KR102416279B1 - Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 - Google Patents

Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 Download PDF

Info

Publication number
KR102416279B1
KR102416279B1 KR1020177001959A KR20177001959A KR102416279B1 KR 102416279 B1 KR102416279 B1 KR 102416279B1 KR 1020177001959 A KR1020177001959 A KR 1020177001959A KR 20177001959 A KR20177001959 A KR 20177001959A KR 102416279 B1 KR102416279 B1 KR 102416279B1
Authority
KR
South Korea
Prior art keywords
compound
optionally substituted
methyl
nitrogen
sulfur
Prior art date
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.)
Expired - Fee Related
Application number
KR1020177001959A
Other languages
English (en)
Korean (ko)
Other versions
KR20170033314A (ko
Inventor
헨리 유
창헤 퀴
폴 템페스트
셀바라즈 쥐. 나타라자
스티븐 에스. 팔머
Original Assignee
아레스 트레이딩 에스.아.
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 아레스 트레이딩 에스.아. filed Critical 아레스 트레이딩 에스.아.
Publication of KR20170033314A publication Critical patent/KR20170033314A/ko
Application granted granted Critical
Publication of KR102416279B1 publication Critical patent/KR102416279B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020177001959A 2014-06-23 2014-12-22 Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도 Expired - Fee Related KR102416279B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2014/080519 WO2015196335A1 (en) 2014-06-23 2014-06-23 Pyrazole compounds as modulators of fshr and uses thereof
CNPCT/CN2014/080519 2014-06-23
PCT/CN2014/094459 WO2015196759A1 (en) 2014-06-23 2014-12-22 Pyrazole compounds as modulators of fshr and uses thereof

Publications (2)

Publication Number Publication Date
KR20170033314A KR20170033314A (ko) 2017-03-24
KR102416279B1 true KR102416279B1 (ko) 2022-07-01

Family

ID=54936412

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177001959A Expired - Fee Related KR102416279B1 (ko) 2014-06-23 2014-12-22 Ｆｓｈｒ의 조절제로서의 피라졸 화합물 및 이의 용도

Country Status (12)

Country Link
US (3) US10208055B2 (enExample)
EP (1) EP3157929B1 (enExample)
JP (3) JP6557331B2 (enExample)
KR (1) KR102416279B1 (enExample)
CN (1) CN106573937B (enExample)
AU (3) AU2014398875B2 (enExample)
CA (1) CA2955415A1 (enExample)
DK (1) DK3157929T3 (enExample)
ES (1) ES2972131T3 (enExample)
MX (1) MX389867B (enExample)
RU (1) RU2752173C2 (enExample)
WO (2) WO2015196335A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
CN106977523A (zh) * 2017-03-30 2017-07-25 河南师范大学 具有苯基并四氢吡咯结构的fshr拮抗剂及其制备方法
CN106866692A (zh) * 2017-03-30 2017-06-20 毛阿龙 具有苯并1,4‑二氧杂环己二烯酮结构的fshr拮抗剂的制备方法
CN106967076A (zh) * 2017-03-30 2017-07-21 河南师范大学 一种具有6h‑二苯并吡喃结构化合物及其制备方法
CN111936484A (zh) * 2017-12-22 2020-11-13 拉文纳制药公司 作为磷脂酰肌醇磷酸激酶抑制剂的色烯并吡啶衍生物
SMT202300212T1 (it) * 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi
TW202112784A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之𠳭唏并嘧啶衍生物
CN113754678B (zh) * 2020-06-02 2023-03-10 江苏恒瑞医药股份有限公司 二氢硫代色烯并吡唑类衍生物、其制备方法及其在医药上的应用
WO2022007924A1 (zh) * 2020-07-09 2022-01-13 江苏恒瑞医药股份有限公司 氧杂氮杂双环类衍生物、其制备方法及其在医药上的应用
WO2022022630A1 (zh) 2020-07-29 2022-02-03 江苏恒瑞医药股份有限公司 氧杂氮杂螺环类衍生物、其制备方法及其在医药上的应用
KR20240101561A (ko) 2021-10-14 2024-07-02 인사이트 코포레이션 Kras의 저해제로서의 퀴놀린 화합물
EP4577206A2 (en) * 2022-08-26 2025-07-02 Celmatix Inc. Novel modulators of fshr and uses thereof
WO2024077006A1 (en) * 2022-10-05 2024-04-11 Radionetics Oncology, Inc. Follicle-stimulating hormone receptor (fshr) targeted therapeutics and uses thereof
WO2024184461A2 (en) 2023-03-08 2024-09-12 Ferring B.V. Small molecule fsh receptor modulators
WO2024263803A2 (en) * 2023-06-21 2024-12-26 Celmatix Inc. Novel modulators of fshr and uses thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003024936A1 (en) 2001-09-19 2003-03-27 Pharmacia Corporation Substituted pyrazolo compounds for the treatment of inflammation
WO2008035356A2 (en) 2006-09-20 2008-03-27 Glenmark Pharmaceuticals Limited Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
US20100216785A1 (en) 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compositions
US20100215741A1 (en) * 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compounds
WO2011058149A1 (en) * 2009-11-13 2011-05-19 Merck Serono S.A. Tricyclic pyrazol amine derivatives

