CA3085937A1 - Diazaindole compounds - Google Patents
Diazaindole compounds Download PDFInfo
- Publication number
- CA3085937A1 CA3085937A1 CA3085937A CA3085937A CA3085937A1 CA 3085937 A1 CA3085937 A1 CA 3085937A1 CA 3085937 A CA3085937 A CA 3085937A CA 3085937 A CA3085937 A CA 3085937A CA 3085937 A1 CA3085937 A1 CA 3085937A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- pyrrolo
- nrx
- piperidinyl
- pyridinyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical class C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 title description 5
- 150000001875 compounds Chemical class 0.000 claims abstract description 153
- 150000003839 salts Chemical class 0.000 claims abstract description 45
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 26
- 150000001204 N-oxides Chemical class 0.000 claims abstract description 22
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract description 14
- -1 diazaspiro[4.5]decanonyl Chemical group 0.000 claims description 477
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 181
- 125000000217 alkyl group Chemical group 0.000 claims description 166
- 125000003386 piperidinyl group Chemical group 0.000 claims description 123
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 113
- 125000004076 pyridyl group Chemical group 0.000 claims description 99
- 125000002757 morpholinyl group Chemical group 0.000 claims description 95
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 92
- 125000004193 piperazinyl group Chemical group 0.000 claims description 86
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 81
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 70
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 68
- 125000001424 substituent group Chemical group 0.000 claims description 65
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 60
- 125000002393 azetidinyl group Chemical group 0.000 claims description 56
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 54
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 45
- 201000006417 multiple sclerosis Diseases 0.000 claims description 44
- 229910052757 nitrogen Inorganic materials 0.000 claims description 44
- 125000005959 diazepanyl group Chemical group 0.000 claims description 42
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 41
- 125000003566 oxetanyl group Chemical group 0.000 claims description 38
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 36
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 35
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 34
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 125000002883 imidazolyl group Chemical group 0.000 claims description 26
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 26
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 25
- 229910052801 chlorine Inorganic materials 0.000 claims description 24
- 229910052731 fluorine Inorganic materials 0.000 claims description 24
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 22
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 20
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 20
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 108010011222 cyclo(Arg-Pro) Proteins 0.000 claims description 19
- 125000001425 triazolyl group Chemical group 0.000 claims description 19
- 125000003725 azepanyl group Chemical group 0.000 claims description 18
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 18
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 17
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 17
- VMWJCFLUSKZZDX-UHFFFAOYSA-N n,n-dimethylmethanamine Chemical compound [CH2]N(C)C VMWJCFLUSKZZDX-UHFFFAOYSA-N 0.000 claims description 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 15
- 125000004432 carbon atom Chemical group C* 0.000 claims description 15
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims description 15
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 15
- 125000003944 tolyl group Chemical group 0.000 claims description 15
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 14
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 14
- 125000001544 thienyl group Chemical group 0.000 claims description 14
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 13
- 239000003937 drug carrier Substances 0.000 claims description 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 13
- 125000000335 thiazolyl group Chemical group 0.000 claims description 13
