HRP20221417T1 - Heterociklički spojevi za liječenje bolesti - Google Patents
Heterociklički spojevi za liječenje bolesti Download PDFInfo
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- HRP20221417T1 HRP20221417T1 HRP20221417TT HRP20221417T HRP20221417T1 HR P20221417 T1 HRP20221417 T1 HR P20221417T1 HR P20221417T T HRP20221417T T HR P20221417TT HR P20221417 T HRP20221417 T HR P20221417T HR P20221417 T1 HRP20221417 T1 HR P20221417T1
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- Croatia
- Prior art keywords
- optionally substituted
- alkylene
- pharmaceutically acceptable
- solvate
- acceptable salt
- Prior art date
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- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- -1 substituted Chemical class 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 239000012453 solvate Substances 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 150000002431 hydrogen Chemical group 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P37/08—Antiallergic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (15)
1. Spoj, naznačen time, da je predstavljen Formulom (I), ili njegova farmaceutski prihvatljiva sol ili solvat:
[image]
u kojoj:
svaki od X1, X2, X3 i X4 je CR1;
[image]
je
[image]
Z je -O-;
svaki R1 se neovisno bira iz skupine koju čine vodik, halogen, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani aril, opcionalno supstituirani heteroaril, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani –(C1-C2 alkilen)-(C3-C8 cikloalkil), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani –(C1-C2 alkilen)-(C2-C9 heterocikloalkil), opcionalno supstituirani –(C1-C2 alkilen)-(aril), opcionalno supstituirani –(C1-C2 alkilen)-(heteroaril), -CF3, -OR10, -SR10, -N(R11)R12, -N(R11)S(O)2R15, -N(R13)N(R11)R12, -N(R13)N(R11)S(O)2R15, -C(O)R14, -C(O)OR10, -C(S)OR10, -C(O)SR10, -C(O)N(R11)R12, -C(S)N(R11)R12, -C(O)N(R11)S(O)2R15, -C(S)N(R11)S(O)2R15, -C(O)N(R13)N(R11)R12, -C(S)N(R13)N(R11)R12, i -C(O)N(R13)N(R11)S(O)2R15;
svaki R2 se neovisno bira iz skupine koju čine halogen, opcionalno supstituirani C1-C6 alkil, -OR20, -SR20, -N(R21)R22, -C(O)R20, -C(O)N(R21)R22, i -N(R23)C(O)R20;
R3 se bira iz skupine koju čine vodik, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril);
svaki od R10, R13 i R14 se neovisno bira iz skupine koju čine vodik, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril);
svaki od R11 i R12 se neovisno bira iz skupine koju čine vodik, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril); ili opcionalno R11 i R12 zajedno s atomom dušika s kojim su vezani, tvore opcionalno supstituirani C2-C9 heterocikloalkil prsten;
R15 se bira iz skupine koju čine opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril);
svaki od R20 i R23 se neovisno bira iz skupine koju čine vodik, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril);
svaki od R21 i R22 se neovisno bira iz skupine koju čine vodik, opcionalno supstituirani C1-C6 alkil, opcionalno supstituirani C2-C6 alkenil, opcionalno supstituirani C2-C6 alkinil, opcionalno supstituirani C3-C8 cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani -(C1-C2 alkilen)-(aril), opcionalno supstituirani C2-C9 heterocikloalkil, opcionalno supstituirani heteroaril, i opcionalno supstituirani -(C1-C2 alkilen)-(heteroaril); ili opcionalno R21 i R22 zajedno s atomom dušika s kojim su vezani, tvore opcionalno supstituirani C2-C9 heterocikloalkil prsten;
n je 0-4; i
p je 1.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da se svaki R1 neovisno bira iz skupine koju čine vodik, halogen, opcionalno supstituirani C1-C6 alkil, -CF3, -OR10, -N(R11)R12, -C(O)R14, -C(O)OR10, i -C(O)N(R11)R12.
