is independently selected from the group consisting of halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and C₁₋₆ haloalkyl; R⁴, in each instance, is independently selected from the group consisting of NR¹²R¹³, OR¹², CN, NO₂, halogen, C (O) OR¹², C (O) NR¹²R¹³, NR¹²C (O) R¹³, NR¹²S (O) ₂R¹⁴ , NR¹²S (O) R¹⁴, S (O) ₂R¹⁴, S (O) R¹⁴ and R¹⁴; R⁵, in each instance, is independently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₁₋₆ hydroxyalkyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl ; R⁶A is independently selected from the group consisting of hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and C₁₋₆ haloalkyl; R⁶ and R⁷, in each instance, are independently selected from each other from the group consisting of hydrogen, R¹⁵, OR¹⁵, SR¹⁵, S (O) R¹⁵, SO₂R¹⁵, C (O) R¹⁵, CO (O) R¹⁵, OC (O) R¹⁵, OC (O) OR¹⁵, NH₂, NHR¹⁵, N (R¹⁵) ₂, NHC (O) R¹⁵, NR¹⁵C (O) R¹⁵, NHS (O) ₂R¹⁵, NR¹⁵S (O) ₂R¹⁵, NHC (O) OR¹⁵ , NR¹⁵C (O) OR¹⁵, NHC (O) NH₂, NHC (O) NHR¹⁵, NHC (O) N (R¹⁵) ₂, NR¹⁵C (O) NHR¹⁵, NR¹⁵C (O) N (R¹⁵) ₂, C (O) NH₂ , C (O) NHR¹⁵, C (O) N (R¹⁵) ₂, C (O) NHOH, C (O) NHOR¹⁵, C (O) NHSO₂R¹⁵, C (O) NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N (R¹⁵) ₂ , CO (O) H, C (O) H, OH, CN, N₃, NO₂, F, Cl, Br and I; or R⁸, in each instance, is independently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein R⁸ C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and C₁₋₆ haloalkyl are optionally substituted with one, two, three, four, five, or six substituents independently selected from the group consisting of R¹⁶ , OR¹⁶, SR¹⁶, S (O) R¹⁶, SO₂R¹⁶, C (O) R¹⁶, CO (O) R¹⁶, OC (O) R¹⁶, OC (O) OR¹⁶, NH₂, NHR¹⁶, N (R¹⁶) ₂, NHC (O ) R¹⁶, NR¹⁶C (O) R¹⁶, NHS (O) ₂R¹⁶, NR¹⁶S (O) ₂R¹⁶, NHC (O) OR¹⁶, NR¹⁶C (O) OR¹⁶, |
| priorityDate | 2011-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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