SG11201407618VA - Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof - Google Patents
Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereofInfo
- Publication number
- SG11201407618VA SG11201407618VA SG11201407618VA SG11201407618VA SG11201407618VA SG 11201407618V A SG11201407618V A SG 11201407618VA SG 11201407618V A SG11201407618V A SG 11201407618VA SG 11201407618V A SG11201407618V A SG 11201407618VA SG 11201407618V A SG11201407618V A SG 11201407618VA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- genentech
- california
- san francisco
- south san
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
Abstract
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau „ (10) International Publication Number (43) International Publication Date ^ ^ WO 2013/173811 A1 21 November 2013 (21.11.2013) WIPO I PCT (51) International Patent Classification: C07D 403/04 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/041728 17 May 2013 (17.05.2013) English English (30) Priority Data: 61/648,536 17 May 2012 (17.05.2012) US (71) Applicant: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, California 94080-4990 (US). (72) Inventors: CHAKRAVARTY, Paroma; c/o Genentech, Inc., DNA 1 Way, South San Francisco, California 94080- 4990 (US). KOTHARI, Sanjeev; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). GOSSELIN, Francis; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). SAVAGE, Scott J.; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). STULTS, Jeffrey; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). (74) Agents: MALEN, Peter L. et al.; Viksnins Harris & Padys PLLP, 7900 International Drive, Suite 670, Bloomington, Minnesota 55425 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) 00 i> i-H o CJ (54) Title: AMORPHOUS FORM OF AN AKT INHIBITING PYRIMIDINYL TIONS AND METHODS THEREOF CYCLOPENTANE COMPOUND, COMPOSI- (57) Abstract: Disclosed is (5)-2-(4-chlorophenyl)-l-(4-((5i?,7i?)-7-hydroxy-5-methyl-6,7-dihydro-5i/-cyclopenta[fi?]pyrimidin-4- yl)piperazin-l-yl)-3-(isopropylamino)propan-l-one monohydrochloride, forms, formulations, pharmaceutical compositions, pro cesses of manufacturing and methods of use thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261648536P | 2012-05-17 | 2012-05-17 | |
| PCT/US2013/041728 WO2013173811A1 (en) | 2012-05-17 | 2013-05-17 | Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201407618VA true SG11201407618VA (en) | 2015-01-29 |
Family
ID=48539412
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201407618VA SG11201407618VA (en) | 2012-05-17 | 2013-05-17 | Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US9290458B2 (en) |
| EP (2) | EP3719014A1 (en) |
| JP (2) | JP6283663B2 (en) |
| KR (4) | KR20210095238A (en) |
| CN (1) | CN104470912B (en) |
| AU (2) | AU2013262548B2 (en) |
| BR (1) | BR112014028593A2 (en) |
| CA (1) | CA2873663C (en) |
| CL (1) | CL2014003115A1 (en) |
| CO (1) | CO7151489A2 (en) |
| CR (1) | CR20140560A (en) |
| DK (1) | DK2858989T3 (en) |
| ES (1) | ES2799512T3 (en) |
| HK (1) | HK1208462A1 (en) |
| HR (1) | HRP20200992T1 (en) |
| HU (1) | HUE051254T2 (en) |
| IL (2) | IL235712B (en) |
| LT (1) | LT2858989T (en) |
| MA (1) | MA37650A1 (en) |
| MX (1) | MX353041B (en) |
| MY (1) | MY170086A (en) |
| NZ (1) | NZ702513A (en) |
| PE (1) | PE20150725A1 (en) |
| PH (1) | PH12014502538B1 (en) |
| PL (1) | PL2858989T3 (en) |
| PT (1) | PT2858989T (en) |
| RS (1) | RS60417B9 (en) |
| RU (1) | RU2650511C2 (en) |
| SG (1) | SG11201407618VA (en) |
| SI (1) | SI2858989T1 (en) |
| WO (1) | WO2013173811A1 (en) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6284928B2 (en) | 2012-05-17 | 2018-02-28 | アレイ バイオファーマ、インコーポレイテッド | Process for making hydroxylated cyclopentylpyrimidine compounds |
