HRP20161390T1 - Derivati azetidina i ciklobutana kao inhibitori jak - Google Patents
Derivati azetidina i ciklobutana kao inhibitori jak Download PDFInfo
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- HRP20161390T1 HRP20161390T1 HRP20161390TT HRP20161390T HRP20161390T1 HR P20161390 T1 HRP20161390 T1 HR P20161390T1 HR P20161390T T HRP20161390T T HR P20161390TT HR P20161390 T HRP20161390 T HR P20161390T HR P20161390 T1 HRP20161390 T1 HR P20161390T1
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- Prior art keywords
- cancer
- compound
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- compound according
- disease
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- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 title 1
- 125000001995 cyclobutyl group Chemical class [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010070834 Sensitisation Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 206010070835 Skin sensitisation Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- XUZMWHLSFXCVMG-UHFFFAOYSA-N baricitinib Chemical compound C1N(S(=O)(=O)CC)CC1(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 XUZMWHLSFXCVMG-UHFFFAOYSA-N 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- 230000008313 sensitization Effects 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 231100000370 skin sensitisation Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P17/00—Drugs for dermatological disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B60—VEHICLES IN GENERAL
- B60Q—ARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
- B60Q3/00—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
- B60Q3/70—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose
- B60Q3/76—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose for spotlighting, e.g. reading lamps
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B60—VEHICLES IN GENERAL
- B60Q—ARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
- B60Q3/00—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
- B60Q3/80—Circuits; Control arrangements
-
- 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
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S362/00—Illumination
- Y10S362/80—Light emitting diode
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S362/00—Illumination
- Y10S362/802—Position or condition responsive switch
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Mechanical Engineering (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Surgery (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (13)
1. Spoj, naznačen time što je {1-(etilsulfonil)-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je njegova sol s trifluoroctenom kiselinom.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je njegova fosfatna sol.
4. Pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, ili njegovu farmaceutski prihvatljivu sol, kao i najmanje jednu farmaceutski prihvatljivu podlogu.
5. Pripravak u skladu s patentnim zahtjevom 4, naznačen time što je pogodan za topikalnu primjenu.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je namijenjen upotrebi u liječenju autoimune bolesti.
7. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 6, naznačen time što je navedena autoimuna bolest poremećaj kože, multipla skleroza, reumatoidni artritis, psorijatični artritis, mladenački artritis, dijabetes tip I, lupus, upalna crijevna bolest, Crohnova bolest, miastenija gravis, imunoglobulinske nefropatije, miokarditis ili autoimuni poremećaj štitnjače.
8. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 7, naznačen time što je navedena autoimuna bolest reumatoidni artritis.
9. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 7, naznačen time što je navedena autoimuna bolest poremećaj kože, te je atopični dermatitis, psorijaza, sensibilizacija kože, iritacija kože, osip na koži, kontaktni dermatitis ili alergijska kontaktna sensibilizacija.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je namijenjen upotrebi u liječenju upalne bolesti.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je namijenjen upotrebi u liječenju raka.
12. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što je navedeni rak rak prostate, rak bubrega, rak jetre, rak dojke, rak pluća, rak štitnjače, Kaposijev sarkom, Castlemanova bolest ili rak gušterače.
13. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što je navedeni rak limfom, leukemija ili multipli mijelom.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US3566208P | 2008-03-11 | 2008-03-11 | |
US14498209P | 2009-01-15 | 2009-01-15 | |
EP09718650.6A EP2288610B8 (en) | 2008-03-11 | 2009-03-10 | Azetidine and cyclobutane derivatives as jak inhibitors |
PCT/US2009/036635 WO2009114512A1 (en) | 2008-03-11 | 2009-03-10 | Azetidine and cyclobutane derivatives as jak inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20161390T1 true HRP20161390T1 (hr) | 2016-12-02 |
Family
ID=40591836
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20161390TT HRP20161390T1 (hr) | 2008-03-11 | 2016-10-25 | Derivati azetidina i ciklobutana kao inhibitori jak |
Country Status (44)
Families Citing this family (275)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005105814A1 (en) * | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
CN103214483B (zh) | 2005-12-13 | 2014-12-17 | 因塞特公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
ES2415863T3 (es) * | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
MX2010005300A (es) * | 2007-11-16 | 2010-06-25 | Incyte Corp | 4-pirazolil-n-arilpirimidin-2-aminas y 4-pirazolil-n-heteroarilpir imidin-2-aminas como inhibidores de cinasas janus. |
CN102083830B (zh) | 2008-03-24 | 2014-11-12 | 梅迪维新技术公司 | 吡啶并[3,4-b]吲哚和应用方法 |
EP2288260A4 (en) * | 2008-06-20 | 2013-10-23 | Genentech Inc | TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD |
CN102131390A (zh) * | 2008-06-20 | 2011-07-20 | 健泰科生物技术公司 | 三唑并吡啶jak抑制剂化合物和方法 |
CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
BRPI1012159B1 (pt) | 2009-05-22 | 2022-01-25 | Incyte Holdings Corporation | Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos |
DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
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