Roman V Rariy

7038085, May 2, 2006

Oct 22, 2003

10/691465

Roman V. Rariy - Allston MA, US
Michael Heffernan - Hingham MA, US
Stephen L. Buchwald - Newton MA, US
Timothy M. Swager - Newton MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

C07C 233/05
A61K 31/165

564165, 564164, 564171, 564190, 514620, 514624

The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC=28. 6 nM for norepinephrine, IC=21. 7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC=10. 3 nM for norepinephrine, IC=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC=88. 5 nM for norepinephrine, IC=40. 3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient. Finally, the present invention relates to methods of treating mammals suffering from various afflictions, e. g.

7309799, Dec 18, 2007

Apr 1, 2005

11/097466

Stephen L. Buchwald - Newton MA, US
Timothy M. Swager - Newton MA, US
Roman V. Rariy - Allston MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

C07C 211/00
C07C 231/00

564133, 564461

One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

7345192, Mar 18, 2008

Nov 10, 2005

11/272250

Anwar Jardien - Brookline MA, US
Roman Rariy - Allston MA, US
Gurpreet S. Ahluwalia - Newton MA, US
Douglas Shander - Acton MA, US

The Gillette Company - Boston MA

C07C 220/00
C07C 53/15
A01N 33/18

560169, 560206, 560226, 514740

Compositions including a conjugate of α-difluoromethylornithine can be applied topically to reduce hair growth.

7399488, Jul 15, 2008

Jul 7, 2003

10/614866

Jane Hirsh - Wellesley MA, US
Alexander M. Kibanov - Newton MA, US
Timothy M. Swager - Newton MA, US
Stephen L. Buchwald - Newton MA, US
Whe Yong Lo - Canton MA, US
Alison B. Fleming - Marshfield MA, US
Roman V. Rariy - Allston MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

A61K 9/14
A61K 9/50

424489, 424464, 424451, 424502

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

7704527, Apr 27, 2010

Sep 16, 2008

12/211780

Jane C. Hirsh - Wellesley MA, US
Roman V. Rariy - Allston MA, US
Shubha Chungi - Chestnut Hill MA, US
Srinivas G. Rao - Encinitas CA, US
Michael T. Heffernan - Hingham MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

A61K 9/22
A61K 9/20
A61K 9/28

424468, 424464, 424465, 424474

A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tof 4-10 hours.

7771707, Aug 10, 2010

Jun 10, 2005

11/149867

Jane C. Hirsh - Wellesley MA, US
Alison B. Fleming - North Attleboro MA, US
Roman V. Rariy - Allston MA, US
Alexander M. Klibanov - Newton MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

A61K 49/00
A61K 31/44

424 101, 514282

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

8021687, Sep 20, 2011

Apr 7, 2010

12/755847

Jane C. Hirsh - Wellesley MA, US
Roman V. Rariy - Allston MA, US
Shubha Chungi - Chestnut Hill MA, US
Srinivas G. Rao - Encinitas CA, US
Michael T. Heffernan - Hingham MA, US

Collegium Pharmaceutical, Inc. - Cumberland RI

A61K 9/14
A61K 31/56
A61K 9/28
A61P 29/00
A61P 25/24
A61P 25/06
A61P 25/08
A61P 25/22
A61P 25/18
A61P 11/08
A61P 11/06
A61P 9/00
A61P 1/00
A61P 21/02

424465, 424490, 424497, 424498, 424494, 424495, 424496, 514619, 514171

A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tof 4-10 hours.

8449909, May 28, 2013

Jun 25, 2010

12/823628

Jane Hirsh - Wellesley MA, US
Alison Fleming - Mansfield MA, US
Roman Rariy - Philadelphia PA, US
Alexander Kilbanov - Boston MA, US

Collegium Pharmaceutical, Inc. - Canton MA

A61K 9/54
A61K 9/42
A61K 31/44

424458, 424476, 514282

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.