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- 125000002541 furyl group Chemical group 0.000 claims description 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 12
- 125000004122 cyclic group Chemical group 0.000 claims description 11
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 10
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 8
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 8
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 claims description 8
- 125000001041 indolyl group Chemical group 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 125000005879 dioxolanyl group Chemical group 0.000 claims description 7
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 7
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 7
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 7
- 125000002971 oxazolyl group Chemical group 0.000 claims description 7
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 7
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims description 7
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 7
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 7
- 125000001984 thiazolidinyl group Chemical group 0.000 claims description 7
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- DBTDEFJAFBUGPP-UHFFFAOYSA-N Methanethial Chemical compound S=C DBTDEFJAFBUGPP-UHFFFAOYSA-N 0.000 claims description 5
- AQWOIRBQLOOZGX-UHFFFAOYSA-N triazolo[1,5-a]pyridine Chemical compound C1=CC=CC2=CN=NN21 AQWOIRBQLOOZGX-UHFFFAOYSA-N 0.000 claims description 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 4
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical compound C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 claims description 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 4
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims description 4
- PZKFSRWSQOQYNR-UHFFFAOYSA-N 5-methyl-1h-1,2,4-triazole Chemical compound CC1=NC=NN1 PZKFSRWSQOQYNR-UHFFFAOYSA-N 0.000 claims description 3
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims description 3
- 208000037976 chronic inflammation Diseases 0.000 claims description 3
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims description 3
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims description 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 3
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 3
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims description 2
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 claims description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- IPZJQDSFZGZEOY-UHFFFAOYSA-N dimethylmethylene Chemical compound C[C]C IPZJQDSFZGZEOY-UHFFFAOYSA-N 0.000 claims description 2
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims description 2
- JJWLVOIRVHMVIS-UHFFFAOYSA-N isopropylamine Chemical compound CC(C)N JJWLVOIRVHMVIS-UHFFFAOYSA-N 0.000 claims description 2
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 241001645982 Crax Species 0.000 claims 3
- SWAOUIZDHXCDEB-UHFFFAOYSA-N 2-methyl-[1,2,4]triazolo[1,5-a]pyridine Chemical compound C1=CC=CN2N=C(C)N=C21 SWAOUIZDHXCDEB-UHFFFAOYSA-N 0.000 claims 2
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 2
- LENLQGBLVGGAMF-UHFFFAOYSA-N tributyl([1,2,4]triazolo[1,5-a]pyridin-6-yl)stannane Chemical compound C1=C([Sn](CCCC)(CCCC)CCCC)C=CC2=NC=NN21 LENLQGBLVGGAMF-UHFFFAOYSA-N 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 1
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 1
- 235000019256 formaldehyde Nutrition 0.000 claims 1
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762607941P | 2017-12-20 | 2017-12-20 | |
| US62/607,941 | 2017-12-20 | ||
| PCT/US2018/066108 WO2019126083A1 (en) | 2017-12-20 | 2018-12-18 | Diazaindole compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3085937A1 true CA3085937A1 (en) | 2019-06-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3085937A Pending CA3085937A1 (en) | 2017-12-20 | 2018-12-18 | Diazaindole compounds |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11299501B2 (enExample) |
| EP (1) | EP3728264B1 (enExample) |
| JP (1) | JP7382938B2 (enExample) |
| KR (1) | KR102722182B1 (enExample) |
| CN (1) | CN111511744B (enExample) |
| AU (1) | AU2018390544A1 (enExample) |
| BR (1) | BR112020012002A2 (enExample) |
| CA (1) | CA3085937A1 (enExample) |
| EA (1) | EA202091530A1 (enExample) |
| ES (1) | ES2904773T3 (enExample) |
| IL (1) | IL275505A (enExample) |
| MX (1) | MX2020006014A (enExample) |
| SG (1) | SG11202005733QA (enExample) |
| WO (1) | WO2019126083A1 (enExample) |
