SG11201811393WA - Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer - Google Patents
Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancerInfo
- Publication number
- SG11201811393WA SG11201811393WA SG11201811393WA SG11201811393WA SG11201811393WA SG 11201811393W A SG11201811393W A SG 11201811393WA SG 11201811393W A SG11201811393W A SG 11201811393WA SG 11201811393W A SG11201811393W A SG 11201811393WA SG 11201811393W A SG11201811393W A SG 11201811393WA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- street
- cancer
- ucsf
- san francisco
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
WO 17 / 2235 16 Al (I) 0 N ‘>-NH R 6 NH N (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 28 December 2017 (28.12.2017) WIPO I PCT o 1E1 olo VIII Holm o Hum! oil Em Hi m° lII ois (10) International Publication Number WO 2017/223516 Al (51) International Patent Classification: CO7D 403/10 (2006.01) CO7D 403/14 (2006.01) CO7D 405/14 (2006.01) A61K 31/502 (2006.01) C07D 471/04 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) (21) International Application Number: PCT/US2017/039119 (22) International Filing Date: 23 June 2017 (23.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/354,449 24 June 2016 (24.06.2016) US 62/426,095 23 November 2016 (23.11.2016) US (71) Applicants: THE REGENTS OF THE UNIVERSI- TY OF CALIFORNIA [US/US]; 1111 Franklin Street, Twelfth Floor, Oakland, CA 94607-5200 (US). AT- LASMEDX, INC. [US/US]; UCSF Mission Bay Cam- pus,1700 4th Street, Byers Hall 214, MC 2522, San Fran- cisco, California 94158-2330 (US). (72) Inventors: TSANG, Tsze; 8367 Kent Drive, El Cerrito, CA 94530 (US). PETO, Csaba, J.; c/o UCSF Mt Zion Can- cer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). JABLONS, David, M.; c/o UCSF Mt Zion Cancer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). LEMJABBAR-ALAOUI, Hassan; c/o UCSF Mt Zion Cancer Research Bldg., 2340 Sutter Street, San Francisco, CA 94143 (US). (74) Agent: ESKER, Todd et al.; Morgan, Lewis & Bockius LLP, One Market, Spear Street Tower, San Francisco, CA 94105 (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). Declarations under Rule 4.17: 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)) Published: — with international search report (Art. 21(3)) (54) Title: PHTHALAZINE DERIVATIVES AS INHIBITORS OF PARP1, PARP2 AND/OR TUBULIN USEFUL FOR THE TREATMENT OF CANCER (57) : The application relates to phthalazine derivatives of formula (I) which are inhibitors of PARP1, PARP2 and/or tubulin and thus useful for the treatment of cancer. Also disclosed are pharmaceuti- cal formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662354449P | 2016-06-24 | 2016-06-24 | |
| US201662426095P | 2016-11-23 | 2016-11-23 | |
| PCT/US2017/039119 WO2017223516A1 (en) | 2016-06-24 | 2017-06-23 | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201811393WA true SG11201811393WA (en) | 2019-01-30 |
Family
ID=59297390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201811393WA SG11201811393WA (en) | 2016-06-24 | 2017-06-23 | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US11072600B2 (en) |
| EP (1) | EP3475272B1 (en) |
| JP (2) | JP7033588B2 (en) |
| KR (1) | KR102494294B1 (en) |
| CN (1) | CN109843874B (en) |
| AU (1) | AU2017280334C1 (en) |
| BR (1) | BR112018076821A2 (en) |
| CA (1) | CA3029004A1 (en) |
| ES (1) | ES2964531T3 (en) |
| HU (1) | HUE066216T2 (en) |
