AR052506A2 - Intermediarios utiles para la preparacion de compuestos heterociclicos - Google Patents
Intermediarios utiles para la preparacion de compuestos heterociclicosInfo
- Publication number
- AR052506A2 AR052506A2 ARP060100824A ARP060100824A AR052506A2 AR 052506 A2 AR052506 A2 AR 052506A2 AR P060100824 A ARP060100824 A AR P060100824A AR P060100824 A ARP060100824 A AR P060100824A AR 052506 A2 AR052506 A2 AR 052506A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- independently
- optionally
- cycloalkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
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- 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
-
- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physical Education & Sports Medicine (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Cooling Or The Like Of Electrical Apparatus (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un compuesto intermediario util en la preparacion de un compuesto de acuerdo con la formula (1) por ser de la formula (2) las mezclas racémicas-diastereoméricas y los isomeros opticos de dichos compuestos y las sales farmacéuticamente aceptables de los mismos, en la que e es 0 o 1; n y w son cada uno de forma independiente 0, 1 o 2, con la condicion de que w y n no pueden ser ambos 0 al mismo tiempo; R1 es h, -CN, -(CH2)qN(X6)C(O)X6, -(CH2)qN(X6)C(O)(CH2)t-A1, -(CH2)qN(X6)SO2(CH2)t-A1, - (CH2)qN(X6) SO2X6, -(CH2)qN(X6)C(O)N(X6)(CH2)t-A1, -(CH2)qN(X6)C(O)N(X6)(X6), -(CH2)qC(O)N(X6)(X6), -(CH2)qC(O)N(X6)(CH2)t-A1, -(CH2) qC(O)OX6, -(CH2)qC(O)O(CH2)t-A1, -(CH2)qOX6, -(/CH2)qOC(O)X6, -(CH2)qOC(O)(CH2)t-A1, -(CH2)qOC(O)N(X6)(CH2)t-A1, - (CH2) qOC(O)N(X6)(X6), -(CH2)qC(O)X6, -(CH2)qC(O)(CH2)t-A1, -(CH2)qN(X6)C(O)OX6, -(CH2)qN(X6)SO2N(X6)(X6), -(CH2)qS(O)mX6, -(CH2)qS(O)m(CH2)t-A1, -alquilo C1-10, -(CH2)t-A1, -(CH2)q-cicloalquilo C3-7, -(CH2)q-Y1-alquilo C1-6, -(CH2)q-Y1-(CH2)t-A1 o - (CH2)q-Y1-(CH2)t-cicloalquilo C3-7, donde los grupos alquilo y cicloalquilo en la definicion de R1 están sustituidos opcionalmente con alquilo C1-4, hidroxilo, alcoxilo C1-4, carboxilo, CONH2, -S(O)m-alquilo C1-6, -CO2alquil C1-4, 1H-tetrazol-5-ilo o 1 átomo de F; Y1 es O, S(O)m, -C(O)NX6-, -CH=CH-, -C:::C-, -N(X6)C(O)-, -C(O)NX6-, -C(O)O-, -OC(O)N(X6)- o -OC(O)-, q es 0, 1, 2, 3 o 4; t es 0, 1, 2 o 3; el grupo (CH2)q y el grupo (CH2)t citados podrían estar cada uno sustituido opcionalmente con 1 a 3 átomos de F, 1 o 2 alquilos C1-4, hidroxilo, alcoxilo C1-4, carboxilo, -CONH2, -S(O)m-alquilo C1-6, éster-CO2alquil C1-4 o 1H-tetrazol-5-ilo; R2 es H, alquilo C1-8, - alquil C0-3-cicloalquilo C3-8, -alquil C1-4-A1 o A1; donde los grupos alquilo y los grupos cicloalquilo de la definicion de R2 están sustituidos opcionalmente con hidroxilo, -C(O)OX6, -C(O)N(X6)(X6), -N(X6)(X6), -S(O)m-alquilo C1-6, -C(O)A1, -C(O)(X6), CF3, CN o 1 a 3 átomos de halogeno; A1 cada vez que se da es de forma independiente cicloalquenilo C5-7, fenilo o un anillo de 4 a 8 miembros parcialmente saturado, completamente saturado o completamente insaturado que tiene 1 a 4 heteroátomos seleccionados de forma independiente del grupo formado por O, S y N, un sistema de un anillo bicíclico formado por un anillo de 5 o 6 miembros parcialmente saturado, completamente insaturado o completamente saturado, que tiene opcionalmente 1 a 4 heteroátomos seleccionados de forma independiente del grupo formado por N, S y O, fusionado a un anillo de 5 o 6 miembros parcialmente saturado, completamente insaturado o completamente saturado, que tiene opcionalmente 1 a 4 heteroátomos seleccionados de forma independiente del grupo formado por N, S y O; A1 cada vez que se da está sustituido opcionalmente de forma independiente, en uno u opcionalmente en ambos anillos si A1 es un sistema de un anillo bicíclico, con hasta 3 