SG11201804204QA - Process for the preparation of tricyclic pi3k inhibitor compounds and methods for using the same for the treatment of cancer - Google Patents
Process for the preparation of tricyclic pi3k inhibitor compounds and methods for using the same for the treatment of cancerInfo
- Publication number
- SG11201804204QA SG11201804204QA SG11201804204QA SG11201804204QA SG11201804204QA SG 11201804204Q A SG11201804204Q A SG 11201804204QA SG 11201804204Q A SG11201804204Q A SG 11201804204QA SG 11201804204Q A SG11201804204Q A SG 11201804204QA SG 11201804204Q A SG11201804204Q A SG 11201804204QA
- Authority
- SG
- Singapore
- Prior art keywords
- genentech
- international
- dna
- san francisco
- way
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine 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
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Microbiology (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physiology (AREA)
- Mycology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau (43) International Publication Date .... ....r .„,„1 22 June 2017(22.06.2017) WIPO I PCT (10) WO International 111111111111311111111111111111111111111111111111111111111111111111111111111111111111111111 2017/106647 Publication Al Number (51) International Patent Classification: (74) Agents: CULLMAN, Louis, C. et al.; K&L Gates LLP, 1 A61K 31/519 (2006.01) CO7D 498/14 (2006.01) Park Plaza, Twelfth Floor, Irvine, CA 92614 (US). A61K 31/5383 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/US2016/067174 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, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 16 December 2016 (16.12.2016) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (25) Filing Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (30) Priority Data: RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 62/268,149 16 December 2015 (16.12.2015) US TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 62/288,832 29 January 2016 (29.01.2016) US ZA, ZM, ZW. 62/291,248 4 February 2016 (04.02.2016) US (84) Designated States (unless otherwise indicated, for every (71) Applicant: GENENTECH, INC. [US/US]; 1 DNA Way, kind of regional protection available): ARIPO (BW, GH, South San Francisco, CA 94080 (US). GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors: STUMPF, Andreas; Genentech, Inc., 1 DNA TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Way, South San Francisco, CA 94080 (US). AN- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, GELAUD, Remy; Genentech, Inc., 1 DNA Way, South LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, San Francisco, CA 94080 (US). MCCLORY, Andrew; SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Genentech, Inc., 1 DNA Way, South San Francisco, CA GW, KM, ML, MR, NE, SN, TD, TG). 94080 YAJIMA, Herbert; Genentech, Inc., 1 DNA (US). Published: Way, South San Francisco, CA 94080 (US). NDUBAKU, Chudi; Genentech, Inc., 1 DNA Way, South San Fran- — with international search report (Art 21(3)) cisco, CA 94080 (US). OLIVERO, Alan; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). (54) Title: PROCESS FOR THE PREPARATION OF TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS FOR US- ING THE SAME FOR THE TREATMENT OF CANCER GDC-0084 in AcOH, Water Mixtures at 70°C 0.7 0.6 0.5 —x—AcOH/water 98:2 0. 4 —s—AcOH/water 9:1 % acetate amide —N—AcOH/water 4:1 0.3 - 0.2 .4t 0.1 IN —4o—AcOH/water 1:1 11. 0 C 1-1 N 1-1 : The present disclosure 0 1 2 3 6 time/h FIG. 1 provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and pur - N (57) ity in aqueous solvent systems.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562268149P | 2015-12-16 | 2015-12-16 | |
| US201662288832P | 2016-01-29 | 2016-01-29 | |
| US201662291248P | 2016-02-04 | 2016-02-04 | |
| PCT/US2016/067174 WO2017106647A1 (en) | 2015-12-16 | 2016-12-16 | Process for the preparation of tricyclic pi3k inhibitor compounds and methods for using the same for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201804204QA true SG11201804204QA (en) | 2018-06-28 |
Family
ID=59057647
