SG11201407189XA - C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity - Google Patents

C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity

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Publication number
SG11201407189XA
SG11201407189XA SG11201407189XA SG11201407189XA SG11201407189XA SG 11201407189X A SG11201407189X A SG 11201407189XA SG 11201407189X A SG11201407189X A SG 11201407189XA SG 11201407189X A SG11201407189X A SG 11201407189XA SG 11201407189X A SG11201407189X A SG 11201407189XA
Authority
SG
Singapore
Prior art keywords
bristol
wallingford
connecticut
myers squibb
lllll
Prior art date
Application number
SG11201407189XA
Inventor
Ny Sin
Zheng Liu
Jacob Swidorski
Sing-Yuen Sit
Jie Chen
Yan Chen
Nicholas A Meanwell
Alicia Regueiro-Ren
Original Assignee
Bristol Myers Squibb Co
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.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of SG11201407189XA publication Critical patent/SG11201407189XA/en

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Classifications

    • 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
    • C07D487/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-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
    • C07D498/02—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 two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • AIDS & HIV (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 14 November 2013 (14.11.2013) WIPOIPCT (10) International Publication Number WO 2013/169578 A1 (51) International Patent Classification: C07J 63/00 (2006.01) A61P 31/18 (2006.01) A61K31/56 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/039389 3 May 2013 (03.05.2013) English (30) Priority Data: 61/643,483 13/799,479 7 May 2012 (07.05.2012) 13 March 2013 (13.03.2013) English US US (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). (72) Inventors: SIN, Ny; c/o Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492 (US). LIU, Zheng; c/o Bristol-Myers Squibb Company, 5 Re­ search Parkway, Wallingford, Connecticut 06492 (US). SWIDORSKI, Jacob; c/o Bristol-Myers Squibb Com­ pany, 5 Research Parkway, Wallingford, Connecticut 06492 (US). SIT, Sing-Yuen; c/o Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492 (US). CHEN, Jie; c/o Bristol-Myers Squibb Com­ pany, 5 Research Parkway, Wallingford, Connecticut 06492 (US). CHEN, Yan; c/o Bristol-Myers Squibb Com­ pany, 5 Research Parkway, Wallingford, Connecticut 06492 (US). MEANWELL, Nicholas A.; c/o Bristol-My­ ers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492 (US). REGUEIRO-REN, Alicia; c/o Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, Connecticut 06492 (US). (74) Agents: LEVIS, John F. et al.; Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, New Jersey 08543- 4000 (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, [Continued on next page] (54) Title: C-17 BICYCLIC AMINES OF TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY Y-X Y-X 00 l> o\ Y-X (57) Abstract: Compounds having drug and bio-affecting properties, their pharma­ ceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III:These compounds are useful for the treatment of HIV and AIDS. Formula I WO 2013/169578 A11 lllll llllllll II llllll III lllll lllll III III III lllll lllll lllll lllll llll llll lllll lllllll llll llll 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: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) — 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))
SG11201407189XA 2012-05-07 2013-05-03 C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity SG11201407189XA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261643483P 2012-05-07 2012-05-07
US13/799,479 US8889854B2 (en) 2012-05-07 2013-03-13 C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity
PCT/US2013/039389 WO2013169578A1 (en) 2012-05-07 2013-05-03 C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity

Publications (1)

Publication Number Publication Date
SG11201407189XA true SG11201407189XA (en) 2014-12-30

Family

ID=49513043

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201407189XA SG11201407189XA (en) 2012-05-07 2013-05-03 C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity

Country Status (17)

