CN107074823B - 治疗性化合物及其用途 - Google Patents

治疗性化合物及其用途 Download PDF

Info

Publication number
CN107074823B
CN107074823B CN201580059718.0A CN201580059718A CN107074823B CN 107074823 B CN107074823 B CN 107074823B CN 201580059718 A CN201580059718 A CN 201580059718A CN 107074823 B CN107074823 B CN 107074823B
Authority
CN
China
Prior art keywords
carbocyclyl
alkyl
compound
cancer
hydrogen
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
CN201580059718.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN107074823A (zh
Inventor
B·K·阿尔布雷克特
A·科特
T·克劳福德
M·杜普莱西斯
A·C·古德
Y·勒布朗
S·马格努森
C·G·那斯维舒克
R·帕斯特
F·A·罗梅罗
A·M·泰勒
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.)
Genentech Inc
Constellation Pharmaceuticals Inc
Original Assignee
Genentech Inc
Constellation Pharmaceuticals Inc
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 Genentech Inc, Constellation Pharmaceuticals Inc filed Critical Genentech Inc
Publication of CN107074823A publication Critical patent/CN107074823A/zh
Application granted granted Critical
Publication of CN107074823B publication Critical patent/CN107074823B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/061,2,4-Triazines
    • C07D253/0651,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/071,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/061,2,4-Triazines
    • C07D253/0651,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/071,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D253/075Two hetero atoms, in positions 3 and 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580059718.0A 2014-09-05 2015-09-02 治疗性化合物及其用途 Expired - Fee Related CN107074823B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462046770P 2014-09-05 2014-09-05
US62/046,770 2014-09-05
PCT/US2015/048174 WO2016036873A1 (en) 2014-09-05 2015-09-02 Therapeutic compounds and uses thereof

Publications (2)

Publication Number Publication Date
CN107074823A CN107074823A (zh) 2017-08-18
CN107074823B true CN107074823B (zh) 2021-05-04

Family

ID=54140703

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580059718.0A Expired - Fee Related CN107074823B (zh) 2014-09-05 2015-09-02 治疗性化合物及其用途

Country Status (5)

Country Link
US (1) US10358437B2 (https=)
EP (1) EP3189046B1 (https=)
JP (1) JP6814730B2 (https=)
CN (1) CN107074823B (https=)
WO (1) WO2016036873A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3189049B1 (en) 2014-09-05 2024-03-20 Genentech, Inc. Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer
EP3242874B1 (en) 2015-01-09 2018-10-31 Genentech, Inc. Pyridazinone derivatives and their use in the treatment of cancer
CN110117271A (zh) * 2018-02-06 2019-08-13 中国科学院上海药物研究所 四氢异喹啉类化合物、其制备方法、包含此类化合物的药物组合物及其用途
TWI840423B (zh) * 2018-10-12 2024-05-01 美商拓臻股份有限公司 甲狀腺素受體β促效劑化合物
CN111320609A (zh) 2018-12-13 2020-06-23 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
WO2021022163A2 (en) * 2019-07-31 2021-02-04 Foghorn Therapeutics Inc. Compounds and uses thereof
KR102085758B1 (ko) * 2019-08-05 2020-03-06 연세대학교 산학협력단 히스톤 아세틸트렌스퍼라제 p300 억제용 신규 화합물 및 이를 포함하는 항섬유화 조성물
AU2020336272A1 (en) 2019-08-23 2022-04-14 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
CN114375193B (zh) 2019-09-12 2024-05-14 拓臻制药公司 甲状腺激素受体β激动剂化合物
WO2024050078A1 (en) 2022-09-02 2024-03-07 Auron Therapeutics, Inc. Pyridazinon derivatives as kat2 degraders for the treatment of proliferative disorders
US20240398794A1 (en) 2023-04-07 2024-12-05 Terns Pharmaceuticals, Inc. COMBINATIONS OF GLP-1R AND THRß AGONISTS AND METHODS OF USE THEREOF

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5591743A (en) * 1993-07-06 1997-01-07 Pierre Fabre Medicament 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT1A ligands
CN102918031A (zh) * 2010-05-28 2013-02-06 通用电气健康护理有限公司 放射标记的化合物及其方法

