EP2809675A4 - Rafamycin analogs and methods for making same - Google Patents

Rafamycin analogs and methods for making same

Info

Publication number: EP2809675A4
Authority: EP; European Patent Office
Prior art keywords: rafamycin; analogs; methods; making same; making
Prior art date: 2012-11-30
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

EP12889107.4A

Other languages

German (de)

French (fr)

Other versions

EP2809675A1 (en

Inventor

Bing Wang

Jonathon Zhong Zhao

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

HANGZHOU ZYLOX PHARMA CO Ltd

Original Assignee

HANGZHOU ZYLOX PHARMA CO Ltd

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2012-11-30

Filing date

2012-11-30

Publication date

2015-08-12

2012-11-30 Application filed by HANGZHOU ZYLOX PHARMA CO Ltd filed Critical HANGZHOU ZYLOX PHARMA CO Ltd

2014-12-10 Publication of EP2809675A1 publication Critical patent/EP2809675A1/en

2015-08-12 Publication of EP2809675A4 publication Critical patent/EP2809675A4/en

Status Withdrawn legal-status Critical Current

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
- C07D498/18—Bridged 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
- A61K31/435—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
- A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Immunology (AREA)
Diabetes (AREA)
Rheumatology (AREA)
Hematology (AREA)
Physical Education & Sports Medicine (AREA)
Orthopedic Medicine & Surgery (AREA)
Endocrinology (AREA)
Neurology (AREA)
Pulmonology (AREA)
Pain & Pain Management (AREA)
Transplantation (AREA)
Ophthalmology & Optometry (AREA)
Biomedical Technology (AREA)
Obesity (AREA)
Neurosurgery (AREA)
Emergency Medicine (AREA)
Oncology (AREA)
Urology & Nephrology (AREA)
Epidemiology (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

EP12889107.4A 2012-11-30 2012-11-30 Rafamycin analogs and methods for making same Withdrawn EP2809675A4 (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
PCT/CN2012/085631 WO2014082286A1 (en)	2012-11-30	2012-11-30	Rafamycin analogs and methods for making same

Publications (2)

Publication Number	Publication Date
EP2809675A1 EP2809675A1 (en)	2014-12-10
EP2809675A4 true EP2809675A4 (en)	2015-08-12

Family

ID=50827071

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
EP12889107.4A Withdrawn EP2809675A4 (en)	2012-11-30	2012-11-30	Rafamycin analogs and methods for making same

Country Status (9)

Country	Link
EP (1)	EP2809675A4 (en)
JP (1)	JP2016500112A (en)
KR (1)	KR20150003156A (en)
CN (1)	CN104854112A (en)
AU (1)	AU2012395673A1 (en)
CA (1)	CA2863243A1 (en)
SG (1)	SG11201404432QA (en)
WO (1)	WO2014082286A1 (en)
ZA (1)	ZA201405746B (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN104327097B (en) *	2014-10-11	2017-02-08	福建省微生物研究所	Triazole derivatives of rapamycin and application
CN104341434B (en) *	2014-10-16	2016-04-06	福建省微生物研究所	The rapamycin triazole derivatives replaced and purposes
CN104557975B (en) *	2014-12-23	2017-06-20	连云港恒运医药有限公司	The preparation method of everolimus intermediate and its degradation impurity
DK3061765T3 (en)	2015-02-27	2018-03-26	Univ Warszawski Medyczny	Protoescigenin derivative, process for its preparation, use of this compound and pharmaceutical composition comprising this compound
CN104876944B (en) *	2015-05-13	2017-11-10	普济生物科技（台州）有限公司	A kind of preparation method of everolimus
EP3109250A1 (en) *	2015-06-23	2016-12-28	Synbias Pharma AG	Method for the synthesis of rapamycin derivatives
EP3345601A4 (en) *	2015-09-03	2019-05-15	Nippon Kayaku Kabushiki Kaisha	Pharmaceutical composition containing rapamycin or derivative thereof
CN105481704A (en) *	2016-01-12	2016-04-13	西安近代化学研究所	Method for synthesis and purification of bonding agent N-propargyl diethanol amine
CN107759616B (en) *	2016-08-23	2020-11-17	上海微创医疗器械（集团）有限公司	Compound and preparation method and application thereof
SG11201908603PA (en) *	2017-04-05	2019-10-30	Harvard College	Macrocyclic compound and uses thereof
CN110770243A (en) *	2017-05-02	2020-02-07	锐新医药公司	Rapamycin analogs as MTOR inhibitors
CN109776569A (en) *	2017-11-14	2019-05-21	上海医药工业研究院	A kind of preparation method of everolimus
CN108484637A (en) *	2018-03-13	2018-09-04	福建省微生物研究所	Target anticancer new drug X-76 salt-forming compounds and application thereof, preparation method
CA3098692A1 (en)	2018-05-01	2019-11-07	Revolution Medicines, Inc.	C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
MX2020011564A (en)	2018-05-01	2021-01-29	Revolution Medicines Inc	C26-linked rapamycin analogs as mtor inhibitors.
CN109776571B (en) *	2019-01-31	2021-06-11	哈药慈航制药股份有限公司	Rapamycin analogue and preparation method and application thereof
CN112057425A (en) *	2020-09-30	2020-12-11	严鹏科	Rapamycin preparation and preparation method thereof
CN115160343B (en) *	2022-06-09	2023-11-14	福建省微生物研究所	Rapamycin derivative, and preparation method and application thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB9221220D0 (en) *	1992-10-09	1992-11-25	Sandoz Ag	Organic componds
US5258389A (en) *	1992-11-09	1993-11-02	Merck & Co., Inc.	O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
AU4246197A (en) *	1996-09-09	1998-03-26	American Home Products Corporation	Rapamycin derivatives with unnatural stereochemistries
JP2001500126A (en) *	1996-09-09	2001-01-09	アメリカン・ホーム・プロダクツ・コーポレイション	Alkylated rapamycin derivative
TW557297B (en) *	1997-09-26	2003-10-11	Abbott Lab	Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same

