HRP20140953T1 - Morfolino pirimidini i njihova uporaba za lijeäśenje - Google Patents
Morfolino pirimidini i njihova uporaba za lijeäśenje Download PDFInfo
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- HRP20140953T1 HRP20140953T1 HRP20140953AT HRP20140953T HRP20140953T1 HR P20140953 T1 HRP20140953 T1 HR P20140953T1 HR P20140953A T HRP20140953A T HR P20140953AT HR P20140953 T HRP20140953 T HR P20140953T HR P20140953 T1 HRP20140953 T1 HR P20140953T1
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- Prior art keywords
- methyl
- methylsulfonimidoyl
- methylmorpholin
- pyrimidin
- benzimidazol
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- 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
- A61K31/435—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1. Spoj s formulom (I):
[image]
naznačen time da:
R1 je odabran od morfolin-4-il i 3-metilmorfolin-4-il;
R2 je
[image]
n je 0 ili 1;
R2A R2C, R2E i R2F svaki neovisno su vodik ili metil;
R2B i R2D svaki neovisno su vodik ili metil;
R2G je odabran od -NHR7 i -NHCOR8;
R2H je fluoro;
R3 je metil;
R4 i R5 svaki neovisno su vodik ili metil, ili R4 i R5 zajedno s atomom na koji su vezani tvore Prsten A;
Prsten A je C3-6cikloalkil ili zasićeni 4-6 člani heterociklički prsten koji sadrži jedan heteroatom odabran od O i N;
R6 je vodik;
R7 je vodik ili metil;
R8 je metil,
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1 naznačen time da R4 i R5 zajedno s atomom na koji su vezani tvore Prsten A, i Prsten A je C3-6cikloalkil ili zasićeni 4-6 člani heterociklički prsten koji sadrži jedan heteroatom odabran od O i N.
3. Spoj prema zahtjevu 1 ili 2 naznačen time da Prsten A je ciklopropil, tetrahidropiranil ili piperidinil prsten.
4. Spoj prema bilo kojem zahtjevu od 1 do 3 naznačen time da R2A je vodik; R2B je vodik; R2C je vodik; R2D je vodik; R2E je vodik; i R2F je vodik.
5. Spoj prema bilo kojem zahtjevu od 1 do 4 naznačen time da R1 je 3-metilmorfolin-4-il.
6. Spoj prema bilo kojem zahtjevu od 1 do 5 naznačen time da spoj s formulom (I) je spoj s formulom (Ia),
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema zahtjevu 6, ili njegova farmaceutski prihvatljiva sol naznačen time da:
Prsten A je ciklopropil prsten;
R2 je
[image]
n je 0 ili 1;
R2A je vodik;
R2B je vodik;
R2C je vodik;
R2D je vodik;
R2E je vodik;
R2F je vodik;
R2G je -NHR7;
R2H je fluoro;
R3 je metil skupina;
R6 je vodik; i
R7 je vodik ili metil,
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema zahtjevu 1 naznačen time da je spoj s formulom (I) odabran od bilo kojeg od slijedećih spojeva:
4-{4-[(3R)-3-Metilmorfolin-4-il]-6-[((R)-S-metilsulfonimidoil)metil]pirimidin-2-il}-1H-pirolo[2,3-b]piridin;
4-{4-[(3R)-3-Metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pilimidin-2-il}-1H-pirolo[2,3-b]piridin;
4-{4-[(3R)-3-Metilinorpholin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-pirolo[2,3-b]piridin;
N-Metil-1-{4-[(3R)-3-metilinorpholin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
N-Metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
4-{4-[(3R)-3-Metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-indol;
4-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-indol;
1-{4-[(3R)-3-Metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il }-1H-benzimidazol-2-amin;
4-Fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
4-fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
4-{4-[(3R)-3-Metilmorfolin-4-il]-6-1-(S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-pirolo[2,3-c]piridin;
N-metil-1-{4-[1-metil-1-((S)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
N-metil-1-{4-[1-metil-1-((R)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
N-Metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[4-((S)-S-metilsulfonimidoil)tetrahidro-2H-piran-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[4-((R)-S-metilsulfonimidoil)tetrahidro-2H-piran-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
4-{4-[(3R)-3-Metilmorfolin-4-il]-6-[4-((S)-S-metilsulfonimidoil)tetrahidro-2H-piran-4-il]pirimidin-2-il}-1H-indol;
4-Fluoro-N-metil-1-{4-[1-metil-1-((S)-S-metilsulfonimidoil)etil]-6-[(3R)-3 metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
4-fluoro-N-metil-1-{4-[1-metil-1-((R)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
6-Fluoro-N-metil-1-{4-[1-metil-1-((R)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
5-Fluoro-N-metil-1-{4-[1-metil-1-((R)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
5-Fluoro-N-metil-1-{4-[1-metil-1-((S)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
6-fluoro-N-metil-1-{4-[1-metil-1-((S)-S-metilsulfonimidoil)etil]-6-[(3R)-3-metilmorfolin-4-il]pirimidin-2-il}-1H-benzimidazol-2-amin;
6-Fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il)-1H-benzimidazol-2-amin;
5-fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin;
5-fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il)-1H-benzimidazol-2-amin; i
6-fluoro-N-metil-1-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-benzimidazol-2-amin, ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 1 naznačen time da spoj s formulom (I) je 4-{4-[(3R)-3-Metilmorfolin-4-il]-6-[1-((S)-S-metilsulfonimidoil)ciklopropil]pirimidin-2-il}-1H-pirolo[2,3-b]piridin.
