USRE41783E1 - Pyrrolo[2,3-D]pyrimidine compounds - Google Patents
Pyrrolo[2,3-D]pyrimidine compounds Download PDFInfo
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- USRE41783E1 USRE41783E1 US12/577,790 US57779009A USRE41783E US RE41783 E1 USRE41783 E1 US RE41783E1 US 57779009 A US57779009 A US 57779009A US RE41783 E USRE41783 E US RE41783E
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- pyrrolo
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- 0 [1*]C1=C2C(=NC=N1)NC([3*])=C2[2*] Chemical compound [1*]C1=C2C(=NC=N1)NC([3*])=C2[2*] 0.000 description 15
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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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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- 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
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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
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- 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
- A61K31/52—Purines, e.g. adenine
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- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
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- 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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Abstract
wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, xeno transplation, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.
Description
or the pharmaceutically acceptable salt thereof; wherein
-
- R1 is a group of the formula
wherein y is 0, 1 or 2; - R4 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkylsulfonyl, (C2-C6)alkenyl, and (C2-C6)alkynyl wherein the alkyl, alkenyl and alkynyl groups are optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C4)alkoxy, (C1-C6)acyloxy, (C1-C6)alkylamino, ((C1-C6alkyl)2 amino, cyano, nitro, (C2-C6)alkenyl, (C2-C6)alkynyl or (C1-C6)acylamino or R4 is (C3-C10)cycloalkyl wherein the cycloalkyl group is optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C6)acyloxy, (C1-C6)acylamino, (C1C6)alkylamino, ((C1-C6)alkylamino, cyano, cyano(C1-C6)alkyl, trifluoromethyl(C1-C6)alkyl, nitro, nitro(C1-C6)alkyl or (C1-C6)alkylamino;
- R5 is (C2-C9)heterocycloalkyl wherein the heterocycloalkyl groups must be substituted by one to five carboxy, cyano, amino, deuterium, hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy, halo, (C1-C6)acyl, (C1C6)alkylamino, amino(C1-C6)alkyl, (C1-C6)alkoxy-CO—NH, (C1-C6)alkylamino-CO—, (C2-C6)alkenyl, (C2-C6) alkynyl, (C1-C6)alkylamino, amino(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)acyloxy(C1-C6)alkyl, nitro, cyano(C1-C6)alkyl, halo(C1-C6)alkyl, nitro((C1-C6)alkyl, trifluoromethyl, trilluoromethyl((C1-C6)alkyl, (C1-C6)acylamino, (C1-C6)acylamino(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)acylamino, amino(C1-C6)acyl, amino (C1-C6)acyl(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)acyl, ((C1-C6)alkyl)2amino(C1-C6)acyl, R15R16N—CO—O—, R15R16N—CO—(C1-C6)alkyl, (C1-C6)alkyl-S(O)m, R5R16NS(O)m, R15R16NS(O)m (C1-C6)alkyl, R15S(O)m R16N, R15S(O)mR16N(C1-C6)alkyl, wherein m is 0, 1 or 2 and R15 and R16 are each independently selected from hydrogen or (C1-C6)alkyl, or a group of the formula
wherein - a is 0, 1, 2, 3 or 4;
- b, c, e, f and g are each independently 0 or 1;
- d is 0, 1, 2, or 3;
- X is S(O)n wherein n is 0, 1 or 2; oxygen, carbonyl or —C(═N-cyano)-;
- Y is S(O)n wherein n is 0, 1 or 2; or carbonyl; and
- Z is carbonyl, C(O)O—, or S(O)n wherein n is 0, 1 or 2;