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8814586D0 (en) * 1988-06-20 1988-07-27 Erba Carlo Spa Tricyclic 3-oxo-propanenitrile derivatives & process for their preparation
WO2002009706A1 (en) 2000-07-27 2002-02-07 Smithkline Beecham Corporation Agonists of follicle stimulating hormone activity
RU2332412C2 (ru) 2003-02-07 2008-08-27 Дайити Фармасьютикал Ко., Лтд. Производные пиразола
EP1879898A2 (en) * 2005-05-12 2008-01-23 Wyeth a Corporation of the State of Delaware Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (fsh-r) antagonists
TWI461426B (zh) * 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
JP6170043B2 (ja) 2011-07-01 2017-07-26 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ジヒドロピラゾール
WO2013012848A1 (en) 2011-07-18 2013-01-24 Merck Patent Gmbh Benzamides
ES2663972T3 (es) 2012-01-10 2018-04-17 Merck Patent Gmbh Derivados de benzamida como moduladores de la hormona folículo estimulante
KR20140120903A (ko) 2012-02-08 2014-10-14 메르크 파텐트 게엠베하 여포 자극 호르몬수용체의 아고니스트로서 중수소화 티아졸리디논 유사체
EP3013823B1 (en) 2013-06-24 2017-11-01 Merck Patent GmbH Imidazole compounds as modulators of fshr and uses thereof
RU2663898C2 (ru) * 2013-06-24 2018-08-13 Мерк Патент Гмбх Пиразольные соединения в качестве модуляторов fshr и их применение
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003024936A1 (en) 2001-09-19 2003-03-27 Pharmacia Corporation Substituted pyrazolo compounds for the treatment of inflammation
WO2008035356A2 (en) 2006-09-20 2008-03-27 Glenmark Pharmaceuticals Limited Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
US20100216785A1 (en) 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compositions
US20100215741A1 (en) * 2009-02-25 2010-08-26 Neuroscienze Pharmaness S.C. A.R.L. Pharmaceutical compounds
WO2011058149A1 (en) * 2009-11-13 2011-05-19 Merck Serono S.A. Tricyclic pyrazol amine derivatives

Also Published As

Publication number Publication date
RU2752173C2 (ru) 2021-07-23
WO2015196759A1 (en) 2015-12-30
EP3157929A4 (en) 2018-03-07
CA2955415A1 (en) 2015-12-30
AU2021204814A1 (en) 2021-08-05
US20220402929A1 (en) 2022-12-22
AU2014398875A1 (en) 2017-02-02
ES2972131T3 (es) 2024-06-11
MX389867B (es) 2025-03-20
KR20170033314A (ko) 2017-03-24
AU2020201240A1 (en) 2020-03-12
EP3157929A1 (en) 2017-04-26
US10208055B2 (en) 2019-02-19
JP2019196375A (ja) 2019-11-14
DK3157929T3 (da) 2024-02-05
US10941152B2 (en) 2021-03-09
JP2021038245A (ja) 2021-03-11
JP2017524733A (ja) 2017-08-31
CN106573937B (zh) 2022-02-11
CN106573937A (zh) 2017-04-19
EP3157929B1 (en) 2023-12-13
MX2017000182A (es) 2017-06-30
US20170253605A1 (en) 2017-09-07
JP6557331B2 (ja) 2019-08-07
RU2017101829A3 (enExample) 2018-08-30
RU2017101829A (ru) 2018-07-27
AU2014398875B2 (en) 2019-11-21
AU2021204814B2 (en) 2023-07-20
WO2015196335A1 (en) 2015-12-30
US20190135823A1 (en) 2019-05-09

Similar Documents

Publication Publication Date Title
US10941152B2 (en) Pyrazole compounds as modulators of FSHR and uses thereof
KR102318498B1 (ko) Fshr의 조절인자로서의 피라졸 화합물 및 이의 용도
JP6523267B2 (ja) Ｆｓｈｒの調節剤としてのイミダゾール化合物及びその使用
HK1218757B (en) Pyrazole compounds as modulators of fshr and uses thereof

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

N231 Notification of change of applicant
PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R13-asn-PN2301

St.27 status event code: A-3-3-R10-R11-asn-PN2301

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20250630

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

H13 Ip right lapsed

Free format text: ST27 STATUS EVENT CODE: N-4-6-H10-H13-OTH-PC1903 (AS PROVIDED BY THE NATIONAL OFFICE); TERMINATION CATEGORY : DEFAULT_OF_REGISTRATION_FEE

Effective date: 20250630

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20250630