10. Spoj prema zahtjevu 1 naznačen time da spoj s formulom (I) je 4-{4-[(3R)-3-metilmorfolin-4-il]-6-[1-((R)-S-metilsulfonimidoil)ciklopropil] pirimidin-2-il}-1H-pirolo[2,3-b]piridin.
11. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem ili više zahtjeva od 1 do 10 naznačen time da je za uporabu za liječenje raka.
12. Farmaceutski pripravak koji sadrži spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, prema bilo kojem ili više zahtjeva od 1 do 10 naznačen time da je u kombinaciji s farmaceutski prihvatljivim pomoćnim sredstvom, sredstvom za razrjeđivanje ili nosačem.
13. Uporaba spoja s formulom (I), ili njegove farmaceutski prihvatljive soli, prema bilo kojem zahtjevu od 1 do 10 naznačena time da je za proizvodnju lijeka za uporabu za sprečavanje ili liječenje onih tumora koji su osjetljivi na inhibiciju ATR kinaze.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35371310P | 2010-06-11 | 2010-06-11 | |
| PCT/GB2011/051074 WO2011154737A1 (en) | 2010-06-11 | 2011-06-09 | Morpholino pyrimidines and their use in therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140953T1 true HRP20140953T1 (hr) | 2014-12-05 |
Family
ID=44168987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140953AT HRP20140953T1 (hr) | 2010-06-11 | 2011-06-09 | Morfolino pirimidini i njihova uporaba za lijeäśenje |
Country Status (38)
| Country | Link |
|---|---|
| US (5) | US8252802B2 (hr) |
| EP (1) | EP2579877B1 (hr) |
| JP (1) | JP5721821B2 (hr) |
| KR (1) | KR101820996B1 (hr) |
| CN (1) | CN103068391B (hr) |
| AR (1) | AR081859A1 (hr) |
| AU (1) | AU2011263491B2 (hr) |
| BR (1) | BR112012031561B1 (hr) |
| CA (1) | CA2800203C (hr) |
| CL (1) | CL2012003503A1 (hr) |
| CO (1) | CO6640270A2 (hr) |
| CR (1) | CR20120628A (hr) |
| CU (1) | CU24109B1 (hr) |
| DK (1) | DK2579877T3 (hr) |
| DO (1) | DOP2012000310A (hr) |
| EA (1) | EA022087B1 (hr) |
| EC (1) | ECSP12012334A (hr) |
| ES (1) | ES2514325T3 (hr) |
| GT (1) | GT201200334A (hr) |
| HR (1) | HRP20140953T1 (hr) |
| MX (1) | MX2012014477A (hr) |
| MY (1) | MY158193A (hr) |
| NI (1) | NI201200184A (hr) |
| NZ (1) | NZ604480A (hr) |
| PE (1) | PE20130306A1 (hr) |
| PH (1) | PH12012502438A1 (hr) |
| PL (1) | PL2579877T3 (hr) |
| PT (1) | PT2579877E (hr) |
| RS (1) | RS53566B1 (hr) |
| SA (1) | SA111320519B1 (hr) |
| SG (1) | SG185711A1 (hr) |
| SI (1) | SI2579877T1 (hr) |
| SM (1) | SMT201400146B (hr) |
| TW (1) | TWI526208B (hr) |
| UA (1) | UA109010C2 (hr) |
| UY (1) | UY33440A (hr) |
| WO (1) | WO2011154737A1 (hr) |
| ZA (1) | ZA201300255B (hr) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SA111320519B1 (ar) | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| NZ727399A (en) | 2014-06-17 | 2022-07-29 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
| TWI656121B (zh) | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | ２－（嗎啉－４－基）－１，７－萘啶 |
| KR102678021B1 (ko) | 2015-09-30 | 2024-06-26 | 버텍스 파마슈티칼스 인코포레이티드 | Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물 |
| WO2018029117A1 (en) * | 2016-08-10 | 2018-02-15 | Rheinisch-Westfälische Technische Hochschule Aachen (RWTH) | New atr inhibitors for the use in cancer therapy |
| US11110108B2 (en) * | 2016-09-27 | 2021-09-07 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| UY37616A (es) | 2017-02-24 | 2018-09-28 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2018218197A2 (en) | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| ES2974334T3 (es) | 2017-07-13 | 2024-06-26 | Univ Texas | Inhibidores heterocíclicos de ATR cinasa |