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| US10071079B2 (en) | 2016-06-29 | 2018-09-11 | Bristol-Myers Squibb Company | [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds |
| ES2965182T3 (es) * | 2017-12-20 | 2024-04-11 | Bristol Myers Squibb Co | Compuestos de indol sustituidos con arilo y heteroarilo |
| MX2020005513A (es) * | 2017-12-20 | 2020-09-03 | Bristol Myers Squibb Co | Compuestos de amino indol utiles como inhibidores de receptores tipo toll (tlr). |
| EP3752505B1 (en) | 2018-02-12 | 2023-01-11 | F. Hoffmann-La Roche AG | Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection |
| BR112020024782A2 (pt) | 2018-06-05 | 2021-03-02 | F. Hoffmann-La Roche Ag | compostos de tetra-hidro-1h-pirazino[2,1-a]isoindolilquinolina para o tratamento de doença autoimune |
| EP3807270B1 (en) | 2018-06-12 | 2023-09-13 | F. Hoffmann-La Roche AG | Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease |
| WO2020020800A1 (en) | 2018-07-23 | 2020-01-30 | F. Hoffmann-La Roche Ag | Novel piperazine compounds for the treatment of autoimmune disease |
| US11639352B2 (en) | 2018-09-04 | 2023-05-02 | Hoffman-La Roche Inc. | Benzothiazole compounds for the treatment of autoimmune diseases |
| EP3847173B1 (en) | 2018-09-06 | 2023-04-12 | F. Hoffmann-La Roche AG | Novel pyrazolopyridine compounds for the treatment of autoimmune disease |
| WO2020048595A1 (en) | 2018-09-06 | 2020-03-12 | F. Hoffmann-La Roche Ag | Novel cyclic amidine compounds for the treatment of autoimmune disease |
| US12421240B2 (en) | 2019-10-31 | 2025-09-23 | Hoffmann-La Roche Inc. | Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease |
| WO2021099284A1 (en) | 2019-11-19 | 2021-05-27 | F. Hoffmann-La Roche Ag | Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease |
| CN114728988B (zh) | 2019-11-20 | 2024-12-10 | 豪夫迈·罗氏有限公司 | 用于治疗自身免疫性疾病的螺(异苯并呋喃氮杂环丁烷)化合物 |
| CN116075510A (zh) | 2020-08-19 | 2023-05-05 | 百时美施贵宝公司 | 1H-苯并[d]咪唑衍生物作为TLR9抑制剂用于治疗纤维化 |
| AR123281A1 (es) | 2020-08-19 | 2022-11-16 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos útiles como inhibidores de tlr9 |
| WO2022166920A1 (zh) * | 2021-02-08 | 2022-08-11 | 杭州中美华东制药有限公司 | 一种吡咯并哒嗪类化合物及其制备方法和用途 |
| CN116783202A (zh) * | 2021-02-09 | 2023-09-19 | 吉利德科学公司 | 噻吩并吡咯化合物 |
| JP2024513945A (ja) | 2021-04-16 | 2024-03-27 | ギリアード サイエンシーズ， インコーポレイテッド | チオノピロール化合物 |
| CN117957234A (zh) | 2021-09-10 | 2024-04-30 | 吉利德科学公司 | 噻吩并吡咯化合物 |
| KR20240148414A (ko) * | 2022-02-18 | 2024-10-11 | 브리스톨-마이어스 스큅 컴퍼니 | Tlr9의 억제제로서 유용한 치환된 이미다조피리디닐 화합물 |
| CN114591339B (zh) * | 2022-05-10 | 2022-08-02 | 上海维申医药有限公司 | 一类Toll样受体抑制剂及其制备和应用 |
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| GEP20053530B (en) | 1999-10-19 | 2005-05-25 | Merck & Co Inc | Tyrosine Kinase Inhibitors, Pharmaceutical Compositions Containing Them and Use Thereof |
| IL162884A0 (en) | 2002-01-07 | 2005-11-20 | Eisai Co Ltd | Deazapurines and uses thereof |
| BRPI0411514A (pt) | 2003-06-20 | 2006-08-01 | Coley Pharm Gmbh | antagonistas de receptor toll-like de molécula pequena |
| US20060235037A1 (en) | 2005-04-15 | 2006-10-19 | Purandare Ashok V | Heterocyclic inhibitors of protein arginine methyl transferases |
| US20090099179A1 (en) | 2006-04-04 | 2009-04-16 | Myriad Genetics, Incorporated | Compounds for diseases and disorders |
| DE102006033109A1 (de) | 2006-07-18 | 2008-01-31 | Grünenthal GmbH | Substituierte Heteroaryl-Derivate |
| US8027888B2 (en) | 2006-08-31 | 2011-09-27 | Experian Interactive Innovation Center, Llc | Online credit card prescreen systems and methods |
| US7977352B2 (en) | 2006-12-01 | 2011-07-12 | Galapagos Nv | Triazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases |
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| EP2340243B1 (en) | 2008-10-17 | 2014-10-08 | Boehringer Ingelheim International GmbH | Heteroaryl substituted indole compounds useful as mmp-13 inhibitors |
| TWI462920B (zh) | 2009-06-26 | 2014-12-01 | 葛萊伯格有限公司 | 用於治療退化性及發炎疾病之新穎化合物 |
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| CN102574788A (zh) | 2009-09-24 | 2012-07-11 | 弗·哈夫曼-拉罗切有限公司 | 作为crac调节剂的吲哚衍生物 |
| CN102665715A (zh) | 2009-10-22 | 2012-09-12 | 沃泰克斯药物股份有限公司 | 治疗囊性纤维化和其他慢性疾病的组合物 |
| JP2013166700A (ja) * | 2010-06-02 | 2013-08-29 | Dainippon Sumitomo Pharma Co Ltd | 新規４，５−縮環ピリミジン誘導体 |
| WO2012054862A2 (en) | 2010-10-21 | 2012-04-26 | The Brigham And Women's Hospital, Inc. | Agents, compositions, and methods for treating pruritis and related skin conditions |
| PL2663550T3 (pl) | 2011-01-12 | 2017-07-31 | Ventirx Pharmaceuticals, Inc. | Podstawione benzoazepiny jako modulatory receptora toll-podobnego |