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU22545A1 (es) 1994-11-18 1999-03-31 Centro Inmunologia Molecular Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico
US4943533A (en) 1984-03-01 1990-07-24 The Regents Of The University Of California Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor
EP0491007B1 (en) 1989-09-08 1996-03-13 The Johns Hopkins University Structural alterations of the egf receptor gene in human gliomas
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
EP0659439B1 (en) 1993-12-24 2001-10-24 MERCK PATENT GmbH Immunoconjugates
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
PL179659B1 (pl) 1994-07-21 2000-10-31 Akzo Nobel Nv Kompozycja cyklicznych nadtlenków ketonów sluzaca do modyfikowania (ko)polimerów zwlaszcza do degradacji polipropylenu PL PL PL PL PL PL PL
US5804396A (en) 1994-10-12 1998-09-08 Sugen, Inc. Assay for agents active in proliferative disorders
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
GB9508565D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
AU6267896A (en) 1995-06-07 1996-12-30 Imclone Systems Incorporated Antibody and antibody fragments for inhibiting the growth oftumors
MX9800215A (es) 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
ID19609A (id) 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
ATE241986T1 (de) 1997-05-06 2003-06-15 Wyeth Corp Verwendung von chinazolin verbindungen zur behandlung von polyzystischer nierenkrankheit
ZA986729B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
CN1278176A (zh) 1997-11-06 2000-12-27 美国氰胺公司 喹唑啉衍生物作为用于治疗结肠息肉的酪氨酸激酶抑制剂的应用
WO2000031048A1 (en) 1998-11-19 2000-06-02 Warner-Lambert Company N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, an irreversible inhibitor of tyrosine kinases
SG154433A1 (en) 2004-06-30 2009-08-28 Janssen Pharmaceutica Nv Phthalazine derivatives as parp inhibitors
FR2882750B1 (fr) * 2005-03-03 2007-05-11 Pierre Fabre Medicament Sa Derives de 1,2,4-triazines, leur preparation et leur application en therapeutique humaine
FR2933979B1 (fr) 2008-07-15 2012-08-24 Pf Medicament Derives de triazines et uraciles, leur preparation et leur application en therapeutique humaine
HRP20170159T1 (hr) * 2011-12-20 2017-03-24 Sanofi Izotiazolopiridin-2-karboksamidi i njihova upotreba kao lijekova
UY35103A (es) 2012-10-29 2014-05-30 Glaxo Group Ltd Compuestos de cefem 2-sustituidos
US9200005B2 (en) 2013-03-13 2015-12-01 AbbVie Deutschland GmbH & Co. KG Inhibitor compounds of phosphodiesterase type 10A
JP2016519672A (ja) 2013-03-15 2016-07-07 ジェネンテック, インコーポレイテッド ブロモドメイン含有タンパク質brd7およびbrd9の阻害によるth2媒介性疾患の治療
EP3189049B1 (en) 2014-09-05 2024-03-20 Genentech, Inc. Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer
EP3242874B1 (en) 2015-01-09 2018-10-31 Genentech, Inc. Pyridazinone derivatives and their use in the treatment of cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5591743A (en) * 1993-07-06 1997-01-07 Pierre Fabre Medicament 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT1A ligands
CN102918031A (zh) * 2010-05-28 2013-02-06 通用电气健康护理有限公司 放射标记的化合物及其方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Anomolous nucleosides and related compounds. XI. Amino acid derivatives of 6-azauracil;Chernetskii, V. P.等;《Khimiya Geterotsiklicheskikh Soedinenii》;19691231(第1期);第173-174页 *

Also Published As

Publication number Publication date
JP6814730B2 (ja) 2021-01-20
EP3189046B1 (en) 2020-08-26
WO2016036873A1 (en) 2016-03-10
US20170334883A1 (en) 2017-11-23
US10358437B2 (en) 2019-07-23
CN107074823A (zh) 2017-08-18
JP2017525740A (ja) 2017-09-07
EP3189046A1 (en) 2017-07-12

Similar Documents

Publication Publication Date Title
CN107108614B (zh) 作为布罗莫结构域抑制剂的取代的吡咯并吡啶
CN107074824B (zh) 作为用于治疗癌症的pcaf和gcn5抑制剂的式(i)的酞嗪衍生物
CN107074823B (zh) 治疗性化合物及其用途
JP6669744B2 (ja) ブロモドメインのインヒビターとしての置換ピロロピリジン
JP6639497B2 (ja) ブロモドメインインヒビターおよびその使用
CN107406429B (zh) 哒嗪酮衍生物及其在治疗癌症中的用途
JP2018510851A (ja) 治療用ピリダジン化合物およびその使用
HK40079390A (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK1242696A1 (en) Therapeutic compounds and uses thereof
HK1242696B (zh) 治療性化合物及其用途
HK1242695A1 (en) Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer
HK1247193A1 (en) Pyridazinone derivatives and their use in the treatment of cancer
HK1247193B (zh) 噠嗪酮衍生物及其在治療癌症中的用途
HK1244282A1 (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK1242695B (zh) 作為用於治療癌症的pcaf和gcn5抑制劑的式(i)的酞嗪衍生物
HK1244282B (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK1243076B (zh) 作為布羅莫結構域抑制劑的取代的吡咯並吡啶

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1242696

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20210504