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201804204QA SG11201804204QA (en) | 2015-12-16 | 2016-12-16 | Process for the preparation of tricyclic pi3k inhibitor compounds and methods for using the same for the treatment of cancer |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US10906918B2 (en) |
| EP (2) | EP3389662B1 (en) |
| CN (2) | CN113999249A (en) |
| AU (3) | AU2016369528B2 (en) |
| CA (1) | CA3008394A1 (en) |
| DK (1) | DK3389662T3 (en) |
| ES (1) | ES2907574T3 (en) |
| HK (1) | HK1256363A1 (en) |
| HR (1) | HRP20220227T1 (en) |
| MY (1) | MY196817A (en) |
| PL (2) | PL3389662T3 (en) |
| SG (1) | SG11201804204QA (en) |
| WO (1) | WO2017106647A1 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3008394A1 (en) | 2015-12-16 | 2017-06-22 | Genentech, Inc. | Process for the preparation of tricyclic pi3k inhibitor compounds and methods of using the same for the treatment of cancer |
| US10767006B2 (en) * | 2017-06-07 | 2020-09-08 | Medtronic, Inc. | Hydrogenation of tyrosine derived polyarylates |
| WO2020167990A1 (en) * | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
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| CU22545A1 (en) | 1994-11-18 | 1999-03-31 | Centro Inmunologia Molecular | OBTAINING A CHEMICAL AND HUMANIZED ANTIBODY AGAINST THE RECEPTOR OF THE EPIDERMAL GROWTH FACTOR FOR DIAGNOSTIC AND THERAPEUTIC USE |
| US4943533A (en) | 1984-03-01 | 1990-07-24 | The Regents Of The University Of California | Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor |
| CA2066428C (en) | 1989-09-08 | 2000-11-28 | Bert Vogelstein | Structural alterations of the egf receptor gene in human gliomas |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| GB9208135D0 (en) | 1992-04-13 | 1992-05-27 | Ludwig Inst Cancer Res | Polypeptides having kinase activity,their preparation and use |
| US6274327B1 (en) | 1992-04-13 | 2001-08-14 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| US5846824A (en) | 1994-02-07 | 1998-12-08 | Ludwig Institute For Cancer Research | Polypeptides having kinase activity, their preparation and use |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| ATE207366T1 (en) | 1993-12-24 | 2001-11-15 | Merck Patent Gmbh | IMMUNOCONJUGATES |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| US5654307A (en) | 1994-01-25 | 1997-08-05 | Warner-Lambert Company | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| US5804396A (en) | 1994-10-12 | 1998-09-08 | Sugen, Inc. | Assay for agents active in proliferative disorders |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| DE69536015D1 (en) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Quinazolinone derivatives |
| GB9508565D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quiazoline derivative |
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| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| AU6267896A (en) | 1995-06-07 | 1996-12-30 | Imclone Systems Incorporated | Antibody and antibody fragments for inhibiting the growth oftumors |
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| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| CA2249446C (en) | 1996-04-12 | 2008-06-17 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
| AU3766897A (en) | 1996-07-13 | 1998-02-09 | Glaxo Group Limited | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| ID18494A (en) | 1996-10-02 | 1998-04-16 | Novartis Ag | PIRAZOLA DISTRIBUTION IN THE SEQUENCE AND THE PROCESS OF MAKING IT |
| UA73073C2 (en) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Substituted 3-cyan chinolines |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6235883B1 (en) | 1997-05-05 | 2001-05-22 | Abgenix, Inc. | Human monoclonal antibodies to epidermal growth factor receptor |
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| ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
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| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| NZ503991A (en) | 1997-11-06 | 2001-11-30 | American Cyanamid Co | Use of quinazoline derivatives as tyrosine kinase inhibitors for treating colonic polyps |