| IL (1) | IL263917B (en) |
| MX (2) | MX2018015893A (en) |
| PL (1) | PL3475272T3 (en) |
| PT (1) | PT3475272T (en) |
| SG (1) | SG11201811393WA (en) |
| WO (1) | WO2017223516A1 (en) |
| ZA (2) | ZA201808562B (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016187620A2 (en) | 2015-05-21 | 2016-11-24 | The Regents Of The University Of California | Anti-cancer compounds |
| US11028055B2 (en) | 2015-11-30 | 2021-06-08 | Children's Medical Center Corporation | Compounds for treating proliferative diseases |
| PL3475272T3 (en) | 2016-06-24 | 2024-04-29 | The Regents Of The University Of California | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
| JP7372253B2 (en) * | 2018-04-05 | 2023-10-31 | ノビガ・リサーチ・エービー | Novel combinations of tubulin polymerization inhibitors and poly(ADP-ribose) polymerase (PARP) inhibitors for use in the treatment of cancer |
| CN112574122B (en) * | 2019-09-27 | 2024-05-31 | 上海天慈国际药业有限公司 | Preparation method of Olaparib key intermediate |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3401171A (en) | 1966-03-11 | 1968-09-10 | Smithkline Corp | 2-amidobenzimidazoles |
| SU1019810A1 (en) | 1981-07-28 | 1991-04-07 | Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского | Methyl ester of 5(6)-/1-(2n)-phthalasionyl-4/-1n-benzaimidozolyl-2-carbamic acid displaying antihelminth activity |
| SU1218649A1 (en) | 1984-09-19 | 1991-04-30 | Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского | Method of producing methyl ester of 5(6)-[1(2n)-phthazinoyl-4-]-benzimidazolyl-2-carbamic acid |
| JP2002502844A (en) | 1998-02-03 | 2002-01-29 | ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト | 5-membered heterocyclic fused benzo derivatives, their preparation and their use as pharmaceuticals |
| KR20010101675A (en) | 1999-01-26 | 2001-11-14 | 우에노 도시오 | 2h-phthalazin-1-one derivatives and drugs comprising these derivatives as the active ingredient |
| DE19907813A1 (en) | 1999-02-24 | 2000-08-31 | Boehringer Ingelheim Pharma | Substituted bicyclic heterocycles, their preparation and their use as pharmaceuticals |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| EA006300B1 (en) | 2000-10-30 | 2005-10-27 | Кудос Фармасеутикалс Лимитед | Phthalazinone derivatives |
| AR042956A1 (en) | 2003-01-31 | 2005-07-13 | Vertex Pharma | GIRASA INHIBITORS AND USES OF THE SAME |
| CA2517629C (en) | 2003-03-12 | 2011-07-12 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| CA2565200C (en) | 2004-05-07 | 2013-12-24 | Exelixis, Inc. | Raf modulators and methods of use |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| CN101291928A (en) * | 2005-10-19 | 2008-10-22 | 库多斯药物有限公司 | 4-heteroarylmethyl substituted phthalazinone derivatives |
| TWI404716B (en) | 2006-10-17 | 2013-08-11 | Kudos Pharm Ltd | Phthalazinone derivative |
| US20080280910A1 (en) | 2007-03-22 | 2008-11-13 | Keith Allan Menear | Phthalazinone derivatives |
| WO2009118382A1 (en) * | 2008-03-27 | 2009-10-01 | Janssen Pharmaceutica Nv | Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors |
| EP2529235B1 (en) | 2010-01-29 | 2019-03-06 | Metanomics GmbH | Means and methods for diagnosing heart failure in a subject |
| CN102372706A (en) | 2010-08-09 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | Phthalazinone derivative, its preparation method and application in medicament |
