AR072816A1 - Derivados heterociclicos de piridazina, inhibidores de smo, composiciones farmaceuticas que los comprenden y uso de los mismos como agentes anticancer. - Google Patents
Derivados heterociclicos de piridazina, inhibidores de smo, composiciones farmaceuticas que los comprenden y uso de los mismos como agentes anticancer.Info
- Publication number
- AR072816A1 AR072816A1 ARP090102720A ARP090102720A AR072816A1 AR 072816 A1 AR072816 A1 AR 072816A1 AR P090102720 A ARP090102720 A AR P090102720A AR P090102720 A ARP090102720 A AR P090102720A AR 072816 A1 AR072816 A1 AR 072816A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- group
- nr6r8
- members
- Prior art date
Links
- 239000002246 antineoplastic agent Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 30
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 7
- 229910052799 carbon Inorganic materials 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000001188 haloalkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- -1 L is a bond Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings 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
- C07D237/20—Nitrogen atoms
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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
- A61K31/435—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
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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
- A61K31/435—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
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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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto de la formula 1 o una sal farmacéuticamente aceptable del mismo, en donde: R1 es un grupo arilo de 6 a 14 átomos de carbono, o un grupa heteroarilo de 5 a 14 miembros, cada uno de los cuales puede estar insustituido o sustituido por uno o más de alquilo de 1 a 8 átomos de carbono, un grupo arilo de 6 a 14 átomos de carbono, halo-alquilo de 1 a 8 átomos de carbono, alcoxilo de 1 a 8 átomos de carbono, halogeno, NH2, CN, OCF3, OH, C(O)NR6R8, C(O)R6, NR6R8, NHC(O)R6, SO2R6, SO2NR6R8; R2 y R3 son independientemente alquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono-OH, o R2 y R3 forman un grupo cicloalquilo de 3 a 14 átomos de carbono, L es un enlace, alquileno de 1 a 8 átomos de carbono, -C(O)O-, -CONR9-, -alquilo de 1 a 8 átomos de carbono-OH-, halo-alquilo de 1 a 8 átomos de carbono, -C(O)-, -NH- u -O-; X y W son independientemente N o CR5, y cuando menos uno de X y W es N; R7 es un grupo arilo de 6 a 14 átomos de carbono, un grupo heteroarilo de 5 a 14 miembros, o un grupo cicloheteroalquilo de 3 a 14 miembros; R4 es alquilo de 1 a 8 átomos de carbono, alquenilo de 2 a 8 átomos de carbono, cicloalquilo de 3 a 14 átomos de carbono, un grupo arilo de 6 a 14 átomos de carbono, un grupo heteroarilo de 5 a 14 miembros, un grupo cicloheteroalquilo de 3 a 14 miembros, alcoxilo de 1 a 8 átomos de carbono, halogeno, NR6R8, C(O)OR6, C(O)NR6R8, halo-alquilo de 1 a 8 átomos de carbono, formilo carbalcoxilo, alquilo de 1 a 8 átomos de carbono-OH, C(O)R6, SO2R6, C(O)NH-alquilo de 1 a 8 átomos de carbono-R6, NR6R8, SO2NR6R8, OCF3, NHC(O)R6, CH2OC(O)NR6R8 CH2NR6R8, NHC(O)OR6, NHC(O)NR6R8, CH2NHSO2R6, CH2NHC(O)OR6, OC(O)R6, o NHC(O)R6, el cual puede estar sustituido o insustituido; Z es alquilo de 1 a 8 átomos de carbono, CN, OH, o halogeno; m y p son independientemente de 0 a 3; Y es un enlace, alquileno de 1 a 8 átomos de carbono, -C(O)-, -C(O)O-,-CH(OH)-, o -C(O)N(R10)-; R5 es H, halogeno, CN, alquilo inferior, OH, OCH3 u OCF3; R9 y R10 son independientemente alquilo de 1 a 8 átomos de carbono o H; R6 y R8 son independientemente H, alquilo de 1 a 8 átomos de carbono, alquenilo de 2 a 8 átomos de carbono, cicloalquilo de 3 a 14 átomos de carbono, un grupo arilo de 6 a 14 átomos de carbono, un grupo heteroarilo de 5 a 14 miembros, un grupo cicloheteroalquilo de 3 a 14 miembros, halo-alquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono-OH, alcoxilo de 1 a 8 átomos de carbono, o R6 y R8 sobre un átomo pueden formar un anillo que contiene heteroátomo; y en donde R4, R6, y R8 pueden estar insustituidos o sustituidos por uno o más de alquilo de 1 a 8 átomos de carbono, cicloalquilo de 3 a 14 átomos de carbono, un grupo arilo de 6 a 14 átomos de carbono, un grupo heteroarilo de 5 a 14 miembros, un grupo cicloheteroalquilo de 3 a 14 miembros, alquilo de 1 a 8 átomos de carbono-OH, OH, oxo, halo-alquilo de 1 a 8 átomos de carbono, carboxi-alquilo de 1 a 8 átomos de carbono, o SO2aIquiIo de 1 a 8 átomos de carbono, halogeno, -OCH3, -OCF3, -OH, -NH2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8190008P | 2008-07-18 | 2008-07-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072816A1 true AR072816A1 (es) | 2010-09-22 |
Family
ID=41130287
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102720A AR072816A1 (es) | 2008-07-18 | 2009-07-16 | Derivados heterociclicos de piridazina, inhibidores de smo, composiciones farmaceuticas que los comprenden y uso de los mismos como agentes anticancer. |
Country Status (43)
Families Citing this family (49)
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| TWI433674B (zh) | 2006-12-28 | 2014-04-11 | Infinity Discovery Inc | 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類 |
| UA102250C2 (ru) | 2008-04-29 | 2013-06-25 | Эли Лилли Энд Компани | Двухзамещенные фталазины - антагонисты проводящего пути hedgehog |
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| EP2358698B1 (en) | 2008-11-17 | 2012-09-05 | Eli Lilly and Company | Tetrasubstituted pyridazine as hedgehog pathway antagonists |
| KR101335770B1 (ko) | 2008-11-17 | 2013-12-12 | 일라이 릴리 앤드 캄파니 | 사치환된 피리다진 헷지호그 경로 길항제 |
| AR077014A1 (es) | 2009-06-19 | 2011-07-27 | Lilly Co Eli | Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer |
| RU2012125152A (ru) * | 2009-11-18 | 2013-12-27 | Новартис Аг | Способы и композиции, предназначенные для лечения солидных опухолей и других злокачественных новообразований |
| KR20120123325A (ko) | 2009-12-15 | 2012-11-08 | 시오노기세야쿠 가부시키가이샤 | 혈관 내피 리파아제 저해 활성을 갖는 옥사디아졸 유도체 |
| AR080908A1 (es) | 2010-04-16 | 2012-05-16 | Novartis Ag | Formulaciones de un piridazin -bipirazinilo |
| SG185515A1 (en) | 2010-05-13 | 2012-12-28 | Amgen Inc | Nitrogen heterocyclic compounds useful as pde10 inhibitors |
| EP2511273B8 (en) * | 2011-04-15 | 2019-06-26 | Hivih | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| SG194800A1 (en) | 2011-06-02 | 2013-12-30 | Novartis Ag | Biomarkers for hedgehog inhibitor therapy |
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| EP3092235A2 (en) | 2014-01-06 | 2016-11-16 | Rhizen Pharmaceuticals S.A. | Novel inhibitors of glutaminase |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
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