| NZ512189A (en) | 1998-11-19 | 2003-10-31 | Warner Lambert Co | N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4- yl-propoxy)-quinazolin-6-yl]-acrylamide useful as an irreversible inhibitor of tyrosine kinases |
| GB2356630A (en) * | 1999-11-10 | 2001-05-30 | Merck & Co Inc | Intermediates used in the preparation of tetrahydronaphthyridine |
| BR0211073A (en) | 2001-07-12 | 2004-12-14 | Avecia Ltd | Catalyst system and processes for the preparation of a microencapsulated catalyst, optionally substituted biphenyls, optionally substituted alkenes, a hydrogenated product and diols |
| WO2009116069A2 (en) | 2008-02-04 | 2009-09-24 | Ipca Laboratories Limited | Process for preparation of 1-(9h-carbazol-4-yloxy)-3-[[2-(2- methoxyphenoxy) ethyl] amino]-2-propanol |
| GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
| PL2467387T3 (en) | 2009-08-20 | 2015-08-31 | Karus Therapeutics Ltd | Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors. |
| JP5585257B2 (en) * | 2010-07-16 | 2014-09-10 | 株式会社リコー | Image forming apparatus, device system, program management method, program |
| EP2621908A2 (en) * | 2010-10-01 | 2013-08-07 | Novartis AG | Manufacturing process for pyrimidine derivatives |
| ES2530545T3 (en) | 2010-12-16 | 2015-03-03 | Hoffmann La Roche | Tricyclic PI3K inhibitor compounds and methods of use |
| EP3052504B1 (en) * | 2013-10-04 | 2019-02-06 | Universität Basel | Conformationally restricted pi3k and mtor inhibitors |
| CA3008394A1 (en) | 2015-12-16 | 2017-06-22 | Genentech, Inc. | Process for the preparation of tricyclic pi3k inhibitor compounds and methods of using the same for the treatment of cancer |
-
2016
- 2016-12-16 CA CA3008394A patent/CA3008394A1/en active Pending
- 2016-12-16 PL PL16876773T patent/PL3389662T3/en unknown
- 2016-12-16 DK DK16876773.9T patent/DK3389662T3/en active
- 2016-12-16 MY MYPI2018702031A patent/MY196817A/en unknown
- 2016-12-16 AU AU2016369528A patent/AU2016369528B2/en active Active
- 2016-12-16 CN CN202111170407.5A patent/CN113999249A/en active Pending
- 2016-12-16 SG SG11201804204QA patent/SG11201804204QA/en unknown
- 2016-12-16 WO PCT/US2016/067174 patent/WO2017106647A1/en active Application Filing
- 2016-12-16 US US15/780,328 patent/US10906918B2/en active Active
- 2016-12-16 CN CN201680073496.2A patent/CN108697713B/en active Active
- 2016-12-16 ES ES16876773T patent/ES2907574T3/en active Active
- 2016-12-16 PL PL21204490.3T patent/PL3978500T3/en unknown
- 2016-12-16 HR HRP20220227TT patent/HRP20220227T1/en unknown
- 2016-12-16 EP EP16876773.9A patent/EP3389662B1/en active Active
- 2016-12-16 EP EP21204490.3A patent/EP3978500B1/en active Active
-
2018
- 2018-12-03 HK HK18115452.9A patent/HK1256363A1/en unknown
-
2020
- 2020-12-08 US US17/115,095 patent/US11643421B2/en active Active
-
2021
- 2021-07-05 AU AU2021204704A patent/AU2021204704B2/en active Active
-
2023
- 2023-03-24 US US18/189,623 patent/US20230242550A1/en active Pending
- 2023-06-29 AU AU2023204160A patent/AU2023204160A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2021204704A1 (en) | 2021-08-05 |
| EP3978500B1 (en) | 2023-11-22 |
| AU2016369528A1 (en) | 2018-06-07 |
| WO2017106647A1 (en) | 2017-06-22 |
| HRP20220227T1 (en) | 2022-04-29 |
| EP3389662A1 (en) | 2018-10-24 |
| AU2021204704B2 (en) | 2023-04-06 |
| DK3389662T3 (en) | 2022-02-28 |
| CN108697713B (en) | 2021-10-26 |
| AU2016369528B2 (en) | 2021-04-22 |
| US20230242550A1 (en) | 2023-08-03 |
| ES2907574T3 (en) | 2022-04-25 |
| CN108697713A (en) | 2018-10-23 |
| CN113999249A (en) | 2022-02-01 |
| US20180354970A1 (en) | 2018-12-13 |
| HK1256363A1 (en) | 2019-09-20 |
| US10906918B2 (en) | 2021-02-02 |
| US20210253599A1 (en) | 2021-08-19 |
| EP3978500C0 (en) | 2023-11-22 |
| EP3978500A1 (en) | 2022-04-06 |
| MY196817A (en) | 2023-05-03 |
| PL3978500T3 (en) | 2024-03-11 |
| EP3389662B1 (en) | 2021-12-01 |
| CA3008394A1 (en) | 2017-06-22 |
| EP3389662A4 (en) | 2019-05-08 |
| AU2023204160A1 (en) | 2023-07-20 |
| PL3389662T3 (en) | 2022-04-04 |
| US11643421B2 (en) | 2023-05-09 |
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