| EP3661560B1 (en) | 2017-08-04 | 2025-02-26 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors |
| CN111886224B (zh) * | 2017-08-17 | 2024-07-23 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| CN111655688B (zh) * | 2017-09-08 | 2023-09-29 | 蓝谷制药有限责任公司 | 经取代的吡咯并吡啶类化合物作为atr抑制剂 |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| US11712440B2 (en) | 2017-12-08 | 2023-08-01 | Bayer Aktiengesellschaft | Predictive markers for ATR kinase inhibitors |
| GB201720989D0 (en) * | 2017-12-15 | 2018-01-31 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| CA3090330A1 (en) * | 2018-02-07 | 2019-08-15 | Shijiazhuang Sagacity New Drug Development Co., Ltd. | Atr inhibitor and application thereof |
| CN112218631B (zh) | 2018-03-16 | 2023-12-22 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| WO2020078788A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| MA54091A (fr) | 2018-10-30 | 2021-09-15 | Repare Therapeutics Inc | Composés, compositions pharmaceutiques, procédés de préparation de composés et leur utilisation en tant qu'inhibiteurs de kinase atr |
| JP7600116B2 (ja) * | 2018-12-18 | 2024-12-16 | アストラゼネカ・アクチエボラーグ | 製薬方法及び中間体 |
| KR20220008869A (ko) | 2019-05-14 | 2022-01-21 | 누베이션 바이오 인크. | 항암 핵 호르몬 수용체-표적화 화합물 |
| GB201908536D0 (en) * | 2019-06-13 | 2019-07-31 | Glaxosmithkline Ip Dev Ltd | Compounds |
| CN112142744A (zh) * | 2019-06-28 | 2020-12-29 | 上海瑛派药业有限公司 | 取代的稠合杂芳双环化合物作为激酶抑制剂及其应用 |
| FI4011881T3 (fi) * | 2019-08-06 | 2025-03-19 | Wuxi Biocity Biopharmaceutics Co Ltd | Atr-inhibiittorin kiteisiä muotoja ja niiden käyttö |
| TW202131930A (zh) | 2019-11-13 | 2021-09-01 | 美商諾維雪碧歐公司 | 抗癌核荷爾蒙受體標靶化合物 |
| JP2023502458A (ja) * | 2019-11-21 | 2023-01-24 | 江蘇恒瑞医薬股▲ふん▼有限公司 | ピラゾロヘテロアリール系誘導体、その調製方法及びその医薬的応用 |
| CN112939966B (zh) * | 2019-12-10 | 2023-03-24 | 武汉光谷亚太医药研究院有限公司 | 嘧啶衍生物、其制备及应用 |
| TW202140474A (zh) * | 2020-01-17 | 2021-11-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合雜芳基類衍生物、其製備方法及其在醫藥上的應用 |
| US20240150333A1 (en) * | 2020-03-20 | 2024-05-09 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Taf1 inhibitors |
| AU2021269764A1 (en) | 2020-05-11 | 2023-01-19 | Astrazeneca Ab | ATR inhibitors for the treatment of cancer |
| AU2021282122B2 (en) * | 2020-05-29 | 2023-09-21 | Wuxi Life Fountain Biotech Co., Ltd | Fluoropyrrolopyridine compound and application thereof |
| CN111646985A (zh) * | 2020-06-01 | 2020-09-11 | 江苏集萃分子工程研究院有限公司 | 一种含嘧啶杂环抗肿瘤药物分子azd6738的合成方法 |
| JP2023542066A (ja) | 2020-06-24 | 2023-10-05 | アストラゼネカ ユーケー リミテッド | 抗体－薬物コンジュゲートとａｔｒ阻害剤との組み合わせ |
| CN115943145A (zh) * | 2020-07-13 | 2023-04-07 | 北京泰德制药股份有限公司 | 作为atr激酶抑制剂的吡唑并嘧啶化合物 |
| WO2022094218A1 (en) * | 2020-10-29 | 2022-05-05 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Process for the preparation of heteroaryl-substituted sulfur(vi) compounds |
| TW202304457A (zh) | 2021-03-22 | 2023-02-01 | 瑞典商阿斯特捷利康公司 | 配製物 |
| WO2022204184A1 (en) | 2021-03-23 | 2022-09-29 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| US20240197748A1 (en) | 2021-03-26 | 2024-06-20 | Astrazeneca Ab | Combination treatment for melanoma |
| JP2024516024A (ja) | 2021-05-03 | 2024-04-11 | ニューベイション・バイオ・インコーポレイテッド | 抗がん核内ホルモン受容体標的化化合物 |