| WO2012166983A1 (en) | 2011-05-31 | 2012-12-06 | Newgen Therapeutics, Inc. | Tricyclic inhibitors of poly(adp-ribose)polymerase |
| KR101546743B1 (en) * | 2012-01-16 | 2015-08-24 | 한국과학기술원 | Indole derivatives, Abl kinase inhibiting composition and pharmaceutical compositions for prevention and treatment of abnormal cell growth diseases comprising the same |
| NZ708255A (en) * | 2012-12-31 | 2016-08-26 | Cadila Healthcare Ltd | Substituted phthalazin-1 (2h)-one derivatives as selective inhibitors of poly (adp-ribose) polymerase-1 |
| TWI527811B (en) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | Benzimidazole derivatives as bromodomain inhibitors |
| PL3475272T3 (en) * | 2016-06-24 | 2024-04-29 | The Regents Of The University Of California | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
-
2017
- 2017-06-23 PL PL17737132.5T patent/PL3475272T3/en unknown
- 2017-06-23 IL IL263917A patent/IL263917B/en unknown
- 2017-06-23 ES ES17737132T patent/ES2964531T3/en active Active
- 2017-06-23 CN CN201780051422.3A patent/CN109843874B/en active Active
- 2017-06-23 MX MX2018015893A patent/MX2018015893A/en unknown
- 2017-06-23 SG SG11201811393WA patent/SG11201811393WA/en unknown
- 2017-06-23 KR KR1020197002267A patent/KR102494294B1/en active IP Right Grant
- 2017-06-23 CA CA3029004A patent/CA3029004A1/en active Pending
- 2017-06-23 JP JP2019519615A patent/JP7033588B2/en active Active
- 2017-06-23 HU HUE17737132A patent/HUE066216T2/en unknown
- 2017-06-23 AU AU2017280334A patent/AU2017280334C1/en active Active
- 2017-06-23 EP EP17737132.5A patent/EP3475272B1/en active Active
- 2017-06-23 WO PCT/US2017/039119 patent/WO2017223516A1/en unknown
- 2017-06-23 BR BR112018076821-9A patent/BR112018076821A2/en active Search and Examination
- 2017-06-23 PT PT177371325T patent/PT3475272T/en unknown
- 2017-06-23 US US16/310,606 patent/US11072600B2/en active Active
-
2018
- 2018-12-17 MX MX2021013641A patent/MX2021013641A/en unknown
- 2018-12-19 ZA ZA2018/08562A patent/ZA201808562B/en unknown
-
2019
- 2019-07-30 US US16/526,620 patent/US10640493B2/en active Active
-
2021
- 2021-07-15 US US17/376,577 patent/US20220402894A1/en active Pending
- 2021-11-26 JP JP2021192564A patent/JP2022037004A/en active Pending
-
2023
- 2023-01-25 ZA ZA2023/01066A patent/ZA202301066B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2019522681A (en) | 2019-08-15 |
| US11072600B2 (en) | 2021-07-27 |
| BR112018076821A2 (en) | 2019-04-02 |
| PT3475272T (en) | 2023-12-15 |
| AU2017280334B2 (en) | 2021-07-29 |
| HUE066216T2 (en) | 2024-07-28 |
| MX2021013641A (en) | 2022-01-06 |
| AU2017280334A1 (en) | 2019-01-17 |
| KR102494294B1 (en) | 2023-01-31 |
| ZA202301066B (en) | 2024-05-30 |
| CA3029004A1 (en) | 2017-12-28 |
| US20190352283A1 (en) | 2019-11-21 |
| ZA201808562B (en) | 2023-12-20 |
| MX2018015893A (en) | 2019-08-01 |
| ES2964531T3 (en) | 2024-04-08 |
| PL3475272T3 (en) | 2024-04-29 |
| WO2017223516A1 (en) | 2017-12-28 |
| US20220402894A1 (en) | 2022-12-22 |
| US10640493B2 (en) | 2020-05-05 |
| EP3475272B1 (en) | 2023-09-13 |
| EP3475272A1 (en) | 2019-05-01 |
| IL263917B (en) | 2022-07-01 |
| JP7033588B2 (en) | 2022-03-10 |
| AU2017280334C1 (en) | 2022-10-20 |
| CN109843874B (en) | 2022-05-27 |
| US20190337928A1 (en) | 2019-11-07 |
| CN109843874A (en) | 2019-06-04 |
| IL263917A (en) | 2019-02-28 |
| KR20190033534A (en) | 2019-03-29 |
| JP2022037004A (en) | 2022-03-08 |
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