SG11201900619XA - Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors - Google Patents
Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitorsInfo
- Publication number
- SG11201900619XA SG11201900619XA SG11201900619XA SG11201900619XA SG11201900619XA SG 11201900619X A SG11201900619X A SG 11201900619XA SG 11201900619X A SG11201900619X A SG 11201900619XA SG 11201900619X A SG11201900619X A SG 11201900619XA SG 11201900619X A SG11201900619X A SG 11201900619XA
- Authority
- SG
- Singapore
- Prior art keywords
- bristol
- route
- international
- new jersey
- myers squibb
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 125000005805 dimethoxy phenyl group Chemical group 0.000 title 1
- 150000002475 indoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 101150057615 Syn gene Proteins 0.000 abstract 2
- 102100039390 Toll-like receptor 7 Human genes 0.000 abstract 2
- 102100033110 Toll-like receptor 8 Human genes 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 102220240796 rs553605556 Human genes 0.000 abstract 2
- -1 DIMETHOXYPHENYL Chemical group 0.000 abstract 1
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 abstract 1
- 101000800483 Homo sapiens Toll-like receptor 8 Proteins 0.000 abstract 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 abstract 1
- 108010060752 Toll-Like Receptor 8 Proteins 0.000 abstract 1
- 102000008235 Toll-Like Receptor 9 Human genes 0.000 abstract 1
- 108010060818 Toll-Like Receptor 9 Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 08 February 2018 (08.02.2018) WIPO I PCT °mons °nolo omolom (10) International Publication Number WO 2018/026620 Al (51) International Patent Classification: CO7D 401/14 (2006.01) A61K 31/404 (2006.01) CO7D 405/14 (2006.01) A61K 31/454 (2006.01) C07D 401/04 (2006.01) A61P 29/00 (2006.01) C07D 417/14 (2006.01) A61P 37/00 (2006.01) (21) International Application Number: PCT/US2017/044091 (22) International Filing Date: 27 July 2017 (27.07.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 11026137 30 July 2016 (30.07.2016) IN (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). (72) Inventors: DYCKMAN, Alaric J.; c/o Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). DODD, Dharmpal S.; c/o Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). MUSSARI, Christopher P.; c/o Bristol-Myers Squibb Company, Route 206 and Province Line Road, Prince- ton, New Jersey 08543 (US). HAQUE, Tasir S.; 351 Denny Drive, Yardley, Pennsylvania 19067 (US). POSS, Declarations under Rule 4.17: Michael A.; c/o Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). LOMBARDO, Louis J.; c/o Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). MACOR, John E.; 55 Com- manders Drive, Washington Crossing, Pennsylvania 18977 (US). PASUNOORI, Laxman; c/o SYNGENE INTER- NATIONAL LIMITED, Biocon Special Economic Zone, Biocon Park, Plot No. 2 & 3, Bommasandra Industrial Area IV Phase, Jigani Link Road, Bommasandra, Banga- lore, Karnataka 560 099 (IN). KUMAR, Sreekantha Rat- na; c/o SYNGENE INTERNATIONAL LIMITED, Biocon Special Economic Zone, Biocon Park, Plot No. 2 & 3, Bom- masandra Industrial Area IV Phase, Jigani Link Road, Bom- masandra, Bangalore, Karnataka 560 099 (IN). (74) Agent: GREENBLATT, Gary D. et al.; Bristol-Myers Squibb Company, Route 206 & Province Line Road, Prince- ton, New Jersey 08543 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) (54) Title: DIMETHOXYPHENYL SUBSTITUTED INDOLE COMPOUNDS AS TLR7, TLR8 OR TLR9 INHIBITORS W O 20 18/0266 20 Al (57) : Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R3, R4, R 5 , m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll- like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and au- toimmune diseases.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201611026137 | 2016-07-30 | ||
| PCT/US2017/044091 WO2018026620A1 (en) | 2016-07-30 | 2017-07-27 | Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201900619XA true SG11201900619XA (en) | 2019-02-27 |
Family
ID=61073069
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201900619XA SG11201900619XA (en) | 2016-07-30 | 2017-07-27 | Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11180474B2 (en) |
| EP (1) | EP3490983B1 (en) |
| JP (1) | JP6995109B2 (en) |
| KR (1) | KR102506321B1 (en) |
| CN (1) | CN109715617B (en) |
| AU (1) | AU2017307208B2 (en) |
| BR (1) | BR112019001270A2 (en) |
| CA (1) | CA3031675A1 (en) |
| EA (1) | EA038972B1 (en) |
| ES (1) | ES2863474T3 (en) |
| IL (1) | IL264462B (en) |
| MX (1) | MX391344B (en) |
| SG (1) | SG11201900619XA (en) |
| WO (1) | WO2018026620A1 (en) |
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| CA3031675A1 (en) | 2016-07-30 | 2018-02-08 | Bristol-Myers Squibb Company | Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors |
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| JP7104775B2 (en) | 2017-08-04 | 2022-07-21 | ブリストル-マイヤーズ スクイブ カンパニー | Substituted indole compounds useful as inhibitors of TLR7 / 8/9 |
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| SG11202005704RA (en) | 2017-12-19 | 2020-07-29 | Bristol Myers Squibb Co | 6-azaindole compounds |
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| CN111566120B (en) | 2017-12-20 | 2023-09-29 | 捷克共和国有机化学与生物化学研究所 | 3’3’ cyclic dinucleotide with phosphonate bond that activates STING adapter protein |
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