| IT202100021863A1 (it) | 2021-08-13 | 2023-02-13 | Univ Degli Studi Milano | Morfolino pirimidine per l’uso nella prevenzione e/o nel trattamento di stati di ipereccitabilità neuronale |
| US20240398800A1 (en) * | 2021-09-10 | 2024-12-05 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compounds for targeted degradation of taf1 |
| CN116283960A (zh) * | 2021-12-21 | 2023-06-23 | 上海安诺达生物科技有限公司 | 取代的稠杂环化合物及其制备方法与应用 |
| WO2023122723A1 (en) | 2021-12-23 | 2023-06-29 | The Broad Institute, Inc. | Panels and methods for diagnosing and treating lung cancer |
| US20250064967A1 (en) | 2021-12-28 | 2025-02-27 | Astrazeneca Uk Limited | Combination of antibody-drug conjugate and atr inhibitor |
| TW202348252A (zh) | 2022-02-16 | 2023-12-16 | 英商梅迪繆思有限公司 | 用治療性結合分子治療癌症的組合療法 |
| EP4539847A1 (en) | 2022-06-15 | 2025-04-23 | Astrazeneca AB | Combination therapy for treating cancer |
| AU2023389547A1 (en) | 2022-12-06 | 2025-07-17 | Astrazeneca Ab | Polq inhibitors |
| WO2024213699A1 (en) | 2023-04-14 | 2024-10-17 | Astrazeneca Ab | Combinations of kras inhibitor and atr inhibitor for the treatment of cancer |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3922735A1 (de) | 1989-07-11 | 1991-01-24 | Hoechst Ag | Aminopyrimidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide |
| WO1998035985A1 (en) | 1997-02-12 | 1998-08-20 | The Regents Of The University Of Michigan | Protein markers for lung cancer and use thereof |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging 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 |
| NZ530832A (en) | 1999-02-10 | 2005-05-27 | Astrazeneca Ab | Quinazoline derivatives as angiogenesis inhibitors |
| CA2389767C (en) | 1999-11-05 | 2010-03-23 | Laurent Francois Andre Hennequin | Quinazoline derivatives as vegf inhibitors |
| CO5280092A1 (es) | 2000-02-15 | 2003-05-30 | Sugen Inc | Indolinas susutituidas con pirroles inhibidoras de proteinquinasas |
| ATE503743T1 (de) | 2000-04-27 | 2011-04-15 | Astellas Pharma Inc | Kondensierte heteroarylderivate |
| CN1431999A (zh) | 2000-05-31 | 2003-07-23 | 阿斯特拉曾尼卡有限公司 | 具有血管损伤活性的吲哚衍生物 |
| UA73993C2 (uk) | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| KR20030014425A (ko) | 2000-07-07 | 2003-02-17 | 앤지오젠 파마슈티칼스 리미티드 | 혈관 손상제인 콜치놀 유도체 |
| SK52003A3 (en) | 2000-07-07 | 2003-07-01 | Angiogene Pharm Ltd | Colchinol derivatives as angiogenesis inhibitors, method for their preparation and pharmaceutical composition comprising the same |
| CN1473156A (zh) | 2000-11-10 | 2004-02-04 | - | 嘧啶衍生物及其作为神经肽y受体配体的用途 |
| EA013811B1 (ru) | 2002-11-21 | 2010-08-30 | Новартис Вэксинес Энд Дайэгностикс, Инк. | 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака |
| EP1626725A4 (en) | 2003-05-29 | 2006-06-14 | Synta Pharmaceuticals Corp | Heterocyclic compounds for the prevention and treatment of disorders associated with excessive bone formation |
| GB0415367D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415365D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415364D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| US7772271B2 (en) | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| WO2007084413A2 (en) | 2004-07-14 | 2007-07-26 | Ptc Therapeutics, Inc. | Methods for treating hepatitis c |
| JP2008519850A (ja) | 2004-11-10 | 2008-06-12 | シンタ ファーマシューティカルズ コーポレーション | Ｉｌ−１２調節化合物 |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| TW200720256A (en) | 2005-05-13 | 2007-06-01 | Synta Pharmaceuticals Corp | IL-12 modulatory compounds |