| US9290458B2 (en) | 2012-05-17 | 2016-03-22 | Genentech, Inc. | Amorphous form of an AKT inhibiting pyrimidinyl-cyclopentane compound, compositions and methods thereof |
| CN105899492B (en) | 2013-11-15 | 2021-08-24 | 豪夫迈·罗氏有限公司 | Process for preparing pyrimidylcyclopentane compounds |
| ES2793530T3 (en) * | 2014-05-19 | 2020-11-16 | Tillotts Pharma Ag | Modified Release Coated Capsules |
| BR112019002007B1 (en) * | 2016-08-10 | 2024-01-16 | F. Hoffmann-La Roche Ag | PHARMACEUTICAL COMPOSITION AND USE OF A PHARMACEUTICAL COMPOSITION |
| EP4013419A1 (en) * | 2019-08-12 | 2022-06-22 | F. Hoffmann-La Roche AG | Treatment of breast cancer using combination therapies comprising an atp competitive akt inhibitor, a cdk4/6 inhibitor, and fulvestrant |
| EP4351522A1 (en) * | 2021-06-09 | 2024-04-17 | Lonza Bend Inc. | Mixed solvents for spray drying for preparation of amorphous solid dispersions |
| WO2023043869A1 (en) * | 2021-09-15 | 2023-03-23 | Teva Pharmaceuticals International Gmbh | Solid state forms of ipatasertib citrate |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9408197A (en) | 1993-12-12 | 1997-08-26 | Agrogene Ltd | Method to protect plants against fungal diseases |
| JP2001524079A (en) | 1997-04-07 | 2001-11-27 | メルク エンド カンパニー インコーポレーテッド | How to treat cancer |
| US6201023B1 (en) | 1997-06-10 | 2001-03-13 | Agrogene Ltd. | Methods and compositions to protect crops against plant parasitic nematodes |
| ES2137137B1 (en) | 1998-05-25 | 2000-08-16 | Medichem Sa | NEW POLYMORPH OF UNHYDRATED GABAPENTINE, ITS PROCEDURE FOR OBTAINING AND ITS USE FOR THE OBTAINING OF PHARMACEUTICAL QUALITY GABAPENTINE. |
| EP0982300A3 (en) | 1998-07-29 | 2000-03-08 | Societe Civile Bioprojet | Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications |
| US6376496B1 (en) | 1999-03-03 | 2002-04-23 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| AU7715300A (en) | 1999-09-27 | 2001-04-30 | Merck & Co., Inc. | Method of preventing osteoporosis |
| CN1309370C (en) | 2002-02-01 | 2007-04-11 | 辉瑞产品公司 | Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus |
| EP1636200A2 (en) | 2003-06-09 | 2006-03-22 | Boehringer Ingelheim International GmbH | Inhibitors of papilloma virus |
| RU2006121990A (en) | 2003-11-21 | 2007-12-27 | Эррэй Биофарма Инк. (Us) | ACT PROTEINKINASE INHIBITORS |
| MY139645A (en) * | 2004-02-11 | 2009-10-30 | Amgen Inc | Vanilloid receptor ligands and their use in treatments |
| US8927546B2 (en) | 2006-02-28 | 2015-01-06 | Dart Neuroscience (Cayman) Ltd. | Therapeutic piperazines |
| UA95641C2 (en) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| TWI450720B (en) | 2007-07-05 | 2014-09-01 | Array Biopharma Inc | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US20100298289A1 (en) | 2007-10-09 | 2010-11-25 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| AU2009204025B2 (en) * | 2008-01-09 | 2014-02-20 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| SG175144A1 (en) | 2009-04-15 | 2011-11-28 | Abbott Lab | Anti-viral compounds |
| WO2011050016A1 (en) | 2009-10-23 | 2011-04-28 | Eli Lilly And Company | Akt inhibitors |
| MX2012011887A (en) * | 2010-04-16 | 2012-11-30 | Genentech Inc | Fox03a as predictive biomarker for pi3k/akt kinase pathway inhibitor efficacy. |
| US9050334B2 (en) | 2010-07-16 | 2015-06-09 | Innov88 Llc | MIF inhibitors and their uses |
| WO2012177925A1 (en) | 2011-06-21 | 2012-12-27 | The Board Institute, Inc. | Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene |
| CN104471070B (en) | 2012-05-17 | 2018-09-25 | 基因泰克公司 | The method for preparing hydroxylating cyclopentapyrimidin compound and its salt |
| PL2861583T3 (en) | 2012-05-17 | 2016-12-30 | Process for making hydroxylated cyclopentylpyrimidine compounds | |
| US9290458B2 (en) | 2012-05-17 | 2016-03-22 | Genentech, Inc. | Amorphous form of an AKT inhibiting pyrimidinyl-cyclopentane compound, compositions and methods thereof |
