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
- 238000000034 method Methods 0.000 title abstract 4
- -1 pyrimidinyl - cyclopentane compound Chemical class 0.000 title abstract 3
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000008569 process Effects 0.000 abstract 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 abstract 1
Classifications
-
- 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 or sparfloxacin
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
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 (5) | KR102678074B1 (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) | PH12014502538A1 (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 |
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SI2861582T1 (en) | 2012-05-17 | 2016-09-30 | Array Biopharma, Inc. | Process for making hydroxylated cyclopentylpyrimidine compounds |
PE20150725A1 (en) | 2012-05-17 | 2015-05-17 | Genentech Inc | FORMS AND FORMULATIONS OF A PYRIMIDINYL CYCLOPENTAN COMPOUND, COMPOSITIONS AND METHODS OF THIS |
MX367620B (en) * | 2013-11-15 | 2019-08-28 | Hoffmann La Roche | Processes for the preparation of pyrimidinylcyclopentane compounds. |
EP2946774B1 (en) | 2014-05-19 | 2020-04-22 | Tillotts Pharma AG | Modified release coated capsules |
JP6875501B2 (en) * | 2016-08-10 | 2021-05-26 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | A pharmaceutical composition comprising an Akt protein kinase inhibitor |
US11576919B2 (en) * | 2019-08-12 | 2023-02-14 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising an ATP competitive AKT inhibitor, a CDK4/6 inhibitor, and fulvestrant |
CA3221313A1 (en) * | 2021-06-09 | 2022-12-15 | Warren Miller | 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)
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CN1134212C (en) | 1993-12-12 | 2004-01-14 | 阿格罗吉恩有限公司 | A novel method to protect plants from fungal infection |
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 |
JP2003524618A (en) | 1999-03-03 | 2003-08-19 | メルク エンド カムパニー インコーポレーテッド | Prenyl protein transferase inhibitors |
WO2001022963A1 (en) | 1999-09-27 | 2001-04-05 | Merck & Co., Inc. | Method of preventing osteoporosis |
ES2878403T3 (en) | 2002-02-01 | 2021-11-18 | Bend Res Inc | Method for preparing spray dried homogeneous solid amorphous drug dispersions using modified spray drying apparatus |
PE20050630A1 (en) | 2003-06-09 | 2005-09-22 | Boehringer Ingelheim Int | HETEROCYCLIC COMPOUNDS AS PAPILLOMA VIRUS INHIBITORS |
AU2004293026B2 (en) | 2003-11-21 | 2012-01-19 | Array Biopharma Inc. | AKT protein kinase 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 |
NZ582692A (en) | 2007-07-05 | 2012-05-25 | Array Biopharma Inc | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
WO2009047255A1 (en) | 2007-10-09 | 2009-04-16 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
CN101932564B (en) * | 2008-01-09 | 2012-12-26 | 阵列生物制药公司 | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
JP5734956B2 (en) | 2009-04-15 | 2015-06-17 | アッヴィ・インコーポレイテッド | Antiviral compounds |
EA020151B1 (en) | 2009-10-23 | 2014-09-30 | Эли Лилли Энд Компани | Akt inhibitors and pharmaceutical compositions comprising them |
WO2011130654A1 (en) * | 2010-04-16 | 2011-10-20 | Genentech, Inc. | Fox03a as predictive biomarker for pi3k/akt kinase pathway inhibitor efficacy |
WO2012009649A1 (en) | 2010-07-16 | 2012-01-19 | Anderson Gaweco | 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 |
SI2850054T1 (en) | 2012-05-17 | 2018-06-29 | Genentech, Inc. | Process for making amino acid compounds |
SI2861582T1 (en) | 2012-05-17 | 2016-09-30 | Array Biopharma, Inc. | Process for making hydroxylated cyclopentylpyrimidine compounds |
KR20150020211A (en) | 2012-05-17 | 2015-02-25 | 어레이 바이오파마 인크. | Process for making hydroxylated cyclopentylpyrimidine compounds |
PE20150725A1 (en) | 2012-05-17 | 2015-05-17 | Genentech Inc | FORMS AND FORMULATIONS OF A PYRIMIDINYL CYCLOPENTAN COMPOUND, COMPOSITIONS AND METHODS OF THIS |
KR102123131B1 (en) | 2012-05-17 | 2020-06-15 | 제넨테크, 인크. | Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof |
US20140121193A1 (en) | 2012-11-01 | 2014-05-01 | Robert S. Katz | Methods for treating fibromyalgia |
CN105263910A (en) | 2013-02-18 | 2016-01-20 | 斯克利普斯研究所 | 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 PE PE2014002029A patent/PE20150725A1/en not_active Application Discontinuation
- 2013-05-17 PT PT137263620T patent/PT2858989T/en unknown
- 2013-05-17 LT LTEP13726362.0T patent/LT2858989T/en unknown
- 2013-05-17 CA CA2873663A patent/CA2873663C/en active Active
- 2013-05-17 RS RS20200729A patent/RS60417B9/en unknown
- 2013-05-17 KR KR1020227034985A patent/KR102678074B1/en active IP Right Grant
- 2013-05-17 NZ NZ702513A patent/NZ702513A/en unknown
- 2013-05-17 KR KR1020247014285A patent/KR20240066293A/en not_active Application Discontinuation
- 2013-05-17 CN CN201380037991.4A patent/CN104470912B/en active Active
- 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 KR KR1020147034925A patent/KR102125588B1/en active IP Right Grant
- 2013-05-17 ES ES13726362T patent/ES2799512T3/en active Active
- 2013-05-17 HU HUE13726362A patent/HUE051254T2/en unknown
- 2013-05-17 JP JP2015512908A patent/JP6283663B2/en active Active
- 2013-05-17 DK DK13726362.0T patent/DK2858989T3/en active
- 2013-05-17 SG SG11201407618VA patent/SG11201407618VA/en unknown
- 2013-05-17 SI SI201331754T patent/SI2858989T1/en unknown
- 2013-05-17 KR KR1020207017092A patent/KR20200074252A/en not_active IP Right Cessation
- 2013-05-17 RU RU2014151016A patent/RU2650511C2/en active
- 2013-05-17 KR KR1020217023442A patent/KR20210095238A/en not_active Application Discontinuation
- 2013-05-17 EP EP13726362.0A patent/EP2858989B9/en active Active
- 2013-05-17 WO PCT/US2013/041728 patent/WO2013173811A1/en active Application Filing
- 2013-05-17 PL PL13726362T patent/PL2858989T3/en unknown
- 2013-05-17 MX MX2014013856A patent/MX353041B/en active IP Right Grant
- 2013-05-17 AU AU2013262548A patent/AU2013262548B2/en active Active
- 2013-05-17 MY MYPI2014703413A patent/MY170086A/en unknown
- 2013-05-17 BR BR112014028593A patent/BR112014028593A2/en not_active Application Discontinuation
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2014
- 2014-11-13 IL IL235712A patent/IL235712B/en active IP Right Grant
- 2014-11-14 PH PH12014502538A patent/PH12014502538A1/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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