AU2023205435A1 - Substituted heterocycles as hset inhibitors - Google Patents

Substituted heterocycles as hset inhibitors Download PDF

Info

Publication number
AU2023205435A1
AU2023205435A1 AU2023205435A AU2023205435A AU2023205435A1 AU 2023205435 A1 AU2023205435 A1 AU 2023205435A1 AU 2023205435 A AU2023205435 A AU 2023205435A AU 2023205435 A AU2023205435 A AU 2023205435A AU 2023205435 A1 AU2023205435 A1 AU 2023205435A1
Authority
AU
Australia
Prior art keywords
mmol
methyl
amino
oxadiazol
hplc
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.)
Pending
Application number
AU2023205435A
Other languages
English (en)
Inventor
Hans-Peter Buchstaller
John Caldwell
Ian Collins
Giampiero COLOMBANO
Daniel Kuhn
Jan LANZ
Thomas Matthews
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.)
Merck Patent GmbH
Cancer Research Horizons
Institute of Cancer Research Royal Cancer Hospital
Original Assignee
Merck Patent GmbH
Cancer Res Horizons
Institute of Cancer Research Royal Cancer Hospital
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 Merck Patent GmbH, Cancer Res Horizons, Institute of Cancer Research Royal Cancer Hospital filed Critical Merck Patent GmbH
Publication of AU2023205435A1 publication Critical patent/AU2023205435A1/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/445—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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2023205435A 2022-01-10 2023-01-09 Substituted heterocycles as hset inhibitors Pending AU2023205435A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP22150667.8 2022-01-10
EP22150667 2022-01-10
PCT/EP2023/050255 WO2023131690A1 (en) 2022-01-10 2023-01-09 Substituted heterocycles as hset inhibitors

Publications (1)

Publication Number Publication Date
AU2023205435A1 true AU2023205435A1 (en) 2024-08-22

Family

ID=79288014

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2023205435A Pending AU2023205435A1 (en) 2022-01-10 2023-01-09 Substituted heterocycles as hset inhibitors

Country Status (8)

Country Link
US (1) US20250084074A1 (https=)
EP (1) EP4463444A1 (https=)
JP (1) JP2025503661A (https=)
CN (1) CN119421877A (https=)
AU (1) AU2023205435A1 (https=)
CA (1) CA3247641A1 (https=)
IL (1) IL314200A (https=)
WO (1) WO2023131690A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR130226A1 (es) * 2022-08-23 2024-11-20 Merck Patent Gmbh Biciclos sustituidos como inhibidores de hset

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4207554A (en) 1972-08-04 1980-06-10 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US4125828A (en) 1972-08-04 1978-11-14 Med-El Inc. Method and apparatus for automated classification and analysis of cells
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE69720965T2 (de) 1996-02-13 2004-02-05 Astrazeneca Ab Chinazolinderivate und deren verwendung als vegf hemmer
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9823871D0 (en) * 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
AU2001258628A1 (en) 2000-05-31 2001-12-11 Astrazeneca Ab Indole derivatives with vascular damaging activity
MXPA02012903A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como inhibidores de angiogenesis.
MXPA02012905A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como agentes de dano vascular..
US7250415B2 (en) * 2003-06-04 2007-07-31 Bristol-Myers Squibb Company 1,1-Disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, β-aminoacids, α-aminoacids and derivatives thereof as factor Xa inhibitors
CA2725911A1 (en) 2008-05-30 2009-12-23 Dana-Farber Cancer Institute, Inc. Methods of treating a meiotic kinesin-associated disease
US20150309031A2 (en) 2013-12-05 2015-10-29 Novazoi Theranostics Compositions and methods for prognosis and treatment of cancer
US9783510B2 (en) * 2014-08-22 2017-10-10 Vanderbilt University Small molecule mediated transcriptional induction of E-cadherin

Also Published As

Publication number Publication date
EP4463444A1 (en) 2024-11-20
JP2025503661A (ja) 2025-02-04
CN119421877A (zh) 2025-02-11
CA3247641A1 (en) 2023-07-13
IL314200A (en) 2024-09-01
US20250084074A1 (en) 2025-03-13
WO2023131690A1 (en) 2023-07-13

Similar Documents

Publication Publication Date Title
AU2014209107B2 (en) Metalloenzyme inhibitor compounds
TWI781920B (zh) 化合物、組合物及方法
JP2022071046A (ja) Ｗｄｒ５タンパク質－タンパク質結合の阻害剤
EP3197883B1 (en) Novel compounds
KR102627266B1 (ko) 암의 치료를 위한 2-헤테로아릴-3-옥소-2,3-디히드로피리다진-4-카르복스아미드
US12377083B2 (en) Lysophosphatidic acid receptor antagonist and preparation method therefor
EP3191478B1 (en) Compounds and compositions as raf kinase inhibitors
AU2021202065A1 (en) Hepatitis B core protein modulators
JP6308504B2 (ja) タンパク質キナーゼ阻害薬
CN111201223A (zh) SHP2的八氢环戊二烯并[c]吡咯别构抑制剂
RS60574B1 (sr) Heteroaril supstituisani piridini i metode upotrebe
CN109790112A (zh) 具有作为usp30抑制剂活性的氰基吡咯烷衍生物
KR20190009369A (ko) 3-옥소-2,6-디페닐-2,3-디히드로피리다진-4-카르복스아미드
KR20100031639A (ko) 증식성 질환의 치료용 삼중 치환된 피리미딘 유도체
KR20090092822A (ko) Ｐｌｋ1 억제제로서의 신규한 아미노피리미딘 유도체
EP2809652B1 (en) Isoquinoline and naphthyridine derivatives
US20230002396A1 (en) Therapeutic compounds
KR20100134693A (ko) 2-아미노퀴나졸린 유도체
CN108349965B (zh) 1,3,4-噻二唑化合物及其在治疗癌症中的用途
JP2023510746A (ja) Ｓｍａｒｃａ２－ｖｈｌ分解剤
US10815226B2 (en) Heteroaryl compounds as inhibitors of necrosis, composition and application thereof
KR20230016674A (ko) 미토콘드리아 기능장애의 치료를 위한 usp30 억제제로서 n-(1-시아노피롤리딘-3-일)-5-(3-(트라이플루오로메틸)페닐)옥사졸-2-카복스아미드 유도체 및 상응하는 옥사다이아졸 유도체
AU2023205435A1 (en) Substituted heterocycles as hset inhibitors
US10494363B2 (en) Non-steroidal glucocorticoid receptor modulators for local drug delivery
CN120265629A (zh) 被取代的双环和三环hset抑制剂