3. Spoj prema patentnom zahtjevu 1 ili zahtjevu 2, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da se svaki R1 neovisno bira iz skupine koju čine vodik, halogen, i -CF3.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da se svaki R2neovisno bira iz skupine koju čine halogen, opcionalno supstituirani C1-C6 alkil, -OR20, i -N(R21)R22.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da se svaki R2 neovisno bira iz skupine koju čine halogen i opcionalno supstituirani C1-C6 alkil.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da se svaki R3 neovisno bira iz skupine koju čine vodik i opcionalno supstituirani C1-C6 alkil.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da:
[image]
je
[image]
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da:
[image]
je
[image]
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time, da n je 1 ili 2.
10. Spoj prema patentnom zahtjevu 1, naznačen time, da je:
[image]
ili njegova farmaceutski prihvatljiva sol ili solvat.
11. Spoj prema patentnom zahtjevu 1, naznačen time, da je:
[image]
ili njegova farmaceutski prihvatljiva sol ili solvat.
12. Spoj prema patentnom zahtjevu 1, naznačen time, da je:
[image]
ili njegova farmaceutski prihvatljiva sol ili solvat.
13. Spoj prema patentnom zahtjevu 1, naznačen time, da je:
[image]
ili njegova farmaceutski prihvatljiva sol ili solvat.
14. Farmaceutski pripravak, naznačen time, da sadrži farmaceutski prihvatljiv razrjeđivač, pomoćno sredstvo ili vezivno sredstvo, i spoj prema bilo kojem od patentnih zahtjeva 1 do 13, ili njegovu farmaceutski prihvatljivu sol ili solvat.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 13, ili njegova farmaceutski prihvatljivu sol ili solvat, naznačen time, da je za uporabu u postupku liječenja multiple skleroze, ulceroznog kolitisa ili Crohnove bolesti.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562255041P | 2015-11-13 | 2015-11-13 | |
| PCT/US2016/061676 WO2017083756A1 (en) | 2015-11-13 | 2016-11-11 | Heterocyclic compounds for the treatment of disease |
| EP16865156.0A EP3373931B1 (en) | 2015-11-13 | 2016-11-11 | Heterocyclic compounds for the treatment of disease |
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| Publication Number | Publication Date |
|---|---|
| HRP20221417T1 true HRP20221417T1 (hr) | 2023-02-03 |
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| Application Number | Title | Priority Date | Filing Date |
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| HRP20221417TT HRP20221417T1 (hr) | 2015-11-13 | 2016-11-11 | Heterociklički spojevi za liječenje bolesti |
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| Country | Link |
|---|---|
| US (4) | US10683291B2 (hr) |
| EP (2) | EP4163281A1 (hr) |
| JP (3) | JP6933384B2 (hr) |
| KR (1) | KR20180095811A (hr) |
| CN (2) | CN108463222B (hr) |
| AU (2) | AU2016353348A1 (hr) |
| BR (1) | BR112018009745B1 (hr) |
| CA (1) | CA3005236C (hr) |
| DK (1) | DK3373931T3 (hr) |
| ES (1) | ES2932049T3 (hr) |
| HR (1) | HRP20221417T1 (hr) |
| HU (1) | HUE060594T2 (hr) |
| IL (1) | IL259297B2 (hr) |
| LT (1) | LT3373931T (hr) |
| MX (1) | MX2018005987A (hr) |
| PL (1) | PL3373931T3 (hr) |
| PT (1) | PT3373931T (hr) |
| RS (1) | RS63837B1 (hr) |
| RU (1) | RU2727194C2 (hr) |
| SI (1) | SI3373931T1 (hr) |