- R6, R7, R8, R9, R10 and R11 are each independently selected from the group consisting of hydrogen and (C1-C6)alkyl optionally substituted by deuterium, hydroxy, amino, trifluoromethyl, (C1-C6)acyloxy, (C1-C6)acylamino, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, cyano, cyano((C1-C6)alkyl, trifluoromethyl((C1-C6)alkyl, nitro, nitro(C1-C6)alkyl or (C1-C6)acylamino;
- R12 is carboxy, cyano, amino, oxo, deuterium, hydroxy, trifluoromethyl, (C1-C6)alkyl, trifluoromethyl(C1-C6)alkyl, (C1-C6)alkoxy, halo, (C1-C6)acyl, (C1-C6)alkylamino, ((C1-C6)alkyl)2 amino, amino(C1-C6)alkyl, (C1-C6)alkoxy-CO—NH, (C1-C6)alkylamino-CO—, (C2-C6)alkenyl, (C2-C6) alkynyl, (C1-C6)alkylamino, hydroxy(C1-C6)alkyl, ((C1-C6)alkoxy(C1-C6)alkyl, (C1-C6)acyloxy(C1-C6)alkyl, nitro, cyano((C1-C6)alkyl, halo(C1-C6)alkyl, nitro( (C1-C6)alkyl, trifluoromethyl, trifluoromethyl(C1-C6)alkyl, (C1-C6)acylamino, (C1-C6)acylamino( (C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)acylamino, amino( (C1-C6)acyl, amino( (C1-C6)acyl( (C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)acyl, ((C1-C6)alkyl)2amino( (C1-C6)acyl, R15R16N—CO—O—, R15R16N—CO—(C1-C6)alkyl, R15C(O)NH, R15OC(O)NH, R15NHC(O)NH, (C1-C6)alkyl-S(O)m, (C1-C6)alkyl-S(O)m-(C1-C6)alkyl, R15R16NS(O)m, R15R16NS(O)m(C1-C6)alkyl, R15S(O)mR16N, R15S(O)mR16N(C1-C6)alkyl, wherein m is 0, 1 or 2 and R15 and R16 are each independently selected from hydrogen or (C1-C6)alkyl;
- R2 and R3 are each independently selected from the group consisting of hydrogen, deuterium, amino, halo, hydoxy, nitro, carboxy, (C2-C6)alkenyl, (C2-C6)alkynyl, trifluoromethyl, trifluoromethoxy, (C1-C6)alkyl, (C1-C6)alkoxy, and (C3-C10)cycloalkyl wherein the alkyl, alkoxy or cycloalkyl groups are optionally substituted by one to three groups selected from halo, hydroxy, carboxy, amino (C1-C6)alkylthio, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, (C5-C9)heteroaryl, (C2-C9)heterocycloalkyl, (C3-C9)cycloalkyl or (C6-C10)aryl; or R2 and R3 are each independently (C3-C10)cycloalkyl, (C3-C10)cycloalkoxy, (C1-C6)alkylamino, ((C1-C6)alkyl)2amino, (C6-C10)arylamino, (C1-C6)alkylthio, (C6-C10)arylthio, (C1-C6)alkylsulfinyl, (C6-C10)arylsulfinyl, (C1-C6)alkylsulfonyl, (C6-C10)arylsulfonyl, (C1-C6)acyl, (C1-C6)alkoxy-CO—NH—, (C1-C6)alkyamino-CO—, (C5-C9)heteroaryl, (C2-C9)heterocycloalkyl or (C6-C10)aryl wherein the heteroaryl, heterocycloalkyl and aryl groups are optionally substituted by one to three halo, (C1-C6)alkyl, (C1-C6)alkyl-CO—NH—, (C1-C6)alkoxy-CO—NH—, (C1-C6)alkyl-CO—NH—(C1-C6)alkyl, (C1-C6)alkoxy-CO—NH—(C1-C6)alkyl, (C1-C6)alkoxy-CO—NH—(C1-C6)alkoxy, carboxy, carboxy((C1-C6)alkyl, carboxy((C1-C6)alkoxy, benzyloxycarbonyl(C1-C6)alkoxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy, (C6-C10)aryl, amino, amino(C1-C6)alkyl, (C1-C6)alkoxycarbonylamino, (C6-C10)aryl( (C1-C6)alkoxycarbonylamino, (C1-C6)alkylamino, (C1-C6)alkyl)2amino, (C1-C6)alkylamino(C1-C6)alkyl, (C1-C6)alkyl)2amino( (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, carboxy, carboxy( (C1-C6)alkyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkoxycarbonyl(C1-C6)alkyl, (C1-C6)alkoxy-CO—NH—, (C1-C6)alkyl-CO—NH—, cyano, (C5-C9)heterocycloalkyl, amino-CO—NH—, (C1-C6)alkylamino-CO—NH—, (C1-C6)alkyl)2amino-CO—NH—, (C6-C10)arylamino-CO—NH—, (C5-C9)heteroarylamino-CO—NH—, (C1-C6)alkylamino-CO—NH—(C1-C6)alkyl, ((C1-C6)alkyl)2amino-CO—NH—(C1-C6)alkyl, (C6-C10)arylamino-CO—NH—(C1-C6)alkyl, (C5-C9)heteroarylamino-CO—NH—(C1-C6)alkyl, (C1-C6)alkylsulfonyl, (C1-C6)aIkylsulfonylamino, (C1-C6)alkylsulfonylamino( (C1-C6)alkyl, (C6-C10)arylsulfonyl, (C6-C10)arylsulfonylamino, (C6-C10)arylsulfonylamino( (C1-C6)alkyl, (C1-C6)alkylsulfonylamino, (C1-C6)alkylsulfonylamino(C1-C6)alkyl, (C5-C9)heteroaryl or (C2-C9)heterocycloalkyl.