2012
- 2012-11-30 WO PCT/CN2012/085631 patent/WO2014082286A1/en active Application Filing
- 2012-11-30 CA CA2863243A patent/CA2863243A1/en not_active Abandoned
- 2012-11-30 JP JP2015544291A patent/JP2016500112A/en active Pending
- 2012-11-30 SG SG11201404432QA patent/SG11201404432QA/en unknown
- 2012-11-30 AU AU2012395673A patent/AU2012395673A1/en not_active Abandoned
- 2012-11-30 CN CN201280077424.7A patent/CN104854112A/en active Pending
- 2012-11-30 EP EP12889107.4A patent/EP2809675A4/en not_active Withdrawn
- 2012-11-30 KR KR20147024024A patent/KR20150003156A/en not_active Application Discontinuation
2014
- 2014-08-04 ZA ZA2014/05746A patent/ZA201405746B/en unknown

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
No further relevant documents disclosed *
See also references of WO2014082286A1 *

Also Published As

Publication number	Publication date
KR20150003156A (en)	2015-01-08
EP2809675A1 (en)	2014-12-10
AU2012395673A1 (en)	2014-08-14
CA2863243A1 (en)	2014-06-05
SG11201404432QA (en)	2014-10-30
AU2012395673A8 (en)	2015-06-11
JP2016500112A (en)	2016-01-07
WO2014082286A1 (en)	2014-06-05
ZA201405746B (en)	2015-11-25
WO2014082286A9 (en)	2014-11-13
CN104854112A (en)	2015-08-19

Legal Events

Date	Code	Title	Description
2014-11-07	PUAI	Public reference made under article 153(3) epc to a published international application that has entered the european phase	Free format text: ORIGINAL CODE: 0009012
2014-12-10	17P	Request for examination filed	Effective date: 20140724
2014-12-10	AK	Designated contracting states	Kind code of ref document: A1 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
2014-12-10	AX	Request for extension of the european patent	Extension state: BA ME
2015-08-12	RA4	Supplementary search report drawn up and despatched (corrected)	Effective date: 20150710
2015-08-12	RIC1	Information provided on ipc code assigned before grant	Ipc: C07D 498/18 20060101AFI20150706BHEP Ipc: A61P 35/00 20060101ALI20150706BHEP Ipc: A61K 31/436 20060101ALI20150706BHEP Ipc: A61P 37/00 20060101ALI20150706BHEP
2016-03-09	DAX	Request for extension of the european patent (deleted)
2017-06-27	STAA	Information on the status of an ep patent application or granted ep patent	Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE
2017-10-06	STAA	Information on the status of an ep patent application or granted ep patent	Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN
2017-11-08	18D	Application deemed to be withdrawn	Effective date: 20170601

Publication	Publication Date	Title
HK1250690A1 (en)	2019-01-11	Methods
ZA201405746B (en)	2015-11-25	Rafamycin analogs and methods for making same
HK1208363A1 (en)	2016-03-04	New methods
GB201212932D0 (en)	2012-09-05	Method
GB201212937D0 (en)	2012-09-05	Method
GB201213636D0 (en)	2012-09-12	Method
GB201212934D0 (en)	2012-09-05	Method
GB201210858D0 (en)	2012-08-01	Method
GB2507760B (en)	2015-07-08	Methods
GB201218570D0 (en)	2012-11-28	Method
EP2880048A4 (en)	2016-05-25	Method
GB201208874D0 (en)	2012-07-04	Methods
GB201202198D0 (en)	2012-03-21	Method
GB201211393D0 (en)	2012-08-08	Method
GB201204280D0 (en)	2012-04-25	Methods
GB201217688D0 (en)	2012-11-14	Method
GB201210147D0 (en)	2012-07-25	Method
GB201208756D0 (en)	2012-07-04	Methods
GB201213858D0 (en)	2012-09-19	Method
GB201203337D0 (en)	2012-04-11	Method
GB201201332D0 (en)	2012-03-14	Method
EP2639418A4 (en)	2015-07-15	Exhaust-heating method
GB201220686D0 (en)	2013-01-02	Methods
AP2012000550S (en)	2012-09-26	E-horn methods
GB201216074D0 (en)	2012-10-24	Methods