| ES2473341T3 (es) | 2005-05-20 | 2014-07-04 | Methylgene Inc | Inhibidores de la se�alizaci�n del receptor del VEGF y del receptor del HGF |
| DE102005024494A1 (de) | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Verwendung von Cyanopyrimidinen |
| KR20080015475A (ko) * | 2005-07-01 | 2008-02-19 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 피리미딘-치환 벤즈이미다졸유도체 |
| WO2007013691A1 (ja) | 2005-07-29 | 2007-02-01 | Takeda Pharmaceutical Company Limited | スピロ環化合物 |
| US20070049603A1 (en) | 2005-09-01 | 2007-03-01 | Greg Miknis | Raf inhibitor compounds and methods of use thereof |
| JP2007091649A (ja) | 2005-09-29 | 2007-04-12 | Taisho Pharmaceut Co Ltd | ピリミジン誘導体及びその使用に関連する治療方法 |
| JP4531027B2 (ja) | 2005-09-29 | 2010-08-25 | 田辺三菱製薬株式会社 | 医薬組成物 |
| KR101487027B1 (ko) | 2005-09-30 | 2015-01-28 | 미카나 테라퓨틱스, 인크. | 치환된 피라졸 화합물 |
| CA2623032A1 (en) | 2005-09-30 | 2007-04-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| GB2431156A (en) | 2005-10-11 | 2007-04-18 | Piramed Ltd | 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase |
| HRP20120824T1 (hr) | 2005-10-28 | 2012-11-30 | Astrazeneca Ab | Derivati 4-(3-aminopirazol) pirimidina za uporabu kao inhibitori tirozin kinaze u lijeäśenju karcinoma |
| CA2636314A1 (en) | 2005-11-29 | 2007-06-07 | Toray Industries, Inc. | Arylmethylene urea derivative and use thereof |
| GB0525080D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525081D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525083D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| AU2007204208A1 (en) | 2006-01-11 | 2007-07-19 | Astrazeneca Ab | Morpholino pyrimidine derivatives and their use in therapy |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EA200870217A1 (ru) | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| WO2007105023A1 (en) | 2006-03-15 | 2007-09-20 | Csir | Modulation of phosphoryl transferase activity of glutamine synthetase |
| JP5243696B2 (ja) | 2006-03-17 | 2013-07-24 | 田辺三菱製薬株式会社 | ベンゼン誘導体 |
| US8044068B2 (en) | 2006-04-04 | 2011-10-25 | Taisho Pharmaceutical Co., Ltd | Aminopyrrolidine compound |
| AU2007240496A1 (en) | 2006-04-19 | 2007-11-01 | Novartis Ag | Indazole compounds and methods for inhibition of CDC7 |
| WO2007126043A1 (ja) | 2006-04-27 | 2007-11-08 | Mitsubishi Tanabe Pharma Corporation | チアゾール環を含むカルボン酸誘導体の医薬用途 |
| GB0610909D0 (en) | 2006-06-05 | 2006-07-12 | Merck Sharp & Dohme | Therapeutic treatment |
| CA2656290A1 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| JP2010501537A (ja) | 2006-08-24 | 2010-01-21 | アストラゼネカ アクチボラグ | 増殖性障害の治療に有用なモルホリノピリミジン誘導体 |
| EP2057140B1 (en) | 2006-08-24 | 2012-08-08 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| WO2008047307A1 (en) * | 2006-10-16 | 2008-04-24 | Gpc Biotech Inc. | Pyrido [2, 3-d] pyrimidines and their use as kinase inhibitors |
| JP2010523637A (ja) | 2007-04-12 | 2010-07-15 | エフ．ホフマン−ラ ロシュ アーゲー | 医薬化合物 |
| CN101801963A (zh) * | 2007-07-09 | 2010-08-11 | 阿斯利康(瑞典)有限公司 | 用于治疗增殖性疾病的三取代的嘧啶衍生物 |
| WO2010054764A1 (de) * | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Heteroaromatische verbindungen zur verwendung als hif-inhibitoren |
| US20110053923A1 (en) * | 2008-12-22 | 2011-03-03 | Astrazeneca | Chemical compounds 610 |
| SA111320519B1 (ar) * | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
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