sustituyentes, seleccionados cada sustituyente de forma independiente del grupo formado por F, Cl, Br, I, OCF3, OCF2H, CF3, CH3, OCH3, -OX6, -C(O)N(X6)(X6), -C(O)OX6, oxo, alquilo C1-6, nitro, ciano, bencilo, -S(O)m-alquilo C1-6, 1H-tetrazol-5-ilo, fenilo, fenoxilo, fenilalquiloxilo, halofenilo, metilendioxilo, -N(X6)(X6), - N(X6)C(O)X6, - SO2N(X6)(X6), -N(X6)SO2-fenilo, -N(X6)SO2X6, -CONX11X12, -SO2NX11X12, -NX6SO2X12, -NX6CONX11X12, -NX6SO2NX11X12, - NX6C(O)X12, imidazolilo, tiazolilo y tetrazolilo, con la condicion de que si A1 está sustituido opcionalmente con metilendioxilo entonces solo puede estar sustituido con un metilendioxilo; donde X11 es H o alquilo C1-6 opcionalmente sustituido; el alquilo C1-6 opcionalmente sustituido definido para X11 está sustituido opcionalmente de forma independiente con fenilo, fenoxilo, alcoxicarbonilo C1-6, -S(O)m-alquilo C1-6, 1 a 5 halogenos, 1 a 3 hidroxilos, 1 a 3 alcanoiloxilos C1-10 o 1 a 3 alcoxilos C1-6; X12 es H, alquilo C1-6, fenilo, tiazolilo, imidazolilo, furilo o tienilo, con la condicion de que cuando X12 no es H, X12 está sustituido opcionalmente con uno a tres sustituyentes seleccionados de forma independiente del grupo formado por Cl, F, CH3, OCH3, OCF3 y CF3; o X11 y X12 se toman en conjunto para formar -(CH2)r-L1-(CH2)r-; L1 es C(X2)(X2), O, S(O)m o N(X2), r cada vez que se da es de forma independiente 1, 2 o 3; X2 cada vez que se da es de forma independiente H, un alquilo C1-6 opcionalmente sustituido o un cicloalquilo C3-7 opcionalmente sustituido, donde el alquilo c1-6 opcionalmente sustituido y el cicloalquilo C3-7 opcionalmente sustituido de la definicion de X2 están opcionalmente sustituidos de forma independiente con -S(O)m-alquilo C1-6, -C(O)OX3, 1 a 5 halogenos o 1 a 3 OX3; X3 cada vez que se da es de forma independiente H, o alquilo C1-6, X6 cada vez que se da es de forma independiente H, alquilo C1-6 opcionalmente sustituido, alquilo C2-6 halogenado, cicloalquilo C3-7 opcionalmente sustituido, cicloalquilo C3-7 halogenado, donde el alquilo C1-6 opcionalmente sustituido y el cicloalquilo C3-7 opcionalmente sustituido de la definicion de X6 están opcionalmente sustituidos de forma independiente con hidroxilo, alcoxilo C1-4, carboxilo, CONH2, -S(O)m-alquilo C1-6, -CO2alquil C1-4, 1H-tetrazol- 5-ilo o 1 o 2 alquilos C1-4; o cuando hay dos grupos X6 en un átomo y los dos X6 son alquilo C1-6, los dos grupos alquilo C1-6 podrían estar opcionalmente unidos y, junto con el átomo al que están unidos los dos grupos X6, formar un anillo de 4 a 9 miembros que opcionalmente tenga O, s o NX7; X7 es h o alquilo c1-6 opcionalmente sustituido con hidroxilo; y m cada vez que se da es de forma independiente 0,m 1 o 2; con la condicion de que: X6 y X12 no pueden ser H cuando se unen a C(O) o SO2 en forma de C(O)X6, C(O)X12, SO2X6 o SO2X12; y cuando R2 es H entonces R1 no es -CH=CH-fenilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US946995P | 1995-12-28 | 1995-12-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR052506A2 true AR052506A2 (es) | 2007-03-21 |
Family
ID=21737850
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP960105571A AR004367A1 (es) | 1995-12-28 | 1996-12-09 | Compuestos heterociclicos, mezclas diastereomericas composiciones farmaceuticas, uso de los compuestos en la preparacion de medicamentos. |
ARP060100824A AR052506A2 (es) | 1995-12-28 | 2006-03-03 | Intermediarios utiles para la preparacion de compuestos heterociclicos |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP960105571A AR004367A1 (es) | 1995-12-28 | 1996-12-09 | Compuestos heterociclicos, mezclas diastereomericas composiciones farmaceuticas, uso de los compuestos en la preparacion de medicamentos. |
Country Status (43)
Families Citing this family (141)
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