Country Link
US (1) US8889854B2 (en)
EP (1) EP2847208B1 (en)
JP (1) JP6212545B2 (en)
KR (1) KR20150013157A (en)
CN (1) CN104540844B (en)
AR (1) AR090955A1 (en)
AU (1) AU2013259894B2 (en)
BR (1) BR112014027669A2 (en)
CA (1) CA2872891C (en)
EA (1) EA027133B1 (en)
ES (1) ES2652510T3 (en)
IL (1) IL235465A (en)
MX (1) MX354914B (en)
PT (1) PT2847208T (en)
SG (1) SG11201407189XA (en)
TW (1) TWI574973B (en)
WO (1) WO2013169578A1 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8906889B2 (en) * 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity
EA027371B1 (en) 2013-02-06 2017-07-31 Бристол-Майерс Сквибб Компани C-19 modified triterpenoids with hiv maturation inhibitory activity
WO2014130810A1 (en) 2013-02-25 2014-08-28 Bristol-Myers Squibb Company C-3 alkyl and alkenyl modified betulinic acid derivatives useful in the treatment of hiv
UY36070A (en) 2014-04-11 2015-10-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware TRITERPENOIDS WITH INHIBITING ACTIVITY OF HIV MATURATION
WO2015195776A1 (en) 2014-06-19 2015-12-23 Bristol-Myers Squibb Company Betulinic acid derivatives with hiv maturation inhibitory activity
US20180094019A1 (en) * 2015-04-14 2018-04-05 ViiV Healthcare UK (No.4) Limited Crystalline forms of modified triterpenoid hydrochloride salts with hiv maturation inhibitor activity
JP2018521093A (en) 2015-07-28 2018-08-02 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ Vetine derivatives for preventing or treating HIV infection
EP3328875A1 (en) 2015-07-28 2018-06-06 Glaxosmithkline Intellectual Property (No. 2) Limited Betuin derivatives for preventing or treating hiv infections
KR20180054826A (en) 2015-09-24 2018-05-24 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 Compounds having HIV maturation inhibitory activity
US20190023733A1 (en) 2016-01-20 2019-01-24 Glaxosmithkline Intellectual Property (No.2) Limited Amine derivatives of lupanes with hiv maturation inhibitory activity
AR107512A1 (en) 2016-02-04 2018-05-09 VIIV HEALTHCARE UK Nº 5 LTD TRITERPENOIDS MODIFIED IN C-3 AND C-17 AS HIV-1 INHIBITORS
CA3075173A1 (en) * 2017-09-13 2019-03-21 Emmyon, Inc. Ursolic acid morpholine and diethanolamine salts
PT3784349T (en) 2018-04-24 2024-01-22 Viiv Healthcare Uk No 5 Ltd Compounds with hiv maturation inhibitory activity
CN109705189B (en) * 2018-12-29 2020-06-05 中国医学科学院药用植物研究所 Triterpene derivative with structure shown in formula I, preparation method and application thereof
PT3924361T (en) 2019-02-11 2023-12-12 Hetero Labs Ltd Novel triterpene derivatives as hiv inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5962527A (en) 1995-03-21 1999-10-05 The Board Of Trustees Of The University Of Illinois Method and composition for treating cancers
US5869535A (en) 1995-03-21 1999-02-09 The Board Of Trustees Of The University Of Illinois Method and composition for selectively inhibiting melanoma
US5679828A (en) 1995-06-05 1997-10-21 Biotech Research Labs, Inc. Betulinic acid and dihydrobetulinic acid derivatives and uses therefor
US20040110785A1 (en) 2001-02-02 2004-06-10 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
KR20050033070A (en) 2002-08-09 2005-04-08 아스트라제네카 에이비이 [1,2,4]oxadiazoles as modulators of metabotropic glutamate receptor-5
US7365221B2 (en) 2002-09-26 2008-04-29 Panacos Pharmaceuticals, Inc. Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
WO2004089357A2 (en) 2003-04-02 2004-10-21 Regents Of The University Of Minnesota Anti-fungal formulation of triterpene and essential oil
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
RU2387665C2 (en) 2004-03-17 2010-04-27 Панакос Фармасьютикалз, Инк. Pharmaceutical salts of 3-o-(3',3-dimethylsuccinyl) betulinic acid
CN101142227A (en) * 2004-11-12 2008-03-12 帕纳克斯医药公司 Novel betulin derivatives, preparation thereof and use thereof
TW200628161A (en) 2004-11-12 2006-08-16 Panacos Pharmaceuticals Inc Novel betulin derivatives, preparation thereof and use thereof
WO2008127364A2 (en) 2006-10-13 2008-10-23 Myriad Genetics, Inc. Antiviral compounds and use thereof
US20110144069A1 (en) 2006-10-16 2011-06-16 Myriad Genetics, Incorporated Compounds for treating viral infections
JP2011511812A (en) 2008-02-14 2011-04-14 バイロケム ファーマ インコーポレイテッド Novel 17β lupine derivative
US9067966B2 (en) 2009-07-14 2015-06-30 Hetero Research Foundation, Hetero Drugs Ltd. Lupeol-type triterpene derivatives as antivirals
PE20121480A1 (en) 2009-12-17 2012-11-10 Merck Sharp & Dohme AMINOPYRIMIDINES AS SYK INHIBITORS
BR112012030818A2 (en) 2010-06-04 2019-09-24 Bristol-Myers Squibb Company "modified c-3 betulinic acid derivatives as inhibitors of hiv maturation"
MX2012013628A (en) * 2010-06-04 2012-12-17 Bristol Myers Squibb Co C-28 amides of modified c-3 betulinic acid derivatives as hiv maturation inhibitors.
MA34397B1 (en) 2010-07-02 2013-07-03 Gilead Sciences Inc NAPHTH-2-YLACETIC ACID DERIVATIVES IN AIDS TREATMENT
AU2012212509B2 (en) * 2011-01-31 2016-01-21 ViiV Healthcare UK (No.4) Limited C-17 and C-3 modified triterpenoids with HIV maturation inhibitory activity
ES2552512T3 (en) 2011-01-31 2015-11-30 Bristol-Myers Squibb Company C-28 amines of C-3 modified betulinic acid derivatives as inhibitors of human immunodeficiency virus maturation
US8754069B2 (en) 2011-09-21 2014-06-17 Bristol-Myers Squibb Company Betulinic acid derivatives with antiviral activity
US8906889B2 (en) 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity

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Publication number Publication date
JP6212545B2 (en) 2017-10-11
TW201350499A (en) 2013-12-16
CA2872891C (en) 2018-10-23
IL235465A (en) 2015-11-30
US8889854B2 (en) 2014-11-18
ES2652510T3 (en) 2018-02-02
CA2872891A1 (en) 2013-11-14
MX354914B (en) 2018-03-26
EA027133B1 (en) 2017-06-30
KR20150013157A (en) 2015-02-04
EP2847208A1 (en) 2015-03-18
AU2013259894A1 (en) 2015-01-15
JP2015516422A (en) 2015-06-11
TWI574973B (en) 2017-03-21
MX2014013089A (en) 2014-12-08
WO2013169578A1 (en) 2013-11-14
CN104540844A (en) 2015-04-22
US20130296554A1 (en) 2013-11-07
AU2013259894B2 (en) 2017-07-13
EP2847208B1 (en) 2017-10-04
PT2847208T (en) 2017-12-14
EA201492016A1 (en) 2015-02-27
BR112014027669A2 (en) 2017-06-27
AR090955A1 (en) 2014-12-17
CN104540844B (en) 2016-12-07

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