| ES2668477T3 (en) | 2012-05-17 | 2018-05-18 | Genentech, Inc. | Amino acid compound preparation process |
| JP6284928B2 (en) | 2012-05-17 | 2018-02-28 | アレイ バイオファーマ、インコーポレイテッド | Process for making hydroxylated cyclopentylpyrimidine compounds |
| US20140121193A1 (en) | 2012-11-01 | 2014-05-01 | Robert S. Katz | Methods for treating fibromyalgia |
| US20150376198A1 (en) | 2013-02-18 | 2015-12-31 | The Scripps Research Institute | Modulators of vasopressin receptors with therapeutic potential |
| AU2014237198A1 (en) | 2013-03-15 | 2015-11-05 | Shifa Biomedical Corporation | Anti-PCSK9 compounds and methods for the treatment and/or prevention of cardiovascular diseases |
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2013
- 2013-05-17 US US14/401,092 patent/US9290458B2/en active Active
- 2013-05-17 EP EP20162228.9A patent/EP3719014A1/en active Pending
- 2013-05-17 SI SI201331754T patent/SI2858989T1/en unknown
- 2013-05-17 CA CA2873663A patent/CA2873663C/en active Active
- 2013-05-17 EP EP13726362.0A patent/EP2858989B9/en active Active
- 2013-05-17 PL PL13726362T patent/PL2858989T3/en unknown
- 2013-05-17 HU HUE13726362A patent/HUE051254T2/en unknown
- 2013-05-17 RS RS20200729A patent/RS60417B9/en unknown
- 2013-05-17 PE PE2014002029A patent/PE20150725A1/en not_active Application Discontinuation
- 2013-05-17 KR KR1020217023442A patent/KR20210095238A/en not_active Application Discontinuation
- 2013-05-17 KR KR1020227034985A patent/KR20220143143A/en active Application Filing
- 2013-05-17 LT LTEP13726362.0T patent/LT2858989T/en unknown
- 2013-05-17 RU RU2014151016A patent/RU2650511C2/en active
- 2013-05-17 WO PCT/US2013/041728 patent/WO2013173811A1/en active Application Filing
- 2013-05-17 BR BR112014028593A patent/BR112014028593A2/en not_active Application Discontinuation
- 2013-05-17 KR KR1020147034925A patent/KR102125588B1/en active IP Right Grant
- 2013-05-17 PT PT137263620T patent/PT2858989T/en unknown
- 2013-05-17 ES ES13726362T patent/ES2799512T3/en active Active
- 2013-05-17 MX MX2014013856A patent/MX353041B/en active IP Right Grant
- 2013-05-17 NZ NZ702513A patent/NZ702513A/en unknown
- 2013-05-17 DK DK13726362.0T patent/DK2858989T3/en active
- 2013-05-17 KR KR1020207017092A patent/KR20200074252A/en not_active IP Right Cessation
- 2013-05-17 JP JP2015512908A patent/JP6283663B2/en active Active
- 2013-05-17 MY MYPI2014703413A patent/MY170086A/en unknown
- 2013-05-17 SG SG11201407618VA patent/SG11201407618VA/en unknown
- 2013-05-17 CN CN201380037991.4A patent/CN104470912B/en active Active
- 2013-05-17 AU AU2013262548A patent/AU2013262548B2/en active Active
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2014
- 2014-11-13 IL IL235712A patent/IL235712B/en active IP Right Grant
- 2014-11-14 PH PH12014502538A patent/PH12014502538B1/en unknown
- 2014-11-17 CL CL2014003115A patent/CL2014003115A1/en unknown
- 2014-12-04 CR CR20140560A patent/CR20140560A/en unknown
- 2014-12-09 CO CO14270817A patent/CO7151489A2/en unknown
- 2014-12-12 MA MA37650A patent/MA37650A1/en unknown
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2015
- 2015-09-21 HK HK15109240.2A patent/HK1208462A1/en unknown
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2016
- 2016-02-08 US US15/018,636 patent/US9505725B2/en active Active
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2017
- 2017-12-19 AU AU2017279607A patent/AU2017279607C1/en active Active
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2018
- 2018-01-29 JP JP2018013099A patent/JP6518352B2/en active Active
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2020
- 2020-01-14 IL IL272037A patent/IL272037B/en active IP Right Grant
- 2020-06-24 HR HRP20200992TT patent/HRP20200992T1/en unknown
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