| WO (1) | WO2017083756A1 (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108463222B (zh) | 2015-11-13 | 2021-10-22 | 奥比兰制药有限公司 | 用于治疗疾病的杂环化合物 |
| US20210163485A1 (en) * | 2017-05-17 | 2021-06-03 | Oppilan Pharma Ltd. | Heterocyclic Compounds for the Treatment of Disease |
| US20200071327A1 (en) * | 2017-05-17 | 2020-03-05 | Oppilan Pharma Ltd. | Prodrugs for the Treatment of Disease |
| GB201815018D0 (en) * | 2018-09-14 | 2018-10-31 | Univ Oxford Innovation Ltd | Enantiomeric compounds |
| WO2024011142A1 (en) * | 2022-07-06 | 2024-01-11 | Oppilan Pharma Limited | Crystalline forms of an s1p receptor modulator |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| US20070043014A1 (en) * | 2003-10-01 | 2007-02-22 | Merck & Co., Inc. | 3,5-Aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists |
| GB0511684D0 (en) * | 2005-06-08 | 2005-07-13 | Novartis Ag | Organic compounds |
| US20080306124A1 (en) * | 2005-06-08 | 2008-12-11 | Rainer Albert | Polycyclic Oxadiazoles or I Soxazoles and Their Use as Sip Receptor Ligands |
| RU2425832C2 (ru) * | 2006-04-03 | 2011-08-10 | Астеллас Фарма Инк. | Гетеросоединение |
| US20110207704A1 (en) | 2006-12-15 | 2011-08-25 | Abbott Laboratories | Novel Oxadiazole Compounds |
| AU2007334436A1 (en) | 2006-12-15 | 2008-06-26 | Abbott Laboratories | Novel oxadiazole compounds |
| US20100160369A1 (en) * | 2008-12-04 | 2010-06-24 | Exelixis, Inc. | S1P1 Agonists and Methods of Making And Using |
| US20100249071A1 (en) | 2009-03-30 | 2010-09-30 | Exelixis, Inc. | Modulators of S1P and Methods of Making And Using |
| US9011494B2 (en) | 2009-09-24 | 2015-04-21 | Warsaw Orthopedic, Inc. | Composite vertebral rod system and methods of use |
| CN102724880B (zh) | 2009-11-13 | 2016-09-14 | 瑞塞普托斯有限责任公司 | 1-磷酸鞘氨醇受体调节剂及手性合成方法 |
| ES2539256T3 (es) * | 2010-07-20 | 2015-06-29 | Bristol-Myers Squibb Company | Compuestos de 3-fenil-1,2,4-oxadiazol sustituidos |
| WO2013059594A1 (en) | 2011-10-20 | 2013-04-25 | Sirtris Pharmaceuticals, Inc. | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| EP3450428A1 (en) | 2013-11-27 | 2019-03-06 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| CN108463222B (zh) | 2015-11-13 | 2021-10-22 | 奥比兰制药有限公司 | 用于治疗疾病的杂环化合物 |
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2016
- 2016-11-11 CN CN201680078856.8A patent/CN108463222B/zh active Active
- 2016-11-11 SI SI201631650T patent/SI3373931T1/sl unknown
- 2016-11-11 HU HUE16865156A patent/HUE060594T2/hu unknown
- 2016-11-11 CN CN202111183182.7A patent/CN114149424A/zh active Pending
- 2016-11-11 IL IL259297A patent/IL259297B2/en unknown
- 2016-11-11 ES ES16865156T patent/ES2932049T3/es active Active
- 2016-11-11 BR BR112018009745-4A patent/BR112018009745B1/pt active IP Right Grant
- 2016-11-11 PT PT168651560T patent/PT3373931T/pt unknown
- 2016-11-11 EP EP22195151.0A patent/EP4163281A1/en active Pending
- 2016-11-11 WO PCT/US2016/061676 patent/WO2017083756A1/en active Application Filing
- 2016-11-11 EP EP16865156.0A patent/EP3373931B1/en active Active
- 2016-11-11 JP JP2018545102A patent/JP6933384B2/ja active Active
- 2016-11-11 AU AU2016353348A patent/AU2016353348A1/en not_active Abandoned
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2020
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2023
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