- R1 is a group of the formula
- Methyl-[4-methyl-1-(propane-1-sulfonyl)-piperidin-3-yl]-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amine;
- 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carboxylic acid methyl ester;
- 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-propan-1-one;
- 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carboxylic acid dimethylamide;
- ({4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carbonyl}-amino)-acetic acid ethyl ester;
- 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile;
- 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-propan-1-one;
- 1-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-but-3-yn-1-one;
- 1-{3-[(5-Chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl}-propan-1-one;
- 1-{3-[(5-Fluoro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl}-propan-1-one;
- N-cyano-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-N′-propyl-piperidine-1-carboxamidine; and
- N-cyano-4,N′,N′-Trimethyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carboxamidine.
Claims (4)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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US12/577,790 USRE41783E1 (en) | 1999-12-10 | 2009-10-13 | Pyrrolo[2,3-D]pyrimidine compounds |
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US17017999P | 1999-12-10 | 1999-12-10 | |
US09/732,669 US6627754B2 (en) | 1999-12-10 | 2000-12-08 | Pyrrolo[2,3-d]pyrimidine compounds |
US12/577,790 USRE41783E1 (en) | 1999-12-10 | 2009-10-13 | Pyrrolo[2,3-D]pyrimidine compounds |
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US09/732,669 Reissue US6627754B2 (en) | 1999-12-10 | 2000-12-08 | Pyrrolo[2,3-d]pyrimidine compounds |
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US09/732,669 Ceased US6627754B2 (en) | 1999-12-10 | 2000-12-08 | Pyrrolo[2,3-d]pyrimidine compounds |
US10/640,227 Expired - Lifetime US6956041B2 (en) | 1999-12-10 | 2003-08-13 | Pyrrolo[2,3-d]pyrimidine compounds |
US11/211,217 Expired - Lifetime US7091208B2 (en) | 1999-12-10 | 2005-08-24 | Pyrrolo[2,3-D]pyrimidine compounds |
US11/474,233 Expired - Lifetime US7265221B2 (en) | 1999-12-10 | 2006-06-23 | Pyrrolo[2,3-d]pyrimidine compounds |
US11/829,217 Expired - Fee Related US7601727B2 (en) | 1999-12-10 | 2007-07-27 | Pyrrolo[2,3-d]pyrimidine compounds |
US12/549,526 Expired - Fee Related US7842699B2 (en) | 1999-12-10 | 2009-08-28 | Pyrrolo[2,3-D]pyrimidine compounds |
US12/577,790 Active 2025-12-08 USRE41783E1 (en) | 1999-12-10 | 2009-10-13 | Pyrrolo[2,3-D]pyrimidine compounds |
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US09/732,669 Ceased US6627754B2 (en) | 1999-12-10 | 2000-12-08 | Pyrrolo[2,3-d]pyrimidine compounds |
US10/640,227 Expired - Lifetime US6956041B2 (en) | 1999-12-10 | 2003-08-13 | Pyrrolo[2,3-d]pyrimidine compounds |
US11/211,217 Expired - Lifetime US7091208B2 (en) | 1999-12-10 | 2005-08-24 | Pyrrolo[2,3-D]pyrimidine compounds |
US11/474,233 Expired - Lifetime US7265221B2 (en) | 1999-12-10 | 2006-06-23 | Pyrrolo[2,3-d]pyrimidine compounds |
US11/829,217 Expired - Fee Related US7601727B2 (en) | 1999-12-10 | 2007-07-27 | Pyrrolo[2,3-d]pyrimidine compounds |
US12/549,526 Expired - Fee Related US7842699B2 (en) | 1999-12-10 | 2009-08-28 | Pyrrolo[2,3-D]pyrimidine compounds |
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Cited By (11)
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