PE20151375A1 - Compuestos ciclicos eter pirazol-4-il-heterociclil-carboxamida y metodos de utilizacion - Google Patents
Compuestos ciclicos eter pirazol-4-il-heterociclil-carboxamida y metodos de utilizacionInfo
- Publication number
- PE20151375A1 PE20151375A1 PE2015000409A PE2015000409A PE20151375A1 PE 20151375 A1 PE20151375 A1 PE 20151375A1 PE 2015000409 A PE2015000409 A PE 2015000409A PE 2015000409 A PE2015000409 A PE 2015000409A PE 20151375 A1 PE20151375 A1 PE 20151375A1
- Authority
- PE
- Peru
- Prior art keywords
- carboxamide
- pyrazol
- methods
- compounds
- heterociclil
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 150000001923 cyclic compounds Chemical class 0.000 title 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 102000020233 phosphotransferase Human genes 0.000 abstract 2
- GZLGJDQCTABTKC-UHFFFAOYSA-N 5-amino-2-(2,6-difluorophenyl)-n-[5-(3,4-dihydro-2h-pyran-6-yl)-1-methylpyrazol-4-yl]-1,3-thiazole-4-carboxamide Chemical compound C=1CCCOC=1C=1N(C)N=CC=1NC(=O)C(=C(S1)N)N=C1C1=C(F)C=CC=C1F GZLGJDQCTABTKC-UHFFFAOYSA-N 0.000 abstract 1
- UTYFQTUHNYURSK-UHFFFAOYSA-N 5-amino-2-(2,6-difluorophenyl)-n-[5-(3,6-dihydro-2h-pyran-4-yl)-1-methylpyrazol-4-yl]-1,3-thiazole-4-carboxamide Chemical compound C=1COCCC=1C=1N(C)N=CC=1NC(=O)C(=C(S1)N)N=C1C1=C(F)C=CC=C1F UTYFQTUHNYURSK-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000004292 cyclic ethers Chemical group 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000011065 in-situ storage Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 210000004962 mammalian cell Anatomy 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
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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
- A61K31/41—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
- A61K31/4353—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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- 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
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- 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
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- 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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- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
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- Health & Medical Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Peptides Or Proteins (AREA)
Abstract
Referida a compuestos ciclicos eter pirazol-4-il-heterociclil-carboxamida de formula I, incluyendo estereoisomeros, isomeros geometricos, tautomeros y sales farmaceuticamente aceptables de los mismos, en los que R2 es un eter ciclico y X es tiazolilo, pirazinilo, piridinilo o pirimidinilo, que resultan utiles para inhibir la quinasa Pim y para tratar trastornos tales como el cancer mediado por la quinasa Pim. Se dan a conocer metodos de utilizacion de compuestos de formula l para el diagnostico, prevencion o tratamiento in vitro, in situ e in vivo de dichos trastornos en celulas de mamifero, o condiciones patologicas asociadas. Son compuestos preferidos: 5-Amino-2-(2,6-difluorofenil)-N-[5-(3,6-dihidro-2H-piran-4-il)-1-metil-pirazol-4-il] tiazol-4-carboxamida; 5-Amino-2-(2,6-difluorofenil)-N-[5-(3,4-dihidro-2H-piran-6-il)-1-metil-pirazol-4-il] tiazol-4-carboxamida; entre otros
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261705791P | 2012-09-26 | 2012-09-26 | |
| US201361864882P | 2013-08-12 | 2013-08-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151375A1 true PE20151375A1 (es) | 2015-09-18 |
Family
ID=49261521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000409A PE20151375A1 (es) | 2012-09-26 | 2013-09-25 | Compuestos ciclicos eter pirazol-4-il-heterociclil-carboxamida y metodos de utilizacion |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9328106B2 (es) |
| EP (1) | EP2900657B1 (es) |
| JP (2) | JP6666147B2 (es) |
| KR (1) | KR102281288B1 (es) |
| CN (1) | CN104640858B (es) |
| AU (2) | AU2013322736A1 (es) |
| BR (1) | BR112015006019B1 (es) |
| CA (1) | CA2881068C (es) |
| CL (1) | CL2015000530A1 (es) |
| CR (1) | CR20150119A (es) |
| DK (1) | DK2900657T3 (es) |
| EA (1) | EA031622B1 (es) |
| ES (1) | ES2791648T3 (es) |
| HR (1) | HRP20200681T1 (es) |
| HU (1) | HUE049611T2 (es) |
| IL (1) | IL237159A0 (es) |
| LT (1) | LT2900657T (es) |
| MX (1) | MX376762B (es) |
| PE (1) | PE20151375A1 (es) |
| PH (1) | PH12015500488A1 (es) |
| PL (1) | PL2900657T3 (es) |
| PT (1) | PT2900657T (es) |
| RS (1) | RS60202B1 (es) |
| SG (1) | SG11201502343RA (es) |
| SI (1) | SI2900657T1 (es) |
| UA (1) | UA119229C2 (es) |
| WO (1) | WO2014048939A1 (es) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2794627T1 (sl) | 2011-12-22 | 2019-02-28 | Alios Biopharma, Inc. | Substituirani nukleozidi, nukleotidi in njihovi analogi |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| EP2844652B1 (en) * | 2012-05-03 | 2019-03-13 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| TW201408688A (zh) | 2012-05-25 | 2014-03-01 | Janssen R & D Ireland | 尿嘧啶基螺氧環丁烷（ｓｐｉｒｏｏｘｅｔａｎｅ）核苷類 |
| GEP201706757B (en) | 2012-12-21 | 2017-10-25 | Alios Biopharma Inc | Substituted nucleosides, nucleotides and analogs thereof |
| WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| PT2945939T (pt) | 2013-01-15 | 2020-06-08 | Incyte Holdings Corp | Compostos tiazole e piridina carboxamidas úteis como inibidores das quinases pim |
| US9556197B2 (en) | 2013-08-23 | 2017-01-31 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| CA2939848A1 (en) * | 2014-03-18 | 2015-09-24 | F. Hoffmann-La Roche Ag | Oxepan-2-yl-pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| MX380940B (es) * | 2015-04-22 | 2025-03-11 | Rigel Pharmaceuticals Inc | Compuestos de pirazol y metodo para elaborar y usar los compuestos. |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| CN105254624B (zh) * | 2015-09-18 | 2019-08-09 | 上海吉铠医药科技有限公司 | 异噻唑衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| US20170107216A1 (en) | 2015-10-19 | 2017-04-20 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| SG11201804152RA (en) | 2015-11-19 | 2018-06-28 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| MA44075A (fr) | 2015-12-17 | 2021-05-19 | Incyte Corp | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1 |
| EP3828171A1 (en) | 2015-12-22 | 2021-06-02 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| TW201808902A (zh) | 2016-05-26 | 2018-03-16 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
| AU2017281285C1 (en) | 2016-06-20 | 2022-05-12 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP3484866B1 (en) | 2016-07-14 | 2022-09-07 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP3504198B1 (en) | 2016-08-29 | 2023-01-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP3558989B1 (en) | 2016-12-22 | 2021-04-14 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| IL295660A (en) | 2016-12-22 | 2022-10-01 | Incyte Corp | Benzooxazole derivatives as immunomodulators |
| WO2018119286A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| PE20200005A1 (es) | 2016-12-22 | 2020-01-06 | Incyte Corp | Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1 |
| US20180179179A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| CA3093445A1 (en) | 2018-03-08 | 2019-11-28 | Incyte Corporation | Aminopyrazine diol compounds as pi3k-.gamma. inhibitors |
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