| HUE032638T2 (en) | 2011-01-12 | 2017-10-30 | Ventirx Pharmaceuticals Inc | Toll receptor modulator substituted benzoazepines |
| AU2012262021B2 (en) | 2011-06-01 | 2016-07-28 | Janus Biotherapeutics, Inc. | Novel immune system modulators |
| KR102052215B1 (ko) | 2011-06-01 | 2019-12-04 | 야누스 바이오테라퓨틱스, 인크. | 신규한 면역 시스템 조절제 |
| AU2012267556B9 (en) | 2011-06-09 | 2017-05-11 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of GPR-119 |
| ES2555167T3 (es) | 2011-07-15 | 2015-12-29 | Janssen Pharmaceuticals, Inc. | Nuevos derivados de indol sustituidos como moduladores de gamma secretasa |
| JP2013075834A (ja) * | 2011-09-29 | 2013-04-25 | Kowa Co | Ｔｌｒ９阻害活性を有するピラゾロピリミジン−７−アミン誘導体 |
| EP2763677B1 (en) | 2011-10-04 | 2020-02-26 | Janus Biotherapeutics, Inc. | Novel imidazole quinoline-based immune system modulators |
| WO2013092444A1 (en) | 2011-12-20 | 2013-06-27 | F. Hoffmann-La Roche Ag | Diazaindole inhibitors of crac |
| RU2636146C2 (ru) | 2012-05-18 | 2017-11-21 | Сумитомо Дайниппон Фарма Ко., Лтд. | Соединения карбоновых кислот |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| WO2014026125A1 (en) * | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| EP2738172A1 (en) | 2012-11-28 | 2014-06-04 | Almirall, S.A. | New bicyclic compounds as crac channel modulators |
| MY192489A (en) | 2013-10-14 | 2022-08-23 | Eisai R&D Man Co Ltd | Selectively substituted quinoline compounds |
| US9643967B2 (en) | 2013-12-13 | 2017-05-09 | Takeda Pharmaceutical Company Limited | Pyrrolo[3,2-c]pyridine derivatives as TLR inhibitors |
| MX386981B (es) | 2014-08-15 | 2025-03-19 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Compuestos de pirrolopirimidina usados como agonistas del receptor de tipo toll 7 (tlr7). |
| WO2016029077A1 (en) | 2014-08-22 | 2016-02-25 | Janus Biotherapeutics, Inc. | Novel n2, n4, n7, 6-tetrasubstituted pteridine-2,4,7-triamine and 2, 4, 6, 7-tetrasubstituted pteridine compounds and methods of synthesis and use thereof |
| US10071079B2 (en) | 2016-06-29 | 2018-09-11 | Bristol-Myers Squibb Company | [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds |
| KR102506321B1 (ko) | 2016-07-30 | 2023-03-03 | 브리스톨-마이어스 스큅 컴퍼니 | Tlr7, tlr8 또는 tlr9 억제제로서의 디메톡시페닐 치환된 인돌 화합물 |
| WO2018049089A1 (en) | 2016-09-09 | 2018-03-15 | Bristol-Myers Squibb Company | Pyridyl substituted indole compounds |
| EP3710440B1 (en) * | 2017-11-14 | 2023-04-05 | Bristol-Myers Squibb Company | Substituted indole compounds |
| LT3728252T (lt) * | 2017-12-18 | 2023-10-25 | Bristol-Myers Squibb Company | 4-azaindolo junginiai |
| US11427580B2 (en) * | 2017-12-19 | 2022-08-30 | Bristol-Myers Squibb Company | 6-azaindole compounds |
-
2018
- 2018-12-18 MX MX2020006014A patent/MX2020006014A/es unknown
- 2018-12-18 CN CN201880082762.7A patent/CN111511744B/zh active Active
- 2018-12-18 AU AU2018390544A patent/AU2018390544A1/en not_active Abandoned
- 2018-12-18 ES ES18830674T patent/ES2904773T3/es active Active
- 2018-12-18 EA EA202091530A patent/EA202091530A1/ru unknown
- 2018-12-18 SG SG11202005733QA patent/SG11202005733QA/en unknown
- 2018-12-18 KR KR1020207020851A patent/KR102722182B1/ko active Active
- 2018-12-18 BR BR112020012002-2A patent/BR112020012002A2/pt not_active Application Discontinuation
- 2018-12-18 CA CA3085937A patent/CA3085937A1/en active Pending
- 2018-12-18 EP EP18830674.0A patent/EP3728264B1/en active Active
- 2018-12-18 JP JP2020534861A patent/JP7382938B2/ja active Active
- 2018-12-18 WO PCT/US2018/066108 patent/WO2019126083A1/en not_active Ceased
- 2018-12-18 US US16/955,108 patent/US11299501B2/en active Active
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2020
- 2020-06-18 IL IL275505A patent/IL275505A/en unknown
Also Published As
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|---|---|
| IL275505A (en) | 2020-08-31 |
| MX2020006014A (es) | 2020-08-17 |
| CN111511744B (zh) | 2023-09-22 |
| US20200308195A1 (en) | 2020-10-01 |
| CN111511744A (zh) | 2020-08-07 |
| AU2018390544A1 (en) | 2020-08-06 |
| SG11202005733QA (en) | 2020-07-29 |
| EA202091530A1 (ru) | 2020-09-14 |
| KR20200100760A (ko) | 2020-08-26 |
| US11299501B2 (en) | 2022-04-12 |
| WO2019126083A1 (en) | 2019-06-27 |
| EP3728264A1 (en) | 2020-10-28 |
| BR112020012002A2 (pt) | 2020-11-17 |
| EP3728264B1 (en) | 2021-12-01 |
| ES2904773T3 (es) | 2022-04-06 |
| JP7382938B2 (ja) | 2023-11-17 |
| KR102722182B1 (ko) | 2024-10-24 |
| JP2021506941A (ja) | 2021-02-22 |
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